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Abbreviations
AVL: Availability (Oral, intramuscular, patch etc)IND: Indications
MOA: Mechanism of action
EVD: Evidence for use
ADM: Administration (how to take/give)
AE: Adverse Events aka side effects
CI: Contraindications
PRG: Pregnancy risk
LAC: Lactation risk
DI: Drug Interactions
PK: Pharmacokinetics (ex. half life)
COS: Cost of the medication and whether it's covered by provincial plans
MON: Monitoring
DOS: Dose
OTH: Other
AUX: Auxillary labels
(-)=gram negative
(+)=gram positive
5-HT=Serotonin
ABx= antibiotics
ac= before meals
ADL=activities of daily living
Alt=alternate
ARV= antiretroviral
BG= blood glucose
BID=twice daily
BMD=bone mineral density
C=constipation
CAP= community acquired pneumonia
CCS=Canadian cancer society
CI=contraindicated
Cl=clearance
d=day
D=diarrhea
D/C=discontinue
DA=dopamine
DBP=diastolic blood pressure
DM=diabetes mellitus
DPI=dry powder inhaler
ED=erectile dysfunction
EF=ejection fraction
ER=extended release
ESRD=end stage renal disease
F= absorption
FEV1=forced expiratory volume in 1 second
FVC=forced vital capacity
GA=gestational age
GAD=generalized anxiety disorder
gen=generation
Gen=generic
GNR=gram negative rods
H=histamine
HA=headache
HC =Health Canada
Hct=hematocrit
Hgb=hemoglobin
Hx=history
HS= bed time
IR=immediate release
LOC=level of consciousness
m=month
M=mol/L
met=metabolized
min=minute
MDI=metered dose inhaler
mvmt=movement
N=nausea
NSR=normal sinus rhythm
OAC=oral anticoagulant
OD= right eye (avoid using for once daily)
OM= Otitis Media
pc=after meals
Ped=pediatric
PFT=pulmonary function test
pt=patient
PO=orally (route of administration)
PR=rectal (route of administration)
PV=vaginal (route of administration)
RDA=Recommended Dietary Allowance
Rx=prescription
RR=respiratory rate
RTI=respiratory tract infection
S/Sx=signs and symptoms
SA=short acting
SAP=special access program
Schedule I=NAPRA Schedule (behind counter, need prescription)
Schedule II=NAPRA Schedule (keep behind counter but no prescription).
Schedule III=NAPRA Schedule (keep OTC but phc needs to be available).
Schedule U=NAPRA Schedule (unscheduled so anyone can sell, Rx not needed).
SS=steady state
SBP= systolic blood pressure
SMI=soft mist inhaler
SOB=shortness of breathe
std=standard
STD=sexually transmitted disease
SVR=sustained virologic response
Sx=symptoms
T=take
TC=total cholesterol
TID=three times daily
TM=tympanic membrane
TOD=target organ disease
TUL=tolerable upper limit
Tx=treatment
U=units
URTI=upper respiratory tract infection
V=vomiting
Vit=vitamin
w=week
w/=with
wt=weight
y=year
yo=years old
5-HT3 Antagonist
IND: Naus, Vom. MOA: Act in CTZ and peripheral gut on serotonin receptors. DI: QT prolonging agents, apomorphine, aripiprazole, tramadol, serotonergic drugs (serotonin syndrome). OTH: Aka setrons.dolasetron: OTH: Taken off market.
granisetron:
ondansetron=Zofran: AVL: Avail IV or PO. IND: Chemo induced N + V. MOA: Blocks 5-HT3 receptor. AE: HA11%, C4%, D, dizziness, flushing/warmth<1%, bradycardia, known QT prolongation. PK: 3A4 substrate. DOS: T 30min before chemo and up to 5d after.
palonosetron:
Anti-Androgens
abiraterone=Zytiga: IND: Metastatic prostate cancer. MOA: CYP17 inhibitor (enzyme in adrenal glands, testes, and prostate tumor). ADM: T on empty stomach (food increases F). AE: D, HTN, decreased K, fluid retention, hepatotoxicity, cardiotoxicity, joint swelling, UTI. PRG: CI. PK: t1/2=12h. Prodrug to aberaterone. Met by 3A4 (major). Inhibits PGP, 1A2, and 2D6. DOS: 1g po daily + 5mg prednisone BID. OTH: T w/ prednisone because of excess aldosterone and cortisol.Antiemetics
aprepitant=Emend: AVL: PO. IND: Chemotherapy induced N/V. MOA: NK1 inhibitor. Binds to substance P in the brainstem and GI tract. AE: Fatigue, D, dizziness, dyspepsia, hiccups. DI: Warfarin, COCs. PK: F=60-65%. Moderate 3A4 inhibitor, 2C9 inducer, 3A4 substrate. OTH: Not used alone.domperidone: AVL: PO, IV, SubQ. DOS: 5-20mg TID – QID before meals.
metoclopramide: AVL: PO, IV, SubQ. DOS: 5-20mg TID–QID before meals.
PHENOTHIAZINES
chlorpromazine: AVL: PO. DOS: PO:10-50mg q4-6h.
prochlorperazine: AVL: Avail PO, IV, IM, PR. IND: Chemo induced N + V. MOA: Blocks DA in chemo receptor trigger zone. AE: Sedation, anticholinergic effects, hypotension, hypersensitivity rxn. DOS: 5-10mg q6-8h prn. OTH: Also classified as a first gen antipsychotic.
promethazine: AVL: PO, IM, IV, PR. DOS: 12.5-25mg q4-6h prn
Aromatase Inhibitors (AIs)
Non-Steroidalanastrazole: IND: Estrogen positive breast cancer. MOA: Blocks aromatase which converts androgens to estrogens. EVD: Only AI that won’t affect lipids. AE: N, hot flashes, HA, bone loss, increased cholesterol, swelling in hands and feet. PK: t1/2=41h. Inhibits 1A2, 2C9, 3A4.
letrozole: IND: Estrogen positive breast cancer. PK: t1/2= 2-4d. Strong inhibitor of 2A6 and moderate for 2C19.
Steroidal
Exemestane: IND: Estrogen positive breast cancer. AE: Weight gain, acne. PK: t1/2=27h.
Corticosteroids
dexamethasone=Decadron: AVL: IV, IM, PO. IND: Chemotherapy induced N + V (increases effect of ondansetron.). ADM: T w/ food. AE: fluid retension, thrush, bone loss, cataracts, indigestion, muscle weakness, back pain, bruising, increased glucose, weight gain, insomnia. PRG: FDA cat C. PK: Induces and metabolized by 3A4. Duration=3d.Gonadotropin-Releasing Hormone (GnRH) Agonists
Aka LH releasing hormone agonist.goserelin=Zoladex: AVL: SubQ biodegradable implant. IND: Breast and prostate cancer. MOA: Produces sex hormones in a non-pulsatile manner that disrupts feedback mechanism. AE: N, stop in periods, hot flashes, dizziness, HA, sweating, sexual dyfunction, change in breast size, vaginal dryness, hair loss. Hormone levels will increase in first few weeks causing increased pain, increased difficulty urinating in men. PRG: CI. PK: t1/2=4.2h. DOS: Max=3.6mg q4w x 6 months.
Prokinetics
metoclopramide: AVL: PO, IM, SubQ, IV. IND: Chemo induced N + V. MOA: Blocks D2 in the chemo trigger zone. Increases gastric emptying rate. AE: D, sedation, insomnia, EPS in children (CI<1yo). PRG: Used in all stages. LAC: Used (<45mg/d). DOS: Should not exceed 0.5mg/kg/d. Adj dose if CrCl<50.Selective Estrogen Receptor Modulators (SERMs)
tamoxifen=Novaldex: IND: Estrogen receptor positive breast cancer (both pre and post menopause. AE: N, hot flashes, vaginal discharge or dryness, menstrual irregularities, muscle/joint pain, hair thinning, weight loss, possible QT prolongation. CI: Hx of DVT or PE. PRG: CI. LAC: CI. DI: 2D6 inhibition (ex. antidepressants) will stop metabolism to prodrug 4-hydroxytamoxifen. PK: t1/2= 5-7d. F=100%. DOS: 20mg/d x 5 years.Tyrosine Kinase Inhibitors
imatinib: AVL: PO. IND: CML. PK: t1/2=18h. F=98%. Metabolised and inhibits 3A4/5.α2 Agonists
clonidine: AVL: PO. IND: ADHD, HT urgency. AE: Drowsiness, rebound HTN, bradycardia. PK: Onset=30-60min. Duration=8h. DOS : ADHD : Initial=50-100ug/d. Std=3–10µg/kg/d (50–400ug/d), once/d or divided. To D/C, reduce dose 0.1mg q3–7d.guanfacine=Intuniv: AVL: PO. IND: ADHD. DOS: Adj for renal fxn. To D/C, reduce dose 1mg q3–7d. ADHD: Initial=1mg/d. Increase dose 1mg/d/week prn. Max=4mg/d.
methyldopa: IND: 1st line for HTN in PRG. AE: Anticholinergic (dry mouth, sedation), fluid retention, , depression, orthostatic hypotension, sexual dysfxn, Na + water retention. Warning: Can cause rebound HTN if stopped abruptly.
Angiotensin-Converting Enzyme (ACE) Inhibitors
IND: HTN, HT crisis , HF (with BB), DM, CAD, renal disease, stroke, post ACS, angina. MOA: Blocks formation of the vasoconstrictor angiotensin II. Also prevents formation of aldosterone which leads to decreased Na and decreased fluid. EVD: Less effective and more angioedema for black pts (less renin type HTN so use thiazide or CCB). ADM: T same time of day (once/d or BID). AE: dry cough20%, increased K (avoid supplements), orthostatic hypotension/fainting, angioedema, increased Cr (>30% would be concerning), renal failure. PRG: CI. LAC: CI. DI: NSAIDs, K sparing diuretics. MON: BUN, Cr, K, BP. DOS: Requires adj for renal fxn.benzapril=Lotensin:
captopril=Capoten: AVL: PO, SL. IND: HT urgency. PRG: CI. LAC: Safe. PK: Onset: SL=10-15min. PO=1-2h. Duration=4-6h. Food decreases F by 30%.
cilazapril=Inhibace:
enalapril=Vasotec: PRG: CI. LAC: Safe.
enalaprilat: AVL: IV. IND: HT emergency. PK: Onset=15-30min. Duration=6-12h.
fosinopril=Monopril:
lisinopril=Zestril=Prinivil: AVL: IND: HTN, post MI, MOA: EVD: ADM: T w/ or without food. AE: Chills, fever, abdominal pain, hypotension, naus, vom, diar, angioedema, joint/muscle pain. CI/Warning: PRG: LAC: DI: PK: COS: AUX: MON: DOS: Adj dose for renal fxn. Std=10-40mg once/d. OTH:
perindopril=Coversyl: Most common ACEI in practice.
quinapril=Accupril:
ramipril=Altace: EVD: HOPE trial used 10mg/d. LAC: Safe. DOS: 2.5-10mg/d (can divide BID).
trandolapril=Mavik:
Angiotensin II Receptor Blockers (ARBs)
IND: DM, uncomplicated HTN, CAD, HF, LVH, renal failure, and alterative if ACEI not tolerated. MOA: Blocks receptor that respond to angiotensin II (vasoconstrictor). EVD: Increased angioedema and decreased efficacy for black pts (less renin type HTN so use thiazide). AE: Rash, orthostatic hypotension/fainting, angioedema, increased K (don’t take supplements), increased Cr (stop if >30%), decreased Na, renal failure. Less cough and angioedema vs ACEI. CI: Already taking ACEI (exception in HF) . PRG: CI. DOS: Adjust for hepatic fxn.candesartan=Atacand: DOS: 8-32mg/d (can divide BID).
eprosartan=Teveten:
irbesartan=Avapro:
losartan=Cozaar:
olmesartan=Olmetec: FDA Warning : severe D and weight loss.
valsartan=Diovan:
Antiarrhythmics
Class IC (Na channel blocker)flecainide: IND: AFib. AE: N, V, D, metallic taste, agranulocytosis<1%, dysrythmias, hypotension, HF/asthma exacerbation, fatigue, HA, anxiety, dizziness. QT prolongation (known).
Class II
sotalol: Class II + III antiarrhythmic. IND: AFib (only for NSR maintenance). MOA: blocks β receptor, blocks potassium channel. AE: N, V, D, fatigue, depression, insomnia, HA, dizziness, dysrhythmia, HF/ asthma exacerbation, masks hypoglycemia. Prolongs QT (known).
Class III
amiodarone: IND: AFib. MOA: Slows HR. ADM: T w/ food. AE: Corneal microdeposits100%, N, C30%, blurred vision5%, insomnia, cough13%, pulmonary fibrosis3%, tremor15%, blue/grey skin discoloration<10%, liver toxicity, photosensitivity50%, hypo20%/hyper3%thyroidism, QT prolongation100%/Torsades0.5%. DI: Inhibits PGP. GFJ interaction. PK: t1/2=53d. Onset=1w-5months. Vd=65.8L/kg. Met by 3A4, 2C8. Inhibits 2D6, 1A2, 2C9, 3A4. MON: Thyroid and liver tests q6 months. Vitals, eye exam, and PFT yearly.
dronedarone: IND: AFib (rhythm control). EVD: Less effective vs amiodarone for NSR maintenance. AE: N, V, D, weakness, dyspnea, cough, interstitial lung disease. Warning: Avoid if HF, permanent AFib. DI: Digoxin.
Antiplatelets
Irreversible Cyclooxygenase Inhibitorsacetylsalicylic acid (ASA)=Aspirin: IND: Primary prevention of MI for high risk pts, secondary prevention of MIISIS 2, angina (81mg/d), during ACS. MOA: Inhibits COX-1. CI: <12yo can cuase Rye's syndrome (<19yo to be safe). PK: Inhibits platelets for 5-7d. DOS: *Angina*: 81mg/d. *MI prevention*: 81mg/d. *Suspected MI*: chew 162mg (2 EC tabs).
P2Y12 Inhibitors
clopidogrel=Plavix: IND: ACS, PAD, stroke, AFib. Used if intolerant to ASA. AE: D, upset stomach10%, rash6%, HA, dizziness, bleeding. CI: If previous ulcer use ASA and esomeprazole instead. DI: PPIs (pantoprazole low risk). PK: Activated by 2C19 (genetic polymorphism may decrease efficacy). DOS: Drug eluting stent: 1 year of Tx. NSTEMI: 300mg stat then 75mg/d was better for death, MI, and StrokeCURE. OTH: Very commonly seen. Hold > 5d before surgery if possible.
prasugrel=Effient: IND: Used w/ ASA for secondary prevention of MI and stroke and stent pts with high risk of thrombosis. MOA: Irreversibly inhibits ADP platelet. AE: Higher risk of bleeding vs. clopidogrel (especially if >75yo or <60kg), confusion, rash. DOS: Post PCI=10mg/d. OTH: Not commonly seen. Hold > 7d before surgery if possible.
ticagrelor=Brilinta: IND: Used w/ ASA (<150mg/d) for secondary prevention of MI and stroke. MOA: Irreversibly inhibits ADP platelets. EVD: In ACS, decreased mortality and ischemic events vs. clopidogrelPLATO. AE: HA, bleeding, dyspnea14%, decreased HR, increased uric acid, ventricular pause. DI: 3A4 + PGP. Can increase digoxin levels. PK: Doesn’t require metabolic activation like clopidogrel. COS: Expensive (not on all formularies). DOS: Post-PCI: 90mg BID. OTH: Hold > 5d before surgery if possible.
β Blockers (BBs)
Cardio-Selective
Acronym for the common cardio-selective drugs=BAAM. IND: Uncomplicated HTN < 60yo, HTN > 60yo with angina (not 1st line in HTN >60yo: no stroke prevention), HF (w/ ACEI), HT urgency, angina, post MICOMMIT/CCS, migraine, tremor, anxiety. EVD: Less effective in black pts. ADM: T at same time of day. AE: Orthostatic hypotension, exercise intolerance, fatigue, HA, insomnia, cold extremities, increased cholesterol, increased asthma, increased K, depression, glycemic effects (DM), impotence. Warning : Don’t stop abruptly (can lead to angina or MI in IHD). Taper to lowest dose for >1week. DI: Non-DHP CCB (both decrease HR).
acebutolol=Sectral: MOA: Has ISA (intrinsic sympathomimetic activity) which acts like NE to stimulate β receptors which increase HR and BP. EVD: May have less cold extremities but rarely used. CI: Angina.
atenolol=Tenormin: PRG: CI.
bisoprolol=Monocor:
esmolol: AVL: IV. IND: HT emergency. AE: bronchospasm, heart block, HF. PK: Onset=1-2min. Duration=10-20min.
metoprolol tartrate=Lopresor: IND: AFib (rate control). Tartrate salt in Canada not approved for HF. EVD: SR form is cheap, selective, has 24h control, and is indicated for angina, post-MI. PRG: Possibly safe. LAC: Safe. DI: 2D6. PK: t1/2=3-7h with no active metabolites.
nebivolol:
Non-Selective
nadolol=Corgard: EVD: Only BB that increases renal blood flow.
oxprenolol=Trasicor: MOA: Has ISA (intrinsic sympathomimetic activity) which acts like NE to stimulate β receptors which increase HR and BP. May see less cold extremities but rarely used. CI : Angina.
pindolol=Visken: MOA: Has ISA (intrinsic sympathomimetic activity) which acts like NE to stimulate β receptors which increase HR and BP. May see less cold extremities but rarely used. CI : Angina.
propranolol=Inderal: AVL: PO. IND: Tremor, social anxiety. DOS: Anxiety: 10mg 30min before task.
sotalol=Sotacor: AE: BB w/ more risk for: fatigue, exercise intolerance, impotence, nightmares, bronchospasms, vasoconstriction, and glycemic effects.
Non-Selective β & α1 Antagonists
carvedilol: IND: Portal HTN.
labetolol=Trandate: AVL: PO, IV. IND: HT urgency and emergency. CI : HR<60. PRG: Safe. LAC: Safe. PK: *PO*: F=25%. Onset=30-120min. *IV*: Onset=5-10min. Duration=3-6h.
felodipine=Plendil=Renedil: AVL: PO. IND: HT urgency. PK: XL: Peak=2-5h. Duration=24h.
Bile Acid Sequesterants aka Resins
IND: Hyperlipidemia instead or w/ statins. MOA: Binds bile in intestine forcing body to use cholesterol to make more bile. LDL receptors increase. EVD: CHD death NNT=59. Decreases LDL 10-30%, increases HDL 3-10%, increases TG 10-25%. ADM: T 4h before or 1h after meds. AE: N, C, flatulence, bloating, liver toxicity. DI: Binds to many medications.
cholestyramine=Questran: EVD: 1984 Trial showed 24g/d had NNT 59 for CHD death or Non Fatal MI. ADM: T before food. DOS: Start=4g/d. Max=30g/d (divided BID-QID).
colestipol=Colestid: DOS: Start=5g/d. Max=24g/d (divided BID-QID).
colesevelam=Lodalis: ADM: T w/ food. DOS: 1.875 g (3 tabs/1 pkg) BID or 3.75g/d.
Calcium Channel Blockers (CCBs)
Dihydropyridine (DHP)IND: HTN, HT urgency, angina. MOA: Peripheral vasodilation by blocking Ca channels that constrict blood vessels. EVD: Use XR formulation to decrease reflex tachycardia (decreased stroke/MI). Increased sensitivity for elderly and black pts. Less evidence for cardio protection vs diuretics, BBs, and ACEIs. Increased edema and decreased effect on the heart vs. non-DHPs. AE: C, flushing, dizziness, reflex tachycardia, ankle edema, gingival hyperplasia5% (> for males: promote dental hygiene), palpitations, HF. CI : HF. DI: 3A4 (ex. GFJ or fluconazole) increased hypotension. Avoid NSAIDs. AUX: Do not chew/crush XR/XL tabs.
amlodipine=Norvasc: AVL: PO. IND: HT urgency. ADM: Only CCB that can be crushed. PK: Peak=6h. Duration=24h. DOS: 5-10mg/d.
felodipine=Plendil=Renedil: AVL: PO. IND: HT urgency. PK: XL: Peak=2-5h. Duration=24h.
nifedipine=Adalat: IND: HT urgency. EVD: Don’t use IR formulation: Was 1st line but increased evidence of stroke and MI due to uncontrolled BP drop and reflex tachycardia. AE: Shell of tab may be stool. PRG: Safe. LAC: Safe. PK: Peak=2h. Duration=24h.
Non-DHP
IND: AFib (rate control). MOA: Blocks AV node which decreases heart contractility and HR. AE: Bradycardia, edema, constipation, heart block. CI/Warning: Abrupt withdrawal may cause chest pain. CI in HF (decreased EF). DI: 3A4, BBs (slower HR).
diltiazem=Cardizem: EVD: Equal BP efficacy to BBs and diuretics. PRG: Possibly safe. LAC: Safe.
verapamil (VPM)=Isoptin: AE: worst CCB for C PRG: Safe. LAC: Safe.
Cardiac Glycosides
digoxin=Toloxin/Lanoxin: IND: AFib, HF. Often used for sedentary pts and as add on to BB or CCB. MOA: Blocks Na/K ATPase pump. + inotrope (heart pump harder). – chronotrope (decreased HR). EVD: Reduced hospitalization in HF. AE: N, V, D, anorexia, abdominal pain, dizziness, fatigue, weakness, confusion, photophobia, halos, bradycardia, heart block, dysrhythmia. CI: HR<60. PRG: Safe. LAC: Safe. DI: Amiodarone, quinidine, and verapamil (reduce digoxin dose 50%). PK: t1/2=30-40h. Steady state=1week. Large Vd but not affected by obesity (use ideal BW). 70% renal elimination. MON: Trough level done just before next dose. Min 6h after dose. Blood targets: 1-2.5nM in AFib, 0.5-0.8nM in HF. DOS: 0.0625–0.25mg/d.Cholesterol Absorption Inhibitors
ezetimibe=Ezetrol: ezetimibe=Ezetrol: AVL: PO (tab10mg). IND: Hyperlipidemia. MOA: Inhibits cholesterol absorption at brush border. EVD: Decreases LDL 14-25%, increases HDL 1%, decreases TG 7-9%. SHARP trial looked at simvastatin + ezetimibe. ADM: T w/ or without food. AE: D, increased LFTs, muscle/joint pain, cough, fatigue. DOS: 10mg/d OTH: Often used w/ statin.Direct Oral Anticoagulants (DOACs)
Formerly know as New Oral Anticoagulants (NOACs).
apixaban=Eliquis: AVL: PO tabs2.5, 5mg. IND: VTE (prophylaxis + Tx), thromboprophylaxis after hip and knee surgery, AFib. MOA: Reversibly binds active site of factor Xa which slows thrombin generation and reduces fibrin formation. EVD: Only NOAC for CrCl=15-30 but limited evidence w/ CrCl<25. Decreased bleeding vs warfarinARISTOTLE. ADM: T w/ or without food. AE: Bleeding (especially w/ antiplatelet), major bleed2%. CI: Indwelling epidural catheters or recent spinal puncture (hematoma risk). PRG: CI. LAC: CI. DI: 3A4 and PGP inducers/inhibitors. PK: t1/2=12h. F~50%. PB=87-93%. Vd=21L. 27% renal elimination. Met by 3A4/5 (major), 1A2, 2C8, 2C9, 2C19, 2J2 (minor). Doesn’t induce or inhibit CYPs or PGP. MW=459.5g/mol. COS: $337.082017 for 90d supply (180 tabs) of 5mg. MON: CrCl yearly. No anticoagulation monitoring. DOS: *AFib*: 5mg BID. Adj if CrCl<50. *VTE Tx*: 10mg BID x 7d then 5mg BID. *VTE prophylaxis* (>6 months after VTE): 2.5mg BID. *Post Hip/Knee surgery*: 2.5mg BID. Start 12-24h after surgery and continue for 14d (knee) or 35d (hip).
dabigatran=Pradaxa: IND: VTE prophylaxis, AFib. MOA: Inhibits IIa. EVD: Dialyzable (apixaban may be too). Warning/CI: Moisture sensitive (keep in original bottle). CI: CrCl<30, liver failure. DI: Separate antacids by 2h. PK: t1/2=12-17h. 80% renal elimination. Low PB. COS: $346.822017 for 90d supply (180 tabs) of 150mg. DOS: Std=150mg BID. If CrCl 30-49 or >80yo 110mg BID.
edoxaban=Lixiana: AVL: PO tabs15, 30, 60mg. IND: AFib, prevention & Tx of VTE. MOA: Inhibits factor Xa in coagulation cascade which reduces thrombin generation which prolongs clotting time. ADM: T w/ or without food. AE: bleeding, anemia. CI: CrCl<30mL/min, dialysis. COS: $300.522017 for 90d supply of 60mg (60 tabs). DOS: *AFib*: 60mg once/d. *Tx/prevention of VTE*: 60mg once/d after 5-10d of heparin. Usually for>3 months. Consider 30mg/d if CrCl=30-50mL/min or Pt<60kg. OTH: 4th DOAC to be released.
rivaroxaban=Xarelto: AVL: PO (tabs2.5, 10, 15, 20mg ). IND: VTE Tx + prophylaxis, AFib. 2.5mg tab used BID w/ once/d 81mg ASA to prevent stroke and MI. MOA: Inhibits factor Xa in coagulation cascade which reduces thrombin generation which prolongs clotting time. EVD: Less intracranial hemorrhage vs. warfarinROCKET-AF. AE: bleeding, rash and fainting. CI: CrCl<30. PK: t1/2=5-9hrs. 36% renal elimination. Food increases F. Met by 3A4. High PB. COS: $300.522017 for 90d supply of 20mg (90 tabs). DOS: Once/d. OTH: Tabs can be crushed. Dose should be followed with food. Can give via NG tube - crush and suspend in 50mL of water. Flush tube w/ water after administering. Avoid NG admin into distal part of the stomach because this can decrease F.
Direct Renin Inhibitors
aliskiren=Rasilez: IND: 2nd line for HTN. MOA: Prevents renin from converting angiotensin I to angiotensin II (similar to ACEI + ARB). EVD: Add on therapy with little evidence. AE: D, dry cough, increased K. PRG: CI.Direct Thrombin Inhibitors
argatroban: IND: HIT. PK: t1/2= 45min. COS: Expensive. DOS: Adjust for hepatic fxn. Continuous infusion based on wt and aPTT. OTH: Doesn't form anti-Plt antibodies. Prolongs INR. Doesn’t cross react w/ Heparin antibodies.Fibric Acid Derivatives (Fibrates)
IND: Hyperlipidemia (mostly for TGs). MOA: Activates PPAR-alpha, a transcription factor and regulator of lipid metabolism. EVD: Decreases LDL 5-20%, increases HDL 10-35%, decreases TG 20-50%. AE: N, abdominal pain, cholelithiasis, liver toxicity, muscle pain/rhabdo. PRG: CI. LAC: CI. DOS: Adj for renal fxn.benzafibrate=Bezalip: DOS: 400mg/d.
fenofibrate microcoated=Lipidil Supra: DOS: 200mg/d.
fenofibrate nanocrystals=Lipidil EZ:
gemfibrozil=Lopid: DI: Repaglinide. Statins (increased risk of rhabdo). DOS: 600mg BID.
GP IIb/IIIa inhibitors (GPI inhibitors)
IND: Before stenting procedures. MOA: Blocks fibrinogen-mediated cross linking of platelets. EVD: Most trials show benefit when used w/ anticoagulant. Abciximab showed increased mortality (don't use). CI: Active bleed, stroke, major surgery.eptifibatide:
tirofiban:
Heparins
heparin=Unfractionated Heparin (UFH): AVL: IV, SubQ. IND: DVT/VTE, PE, ACS. MOA: Binds ATIII in coagulation cycle. EVD: Preferred anticoagulant in renal impairment. AE: Bleeding, osteoporosis, HIT (flu like symptoms), hair loss, skin necrosis, increased K, hypersensitivity rxn. PK: t1/2~1h. MON: aPTT (q6h after LD and min once/d after). CBC q48h and K q2d. DOS: Dosed in units not mg. OTH: MW 3000-30,000Da. Comes from pork/beef. Antidote=protamine sulfate.Low Molecular Weight Heparins (LMWHs)
IND: VTE (prophylaxis + Tx), ACS. EVD: Less hyperkalemia and osteoporosis vs Heparin. In renal failure heparin is preffered. ADM: Can be given at home. AE: Bleeding, HIT (less), local pain/irritation. PK: Less PB than Heparin (more predictable). MON: baseline cbc, Scr, INR. CBC q2d. Anti-Xa levels done in severe cases. DOS: Once/d or BID. Can’t interchange dosing with heparin. OTH: ~1/3 size of heparin. Protamine reverses IIa effect but not Xa (Partial antidote).
dalteparin=Fragmin: DOS: Units/kg.
enoxaparin=Lovenox: AVL: SubQ. IND: STEMI. DOS: mg/kg.
nadroparin=Fraxiparine: DOS: Units/kg.
tinzaparin=Innohep: DOS: Units/kg.
fondaparinux=Arixtra
Same pentasaccharide sequence as UFH and LMWH but is not considered a heparin (see Indirect Factor Xa Inhibitors)
HMG-CoA Reductase Inhitors aka Statins
MOA: Inhibits HMGcoa reductase which leads to increased LDL receptors in liver. Also stabilizes plaques (useful for secondary prevention after MI). EVD: NNT CV event =60/33 for primary/secondary prevention. Doubling dose reduces LDL 6%. AE: Muscle pain10%, myositis1% (CK>ULN), rhabdomyolysis0.1% (dose dependent where CK>10xULN which can lead to kidney failure – watch for dark urine), liver toxicity (ALT/AST >3xULN)1%, indigestion, HA, impotence, T2DM9% RRI. For every T2DM case, 10 CV events are avoided. PRG: CI. LAC: CI. PK: Cell uptake by OATP transporters except fluvastatin. DOS: Can be fixed or based on LDL target (<2mM or 50% reduction). OTH: Inhibits CoQ10 (important for muscle fxn). Primary prevention adherence rate is only 30%.atorvastatin=Lipitor: AVL: PO tab10, 20, 40, 80mg. EVD: Decreases total cholesterol 29-45%, decreases LDL 39-60%, increases HDL 5-9%, decreases triglycerides 19-37%. ADM: T w/ or without food. AE: D11%, joint pain10%, nasopharyngitis13%, N, stomach upset, increased BG, muscle pain, jaudince. CI: Liver disease. DI: 3A4 inhibitors ex. clarhithromycin (risk of rhabdo). PK: Metablolized by 3A4. DOS: Once/d. No dose adj for kidney fxn. *Primary prevention*: 10mg/dASCOTT LLA. *Secondary prevention*:10mg/dALLIANCE. 80mg/dMIRACL/PROVE-IT/TNT(compared vs 10mg)/IDEAL. *Pts >75yo*: usual max=20mg/d.
fluvastatin=Lescol: EVD: Decreases total cholesterol 20%, decreases LDL 25-34%, increases HDL 7%, decreases triglycerides 10-23%. PK: Metablolized by 2C9. DOS: Secondary prevention: 40mg BIDLIPS. OTH: Not commonly seen.
lovastatin=Mevacor: EVD: Decreases total cholesterol 18-34%, decreases LDL 20-40%, increases HDL 5-15%, decreases triglycerides 10-20%. DI: 3A4 inhibitors (ex. gemfibrozil). PK: Metabolized by 3A4. DOS: Primary prevention: 20-40mg/dAFCAPS/TexCAPS.
pravastatin=Prevachol: EVD: Decreases total cholesterol 17-27%, decreases LDL 20-40%, increases HDL 5-15%, decreases triglycerides 10-20%. PK: Less CYP metabolism vs other statins. DOS: *Primary Prevention*: 10-20mg/dMEGA 40mg/dWOSCOPS/ALLHAT. Secondary prevention: 40mg/dCARE/LIPID.
rosuvastatin=Crestor: EVD: Decreases total cholesterol 33-46%, decreases LDL 45-63%, increases HDL 13%, decreases triglycerides 28-35%. PK: Less CYP metabolism vs other statins. DOS: Primary prevention: 20mg/dJUPITER.
simvastatin=Zocor: EVD: Decreases total cholesterol 21-33%, decreases LDL 20-40%, increases HDL 5-15%, decreases triglycerides 10-20%. DI: 3A4 inhibitors (ex. gemfibrozil). PK: Metabolized by 3A4. DOS: Secondary Prevention: 20-40mg/d4S. 40mg/dHPS. 80mg/d associated w/ increased muscle problemsSEARCH.
Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channel Blockers
ivabradine: IND: HF w/ EF <35%, angina. MOA: Reduces HR by blocking funny channel in SA node. ADM: T w/ food (F increases 30% w/ food). AE: Enhanced brightness14.5%, bradycardia, HA, dizziness. DI: 3A4 inhibitors. PK: t1/2=6h. F~40%. COS: ~$100 for 3 months. DOS: Not studied CrCl<15mL/min. No dose adj >15mL/min. Std=5mg/d (once/d or 2.5mg BID). Max=7.5mg/d. Adj to target HR=50-60bpm. OTH: Not commonly seen.Indirect Factor Xa Inhibitors
fondaparinux: AVL: SubQ. IND: VTE (Tx + prophylaxis), post surgery, ACS. MOA: Potentiates ATIII ~300x which selectively inhibits Xa. AE: Increased bleeding, osteoporosis. CI: CrCl <30mL/min. PK: t1/2=20hrs. PB=0. MON: Xa assay if necessary. DOS: Once/d. OTH: No risk of HIT. Not reversed by protamine like Heparin.Loop Diuretics
furosemide=Lasix: IND: Edema, HF, HTN w/ kidney failure. ADM: T in the am (makes you pee). AE: orthostatic hypotension, increased urination, decreased: Ca, Na, K. Can affect BG levels. PK: t1/2=6h (Lasix).Nitrates
nitroglycerine (NTG): AVL: Patch NitroDur=Minitran=Transderm-Nitro, SL spray Nitroligual, SL tabs Nitrostat , IV. IND: Angina, ACS. SL spray can be used prophylactically before exercise. IV used for HT emergency. MOA: Dilates blood vessels in the heart. ADM: Stop activity and sit down if experiencing angina. *Patch*: T off patch hs and place new one in am (less tolerance to the drug and low risk of angina while sleeping). Rotate site to avoid irritation. Apply to dry skin anywhere except below knee, on skin folds, injured site (chest preferred). Applied like a Band-Aid without touching sticky surface. Don’t cut or reuse. *SL spray*: prime but don't shake. AE: HA, facial flushing, syncope, dizziness, fainting, hypotension, tachycardia. CI: severe aortic stenosis. DI: Viagra, Cialis etc. PK: *Patch*: Onset=30-60min. Duration=variable. *SL spray*: Onset<2min. Duration=up to 30min. *SL tabs*: Onset<2min. Duration=up to 30min. *IV*: Onset=2-5min. Duration=5-10min. DOS: *SL spray*: 1 spray (0.4mg) q5 min Rx2. Call 911 if no resolution after 2nd spray. OTH: Doesn’t prevent or reverse MI. SL tabs rarely seen because of short expiry.Potassium-Sparing Diuretic
spironolactone: IND: HTN, HF. EVD: Decreased mortality if added on after ACEi + BB for systolic HFRALES. AE: increased K, breast enlargement.Thiazide/Thiazide-Like Diuretics
ADM: T in am (makes you pee). hydrochlorothiazide (HCTZ)=Hydrodiuril: EVD: Preferred thiazide for HTN. First among equals vs ACEI + CCB. Less effective if Cr<30 (use loop). Effective in elderly and black pts. AE: N, V, rash, orthostatic hypotension, photosensitivity, impotence1%, muscle cramps, weakness, decreased K, decreased Na, increased Ca, decreased Mg, increased cholesterol, increased uric acid (gout1%), increased BG. LAC: Safe.chlorthalidone=Hygroton: AVL: PO tab50,100mg. PK: t1/2=40-80h.
indapamide=Lozide:
Thrombolytics
alteplase (TPA): IND: STEMI. EVD: Vs TNK, TPA is less expensive, more non-cerebral bleeding, worse 30d mortality for pts treated >4h after symptoms. DOS: Max=100mg in 90min.tenecteplase (TNK): AVL: IV. IND: STEMI. EVD: Vs TPA, TNK is easier, more $, has less non-cerebral bleeding, improved 30d mortality if pts treated >4h after symptom onset. CI: Past intracranial bleed, head trauma/surgery within 3 months. DOS: Ideally given within 30min of entering hospital.
Vasodilators
hydralazine=Aprezoline: AVL: PO, IV. IND: HT urgency and emergency, HF (in black pts). AE: Reflex tachycardia, lupus like syndrome. PK: *PO*: Onset=20-30min. Duration=8h. F=50%. *IV*: Onset=10-20min. Duration=12h.Vitamin K Antagonists
warfarin=Coumadin: IND: VTE/PE, AFib, valve replacement. MOA: Inhibits vitamin K dependent clotting factors: 2, 7, 9, 10 and proteins C+S. ADM: T at same time of day. INR testing usually in am so hs dosing is more convenient for dose adj. AE: N, D, cramping, bleeding, purple toe syndrome, skin necrosis. PRG: CI. DI: Cholestyramine (inhibits F), septra, metronidazole (inhibit met), rifampin, carbamazepine (induces met), celebrex/NSAIDs, garlic (antiplatelet), American ginseng (decreases INR), cranberry (increased INR). PK: S enantiomer more active. F~100%. R met by 1A2. S met by 2C9. MON: INR q2d, then q7d, q14d, q28d, max=12 weeks. DOS: INR dose adj: [INR<2=increase weekly dose 5-15%]. [INR:2-3=no dose change]. [INR: 3.1-3.5=decrease weekly dose 5-15%]. [INR:3.6-4=hold 0-1 doses and decrease weekly dose 10-15%]. [INR>4=hold 0-2 doses and decrease weekly dose 10-15%] OTH: Keep consistent vitamin K diet/supplement. Limit alcohol. Avoid contact sports. Overlap with heparin/LMWH/fondaparinux at >5d and INR>2 for 24h.Acetylcholine Esterase Inhibitors (AChEI)
Aka cholinesterase inhibitors. EVD: May stabilize dementia & behavior and decrease visual hallucinations in Lewy Body dementia. AE: N, V, D, muscle cramps, insomnia, syncope, nightmares. DI: Can inhibit anticholinergic drugs. DOS: Restart at low dose if off drug for >3d. Taper for 1w if D/C. OTH: 3-6 months of Tx for modest benefit.donepezil=Aricept: AVL: PO. IND: Mod-severe Alzheimer’s, PD dementia. AE: N11%, D10%, V5%, insomnia9%, fatigue5%, muscle cramps6%, anorexia4%, dizziness8%, depression3%. Known QT prologation. PK: t1/2=70h. F~100%. DOS: Start=5mg/d. Max=10mg/d (consider after 4-6w).
galantamine=Reminyl: AVL: PO. IND: Mild-mod Alzheimer’s. ADM: T w/ food in am. AE: N24%, V13%, D9%, HA8%, fatigue5%, dizziness9%, indigestion5%, anorexia9%, depression7%. HC Warning: Potential to cause SJS. PK: t1/2=6h. DOS: Start=8mg/d x4w. Maint=16mg/d. Max=24mg/d (if std dose tolerated for 4w).
rivastigmine=Exelon: AVL: PO, topical (patch). IND: Mild-moderately severe Alzheimer’s, Lewy Body Dementia, PD dementia. AE: *PO*: N23%, V17%, D5%, weakness6%, anorexia5%, dizziness7%, HA6%, depression4%. *Patch*: N21%, V19%, D10%, abdominal pain4%, anorexia4%, dizziness7%, insomnia4%. PK: t1/2=2h.
Anticholinergics
IND: Restore DA/acetylcholine balance in Parkinson's. EVD: Useful for tremor, foot dystonia, and drooling. AE: Dry mouth, C, urinary retention, hyperthermia, confusion, sedation, worsening glaucoma. Warning: Avoid in elderly. DI: amantadine (also has anticholinergic effect).benztropine=Cogentin: AVL: PO, injection. DOS: PD: 1-2mg BID.
ethopropazine=Parsitan: AVL: PO. DOS: PD: Initial=25mg BID. Max=50mg TID.
procyclidine=Kemadrin: AVL: PO (tab, elixir). DOS: Adj for renal fxn. PD=5mg TID
trihexyphenidyl=Artane: AVL: PO. DOS: Adj for renal fxn. PD: Initial=1mg BID. Std=2mg TID.
Anticonvulsants aka Antiepileptics
brivaracetam=Brivlera: AVL: PO. IND: Epilepsy.carbamazepine=Tegretol: AVL: PO (tab200mg, CR tab200, 400mg, liq20mg/mL, chewtab100, 200mg). IND: Bipolar, epilepsy. AE: Rash5-10%. PK: t1/2=35-40h then 12-17h after 2w of use. F=85%. PB=70%. Vd=1L/kg. Cleared hepatically. Metabolized by 3A4. Induces 3A4, 2D6. MON: Serum level=17-50uM. DOS: *Bipolar*: Initial=100mg BID. Std=800-1200mg/d divided BID-QID. Max=1600mg/d. *Epilepsy*: Initial=100mg BID. Increase by 200mg/d q3–4d. Usual maintenance: 400–1200mg/d in 2–4 divided doses, with meals when possible.
divalproex=Epival: AVL: PO. IND: Bipolar, epilepsy. MON: Serum level=350-800uM. DOS: *Bipolar*: 750-2000mg/d adj to serum levels. *Epilepsy*: Initial=250mg BID. Increase by 250mg/d q3–4d. Std=750–1000mg/d in 2 divided doses.
eslicarbamazepine=Aptiom: AVL: PO. IND: monotherapy for partial-onset seizures. DOS: Adj for renal fxn. Epilepsy: Initial=400 mg once/d × 1w. Std=800-1200mg once/d. Max=1600mg once/d (monotherapy).
ethosuximide=Zarontin: AVL: PO (cap, syrup50mg/mL). IND: Absence seizures. AE: GI upset. DOS: Initial=500mg/d in 1 or 2 divided doses. Increase by 250 mg/d q4–7d. Std=750–1000mg/d.
gabapentin=Neurontin: AVL: PO. IND: Bipolar (not 1st line), neurological pain. AE: Tremor, vision changes. DOS: Adj for renal fxn. Max=4g/d. *Epilepsy*: Initial=300mg once/d. Increase by 300mg/d q5–7d up to 300 mg TID, then titrate TID dose. Std=900–3600mg/d divided Q6–8H. OTH: GABA derivative.
lacosamide=Vimpat: IND: Epilepsy.
lamotrigine=Lamictal: AVL: PO (tab25, 100, 150, 200mg, chewtab2, 5, 25mg). IND:Bipolar (maintenance & depression), epilepsy. AE: Cog impairment, dizziness, ataxia (loss of control of movements), sedation, HA, diplopia, N, V, rash10% (can be serious). DI: Valproic acid significantly inhibits lamotrigine’s clearance (often used together). PK: t1/2=25h. MON: No blood level monitoring. DOS: Adj for renal and hepatic fxn. *Bipolar*: Initial=12.5-25mg qhs. Std=50-250mg divided BID. Max=250mg/d. *Epilepsy*: Initial=25mg q2d to 50 mg/d x 2w. Then same dose BID × 2w. Then increase by 100mg/d at 1-2-w intervals. Std=200–400mg/d in 2 divided doses. OTH: No antidote for overdose.
oxcarbazepine=Trileptal: AVL: PO. IND: Epilepsy.
perampanel=Fycompa: AVL: PO. IND: Epilepsy.
phenytoin=Dilantin: AVL: PO, IV. IND: Partial and tonic-clinic seizures. MOA: Blocks Na channels. AE: Gingival hyperplasia, rash5-10%, PK: t1/2=7-42h (non-linear kinetics). F~1. PB=90%. Vd=0.7L/kg. Salt Factor (S)=0.92 for caps and injection. S=1 for infatabs. 95% eliminated by the liver. Cleared mainly by 2C9 but also 2C19. Follows Michalis Menten kinetics. DOS: Loading dose=20mg/kg (used adjusted wt if obese).
pregabalin=Lyrica: AVL: PO. DOS: Adj for renal fxn. Anxiety: Initial=150 mg/d divided BID or TID. Can increase to 150mg BID after 1w.
rufinamide=Banzel: AVL: PO. IND: Epilepsy.
stiripentol=Diacomit: AVL: PO. IND: Epilepsy.
topiramate=Topamax: AVL: PO. IND: Epilepsy.
valproic acid=Depakene: AVL: PO (cap250, 500mg, liq50mg/mL). IND: Bipolar, epilepsy. AE: N, D, sedation, thrombocytopenia, leukopenia, hair loss, wt gain, menstrual disturbances, polycystic ovaries, encephalopathy. PK: t1/2=6-16h. F=90%. Cleared hepatically. Inhibits 2C9. MON: Plasma level=350-700uM. DOS: *Bipolar*: Initial=250mg BID. Std=1000-3000mg divided BID or TID. Max=60mg/kg. *Epilepsy*: Initial=250mg BID. Increase by 250mg/d Q3–4d as necessary. Std=750–1000mg/d in 2–4 divided doses.
vigabatrin=Sabril: AVL: PO. IND: Epilepsy. DOS: Initial=1000 mg/d in 1–2 divided doses. Std=2000–4000mg/d in 1–2 divided doses.
Antipsychotics
IND: Schizophrenia, bipolar, delirium, Tourette’s, PTSD, ADHD w/ aggression. EVD: All FGAs and SGAs (except clozapine), have similar efficacy for positive/psychotic symptoms. SGAs may be better for negative symptoms, mood and cognitive deficits. AE: Sedation, weight gain, neuroleptic Malignant Syndrome (NMS) (keep hydrated to avoid), insomnia, extrapyramydal symptoms (EPS), tardive dyskinesia, hyperprolactinemia, hypotension, anticholinergic AEs. OTH: Low potency antipsychotics tend to cause sedation while high potency causes EPS. Switching antipsychotic res: *Psychiatry.net* and *SwitchRx* (free but need to register).★First-Generation Antipsychotis (FGAs) aka Typical, Traditional, Conventional ★
chlorpromazine=Largactil: AVL: PO,IM. PK: t1/2=30h. DOS: Equivalence (vs olanzapine 20mg)=600mg. Start=100mg/d. Maint=300-600mg/d. Max=800mg/d. Divided HS-TID.
flupentixol=Fluanxol: AVL: PO. PK: t1/2=35h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=3mg/d. Maint=6-12mg/d. Max=18mg/d. Divided HS-BID.
fluphenazine=Moditen: AVL: PO. PK: t1/2=13-33h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=2.5mg/d. Maint=5-15mg/d. Max=20mg/d. Divided HS-BID.
haloperidol=Haldol: AVL: PO, IM (haloperidol decanoate). PK: *PO*: t1/2=20h. *IM*: t1/2=3w. DOS: *PO*: equivalence (vs olanzapine 20mg)=30mg. Start=0.5-1mg/d. Maint=1-5mg/d. Max=10mg/d. Divided HS-BID. *IM*: equivalence (vs olanzapine 20mg)=5.4mg. Start=50mg. Maint=50-150mg. Max=200mg. Given q4w.
loxapine=Loxapac=Xylac: AVL: PO, IM. PK: t1/2 (of active metabolite)=5-19h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=10-20mg/d. Maint=20-100mg/d. Max=200mg/d. Divided HS-TID.
methotrimeprazine=Nozinan: AVL: PO, IM. PK: t1/2=30h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=50mg/d. Maint=100-300mg/d. Max=500mg/d. Divided HS-TID.
perphenazine=Trilafon: AVL: PO (tab, liquid). PK: t1/2=9-21h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=8mg/d. Maint=12-24mg/d. Max=40mg/d. Divided HS-BID.
pimozide=Orap: AVL: PO. PK: t1/2=29-55h. DOS: equivalence (vs olanzapine 20mg)=30mg. Start=2mg/d. Maint=4-6mg/d. Max=10mg/d. Divided BID.
thiothixene=Navane: AVL: PO. PK: t1/2=34h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=5mg/d. Maint=15-30mg/d. Max=40mg/d. Divided HS-BID.
trifluoperizine=Stelazine: AVL: PO (tab,liquid). PK: t1/2=7-18h DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=5mg/d. Maint=10-20mg/d. Max=40mg/d. Divided HS-BID.
zuclopenthixol=Clopixol: AVL: PO. ADM: T HS. PK: t1/2=20h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=20mg/d. Maint=20-60mg/d. Max=80mg/d. Not divided.
★★ Second-Generation Antipsychotis (SGAs) aka Atypical or Novel ★★
AE: Can affect BG levels. OTH: Have greater 5-HT affinity relative to D2.
aripiprazole=Abilify: AVL: PO (SL), IM (long acting). IND: Bipolar. MOA: Has slightly different binding affinities vs other SGAs. Partial agonist at D2 and 5-HT1A and potent antagonist at 5-HT2A. EVD: Potentially effective for negative and depressive symptoms. ADM: T w/ or without food in am (stimulating). Don’t eat/drink for 10min after taking SL. PK: t1/2 (of active metabolite)=75-94h. DOS: Equivalence (vs olanzapine 20mg)=30mg. Start=10mg/d. Maint=15-30mg/d. Max=30mg/d. Not divided.
asenapine=Saphris: AVL: PO (SL). IND: Bipolar. MOA: Has slightly different binding affinities vs other SGAs. Potent antagonist for many 5-HT and DA receptors. ADM: SL: Don’t eat or drink for 10min. PK: t1/2 =24h. DOS: Start=10mg/d. Maint=10-20mg/d. Max=20mg/d. Divided BID.
clozapine=Clozaril: AVL: PO. MOA: Weak D2 antagonist. EVD: Only antipsychotic w/ efficacy for Tx resistant schizophrenia. Used after 2 failed antipsychotics due to risk of agranulocytosis and need for blood monitoring. AE: agranulocytosis1.3% PK: t1/2=14h. MON: Clozapine level: clozapine+desmethylclozapine=total clozapine. Lower limit=1050nM. Upper limit=N/A. DOS: Equivalence (vs olanzapine 20mg)=4000mg. Start=25mg/d. Maint=200-500mg/d. Max=800mg/d. Divided HS-TID.
lurasidone=Latuda: AVL: PO. IND: Bipolar (depressive episode). ADM: T w/ meal >500Cal (to increase F). PK: t1/2=18h. DOS: Start=40mg/d. Maint=40-80mg/d. Max=160mg/d. Once/d (not divided). OTH: Minimal effect on weight, glucose, cholesterol, TG.
olanzapine=Zypexa: AVL: PO, IM. IND: Bipolar. PK: t1/2=21-54h. DOS: Start=5mg/d. Maint=10-20mg/d. Max=30mg/d. T HS.
paliperidone=Invega: AVL: PO, IM. IND: Bipolar. ADM: T w/ or without food HS. PK: *PO*: t1/2=23h. *IM*: t1/2=25-49d. DOS: *PO*: equivalence (vs olanzapine 20mg)=9mg. Start=3mg/d. Maint=6-9mg/d. Max=12mg/d. Not divided. *IM*: Start=150mg (then 100mg on day 8). Maint=25-150mg. Max=150mg. OTH: Paliperidone is an active metabolite of risperidone.
quetiapine=Seroquel: AVL: PO (IR and ER). IND: GAD, bipolar. PK: t1/2 (of active met)=6-12h. DOS: Equivalence (vs olanzapine 20mg)=750mg. *Bipolar*: Std=300mg/d. Max=600 mg/d. *GAD*: Start=50mg/d. Maint=150mg/d. Max=400mg/d. *Other*: Start=100mg/d. Maint=400-800mg/d. Max=1000mg/d. Divided HS-BID.
risperidone=Risperdal: AVL: PO, IM (Risperidal Consta). IND: ADHD. PK: *PO*: t1/2 (of active met)=20-24h. *IM*: t1/2=3-6d. DOS: *PO*: Equivalence (vs olanzapine 20mg)=6mg. Schizophrenia: Start=1mg/d. Maint=4-6mg/d. Max=8mg/d. Divided HS or BID. *ADHD*: Initial=0.25–0.5 mg HS. Increase weekly by 0.5 mg/day prn. Std=0.75–1.5 mg/d. *IM*: Equivalence (vs olanzapine 20mg)=3.6mg. Start=25mg. Maint=25-50mg. Max=50mg. Given q2w.
ziprasidone=Zeldox: AVL: Avail PO. IND: Bipolar. MOA: Unlinke other SGAs, has antagonist activity at 5-HT1D. EVD: First SGA to not be associated w/ significant wt gain. ADM: T w/ meal >500Cal (doubles F). PK: t1/2=6-10h. DOS: Equivalence (vs olanzapine 20mg)=160mg. Start=40mg/d. Maint=120-160mg/d. Max=200mg/d. T once/ in am or divide BID.
Azapirone
buspirone=BuSpar: AVL: PO (tab10mg). White splitable tab. Brand not availableNS. IND: GAD, anxiety w/ Hx of aggression or if benzos cause disinhibition. MOA: 5-HT1A receptor agonist on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus. This slows the firing rate of the neurons in the dorsal raphe. Buspirone also binds and blocks at DA2 presynaptic receptors. It also causes increased firing in the locus ceruleus. Net result is 5HT activity is suppressed while NE and DA cell firing is enhanced. EVD: Similar efficacy vs benzos without risk of dependence. Less sedation vs benzos. Anxiolytic effect can be after days but max Tx effect after >3w. Pts 6–17yo w/ GAD taking 7.5–30mg BID x 6w found no more effective vs placebo. ADM: T w/ or without food consistently (not prn). AE: Dizziness12% , drowsiness10%, common AE (1-10%): Numbness, HA, tremor, fainting, seizures, tachycardia/chest pain, rash, sweating, N, dry mouth, upset stomach, D, C, V, muscle ache, tinnitus, sore throat, insomnia, nervousness, excitement, anger/hostility, confusion, depression, sleep disturbances. PRG: FDA cat B. LAC: Distributed into milk in rats. Avoid if possible. DI: MAOIs, 3A4 inhibitors. PK: t1/2=2-4h. Tmax=40-90min. F=4%. PB=86–95% Metabolized by 3A4. Excreted mainly as metabolites in the urine (mostly) adn feces. COS: Expensive vs other antidepressants. DOS: Adj for hepatic and renal fxn. Start=5 mg BID or TID. Increase by 5mg/d q2–4d prn. Max=60mg/d divided Bid or TID. OTH: Not well studied <18yo. Has been used in pts 6–17yo w/ GAD without unusual AEs.Barbiturates
phenobarbital=Phenobarb: AVL: PO. IND: Epilepsy. AE: Sedation, rash5%, depression, decreased libido. PK: Potent CYP inducer. DOS: Epilepsy: 90-120mg once/d at HS.primidone: AVL: PO. IND: Epilepsy. AE: Sedation, rash5%, depression, decreased libido. PK: Gets metabolized to phenobarbital. Potent cyp inducer. DOS: Epilepsy: Initial=125mg HS × 3d then 125mg BID × 3d then 125mg TID × 3d. Std=500–1000mg/d in 3–4 divided doses.
Benzodiazepines aka Benzos
MOA: Binds to GABAA receptors.alprazolam=Xanax: DI: fluvoxamine, grapefruit juice, ketoconazole, nefazodone, theophylline.
bromazepam:
clobazam=Frisium: AVL: PO. IND: Epilepsy. AE: Irritability, depression. DOS: Epilepsy: Initial=5–15mg/d at HS. Std=20–40mg/d once/d or divided BID.
clonazepam=Rivotril=KlonopinUSA: AVL: PO. IND: GAD, panic, agoraphobia. AE: Sedation/fatigue, hallucinations, lightheadedness, Fatigue often lessens w/ time as body gets used to medication. CI: Myasthenia Gravis, closed angle glaucoma. PK: t1/2=20-80hrs. time to peak=1-2hrs. DOS: ANXIETY=0.25–0.5mg BID. SEIZURE:0.5mg TID. Max=20mg/d.
diazepam:
flurazepam:
lorazepam=Ativan: AVL: PO (tab0.5, 1, 2mg),SL, IV. IND: Anxiety (airplane, panic attack), akathesia, agitation, social phobias. AE: sedation, decreased cognition, memory impairment, repiratory depression, confusion, muscle weakness, HA, anticholinergic, sexual dysfunction, gynecomatia, D/C syndrome. CI: Sleep apnea. PK: Short acting vs other benzos. DOS: *Anxiety*: 1-10mg/d divided BID or TID. *Insomnia*: 1-4mg HS.
midazolam:
nitrazepam=Mogadon: AVL: PO. IND: Epilepsy.
oxazepam:
temazepam:
triazolam:
Catechol-O-Methyl Transferase (COMT) Inhibitors
IND: Parkinson's pts w/ wearing off. MOA: Inhibits the COMT enzyme which breaks down levodopa in periphery. Only beneficial if given w/ levodopa. DOS: Reduce levodopa dose 10-30% when starting COMT inhibitor (risk of dyskinesia).entacapone=Comtan: AVL: Avail PO (tab200mg). ADM: T w/ each Levodopa dose. AE: Orange urine and skin discoloration, N, V, D. AUX: Don't crush. DOS: 100 or 200mg w/ each dose of levodopa. Max=1.6g/d.
tolcapone=Tasmar: AVL: PO (tab200m) SAP only. Pts must already been taking (hepatotoxic).
Cholinesterase Inhibitors
IND: Mild-moderate dementia. EVD: All 3 appear to be equally effective. AE: N, D, HA, V, syncope, insomnia/nightmares, agitation, leg cramps, urinary incontinence.donepezil=Aricept: IND: May be used in mod-severe dementia. Black Box Warning: Neuroleptic malignant syndrome and rhabdomyolosis. DOS: Initial=5mg/d x 4-6w. Target=10mg/d.
galantamine=Reminyl: Black Box Warning: SJS. DOS: Initial=8mg/d x 1-2w. Target=16mg/d. Max=32mg/d.
rivastigmine=Exelon: AVL: PO, Patch. IND: Lewy Body Dementia. DOS: *PO*: Initial=1.5mg BID x 2w & increase 1.5mg per dose x 2w. Target=3mg BID. Max=6mg BID. *Patch*: Placed and removed q24h. If naïve: Patch 5 x 4w. Target=Patch 10. Conversion from oral to patch: If oral dose <6mg/d use patch 5. If oral dose=6-12mg/d use patch 10. Apply 1st patch the day after the last oral dose.
CNS Stimulant (Miscellaneous)
modafinil=AlertecCAN=ProvigilUS: AVL: Avail PO (tab100mg). IND: Insomnia, ADHD (not approved). DOS: Initial=100mg/d. Std=200-400mg/d. Max=400mg/d. OTH: Not classified as controlled substance like other stimulantsCAN (reg schedule I)DOPA Decarboxylase Inhibitors
IND: Parkinson's. ADM: Given w/ levodopa to increase distribution to brain and decrease N, V. OTH: Doesn’t cross BBB.carbidopa:
benserazide:
pergolide: AVL: Only through SAP. Withdrawn due to cardiac valvulopathy.
Dopamine Agonists
IND: Single thereapy in early Parkinson's and w/ levodopa for later stages. Often preferred for younger patients (<50-70yo) MOA: Activates DA receptor. Doesn’t slow disease progression. EVD: Less motor complications than L-dopa but more hallucinations. AE: Reward seeking behavior, N, dizziness, sleep attacks, confusion, hallucinations, C, Edema, orthostatic hypotension. Can give w/ domperidone to decrease N. DI: SSRIs and MOIs increase risk of serotonin syndrome but less than levodopa. DOS: Increase dose q4-6w.bromocriptine: DOS: Parkinson's: Initial=1.25mg BID. Std=5–10mg TID. OTH: Ergot/fungal derivative.
pergolide: AVL: Withdrawn in Canada2007 due to association w/ cardiac valvulopathy.
pramipexole=Mirapex: AVL: PO. IND: Parkinson's RLS. DOS: Adj for renal fxn. Initial=0.125mg TID. Usual=0.5–1.5mg TID. Max=1.5mg TID.
ropinirole=ReQuip: IND: Parkinson's RLS. PK: Metabolized by CYPs.
rotigotine=Neupro: AVL: Patch. ADM: Can be applied to belly, thigh, hip, flank, shoulder, upper arm. Avoid same site twice within 2w. CI: skin disease. DOS: Initial=2mg/24h. Maint=6-8mg/24h. Max=16mg/24h. Can increase dose weekly.
Dopamine Precursor
levodopa=L-DOPA: IND: Parkinson’s. MOA: Gets converted to DA in the CNS by dopa decarboxylase. EVD: Delaying use can preserve its effectiveness (especially in young pts). Improves: tremor, rigidity, bradykinesia. ADM: Needs to be given w/ DOPA decarboxylase inhibitors to enhance distribution to brain and decrease N, V. Don’t T w/ protein (decreased F). AE: N, V, anorexia, hallucination, night mares, increased libido, dyskinesia50% at 5y, decreased BP, psychosis. DI: MAOI (hypertensive crisis), serotonergic drugs (serotonin syndrome), Fe (decreased F). Amino acids from protein compete for F in gut and through BBB (F decreases 30% w/ meal). PK: *IR*: Onset=30min. Duration=4h. *CR*: Onset=1-3h. Duration=5h. DOS: Start=100mg/d. Maint=300-2000mg/d. Can be divided 6x/d. Increase dose 20-30% if going from IR to CR (Less F w/ CR). Avoid abrupt withdrawal. Increase frequency if wearing off effect. OTH: Levodopa crosses BBB.Lithium Salts
lithium carbonate=Carbolith=Litane=Duralith(ER)=Lithmax(CR): AVL: PO (cap150, 300, 600mg, ER tab300mg). MOA: Increases the release of 5HT and possibly increases the reuptake of NE. EVD: Starts to work in 1-2w. Reduces risk of suicide in people with bipolar disorder. AE: Memory loss, problems creating new memories, blunting emotions (ex. not feeling happy at party or not feeling sad at funeral), tremor, N, V, D, polyuria/polydipsia, increased K, kidney & thyroid toxicity, acne, psoriasis, wt gain. Possible QT prologation. DI: Increased [Li] with NSAIDs, Ca channel blockers, ACEi, ARBs, low Na. PK: t1/2=20-26h. PB=0. Cleared renally. MON: Serum levels=0.8-1.1mM (geriatric=0.4-0.6mM). Measure 9-13h after first dose. DOS: Initial=300mg BID. Then adj based on levels. IR divided once/d-TID. ER divided once/d or BID. OTH: Maintain consistent salt diet.lithium citrate: AVL: PO (liq60mg/mL). IND: Bipolar. PK: t1/2=20-26h. PB=0. Cleared renally. DOS: Initial=5mL BID. Then adj based on levels. Divided once/d-TID.
Monoamine Oxidase Inhibitors (MAOIs)
MOA: Irreversibly inhibits MAO which is an enzyme that metabolizes 5HT, noradrenaline, DA. AE: Common: Dizziness/lightheadedness, weight gain/fluid retention, sexual dysfunction, insomnia. DI: Serotonergic drugs like SSRIs (serious risk of serotonin syndrome). DA agents like levodopa can cause hypertensive crisis. Foods w/ tyramine can cause hypertensive crisis ex: Aged cheese, cured meats, tap beer, marmite, fava beans, soy products, beer/wine in moderation. OTH: Switching antidepressants res: *Psychiatry.net* and *SwitchRx* (free but need to register).phenelzine=Nardil: IND: Panic, agoraphobia. DOS: Anxiety=45–90mg/d.
tranylcypromine=Pamate:
Monoamine Oxidase-B (MAO-B) Inhibitors
IND: Parkinson's. Often used early in Parkinson's to decrease need/dose of L-dopa. MOA: Irreversibly inhibits monoamine oxidase B (enzyme that metabolizes DA in the brain). DI: SSRIs, SNRIs, TCAs, MAOIs (serotonin effect), meperidine, DM, alpha-agonists. PK: Can be metabolized to amphetamine metabolite.rasagiline=Azilect: AVL: PO (tab0.5, 1mg). EVD: 5-10x more potent vs selegiline. AE: HA, arthralgia’s, dyspepsia, depression, orthostatic hypotension. DOS: Adj for hepatic fxn. PD: Monotherapy: 1mg/d. Multitherapy=0.5-1mg once/d. OTH: 2nd Generation MAO-B.
selegiline=Emsam: aka L-deprenyl. AVL: PO (tab5mg). AE: Insomnia, agitation, N, dizziness, orthostatic hypotension, rash. PK: Has amphetamine metabolite causing stimulant like AEs. DOS: 2.5-5mg once/d. OTH: 1st generation MAO-B.
N-Methyl-D-Aspartate (NMDA) Antagonist
amantadine=Symmetrel: AVL: PO (tab100mg or syrup10mg/mL). IND: Parkinson's (early for tremor and late for dyskinesia). AE: Confusion, nightmares, insomnia, anticholinergic effects. DOS: Adj for renal fxn. PD: Initial=100mg/d. Maint=100mg BID or TID. Max=200mg BID. Give 2w trial to evaluate efficacy.memantine=Ebixa: AVL: PO. IND: Mod-severe Alzheimer’s. EVD: May help with agitation/aggression. AE: Dizzy, drowsy, confusion. Caution if: Hx of seizures or heart disease. DOS: Dementia: Initial=5mg/d. Increase by 5mg/d at weekly intervals. Target=10mg BID at week 4. OTH: Can be used w/ cholinesterase inhibitors.
Noradrenaline-Dopamine Reuptake Inhibitor (NDRI)
OTH: Switching antidepressants resource: *Psychiatry.net* and *SwitchRx* (free but need to register). bupropion=Wellbutrin=Zyban: AVL: PO (XR tab150,300mg). IND: ADHD, depression, seasonal affective disorder, smoking cessation. Zyban only used for smoking cessation. MOA: Inhibits the reuptake of NE and DA. No effect on 5HT. EVD: Not very effective for anxiety. No sexual AEs. Can delay weight gain. May be more effective with an NRT patch. Smoking cessation efficacy=19%. ADM: T w/ or without food. Typically in the am (stimulating). D/C syndrome less frequent w/ bupropion vs other antidepressants but still need to taper. AE: HA30% rapid HR11% N, V insomnia25%, agitation17% dizziness15% , sweating22%, weight loss22% C15% irritability, restlessness, dry mouth, dry skin, rash, blurred vision, tremor, seizures0.5-1%. CI: Seizure disorder, heavy drinking, bulimia/anorexia, past stroke or head trauma. DI: EtOH decreases seizure threshold. PK: t12/=21h. Metabolized by and inhibits 2B6. XL tabs given q24h while XR q8h. AUX: Don't crush/chew. DOS: Smoking Cessation: Start 1-2w before quit date. 150mg OD x 3d then BID x 7-12w. ADHD: Initial=2–3mg/kg/d. Std=200–300 mg/d divided in 2 doses. Single dose max=150mg. Decrease dose for kidney or liver impairment.Reversible Inhibitor of Monoamine Oxidase A (RIMA)
OTH: Switching antidepressants resource: *Psychiatry.net* and *SwitchRx* (free but need to register).moclobemide=Manerix: AVL: PO (tab100, 150, 300mg). IND: Social anxiety. MOA: Selectively and reversibly inhibits MAO-A which is an enzyme that metabolizes 5HT and noradrenergic neurotransmitters. AE: N, insomnia. DI: meperidine, SSRIs, TCA. PK: t1/2=1-3h. DOS: Anxiety=300-600mg/d. Other: Initial=150mg BID. Maint=300-600mg TID. Max >600mg TID.
Selective Presynaptic Norepinephrine Reuptake Inhibitor
atomoxetine=Strattera: AVL: PO (cap10, 18, 25, 40, 60, 80,100mg). MOA: Potent inhibitor of NE without affecting DA, 5HT. EVD: Takes 3-4w to see effect. 6–12w of Tx reduced ADHD symptoms by at least 25–30% in 60–70% of pts. ADM: T w/ food to minimize GI upset. AE: Abdominal pain18%, decreased appetite16%, V11%, tierdness10%, N9%, sexual dysfunction6%, indigestion5%, dizziness5%, rash3%, insomnia, liver toxicityrare, MI/strokerare, anaphalaxisrare, suicidal ideationrare. DI: MAOI, SSRIs, DM (serotonin syndrome), 2D6 inhibitors (paroxetine, fluoxetine, quinidine). PK: t1/2: Extensive metabolizers=5.2h. Poor metabolizers=21.6h. F=63-94%. PB=98%. Met by 2D6 (main). Doesn’t inhibit CYPs. DOS: Adj for hepatic fxn. Can T once/d in am or divide BID (am & afternoon) ADHD: *Children <70kg*: 0.5mg/kg/d x 7-14d. Then: 0.8mg/kg/d x7-14d. Then 1-1.2mg/kg/d ongoing. *>70kg*: 40 mg/d x 7-14d. Then 60mg/d x 7-14d. Then 80 mg/d if necessary. Max=100mg/d. Safety <6yo not established. OTH: Not classified as a stimulant.Selective Serotonin Reuptake Inhibitors (SSRIs)
AE: Agitation (on initiation), N, anorgasmia, insomnia, D, GI bleed, dose-dependent QT prolongation. Discontinuation syndrome: anxiety, N, insomnia, chills, confusion. DI: Serotonin syndrome w/ MAOIs. DOS: Taper should be over 1-4w. OTH: Switching antidepressants resource: *Psychiatry.net* and *SwitchRx* (free but need to register).citalopram=Celexa: AVL: PO. IND: Panic, agoraphobia, social anxiety. EVD: SSRI w/ fewest DIs. AE: Prolonged QT (8.5msec at 20mg/d. 18.5msec at 60mg/d). DOS: Anxiety: Std=20–40mg/d. Max=60mg/d.
escitalopram=Cipralex: AVL: PO. IND: agoraphobia, panic, GAD. AE: QT prologation. DOS: Anxiety=10-20mg/d.
fluoxetine=Prozac: IND: Panic, agoraphobia, social anxiety. EVD: Typically no D/C syndrome because of long t1/2. Most anorexic and most stimulating SSRI. PK: t1/2=10-14d. DOS: Anxiety=20-80mg/d.
fluvoxamine=Luvox: AVL: PO. IND: agoraphobia, panic, social anxiety. EVD: SSRI w/ most C, N, and sedation. ADM: T HS (sedating). DOS: Anxiety= 150–300mg/d.
paroxetine=Paxil: AVL: PO (IR and CR). IND: Agoraphobia, panic, social anxiety. AE: SSRI w/ most anticholinergic AEs. PK: t1/2=3-65h. DOS: Anxiety: IR=20-60mg/d. CR=12.5–37.5mg/d.
sertraline=Zoloft: AVL: PO. IND: Agoraphobia, panic, social anxiety. AE: SSRI w/ most male sexual dysfunction and D.
Serotonin Antagonist/Reuptake Inhibitor (SARI)
OTH: Switching antidepressants resource: *Psychiatry.net* and *SwitchRx* (free but need to register).trazodone=Desyrel: AVL: PO. IND:Insomnia, dementia. AE: Hypotension, priapism0.02%, QT prolongation. DI: Serotonergic drugs (serotonin syndrome).
Stimulants
EVD: 70% of pts will have clinically significant decrease in ADHD symptoms. If no effect after 4w, switch to a different stimulant. Kids treated with stimulants have a lower risk of substance-use disorders (drug and alcohol) later in life than untreated ADHD kids. AE: Decreased appetite, wt loss, insomnia HA, N, V, D, rebound hyperactivity, anger/irritability, depression, anxiety, psychosis, suicidal thoughts, priapismrare. MTA study found after 3y, children where 2cm shorter and weighed 2.7kg less than children not medicated.amphetamine (mixed salts)=Adderall XR: AVL: PO (Cap5, 10, 15, 20, 25, 30mg). ADM: T in AM to avoid insomnia. DOS: ADHD: Initial=5mg once/d. Std=10-30mg once/d in am. Max=30mg/d.
dextroamphetamine(DEX)=Dexedrine: AVL: PO (IR tab5mg and SR spansule10, 15mg). PK: t1/2=1-2h. F=75%. Hepatic metabolism by 2D6. DOS: ADHD: IR: 2.5-40mg/d or 0.15mg/kg/d divided in 1-3 doses. SR: 10–40mg or 0.15mg/kg once/d in am.
lisdexamfetamine=Vyvance: AVL: PO (cap20, 30, 40, 50, 60mg). ADM: T in am to avoid insomnia. PK: t1/2=13h (metabolite). DOS: ADHD: >6yo: Initial=30mg once/d in am. Increase to 50mg after 1w if necessary.
methylphenidate(MPH)=Biphentin=Concerta=Ritalin: EVD: ~90% of stimulants used. PK: t1/2=2-3h. Onset=20-30min. F=20-25%. Delivery: Ritalin=IR&SR. Concerta=Bi-layer Controlled Release Tabs. Biphentin=Controlled Relase. DOS: ADHD=5-60mg/d (0.3mg/kg/d).
Tricyclic Antidepressants (TCAs)
MOA: Inhibit reuptake of NE and 5HT. EVD: Secondary amines have less dry mouth, weight gain, and dizziness. AE: : Increased BP, weight gain, sexual dysfunction. DI: MAOI (serotonin syndrome), cimetidine (increased TCA). OTH: *Psychiatry.net* and *SwitchRx* (free but need to register).2o(Secondary) Amine
Have greater effect on NE than 5HT. Less AE vs tertiary TCAs.
desipramine=Norpramin: AVL: PO. IND: ADHD, agoraphobia, GAD, panic. AE: Possible QT prolongation. DOS: *Anxiety*=75-300mg/d. *ADHD*: 6–12yo=10–20mg/d in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150mg/d.
nortriptyline=Aventyl: AVL: PO. IND: Depression (best TCA), smoking cessation. MOA: Noradrenergic (not sedating). ADM: AE: C, weight gain, trouble urinarting, drowsiness, dizziness, dry mouth, sun sensitivity, suicidal thoughts (especially <25yo). Possible QT PK: t1/2=37h. DOS: *ADHD*: 6–12yo=10–20 mg/d po in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150 mg/d. OTH:
3o Teriary Amines
Works on 5HT and NE. May have > effect on men than women. amitriptyline=Elavil: AVL: PO. IND: Sedation, neuropathic pain, depression, anxiety.
clomipramine=Anafranil: IND: Agoraphobia, OCD, panic, depression, and chronic pain. MOA: Similar to SSRI. DOS: Anxiety=75–225mg/d.
imipramine=Tofranil AVL: PO. IND: ADHD, agoraphobia, GAD, panic. AE: Possible QT prolongation. DOS: *Anxiety*: 75-300mg/d. *ADHD*: 6–12yo=10–20 mg/d po in 3 or 4 divided doses. Adolescents=30–50mg/d in 3–4 divided doses. Max=150 mg/d.
Z-Drugs (Nonbenzo Sedative/Hypnotic)
zolpidem=Sublinox=AmbienUSA: AVL: SL10mg tabs IND: Insomnia. PK: t1/2=2.5h. tpeak=1.5h DOS: 10mg HSzopiclone=Imovane AVL: PO5,7.5mg tabs IND: Insomnia MOA: Binds to the GABAa receptor (same as benzos). AE: Metallic taste in the mouth, dry mouth, upset stomach, D, dizziness (increased risk of falls), confusion, amnesia. CI: liver failure, severe sleep apnea. DI: EtOH (both CNS depressants). PK: t1/2=4-7h. tpeak=1.5h DOS: Pts >65 should start w/ half of a 7.5mg tab. Should not exceed 7-10d of use but often used daily. OTH: There is a risk of dependence which is dose dependent.
Anthracene Derivatives
anthralin: AVL: Topical (cream, ointment). IND: Psoriasis. ADM: Wash off 15min-hours after application depending on formulation.Combination Topicals
Fucibet=fusidic acid2%+betamethasone valerate 0.1%: IND: Eczema w/ secondary bacterial infection. For flare-ups or short-term Tx (max=2 weeks). MOA: Betamethasone has anti-inflammatory, antipruritic and vasoconstrictive actions. Fusidic acid inhibits bacterial protein synthesis. Action is mainly bacteriostatic, but may be bactericidal at higher concentrations. EVD: Primarily active for gram (+) bacteria. Particullarly effective for (Staph aureus including MRSA). Also active against Streptococcus species, Corynebacterium minutissimum, some Neisseria species, and certain Clostridium species. ADM: Apply thin layer. AE: Pruritus and skin burning sensation, pain, irritation, swelling and vesicles at the application site, aggravated eczema, dry skin, erythema, urticaria, rash, contact dermatitis, skin atrophy, application site irritation, skin discolouration and striae. CI: <6yo. DI: None. DOS: Thin layer to affected area BID until cleared. Max=2 weeks. Children (6–18yo) should avoid large amounts and occlusion (more susceptibile to corticosteroid-induced AEs).Immune Modulator
imiquimod=Aldara: AVL: Topical cream. IND: Genital warts. ADM: AAA qhs and remove in am. Rub in until clear. Wash hands before and after. AE: Site rxn30%, redness and peeling of skin, burning sensation15%, skin ulcer45%, flu like symptoms4% CI: Immunosuppressed/ transplant. OTH: Can make condoms ineffective.Phosphodiesterase 4 (PDE-4) inhibitors
crisaborole=Eucrisa: AVL: 2% brand name ointment only2018 IND: Mild to mod atopic dermatitis in pts > 2yo. MOA: PDE-4 inhibition leads to less production of some inflammatory cytokines that are involved in atopic dermatitis. EVD: Pts treated w/ Eucrisa had ~20-30% higher reate of clear/almost clear dermatitis vs vehicle alone. ADM: Apply a thin layer then wash hands. AE: Application site pain/burning/stinging, dermatitis flare, skin infection, allergic rxn. DI: None. DOS: Thin layer BID. OTH: Manufactured by Pfizer.Retinoids
Oralisotretinoin=Accutane=Epuris: EVD: Takes up to 8w to show full effect. AE: Dry lips93%, dry mouth33%, dry eyes35%, dry nose80%, nose bleed20%, rare: depression, suicide (reported but not shown to increase risk), insomnia, mood swings, peeling of finger tips, dry skin, itching, hair loss rash. CI: Increased lipids, prg, LASIK surgery. PRG: Very contraindicated (Monthly HCG testing).
Topical
IND: Mild-mod comedonal acne. EVD: 12w for max response. AE: May worsen acne at 2-4w.
Adapalene (ADA)=Differin EVD: Least irritation vs TAZ and TRE.
Tazarotene (TAZ)=Tazorac: OTH: Rarely seen (most irritation vs TAZ and TRE.
Tretinoin (TRE)=Retin-A=Stevia-A: COS: Cheapest vs TAZ and ADA.
Topical Antibiotics
bacitricin: AVL: Only use topically cause can cause kidney damage. Also used for eyes. IND: Treats gram (+) and (–) organisms. MOA: Breaks the peptidoglycan cell wall. PK: Mixture of cyclic peptidesbenzoyl peroxide (BPO)=Acetoxyl=Benzagel=Benoxyl=Benzac=Oxy 5=Panoxyl=Solugel: AVL: Water, alcohol, or acetone based. IND: Mild-mod acne. EVD: Takes 8-12w to work. Can worsen acne at 2-4w. ADM: Could apply q2-3d then increase to tolerance. Apply to entire effected area. AE: Dermatitis, dry skin. OTH: Can stain clothing. Use water base for sensitive skin.
fusidic acid=Fucidin: IND: Impetigo 1st line. MOA: Stops protein synthesis. Covers Gram (+) only. AE: Mild irritationrare, dermatitisrare. DOS: Impetigo: AAA BID or TID × 5d or until all lesions heal.
gramacidin: EVD: Active against some gram (+) and some gram (-). AE: Causes hemolysis (Only use topically).
mupirocin=Bactroban: IND: Gram (+) including MRSA. furuncles, Impetigo1st line, folliculitis, open wounds, nasal eradication therapy. MOA: Inhibits protein synthesis. EVD: More effective than fusidic acid but more expensive. ADM: AE: Burninginfrequent, stinginginfrequent, dermatitisrare. DOS: Impetigo: AAA BID or TID × 5d or until all lesions heal. OTH: Covers gram + only. Resistance does develop.
neomycin=Neosporin: AVL: Topical, ophthalmic. MOA: Inhibits protein synthesis. EVD: Active against gram (–) and partially for gram(+). OTH: Drug class aminoglycoside.
polymyxin b=Polysporin: AVL: Topical, opthalmic. IND: Used mainly for gram (-) resistant organisms, meningitis, UTIs, clears endotoxins. MOA: Makes outer cell membrane more susceptible to water uptake (Gram positive don’t have outside membrane).
Topical Corticosteroids
clobetasone: AVL :Topical (cream 0.05% ). IND: Eczema, psoriasis. DOS: AAA BID or TID x 2-3w. OTH:hydrocortisone=Emo-Cort: IND : Dermatitis, psoriasis. AE : skin irritation, allergic rxn rare. DOS : Dermatitis & psoriasis: Apply thin layer BID-TID prn.
Aminosalicylates
AVL: PO, PR. IND: UC and CD-not very effective. MOA: Anti-inflammatory that inhibits nuclear factor kappa B and chemoattractant leukotrienes which alters prostaglandin metabolism. EVD: Time to effect 2-4w. ADM: AE: Abdominal pain, cramps, diar, headach, naus, rash including urticaria, vom, interstitial nephritisrare, pancreatitisrare, pneumonitisrare, pericarditisrare, hepatitisrare. OTH: Main drug=5-aminosalicylic acid (5-ASA).5-ASA=Asacol: PK: Gets released primarily in the colon. DOS: Flare up: Max=4.8g/d in divided doses. Maintenance=1.6 g/d in divided doses.
5-ASA=Mesasal: PK: Gets released in the SI so it works from the SI to the colon. DOS: Flare up=1.5–3g/d in divided doses. Maint=1.5g/d in divided doses.
5-ASA=Mezavant: PK:Gets released primarily in the colon. DOS: Flare up= 2.4–4.8g once/d. Maint=2.4g once/d.
5-ASA=Pentasa: PK: Gets released primarily in the colon. DOS: Flare up=2–4g/d in divided doses. Maint=1.5–3g/d in divided doses.
5-ASA=Salofalk: PK: Gets released in the SI so it works from the SI to the colon. DOS: : Flare up=3–4 g/d in divided doses. Maint=1.5–3g/d in divided doses.
olsalazine=Dipentum: AVL: PO. IND: 2nd line for UC. DOS: Flare up=500mg QID. Maint=500mg BID. OTH: 5-ASA dimer linked by azo bond that gets cleaved into 2 molecules of 5-ASA.
sulfasalazine (SSZ)=Salazopyrin: AVL: Tab or compounded suspension. EVD: May be more effective than 5-ASA but has least favourable AEs. ADM: AE: Naus, headache, rash, haemolytic anemia and hepatotoxicity. Reversible oligospermia reported w/ sulfasalazine, but not with 5-ASA. PK: Gets released primarily in the colon. DOS: Flare up=1-2g TID-QID. Maintenance=1g BID-TID. OTH: Different class but gets cleaved into 5-ASA.
Alginates
IND: GERD. MOA: Forms a foam barrier that floats to top of stomach. EVD: Provides symptom relief but does not prevent reflux.alginic acid/Al hydroxide=Gaviscon liquid: AE: Naus, vom, belching, flatulence. DI: Binds w/ digoxin, tetracyclines, quinolones. PK: Onset=minutes. Duration=30-45min. DOS: 10-20mL prn after meals.
alginic acid/Mg hydroxide=Gaviscon Tabs: IND: GERD. ADM: Follow w/ glass of water. AE: Naus, vom, belching, flatulence. DI: Binds w/ digoxin, tetracyclines, quinolones. PK: Onset=minutes. Duration=30-45min. DOS: Chew 2-4 tabs prn after meals.
H2 Receptor Antagonists (H2RA)
IND: GERD. EVD: All 4 H2RAs have similar efficacy. ADM: T 30min before meal. OTH: Can develop tolerance/tachyphylaxis.cimetidine=NU-CIMET: AVL: PO. AE: Diar, const, headache, fatigue, confusion, gynecomastiarare, impotencerare. DI: High potential to increase drug levels. PK: Inhibits: 1A2, 2C9, 2C19, 3A4 and 2D6. DOS: Adj for renal fxn. 800mg once/d or 600mg BID or 300mg QID.
famotidine=Pepcid: AVL: PO. PK: Does not inhibit CYPs. DOS: Adj for renal fxn. 10-40mg BID.
nizatidine=Axid: AVL: PO. AE: Diar, const, headache, fatigue, confusion. DOS: 150mg BID.
ranitidine=Zantac: AVL: PO. AE: Diar, const, headache, fatigue, confusion. PRG: Safe. LAC: Safe. DI: warfarin. PK: Doesn't inhibit CYPs. DOS: 75-150mg BID-QID or 300mg qHS. Non-Rx dose=75–150 mg/d. OTH: Schedule: U, III, I (depending on strength&size).
Laxatives
5-HT4 RECEPTOR AGONISTprucalopride=Resolor: AVL: PO. IND: Chronic constipation for females who have failed alternatives. MOA: 5-HT4 receptor agonist with prokinetic activity. COS: ~$100/month DOS: 2mg once/d. D/C if not effective after 4w.
BULK FORMING LAXATIVES
calcium polycarbophil=Prodiem: OTH: synthetic fiber with less chance of flatulence, bloating.
inulin=Benefibre:
psyllium=Metamucil:
GUANYLATE CYCLASE-C AGONISTTS
linaclotide: AVL: PO. IND: Chronic adult constipation after failing laxatives. MOA: Guanylate cyclase-C receptor agonist which leads to increased chloride and bicarb in the intestines. This decreases absorption of sodium increased water secretion into the intestine. COS: =$120/month. DOS: Constipation=145 mg once/d.
LUBRICANT LAXATIVE
mineral oil: AVL: PO (liquid), PR (enema). IND: Constipation. MOA: Lubricates GI tract to aid stool passage and slows water reabsorption in the GI tract. PK: PO onset=6-8h.
OSMOTIC LAXATIVES
MOA: Sugar isn’t broken down and osmotically draws fluid in lumen and stimulates peristalsis.
glycerin: AVL: PR (rectal suppositories).
lactulose: PRG: Safe. LAC: Safe. PK: Onset=24-48h.
magnesium hydroxide=Milk of Magnesia: AVL: PO (oral susp).
polyethylene glycol (PEG 3350)=Lax-A-Day=Restoralax: AVL: PO (oral powder to make solution).
sorbitol: AVL: PO, PR.
STIMULANT LAXATIVES
bisacodyl=Dulcolax: AVL: PO, rectal suppositories.
sennosides=Senokot=Ex-Lax=Prodiem:
STOOL SOFTENERS
docusate sodium=Colace:
docusate calcium=Soflax: PRG: Safe. LAC: Safe.
Proton Pump Inhibitors (PPIs)
MOA: Block final step of acid secretion by irreversibly binding and inhibiting the H+/K+ ATPase (AKA the proton pump) in parietal cells of the stomach. DI: Reduced gastric acidity will changes absorption of drugs that are pH dependent (ex. ketoconazole, itraconazole or erlotinib)ref. PPIs should be taken at least 30min before sucralfate so that PPI absorption is not affected. Some reports of increased INR and prothrombin time in pts taking PPIs and warfarinref. PK: All PPIs are competitive inhibitors of 2C19. Order from strongest to weakest 2C19 inhibitors: lansoprazole, omeprazole, esomeprazole, pantoprazole, rabeprazole. MON: If treating GERD there should be significant improvement at 2wks. If not investigate further. Follow up at 4-8w. OTH: Goal w/ PPI is to make stomach pH>4. Beers criteria: Consider avoiding in pts >65yo because of risk of bone loss/fracture. Should also limit to 8w of use if possible. PPIs decrease both basal and stimulated acid secretion in the stomach leading to higher pH. AUX:
dexlansoprazole=Dexilant:
AVL: PO (delayed release cap30, 60mg) ref.
IND: GERD, esophagitis ref.
EVD: Shouldn’t be used if <1 yo because it wasn’t effective at treating symptomatic GERD in a multicenter, double-blind controlled trial ref.
ADM: T w/ or without food. Don’t cut or chew. Applesauce: May open cap and mix in 1 tbsp of applesauce. Don’t chew granules and eat full amount. Syringe: Open cap into 20mL of water, use syringe to draw up liquid, gently swirl, spray into mouth, reload syringe w/ 10mLs of water, spray in mouth and repeat once again to drain all the granules. NG tube: Use same syringe technique ref.
AE: Diar4%, abdominal pain3%, Naus2%, flatulence2%, Const1%. May decrease absorption of: Vit B12, Mg+2, K+1, and Ca+2. May increase osteoporosis risk ref.
Warning: Admin w/ rilpivirine CI. May mask ulcer symptoms. May increase risk of GI infections (ex C.difficile) ref.
PRG: No safety data ref.
LAC: No safety data ref.
DI: Clopidogrel AUC was decreased 9% when given w/ dexlansoprazole 60mg/d. May elevate [methotrexate] when MTX is given at high dose. May effect absorption or clearance of antiretrovirals. May increase [tacrolimus]. Take >30min before sucralfate to increase [dexlansoprazole] ref.
PK: t1/2=1-2hrs. PB=97%. Vd=40.3L. MM=369.36g/mol. Dexilant has a “Dual Delayed Release” w/ a concentration peak at 1-2hrs followed by a second at 4-5hrs. Met by 2C19 and 3A4. May slightly inhibit 2C19. Dexlansoprazole is R-enantiomer of lansoprazole. Not expected to be removed from dialysis
ref.
COS: $279 for 100x60mg caps2019. Not covered in AB, BC, MB, NB, NL, NS, ON, PE, SK.
MON: Re-evaluate at 4-8wks to see if still necessary. ref.
DOS: >12yo: Esophagitis healing= 60mg once/d x up to 8wks. Esophagitis maintenance=30mg/d. GERD: 30mg once/d x4wks. Max of 30mg/d if moderate hepatic impairment. Severe hepatic impairment not studied. No dose adj for renal fxn. No dose adj for elderly. Not studied in pts <12yo ref.
OTH: Stopping could cause rebound acid hypersecretion ref.
esomeprazole=Nexium:
AVL: PO (delayed release tabs20, 40mg, sachet10mg) ref.
IND: GERD, NSAID induced ulcers, Ellison syndrome, H. pylori (w/ clarithromycin and amoxicillin) ref.
EVD: Found superior vs ranitidine 150mg BID when using non-selective NSAIDsref.
ADM: T w/ or without food. May disperse tab in half glass of water. Stir until disintegration and drink whole glass within 30min. Rinse glass w/ water and drink. Don’t crush or chew pellets. For NG tube: Disperse tab in 50mL of water, draw up w/ syringe, admin through tube, flush tube w/ 25-50mL of water. ref.
AE: Diar6%, abdominal pain5%, Const2%, May decrease absorption of: Vit B12, Mg+2, K+1, and Ca+2. May increase osteoporosis risk. Withdrawal may lead to rebound acidity ref.
Warning: May mask ulcer symptoms. May increase risk of GI infections (ex C.difficile) ref.
PRG: No safety data ref.
LAC: No safety data ref.
DI: Admin w/ rilprivirine CI. Clopidogrel’s active metabolite decreased by ~40% when also taking esomeprazole 40mg. May elevate [methotrexate] when MTX is given at high dose. Nexium 30mg/d x 5d decreased diazepam clearance by 45%. May increase [tacrolimus] and [phenytoin].
ref.
PK: t1/2=1.4hrs. tmax=1-2hrs. F~75%. Vd=0.22L/kg. PB=97%. Met by 2C19 and 3A4. MM=713.1 g/mol. Esomeprazole is S-isomer of omeprazole ref.
COS: $218 for 100x40mg tabs2019. Covered in MB, NL, ON, QE, SK. Partially covered in BC. Not covered in AB, NB, NS, PE.
MON: Follow up at 4-8w to see if Tx still necessary ref.
DOS: Adult: Reflux Esophagitis=40mg once/d x 4-8wks. GERD/esophagitis/NSAID induced GERD=20mg once/d. Zollinger-Ellison Syndrome= 40mg BID. H.pylori=20mg BID x 7d (combo Tx). No dose adj for elderly. No dose adj for renal fxn. Max 20mg/d for severe hepatic impairment. Peds (1-11yo): Esophagitis: <20kg=10mg once/d x8w. >20kg=10-20mg once/d x8w. NERD: 10mg once/d x 8w regardless of weight. Safety not established <1yo ref.
lansoprazole=Prevacid:
AVL: PO (delayed release caps and tabs15, 30mg)ref.
IND: Ulcer, NSAID induced ulcer, GERD, Zollinger-Ellison Syndrome, H.pylori (combo Tx)ref.
ADM: Food decreases peak concentration and absorption by ~60% (T before breakfast). May open caps and put in applesauce, juice, water, and through NG tube. The “FasTabs” can be placed on tongue to dissolve, placed in water and drawn up w/ oral syringe, or given via NG tube via syringeref.
AE: Diar4%, abdominal pain2%, dizziness1%. May decrease absorption of: Vit B12, Mg+2, K+1, and Ca+2. May increase osteoporosis riskref.
Warning: May mask ulcer symptoms. May increase risk of GI infections (ex C.difficile)ref.
PRG: Safe in rabbits and rats. Not human dataref.
LAC: Excreted in milk of rats. No human dataref.
DI: No dose adj for clopidogrel (no clinically important effect on [clopidogrel metabolite] or platelet inhibition). May increase [tacrolimus] and decrease [theophylline]. May elevate [methotrexate] when MTX is given at high dose. May affect absorption of protease inhibitorsref.
PK: t1/2=1.5hrs. tmax=1.7hrs. Duration=>24hrs. Vd=16L. PB=97%. F=~83%. MM=369.37g/molref.
COS: $67 for 100x30mg caps2019. Covered in AB, MB, PE, QE, SK. Partially covered in BC, ON. Exception status in NB, NL, NS.
DOS: Adult (>11yo): Duodenal/gastric ulcer=15mg once/d x ~4wks. NSAID ulcer=15-30mg once/d up to 8wks. GERD=15mg once/d. H.pylori=30mg BID x 7-14d (combo Tx). Zollinger-Ellison Syndrome=60mg once/d. Max 30mg/d for elderly. No dose adj for renal fxn. Consider lower dose if severe hepatic disease. Ped (1-11yo): GERD: 15mg (weight<30kg) and 30mg (weight>30kg) once/d up to 12wks. Safety and effectiveness not established <1yoref.
omeprazole=Losec:
AVL: PO (delayed release cap10, 20mg) ref.
IND: GERD, NSAID induced GI lesions, reflux esophagitis, duodenal/gastric ulcers, Zollinger-Ellison Syndrome ref.
EVD: ~80% decrease of 24hr gastric acidity after repeated 20mg/d doses ref.
ADM: T w/ sufficient water w/ or without food ref.
AE: Diar2.8%, headache2.6%, flatulence2.3%, abdominal pain 2%, Const1%, dizziness/vertigo1%. May decrease absorption of: Vit B12, Mg+2, K+1, and Ca+2. May increase osteoporosis risk. Withdrawal may lead to rebound acidity ref.
Warning: May mask ulcer. May increase risk of GI infections (ex C.difficile) ref.
PRG: Safety not established ref.
LAC: Safety not established ref.
DI: Could decrease [clopidogrel]. Decreases diazepam clearace by 26-40%. May elevate [methotrexate] when MTX is given at high dose. Phenytoin clearance reduced when omeprazole given at 40mg/d. May effect absorption or clearance of antiretrovirals. May increase effect of warfarin ref.
PK: t1/2=40min. F=35-43%. Tmax=4hrs. PB=95%. MM=345.42g/mol. Met by 2C19 (major) and 3A4 (minor) ref.
COS: $37 for 100x20mg caps2019. Covered in AB, MB, NB, NL, NS, ON, PE, QE, SK. Partially covered in BC.
MON: Healing of ulcers/esophagitis happens in 2-4w. Trial D/C after 4w. ref.
DOS: Adult: GERD/Esophagitis/Ulcer: 20mg once/d x 4wks. Maintenance dose=10mg/d. Refractory esophagitis=40mg/d. No dose adj for kidney fxn. Don’t exceed 20mg/d in elderly or severe liver disease. Not studied in children ref.
pantoprazole Mg+2=Tecta:
AVL: PO (EC tab40mg) ref.
IND: GERD, reflux esophagitis, duodenal/gastric ulcers, H.pylori (in combo w/ Abx) ref.
EVD: At 40mg/d acid production was inhibited 51% Day 1 and 85% on Day 7. Acidity was reduced by 37% on Day 1 and 98% on Day 7 ref.
ADM: T in AM before, during, or after breakfast ref.
AE: Headache2%, Diar2%, Naus1%. May decrease Vit B12 absorption and increase risk of osteoporosis ref.
Warning: Could mask stomach ulcers symptoms. Increased risk of GI infections (ex. C.difficile) due to less stomach acid ref.
PRG: No data for humans ref.
LAC: Crosses into breast milk. No safety data ref.
DI: Some reports of increased INR when used w/ warfarin. Increased levels of methotrexate when MTX used at high dose ref.
PK: t1/2=~1hr. tmax=2.5hrs. F=77%. PB=98%. MM=825.08g/mol. Cmax is ~70% of pantoprazole Na+1 values. Met in liver. Doesn’t induce or inhibit enzymes ref.
COS: $33 for 100x40mg tabs2019.Covered in AB, BC, MB, NB, ON, PE, QE, SK. Exception status in NL, NS.
MON: GERD: If symptomatic after 4wks investigate further ref.
DOS: Adult: GERD/gastric or duodenal ulcer: 40mg once/d x 4wks. H.pylori: 40mg BID x7d. Not studied in children. Choose alternative in sever hepatic disease. No dose adj for renal fxn ref.
OTH: Amount of Mg+2 in each tab is negligibly low. Have been reports of false-positives for THC urine screening ref.
pantoprazole Na+1=Pantoloc:
AVL: PO (EC tab20, 40mg) ref.
IND: GERD, NSAID induced GI lesions, reflux esophagitis, duodenal/gastric ulcers ref.
ADM: T w/ or without food. Do not crush or chew ref.
AE: Headache2%, Diar2%, Naus1%. May decrease Vit B12 absorption and increase risk of osteoporosis ref.
Warning: Could mask stomach ulcers symptoms. Increased risk of GI infections (ex. C.difficile) due to less stomach acid.
PRG: Risk for humans unknown ref
LAC: Does get excreted in breast milk. Safety not established ref.
DI: Some reports of increased INR when used w/ warfarin. Increased levels of methotrexate when MTX used at high dose ref.
PK: t1/2=~1hr. tmax=2-3hrs. F=77%. PB=98%. MM=432.4g/mole. Met by 2C19 and 3A4 ref.
COS: $34 for 100x40mg tabs2019. Covered in AB, MB, NB, NS, ON, PE, QE, SK. Partially covered in BC. Exception status in NL.
MON: Further investigation should be done if symptomatic after 4wks ref.
DOS: Adult: GERD: 40mg once/d x 4wks. May use 20mg once/d for maintenance/healing of reflux esophagitis and NSAID induced lesions. No adj for renal fxn. Severe liver disease: max=20mg/d. Not studied in children ref.
rabeprazole=Pariet:
AVL: PO (EC tab10, 20mg) ref.
IND: GERD, duodenal/gastric ulcers, Zollinger-
Ellison syndrome ref.
ADM: T w/ or without food. Don’t crush or chew ref.
AE: Diar3%, rash, dizziness. May decrease Vit B12 absorption and increase osteoporosis risk. Withdrawal could cause rebound acid secretion that starts within days and last up to 11 months ref.
Warning: Could mask symptoms of stomach ulcer. Increased risk of gastrointestinal infections (ex. C.difficile) because of decreased stomach acid. ref
PRG: Safety not established ref.
LAC: Safety not established ref.
DI: Some reports of increased INR when used w/ warfarin. Increased levels of methotrexate when methotrexate used at high dose. ref
PK: t1/2=~1hr. Cmax=1.6-5hrs. F=52%. PB=96%. MM=381.43g/mol. Antisecretion stars within 1hr. Max effect after 2-4hrs. Met by CYP450s but does not inhibit or induce. ref.
COS: $27 for 100x20mg tabs2019. Covered in AB, BC, MB, NB, NL, NS, ON, PE, QE, SK. Only PPI covered for BID dosing in NS.
MON: Should D/C after 4-6 weeks and see if pt still needs it ref.
DOS: Adult:GERD: 10 or 20mg once/d. Max=20mg BID. Tx should only be for 4-6w then reassess. Adj dose for severe hepatic impairment but not renal impairment. Not studied <18yo ref.
Purine Antimetabolites
IND: UC and CD. Used to reduce the dose of prednisone and maintain remission of quiescent disease (not inducing remission). MON: CBC q2w while titrating dose then q month. Can cause leukopenia/myleosupression. LFTs q2w then monthly (hepatotoxicity). Symptoms of pancreatitis – naus/vom/arthralgia (flu like Sx). OTH: Time to effect=3-6 months.azathioprine (AZA)=Imuran: AVL: PO. AE: Naus, Diar, stomatitis, arthralgias, anorexia, opportunistic infection, blood dyscrasias, pancreatitisrare, hepatotoxicityrare DOS: 1-2.5mg/kg/d. OTH: Prodrug to 6MP.
6-mercaptopurine (6MP)=Purinethol: AVL: PO. AE: Naus, diar, stomatitis, arthralgias, anorexia, opportunistic infection, blood dyscrasias, pancreatitisrare, hepatotoxicityrare. DOS: Adj for renal fxn. 100mg/d.
Alpha-Glucosidase Inhibitors
acarbose=Glucobay: IND: T2DM. MOA: Delays/prevents digestion of complex carbs by inhibiting alpha-glucosidases. EVD: Lowers A1C 0.4-0.9% (relatively small effect). Max effect in ~8w. ADM: T w/ first bite of meal. AE: abdominal pain21%, Diar33%, flatulence71%. CI: IBD/IBS, past bowel obstruction. MON: LFT q3 months for 1y DOS: Start=25mg once/d. Maint=50-100mg TID. OTH: No hypoglycemia or weight gain. Tx hypoglycemia w/ glucose not sucrose.miglitol: Not avail in Can.
Antithyroid
methimazole=Tapazole: IND: Hyperthyroidism. EVD: Improvement in 1-3 weeks. AE: Rash, upset stomach, heartburn, joint pain.Biguanides
metformin=Glucophage=Glumetza: AVL: PO. IND: T2DM. MOA: Increases insulin sensitivity, decreases glucose production in liver, increases glucose uptake in muscle and fat, and decreases glucose absorption in small intestine. EVD: Reduces A1C by 1-1.5%. ADM: T w/ food to decrease stomach upset. AE: Diar, Naus, anorexia, metallic taste, lactic acidosisrare, anemia, photosensitivity, B12 malabsorption. CI: >80yo, CrCl<30, alcoholism, liver failure, severe CV/pulmonary disease. AUX: T w/ food. DOS: Start=500mg once/d. Max=1000mg BID. OTH: Can improve ovulation in Polycystic Ovarian Syndrome.Combination Antidiabetics
Soliqua=insulin glargine100U/mL + lixisenatide33μg/mL AVL: SubQ (3mL prefilled disposable pen). IND: adults w/ T2DM inadequately controlled on basal insulin alone or in combination w/ metformin. ADM: Once/d within 1hr of first meal. Inject SubQ in abdomen, deltoid or thigh. DOS: Once/d injection. 1U of Soliqua=1U insulin glargine and 0.33μg of lixisenatide. Dose must be individualized. Max=60U/d. Not intended for pts who require <15 or >60U basal insulin/d. OTH:Steglujan=ertugliflozin + sitagliptin: AVL: PO (tabertugliflozin/sitagliptin 5/100mg and 15/100mg tabs) IND: With metformin in pts w/ T2DM inadequately controlled w/ metformin and sitagliptin, or already controlled w/ metformin, sitagliptin and ertugliflozin, as individual drugs. AUX: Take in AM. DOS: Start=5/100mg once/d. Max=15/100mg once/d. OTH:
Xultophy=Insulin degludec+liraglutide: AVL: SubQ disposable pen3mLs/pen containing 100U/mL insulin degludec + 3.6mg/mL liraglutide. IND: T2DM. Not inidcated for T1DM or diabetic ketoacidosis. ADM: SubQ into thigh, upper arm or abdomen. Rotate site to avoid lipodystrophy. Any time of day w/ or without food, ideally same time of day. AE: Hypoglycemia, naus, diar, decreased appetitie, severe hypoglycemia<0.5%. CI: Not studied in combo w/ short acting insulins. DOS: Start=16U (16U degludec + 0.58mg liraglutide) once/d. Titrate up or down by 2U q 3-4d. Max=50U/d. Use alternate if pt insulin dose is <16U/d or >50U/d OTH: Essentially this is Tresiba+Victoza in one pen. Can be used w/ metformin and sulfonylureas.
Dipeptidyl Peptidase 4 Inhibitors (DPP-4I)
IND: T2DM (not as monotherapy). MOA: Inhibits DPP-4 which degrades GLP-1. EVD: A1C decreases 0.6-1%. ADM: T w/ or without food. COS: More expensive vs sulfonylureas and insulin. OTH: Typically prescribed w/ metformin. No weight gain or hypoglycemia.alogliptin=Nesina: DI: Low potential for DIs. PK: Doesn’t inhibit CYPs. DOS: Adj for renal fxn. 25mg once/d. OTH: Kazano is a combination alogliptinmetformin.
linagliptin=Trajenta: PK: Met by 3A4. DOS: No adj for CrCl. 5mg once/d. OTH: Jentadueto is a combo=linagliptin+metformin.
saxagliptin=Onglyza: IND: Only DPP-4I not approved for monotherapy. DI: More 3A4 interactions vs sitagliptin PK: Met by 3A4/5 DOS: Adj for renal fxn. Std=2.5-5mg once/d.
sitagliptin=Januvia: DI: Low potential for 3A4 DIs vs saxagliptin. PK: Doesn’t inhibit CYPs. DOS: Adj for renal fxn. Std=100mg once/d (no titration). OTH: Janumet is a combo=sitagliptin+metformin (Avail as XR).
Glucagon-Like Peptide-1 (GLP-1) Agonists
AVL: SubQ. Often as add on to metformin, sulfonylurea, or LAIA. IND: T2DM. MOA: Binds to GLP-1 receptor which will increase glucose dependent insulin secretion and suppresses glucagon secretion during hyperglycemia. Increase GLP-1 activity 5-fold. EVD: Weight loss=1.5-2.8kg. Lowers A1C more than DPP4Is but more Naus at initiation. ADM: Inject 60min before breakfast or supper. AE: Hypoglycemia, Naus, Vom, Diar, increased HR, injection site rxn, acute pancreatitisrare. CI: CrCl<30. PRG: CI. DI: Causes delayed gastric emptying. DOS: Titrate dose q1-2w.albiglutide=Eperzan: DOS: Once/w injections.
dulaglutide=Trulicity: DOS: No adj for CrCl. Start=0.75mg SubQ once/w. Maint=1.5mg SubQ once/w.
exenatide=Byetta=Bydureon: DOS: Adj for CrCl. Solution: Start=5μg SubQ BID Max=10μg BID SubQ. Suspension: 2mg/w.
liraglutide=Victoza: DOS: No adj for CrCl. Start=0.6mg SubQ once/d. Maint=1.2-1.8mg SubQ once/d without regard for meals.
Insulins
AVL: SubQ, IV. IND: T1DM and T2DM. EVD: Reduces A1C 1.5-2.5%. ADM: Inject in abdomen 5cm away from umbilicus, upper arm, anterior/lateral thigh, buttocks. Alcohol before not recommended (will sting). AE: Lipodystrophies, weight gain, hypoglycemia. DOS: T1DM: Typical=0.3-0.5 U/kg/d. “500 rule”: Take 500 and divide by units used/d. If 50 units used/d then 500/50=10. This means 1U of insulin covers 10g of carbs. Use “450 rule” if using R insulin instead of RAIA. T2DM: Insulin naïve=0.1-0.5 U/kg once daily. Maint~0.5-1.5 u/kg*d. Basal insulin should be ~50% of total insulin. Adjust 1 insulin at a time by 1-2U. OTH: Stability: 28d at room temp. Schedule II (available without Rx).RAPID-ACTING INSULIN ANALOGUE (RAIA)
ADM: Inject <15min before meal. DOS: 1U~10-15g carbs. OTH: Clear liquid. Can mix w/ NPH if used immediately.
insulin aspart=NovoRapid: AVL: Avail vial, cartridge. PRG: Safe. LAC: Safe. PK: Onset=10-15min. Peak=1-1.5h. Duration=4-5h.
insulin glulisine=Apidra: AVL: Vial, cartridge, disposable. LAC: Safe. PK: Onset=10-15min. Peak=1-1.5h. Duration=4-5h.
insulin lispro=Humalog: AVL: Vial, cartridge, disposable. Avail as 200U/mL. PRG: Safe. LAC: Safe. PK: Onset=10-15min. Peak=1-1.5h. Duration=4-5h.
SHORT-ACTING/REGULAR (R)
ADM: Inject 30-45min before meal. OTH: Clear liquid. Can mix with all except long/extra acting
regular insulin=Humulin R=Novolin ge Toronto: AVL: Vial, cartridge. PRG: Safe. LAC: Safe. PK: Onset=0.5-1h. Peak=2-4h. Duration=5-7h. Abdomen site gives faster F.
INTERMEDIATE-ACTING/NHP (N)
ADM: If mixing draw up R first. Shake before giving. OTH: Cloudy liquid. Can mix with R and RAIA.
NPH insulin=Humulin N=Novolin-ge NPH: AVL: Vial, cartridge, Humulin Pen. PRG: Safe. LAC: Safe. PK: Onset=1-2h. Peak=4-10h. Duration=12-18h. DOS: Often given at HS +/- am dose.
LONG-ACTING INSULIN ANALOGUE (LAIA)
DOS: When switching from NPH decrease dose 20%. OTH: Clear liquid. Don’t mix.
insulin determir (D)=Levemir: AVL: Avail cartridge. LAC: Safe. PK: Onset=1-3.5h. Peak=none. Duration=16-24h. DOS: Once/d or BID. OTH: Neutral pH.
insulin glargine (G)=Lantus=Toujeo: AVL: Vial, cartridge, disposable. LAC: Safe. PK: Onset=1.5-4h. Peak=none. Duration=24h. DOS: Once/d or BID. OTH: Acidic pH (increased pain) to form microprecipitates which slows release.
ULTRA-LONG ACTING
insulin degludec=Tresiba: AVL: SubQ (3mL prefilled pens100 or 200U/mL). IND: T!DM (>2yo), Adults w/ T2DM. ADM: : Can inject in thigh, upper arm, or abdominal wall. Rotate sites. AE: Hypoglycemia, weight gain, lipodystrophy (rotate sites). DI: pioglitazone. PK: t1/2=25h. DOS: Once/d at any time of day (individualized dose). Start (insulin naïve)=10U once/d. OTH: Can be used w/ PO antidiabetics and short or rapid insulin. 1U of degludec=1U of glargine. Refridgerate. Stable at room temp for 8w. Keep cap on to protect from light.
PREMIXED (R/N)
AVL: Humulin (30/70) Novolin GE (30/70), (40/60), (50/50). DOS: Inject once/d-TID but not HS. OTH: Can only mix in syringe (not pen).
Meglitinides
IND: T2DM as monotherapy if metformin and sulfonylurea not tolerated. Often used for people who skip/shift meals. MOA: Stimulates β cells to release insulin (shorter duration vs SUs). EVD: Possibly more effective for pc glucose levels vs SUs. ADM: Skip dose if skipping meal DI: gemfibrozil. 3A4. DOS: No dose adj for Cr Cl.repaglinide=Gluconorm: ADM: T 0-30min before meals. DOS: 0.5mg BID-QID.
Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors
AVL: PO. As monotherapy or w/ metformin. IND: T2DM. MOA: Blocks/reduces glucose reuptake in proximal tubule (part of the nephron in the kidneys). This is where 90% of reabsorption happens so glucose is urinated out. AE: UTI, candidiasis, increased urination, increased K, increased BUN/SCr, increased LDL, decreased BP, hypovolemia. Possible DKA, fracture risk. CI: CrCl<45. OTH: Some weight loss. No hypoglycemia.canagliflozin=Invokana: AVL: PO. DI: UGT1A9/2B4. DOS: Adj for CrCl. 100 or 300mg once/d. OTH: Invonkamet=canagliflozin+metformin.
dapagliflozin=Forxiga: AVL: PO. CI: CrCl<60mL/min. DOS: Adj for CrCl. 5 or 10mg once/d. OTH: Xigduo=dapagliflozin+metformin.
empagliflozin=Jardiance: AVL: PO. EVD: Showed CV benefits in T2DM with CV disease. CI: CrCl<45mL/min. DOS: Adj for CrCl. 10-25mg once/d. OTH: Synjardy=empagliflozin+metformin.
ertugliflozin=Steglatro: AVL: PO (tab5, 15mg) IND: T2DM when metformin isn’t tolerated or with metformin +/- sitagliptin for better glycemic control. Shouldn’t be used for T1DM or w/ insulin. ADM: T in am w/ or without food. AE: Genital/urinary tract infections (especially females), increased urination, volume depletion leading to hypotension, diabetic ketoacidosis, lower limb amputation, kidney impairment/injury. CI: eGFR<45mL/min/1.73m2. Shouldn't start if eGFR=45-60mL/min/1.73m2. DI: Can have additive volume depletion effect w/ diuretics (particularly w/ loops) . MON: Kidney function must be assessed before and periodically after. DOS: Start=5mg once/d. If necessary increase to Max=15mg once/d. No dose adj if eGFR >60mL/min/1.73m2. OTH: 4th SGLT2 to come out. Segluromet=Steglatro+metformin. Steglujan=Steglatro+sitagliptin.
Sulfonylureas (SUs)
IND: 2nd line for T2DM as monotherapy or combo. MOA: Stimulates β cells to secrete endogenous insulin (both basal and from meals). Also increases insulin sensitivity. EVD: Max effect at half of max dose. Lowers A1C by 1-1.5%. ADM: T w/ or before meal. Don’t take without. AE: Hypoglycemia2-30%, weight gain (1.6kg), alcohol induced flushing, low Na, rash. CI: T1DM, ketoacidosis. DI: Alcohol can cause flushing, changes in glucose, and tachycardia. DOS: Titrate dose q1-2w. OTH: Not CI if sulfa allergy but monitor (Theoretically not related). Body becomes less sensitive after long term use.FIRST GENERATION
EVD:Typically not used due to PKs and DI.
chlorpropamide=Diabinese: AVL: PO. AE: Alcohol associated flushing, hyponatremia. PK: t1/2=36h. Duration=24-72h. DOS: Adj for CrCl. 100-500mg once/d.
tolbutamide=Orinase: AVL: PO. PK: t1/2=4.5-6.5h. Duration=6-12h. DOS: No adj for CrCl. 500-3000mg/d divided once-TID.
SECOND GENERATION
gliclazide=Diamicron: AVL: PO. Long-acting form=Diamicron MR. PK: t1/2=10h. Duration=12-24h. F=97%. One 80mg IR tab=30mg MR tab. DOS: Long-acting=30-120mg once/d. IR: 40-320mg divided Once-BID.
glimepiride=Amaryl: AVL: PO. PK: t1/2=5h. Duration=24h. DOS: Adj for CrCl. 1-4mg once daily.
glyburide=Diabeta=Euglucon: EVD: Only SU not CI in P + L but insulin preferred. ADM: AE: Higher risk of hypoglycemia vs other SUs (especially elderly/renal impairment). On BEERS list (avoid in elderly). PK: t1/2=10h. Duration=18-24h. COS: Cheap. DOS: Adj for CrCl. 2.5-20mg/d divided once/d or BID if >10mg. Max=10mg BID
Synthetic T4
levothyroxine=Synthroid=Eltroxin: AVL: PO (tab , IV, IM). IND: Replaces hormones produced by the thyroid. ADM: T in am 30-60min before food. Interacts with meds/ions so space 4hrs apart. AE: Increased HR, tremor, anxiety, D, exacerbation CVD. Hypothyroidism/low dose can cause hair loss. Warning: Prescribed in micrograms not miligrams. DI: Li decreases release of T3 and T4. PK: t1/2=6-7d. F=40-80% (can change w/ brand). PB=99%. Peak=2-4h. MON: (levels q4w when first starting). DOS: Start=25-50ug. Then adj accoding to bloodwork. Elderly typically require 20-30% lower dose.Thiazolidinediones (TZDs)
IND: T2DM. MOA: Enhances insulin sensitivity by changing gene expression. EVD: Longer glycemic control vs metformin or glyburide. Lowers TGs, increases HDL. Mild BP lowering. Takes 6-12w for full glycemic effect. ADM: AE: Weight gain, edema, can increase LDL, HF, edema, fractures. Low risk of hypoglycemia as monotherapy. CI: HF, liver disease. MON: LFTs. OTH: Aka glitazones. Need written consent to prescribe. May cause ovulation in anovulatory women.pioglitazone=Actos: AVL: PO. Warning: Possible risk of bladder cancer. DOS: 15-45mg once/d.
rosiglitazone=Avandia: AE: Possible increased MI risk. Possible 2-3X fracture risk increase. DOS: 4-8mg/d divided once-BID. OTH: Avandamet=rosiglitazone+metformin.
Alpha Agonists
IND: Glaucoma. AE: Local allergic reaction40%, dry mouth, tachycardia, hypotension, headache, tremor. CI: MAOIs.apraclonidine: AVL: Ophthalmic drops0.5, 1%. DOS: 1-2 drops BID or TID.
brimonidine=Alphagan (P): AVL: Ophthalmic drops0.15, 0.2%. DOS: 1 drop BID.
Beta (β) Blockers
IND: Glaucoma. EVD: Decreases IOP by 20-25%. AE: Usually well tolerated but could get stinging, dry eyes, rarely conjunctivitis. Systemic effects: bronchospasm, exacerbation of CHF, dyspnea, bradycardia, hypotension, syncope, depression, impotence, altered response to hypoglycemia, reduction of high-density lipoproteins. CI: Asthma.betaxolol=Betoptic S: AVL: Ophthalmic drops0.25%. DOS: 1 drop once in am or BID.
levobunolol=Betagan: AVL: Ophthalmic drops0.25,0.5%. DOS: 1 drop once in am or BID.
timolol: AVL: Ophthalmic (drops0.25,0.5%, gel0.25,0.5%). ADM: Shake gel before each use. DOS: DROPS: 1 drop once in am or BID. GEL: 1 drop once/d.
Carbonic Anhydrase Inhibitors
IND: Glaucoma.brinzolamide=Azopt: AVL: Ophthalmic drops1%. DOS: Adj for renal fxn. 1 gtt q12h. OTH:
dorzolamide=Trusopt: AVL: Ophthalmic drops2%.
Cholinergic Agonists
IND: Glaucoma.pilocarpine: AVL: Ophthalmic drops1, 2, 4%. DOS: 1 gtt QID.
Prostaglandin Analogues
IND: Glaucoma. EVD: Decreases IOP 25-30%. AE: Can change eye color and cause excess eyelash growth.bimatoprost=Lumigan RC: AVL: Ophthalmic drops0.01, 0.03%. DOS: 1 gtt in evening.
latanaprost=Xalatan: AVL: Ophthalmic drops0.005%. DOS: 1 gtt in evening.
travoprost=Izba=Travatan Z: AVL: Ophthalmic drops0.003, 0.004%. DOS: 1 gtt in evening.
5-α Reductase Inhibitors
IND: BPH w/ enlarge prostate (>40mL). MOA: Inhibits conversion of testosterone to DHT which shrinks prostate. EVD: Lowers PSA level ~50%. AE: sexual dysfunction, breast tenderness. Warning: Pregnant women shouldn't touch the pills. PK: Onset=3-6 months.dutasteride=Avodart: DI: diltiazem, ketaconazole and ritonavir. PK: t1/2=5wks. F=60%. Met by 3A4. DOS: 0.5mg/d.
finasteride=Proscar: IND: Also marketed as Propecia for hair loss. DI: No significant DIs. PK: t1/2=4.5h. DOS: 5mg/d.
α1 Adrenergic Antagonists
IND: BPH. MOA: Relaxes prostate muscles surrounding urethra. EVD: 60% of pts will see effect. ADM: T at bedtime. AE: dizziness15%, congestion10%, headache15%, weak/lethargic10%. DI: BP lowering meds, phosphodiesterase inhibitors. PK: Onset: 1-2w. OTH: aka alpha blockers. Won’t affect PSA or cause sexual dysfunction. Efficacy doesn’t depend on prostate size.SELECTIVE
AE: Typically fewer AE vs non-selective. COS: More expensive vs non-selective.
tamsulosin=Flomax: AE: Retrograde ejaculation7%. PK: t1/2=6h (IR), 12h (CR). F=90%. Met by 3A4 and 2D6. DOS: 0.4mg/d.
silodosin: AE: Retrograde ejaculation28%.
NON-SELECTIVE
IND: Also used to lower BP. DOS: Start w/ low dose then increase.
doxazosin=Cardural: PK: t1/2=17h. F=65%. Met by 3A4>2D6>2C19 DOS: 1-12mg qHS.
prazosin: PK:F=90%. t1/2=3h (short acting).
terazosin=Hytrin: PK: t1/2=12h. F>90%. DOS: 1-10mg qHS.
Abortion Drugs
Mifegymiso=mifepristone+misoprostol : AVL: Myfegymiso kit= mifepristone (PO1x200mg tab) + misoprostol (buccal4x200ug tabs). MOA: Mifeprstone is a selective progesterone receptor modulator (SPRM) aka anti-progestin. It works by inducing progestin blockade, causing endometrial degeneration, uterine contractility, resumption of prostaglandin production, and decreased βhCG. It also contributes to cervical softening and dilation via a non-prostaglandin pathway (increase of the matrix metalloproteinase-2 expression). Misoprostol is a potent synthetic prostaglandin E1 (PGE1) that induces cervical ripening and uterine contractions. EVD: Three Phase 3 trialsn=146, 214, 551 of Mifegymiso showed efficacy=95.2%-98%. There is slightly higher efficacy and less AE for buccal misoprostol vs PO when combined w/ mifepristone. Mifegymiso is 87-98% effective up to 70d gestational age (off label use). ADM: Can T 63d into Pregnancy. Mifepristone (1 PO tab) taken first then misoprostol (4 buccal tabs) taken 24-48h after. Buccal tabs: hold 4 tabs between cheek and gums for 30min then swallow any remaining fragments. Once mifepristone is taken misoprostol must be taken as well. AE: >10%: Naus, vom, diar, abdominal pain, headache, vaginal bleeding (heavier than period), uterine cramping, fatigue, chills, fever, dizziness. 1-10%: Prolonged bleeding, breast tenderness, endometreitis. <1%: rupture of ectopic pregnancy (severe bleeding and cramping), toxic shock syndrome, hot flush, hypotension, arrhythmia, bronchospasm, rash. mortality risk (4 in 1,000,000) usually from infection or undiagnosed ectopic pregnancy. CI: AnemiaHgb<9.5g/dL (less blood loss w/ surgical abortion), recent bleeding or pelvic pain, ectopic pregnancy, uncontrolled astma, IUD in place. PRG: Mifepreistone alone possibly not teratogenic (rarely studied alone). Misoprostol has been linked to teratogenicity. LAC: <1.5% of dose found milk. Breastfeeding is likely safe in lactation. DI: Mifepristone: 3A4 inducers (Rifampin, SJW etc.), 3A4 inhibitors (Ketoconazole, GFJ etc). PK: mifepristone: t1/2=83-90h. Tmax=1-2h. PB=94-99%. Met by 3A4. Irreversibly inhibits 3A4, and to a lesser extent 1A, 2B, 2D6, 2E1. Excretion is primarily fecal (<10% in urine). misoprostol: t1/2=20-40min. Tmax=30min. Not met by CYPs. Rapidly de-esterified in liver. SL Tmax=30min. *Buccal:* contractions in ~67min w/ sustained action 90min later and declines at 5h. *Vaginal:* first contractions in ~98min. Sustained action at 128min and contractions declines at 5h. Moistened tabs may increase AUC when administered vaginally. COS: $350.62 for 1 pack2017 (Covered completely in NS through MSI). DOS: Less than 1% of active misoprostol metabolite is excreted in urine, and renal dosing is generally not required. OTH: Partner’s consent is also not necessary. Pt doesn’t have to attend abortion clinic to get prescribe Myfegymiso. Ovulation possible 8d after abortion. COCs patches, rings can be inserted on the same day or day after abortion. IUDs can be inserted at 1w follow up. Misoprostol is unstable outside blister pack. Doesn’t affect future fertility or rate of complications. PhC can’t prescribe mifegymiso. Blood levels for mifepristone are similar after 100-600mg doses leading Canada to have a lower dose vs USA. Misoprostol:Anticholinergic/Antispasmodics
IND: Overactive bladder. MOA: Competitive antagonist of acetylcholine which relaxes bladder smooth muscles.oxybutynin=Oxytrol: AVL: PO, patch. IND: Urge incontinence, urgency, and frequency. ADM: T w/ or without food. Patch can be applied to abdomen, hip, or butt. AE: Dry mouth/eyes/skin, sedation, dizziness, blurred vision, Naus, Vom, Com, Diar, headache, unusual taste, application site itch/redness. CI: <5yo PK: Racemic mixture of R and S enantiomers (R=most active). DOS: BID or TID.
Contraceptives - Combination Oral Contraceptives (COCs)
AVL: PO tabs. Contraception, acneAlesse MOA: Estrogen and progestins suppress gonadotropins which inhibits ovulation, and may change endometrium and cervical mucusref. CI: Hx or actual thrombophlebitis or thromboembolic disorder, Hx or actual cerebrovascular disorders, Hx or actual MI or coronary arterial disease, DVT, thrombogenic valvulopathies and thrombogenic rhythm disorders, hereditary or acquired thrombophilias, migraine w/ aura (current or history), liver disease or abnormal liver fxn test, Hx or actual liver tumours, breast cancer, estrogen-dependent neoplasia, undiagnosed abnormal vaginal bleeding, jaundice, ocular lesion arising from ophthalmic vascular disease, such as loss of vision, pregnancy, diabetes w/ vascular involvement, uncontrolled HTN, pancreatitis associated with severe hypertriglyceridemia (current or Hx). Warning: Increased risk of heart/vessel conditions of smoking + COC (especially >35yo). D/C after any of the following: Thromboembolic and cardiovascular disorders, such as thrombophlebitis, PE, cerebrovascular disorders, MI, mesenteric ischemia, mesenteric thrombosis and retinal thrombosis, immobilization/confinement to bed, visual defects, papilledema or ophthalmic vascular lesions, severe headache of unknown etiology, or worsening of pre-existing migraine headache, increase in epileptic seizures. No STI protection (use condoms). PRG: Fetal abnormalities reported in babies of women who have taken COCs early in pregnancyref. LAC: hormones excreted in breast milk and may reduce quantity and quality. Long-term effects unknown. Cases of breast enlargement reported in breast-fed infantsref. DI: Anti-viral Hep C Virus (HCV) combination drug regimen ombitasvir, paritaprevir, ritonavir and dasabuvir, w/ or without ribavirin. PK: Vom and/or Diarr, may reduce absorption of COCs (use backup). EE: t1/2=6-20hrs. tmax=1-2hrs. F=40%. PB=98%. Partially eliminated in feces via biliary excretionref. DOS: New users COCs should be started on <50ug of estrogen. OTH: EE= ethinyl estradiol.FIRST GEN PROGESTINS - NORETHINDRONE
Brevicon(0.5)=Ortho(D/C)=0.5mg norethindrone + 0.035mg EE:
AVL:21+28pkref.
EVD: ref.
ADM: ref.
AE: Naus, Vom, headache, bloating, breast tenderness, swelling of ankles/feet, weight change, spotting.ref.
CI: ref.
PRG: ref.
LAC: ref.
DI: ref.
PK: Norethindrone: t1/2=5-14hrs. tmax=0.5-4hrs. F=65%. PB=80%. Partially eliminated in feces via biliary excretionref.
COS: ref.
AUX: ref.
MON: ref.
DOS: ref.
OTH: ref.
Brevicon(1)=Select= 1mg norethindrone + 0.035mg EE:
AVL:21+28pkref.
EVD: ref.
ADM: ref.
AE: Naus, Vom, headache, bloating, breast tenderness, swelling of ankles/feet, weight change, spotting.ref.ref.
CI: ref.
PRG: ref.
LAC: ref.
DI: ref.
PK: Norethindrone: t1/2=5-14hrs. tmax=0.5-4hrs. F=65%. PB=80%. Partially eliminated in feces via biliary excretionref.
COS:
AUX: ref.
MON: ref.
DOS: ref.
OTH: ref.
SECOND GEN PROGESTINS - LEVONORGESTREL
Alesse=Alysena=Aviane=0.1mg levonorgestrel + 0.02mg EE:
AVL: 21+28pkref.
IND: Contraception, moderate acne(>14yo)ref.
MOA: ref.
EVD: Pearl Index=0.84
ADM:
AE: Headache31%, abnormal bleeding22%, Naus14%, abdominal pain8%, menstural disorder6%, allergic rxn5%, breast pain5%, weakness4%, weight gain3%, emotional lability3%, acne3%, migraine3%, dizziness3%, Vom3%
CI: See above.
PRG:
LAC:
DI:
PK:
COS: Alesse is Brand (more expensive).
AUX:
MON:
DOS: 1 tab daily w/ 7 days of placebo or no pill. Missed dose see monograph. Don't use before menarche
OTH:
ref.
AB
BC
MB
NB
NL
NS
ON
PE
SK
Min-Ovral=Ovima=Portia(D/C)=0.15mg levonorgestrel + 0.03mg EE:
AVL:21+28pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
Seasonale=Indayo=0.15mg levonorgestrel + 0.03mg EE:
AVL:91pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
Triquilar=0.05/0.075/0.125mg levonorgestrel + 0.03/0.04/0.03mg EE (triphasic):
AVL:21+28pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
THIRD GEN PROGESTINS - DESOGESTREL OR NORGESTIMATE
Cyclen=0.25mg norgestimate + 0.035mg EE:
AVL:21+28pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
Linessa=Orthocept(D/C)=0.1/0.125/0.15mg desogestrel (triphasic) + 0.025mg EE:
AVL: 21+28pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
Marvelon=Apri=Freya=Mirvala=0.15mg desogestrel + 0.03mg EE:
AVL:21+28pk
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
ref.
Tri-Cyclen=0.18/0.215/0.25mg norgestimate (triphasic) + 0.035mg EE:
AVL:21pk onlyref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
Tri-Cyclen Lo=Tricira Lo=0.18/0.215/0.25mg norgestimate + 0.025 mg EE:
AVL: 21+28pkref.
IND:
MOA:
EVD:
ADM:
AE:
CI:
PRG:
LAC:
DI:
PK:
COS:
AUX:
MON:
DOS:
OTH:
FOURTH GEN PROGESTINS - DROSPIRENONE
Yasmin=Zarah(D/C)=Zamine=3mg drospirenone + 0.03mg EE:
AVL: 21+28pkref.
IND: .
MOA: .
EVD: .
ADM: .
AE: .
CI: .
PRG:
LAC: .
DI: .
PK: .
COS: .
AUX: .
MON: .
DOS: .
OTH: .
Yaz=MYA=3mg drospirenone + 0.02mg EE:
AVL: 28pk onlyref.
IND: .
MOA: .
EVD: .
ADM: .
AE: .
CI: .
PRG:
LAC: .
DI: .
PK: .
COS: .
AUX: .
MON: .
DOS: .
OTH: .
Yaz Plus=3mg drospirenone + 0.02mg EE + 0.451mg levomefolate:
AVL: 28pk onlyref.
IND: .
MOA: .
EVD: .
ADM: .
AE: .
CI: .
PRG:
LAC: .
DI: .
PK: .
COS: .
AUX: .
MON: .
DOS: .
OTH: .
ACNE ONLY INDICATION - CYPROTERONE
Diane-35=Cléo-35=Cyestra-35=2mg cyproterone + 0.035mg EE:
AVL: 21pk onlyref.
IND: .
MOA: .
EVD: .
ADM: .
AE: .
CI: .
PRG:
LAC: .
DI: .
PK: .
COS: .
AUX: .
MON: .
DOS: .
OTH: .
Contraceptives (Progesterone Only)
Depo-Provera=medroxyprogesterone: AVL: IM susp150mg/mL x1mL or 50mg/mL x5mL ref. IND: Contraception, endometriosisref. MOA: Prevents ovulation, thins endometrial lining, and thickens cervical mucusref. EVD: 99.7% effectiveref. ADM: Shake vialref. Inject in deltoid or gluteal muscleref. AE: Headache17%, abdominal distress12%, nervousness12%, dizziness6%, decreased libido6%, irregular bleeding or spotting, wt gainmean=5.4Ilbs after 1yr (~30% loose wt), return of fertility on average 9mths after last injection. Reduced bone density (especially <18yo), amenorrheaafter 1yr=55%. 2yrs=68%, site rxn, no side effects54% ref. CI: Already pregnant, breast or progestin-dependent cancer, history or clotting dissorder (VTE, stroke, MI), BP >160/100, >15 cigarettes/day + >35yo, diabetes w/ vascular involvement, migraine w/ aura, liver disease, loss of visionref. PRG: Exposure to Depo-Provera increases risk of low birth wt, limb malformation, chromosomal anomalies and neonatal death (pregnancy unlikely)ref. LAC: Secreted in breast milk. Can be given >6wks postpartum. May affect neonatal feeding disordersref. DI: Rifampin may increase clearance of medroxyprogesteroneref. PK: t1/2=~1000hrs. tmax=4-20days. Vd=20L. PB=90-95%. MM=386.53g/mol. Metabolized by 3A4ref. COS: $48.25 (150mg=1mL=90days)NS-2020. Covered in AB, BC, MB, NB, NS, ON, SK. Not covered in NL, PE, QE. AUX: Do Not Take This Drug If You Become Pregnant. Store At Room Temperatureref. MON: Pap smear and BP should be done before starting and yearly after. Carefully observe women w/ history of depression. Bone density test after 2yrs of useref. DOS: Contraception: 150mg=1mL q3mths (10-13wks) IM. For first admin, give within first 5d of cycle to assure non-pregnancy. If after 5d use backup for 4wks. Don't start before menarche. Not typically given <18yo because of bone loss. Endometriosis: 50mg weekly or 100mg q2wks IM x at least 6mthsref. OTH: Keep vial at room temp. Decreased risk of endometrial cancer. Slight or no increased risk of breast cancer. No increased risk of ovarian, liver, or cervical cancerref. norethindrone=Micronor=Jencycla=Movisse:
AVL: PO0.35mg tab-28 pack only ref.
IND: Contraceptionref.
MOA: Thickens cervical mucus, makes endometrium inhospitable, sometimes prevents ovulationref.
EVD: Perfect use=99.5% effective. Typical use=95% effective. COCs are 99.9% effective w/ perfect useref.
ADM: Take at same time every day. If >3hrs late, take missed pill and use backup for 48hrsref.
AE: Abnormal bleeding34%, Naus9%, headache6%, amenorrhea5%, Vom2%, dizziness2%, breast tenderness1%, fatigue1%, weight increase1% ref.
CI: Pregnancy, liver disease, breast cancer, abnormal vaginal bleedingref.
PRG: May increase risk of ectopic pregnancyref.
LAC: Small amounts of progestins pass through breast milk. No AEs for infant. If fully breast-feeding may start >6wks post-delivery. If partially breast-feeding may start >3wks post-deliveryref.
DI: Antiepileptics, rifampin, antiretroviarals, St. John’s wortref.
PK: tmax=2hrs. MM=298.42g/molref.
COS: Generic=$24.04/28daysNS-2020. Covered in: AB, BC, MB, NB, NL, NS, ON, PE,
SK. Micronor is the brand name (more expensive) formulation.
AUX: Do not take this drug if you become pregnantref.
MON: BP, breasts, liver, pelvic organs, pap smear before prescribing. Repeat 3 months after and ~q3years. Monitor for changes in mood (especially if history of depression)ref.
DOS: 0.35mg once/d. No pill free interval. Start on days 1-5 of menses. If taken on other day, use backup for 48hrs. Can start day after miscarriage or abortion. If switching from COC, start norethindrone the day after the last active pill. If switching to COC, start COC on day 1 of period even if pack is not finishedref.
OTH: Aka progesterone-only pill (POP) or mini-pill. No delay of fertility after D/C. Doesn't protect from STDsref. Good alternative to COCs for smokers.
Plan B:
AVL: 1 pill as a high dose of progesterone.
EVD: Possibly less effective if obese.
ADM: Take w/ food.
Contraceptives (Other)
Evra Patch=norelgestromin+ethinyl estradiol: AVL: Transdermal patch6mg norelgestromin+0.6mg ethinyl estradiol/patch. 3 patches/boxref. IND: Contraceptionref. MOA: Inhibits ovulation, changes cervical mucus (difficult for sperm to enter uterus) and endometrium (decreased chance of implantation)ref. EVD: Comparable efficacy to COCs. May be less effective if >90kg and increased VTE risk if BMI>30kg/m2. Pts more adherent to patches (weekly) vs oral contraceptives (daily)ref. ADM: Apply to clean, dry, hairless, intact healthy skin on the butt, abdomen, upper outer arm or upper torso. Avoid breasts or areas rubbed by clothing. Avoid red, irritated or cut skin. Change patch on same day of week. Don't cut patch. Fold into itself to disposeref. AE: Headache21%, Naus17%, site rxn17%, breast discomfort17%, dysmenorrhea10%, abdominal pain9%, vaginitis5%, Vom5%, Diar4%, emotional lability4%, breast pain4%, itching4%, acne3%, fatigue3%, yeast infection3%, weight increase3%, dizziness3%, depression3%, migraine3%, spoting3%, heavy period3%, dyspepsia2%, flatulence2%, gastroenteritis2%, fever2%, muscle pain2%, UTI2%, breast engorgement/enlargement2%, rash2%, vaginal discharge2%, malaise1%, allergy1%, tendon disorder1%, decreased libido1% ref. CI: Current or history of clots (ex. MI, stroke), liver disease, jaundice, breast or endometrium cancer, unusual vaginal bleeding, loss of vision, pregnancy, migraine w/ aura, BP >160/100, >35+smoking, diabetes w/ vascular involvment, immobilizationref. PRG: D/C patch if pregnant but no evidence of harm if used while pregnantref. LAC: Don't use until child is completely weaned. Hormonal components found in breast milk and may affect quantity and quality. Child may get jaundice and breast enlargement ref. DI: Hep C/HIV antivirals, rifampin, antibiotics (possibly), St. John's wortref. PK: tmax=48hrs. Dose could increase w/ fever or if heat pad is placed on patchref. COS: Not covered in: AB, BC, NB, NL, NS, ON, PE, SK. AUX: FOR EXTERNAL USE ONLY. DO NOT USE IF YOU BECOME PREGNANTref. MON: Follow up at 3 months then yearly. Monitor breast, BP, and Pap smear if pt sexually activeref. DOS: ~200μg norelgestromin+35μg ethinyl estradiol released/24hrs. Start 1st patch on 1st day of period. New patch q wk x 3wks. No patch wk 4 (withdrawl bleed)ref. OTH: Doesn't stop STIs. Decreased risk of endometrium and ovarian cancer. Decreased blood loss and more regular cycles. May decrease severity of dysmenorrhea and PMS. May improve acne and hirsutism. Decreased pelvic inflammatory disease and ectopic pregnancy. If patch comes off, no need for backup if off for <24hrs. If patch is off for >24hrs or doing Sunday start, use backup for 1wk. If unsure when patch fell off restart new cycle and use backup for 1wk. When patch change is missed (day 8 or 15), if within 48hrs, apply new patch then return to usual patch day. No backup needed. If >48hrs, start new cycle and use backup for 1wk. If patch removal (day 22) is missed, remove patch and return to usual patch day. If switching from COC, start patch on 1st day of withdrawal bleed (<7 days of last active pill). If not breast-feeding, wait >4wks post-partum before starting patch. After abortion or miscarriage (<20wks gestation) may start patch on Day 21 post-abortion or on first day of period (whichever comes first)ref. NuvaRing=etonogestrel+ethinyl estradiol:
AVL: Slow release vaginal ring etonogestrel/ethinyl estradiol (11.4mg/2.6mg). 1 or 3 rings/pack ref.
IND: Contraceptionref.
MOA: Inhibits ovulation (main), changes cervical mucus (less sperm into uterus) and endometrium (implantation less likely)ref.
EVD: 98-99% effectiveref.
ADM: Position self comfortably (standing w/ one leg up, squatting, or lying down). Compress ring and insert in vagina until comfortable. Exact position in vagina not critical. Remove using finger(s). Don't remove ring during sex. Check periodically for expultionref.
AE: Headache6%, vaginitis6%, vaginal discharge5%, device related problems4% weight increase4%, emotional lability3%, breast pain3%, painful period3%, Naus3%, vaginal discomfort2%, acne2%, abdominal pain2%, expulsion2%/yr, migraine1%, decreased libido1%, depression1%, tissue growth over ring (removal by Dr)very rare. During sex some partners may feel the ringnot problem for 90% of couples
ref.
CI: History or present blood clot (VTE, MI, Stroke), BP>160/110, severe dyslipoproteinemia, smoking + >35yo, diabetes w/ vascular involvemnet, imobilization, migraine w/ aura, vascular eye disease, pancreatitis, liver disease, undiagnosed vaginal bleeding, pregnancyref.
PRG: D/C if pregnant but no evidence of harmref.
LAC: Not recomended but no evidence of harmref.
DI: Hep C/HIV drugs, rifampin, St. John's wort. May interfere w/ diaphragm, cervical cap or female condomref.
PK: t1/2=6/29hrs. tmax=70/67hrs. PB=98%(both). Met by 3A4ref.
COS: Covered in: NB, NSfamily only,
SK. Not covered in: AB, BC,
MB, NL, ON, PE.
AUX: For vaginal use only. Exp 4 months after dispensingref.
MON: BP, breasts, liver, extremities pelvic organs (before prescribing). Pap smear if sexually active. Follow up at 3mths then yearlyref.
DOS: 1 ring left in place for 3wks then removed for 1wk. Start within 5 days of period. Use backup for 7 days for first cycle. Safety and efficacy <18yo not established. 120ug etonogestrel+15 mcg ethinyl estradiol realeased /24hrsref.
OTH: If ring expelled and left outside vagina <3hrs, rinse w/ cool-lukewarm water and re-insert (no backup needed). If ring lost, Insert new ring and resume usual schedule. If out >3hrs, for 1st or 2nd wk, use backup for 7 days. If out >3hrs during 3rdrd wk, either insert new ring immediately and leave in for 3wks or have withdrawal bleeding and insert new ring < 7 days from when previous ring was removed. Never > 7 days without ring. Withdrawal bleed starts ~2-3 days after removal and may not be finished before next ring is inserted. If removed on wk 4, remove and keep same schedule. Store in fridge. Stable up to 4 mths at 2-30°Cref.
Mirena IUD: MOA: Thickens cervical mucus, stops endometrial perforation, may inhibit implantation, may inhibit ovulation. EVD: Takes 7d to be effective unless started within first 7d period. Fertility can return immediately after removal. Has less bleeding and cramps vs copper IUDs. MON: Check strings after each period. OTH: Progestin only IUS. 50% of pts will stop having period.
Phosphodiesterase inhibitors (PDE5I)
IND: Erectile disfunction (ED), pulmonary HTN. MOA: Inhibits the enzyme that degrades cGMP in the corpus carvenosum. cGMP is a molecule that dilates the blood vessels leading to the penis. Warning: See Dr. for erection lasting >4h. DI: Nitrates, alpha blocker (hypotension), 3A4 inducers/inhibitors. COS: Typically not covered by insurance. OTH: Won’t increase sex drive.sildenafil=Viagra: AVL: PO (tabs25,50,100mg). IND: ED, pulmonary HTN. ADM: T ~1h (30min-4h) before sexual activity. AE: Headache15%, flushing10%, upset stomach6%, indigestion7%, vision changesrare. CI/Warning: Wait >24h to give nitrates. PK: t1/2=3-5h. Tmax=30-120min. Met by 3A4(major) and 2C9(minor). Excreted 80% in feces and 13% in urine. COS: 4 tabs (1box)2017: 25mg generic=$48.41. 50mg generic=$50.93. 50mg brand=$54.00. 100mg generic=$52.52. 100mg brand=$55.71. DOS: Start=25mg. OTH: Doesn’t increase MI or death. Drops BP by 8.3/5.3 mmHg at peak 1-2h after dose.
tadalafil=Cialis: IND: Also used w/ alpha blockers (if dose is stabilized) for BPH. ADM: Can be taken 0.5-36h before sexual activity. AE: Headache11%, indigestion7%, back/muscle pain4%, flushing4%, dizziness1.7%, vision changesrare. CI: Wait >48h to give nitrates. Not studied <18yo. PK: t1/2=17.5h. Met by 3A4. COS: 4 tabs (1 box)2017: 10mg generic=$64.81. 10mg brand=$64.97. 20mg generic=$66.77. 20mg brand=$66.91. DOS: 2.5mg or 5mg daily for daily dosing. 10mg or 20mg for prn dosing.
vardenafil=Levitra: AVL: PO (tab5,10,20mg). ADM: T 25-60min before sexual activity. Can T w/ food but will delay effect. AE: Headache10%, Naus1.2%, nasal congestion4%, flushing11.3%, indigestion2.5%, hearing lossrare, priapismrare. minor QT prolongation. PK: t1/2=4-5h. F=15%. PB=high. Met by 3A4 (main), 3A5, 2C9. DOS: >65yo start=5mg. Adult start=10mg. Max=20mg. OTH: Only avail as Brand2017. Decreases BP by 7/8 mmHg.
Aminoglycosides (AGs)
MOA: Bind 30S subunit of ribosomes. AE: nephrotoxicity/ototoxicity. Nephrotoxicity comparison: neomycin > gentamicin=tobramycin=amikacin=netilmicin>streptomycin. DI: Administering w/ vancomycin or loop diuretic can lead to more nephro/ototoxicity. Direct contact w/ penicillins can inactivate aminoglycosides. OTH: Bactericidal. Concentration dependent killer. Most effect on gram (-) some (+). Has post antibiotic effect against gram (-). Doesn’t penetrate pulmonary tissue well.amikacin: AVL: IV, IM. PK: t1/2=2.5h. PB~10%. DOS: Adj for renal fxn. OTH: Covers Pseudomonas.
gentamicin: AVL: Avail IV, IM, implantable beads, topical. IND: Meningitis. AE: Nephrotoxicity, ototoxicity. LAC: Safe. PK: t1/2=2.5h. PB~10%. DOS: Adj for renal fxn. Std=1.5mg/kg q8h. Extended interval=4-7mg/kg once/d. OTH: Covers some MSSA (+), some Strep (+), some Enterococcus (+), GNR, Pseudomonas (-) but 2-4 times less active than tobramycin.
neomycin: IND: Surgical prophylaxis, hepatic encephalopathy, acne. AE: Naus, Vom, Diar, sore mouth, anorectal pain/irritation. PK: F=3%.
streptomycin: AVL: IM. IND: TB, MAC. AE: ototoxicity, Naus, Vom, vertigo, rash, fever; hives, edema. PK: t1/2=2.5h. DOS: Adj for kidney fxn.
tobramycin: AVL: IV, IM, ophthalmic, oral inhalation. IND: Cystic fibrosis. LAC: Safe. PK: t1/2=2.5h. DOS: Adj for renal fxn. Std=1.5mg/kg q8h. Extended interval=4-7mg/kg once/d. OTH: Covers some MSSA (+), some Strep (+), some Enterococcus (+), GNR, Pseudomonas (-).
Anthelmintics
mebendazole=Vermox: AVL: PO. IND: Threadworms/pinworms. MOA: Inhibits glucose update by helminthes. EVD: Close to 100% cure rate. May be best option in prg + lac. Fewer AEs than pyrantel pamoate. AE: Drowsiness, headache, diar, vom, dizziness, increased AST/ALT, flatulence, skin itch. DI: metronidazole (SJS risk), cimetidine inhibits metabolism of mebendazole. DOS: >2yo: 100mg single dose. Repeat in 1-2w.pyrantel=Combantrin: AVL: PO. IND: Threadworms/pinworms. MOA: Interferes with neurologic function of helminth. EVD: Cure rate~90%. AE: Headache, naus, vom, diar, dizziness, drowsiness, abdominal pain, anorexia, transient increase in AST. CI: Liver disease. PRG: CI in 1st trimester. DOS: >1yo: 11mg/kg (base) as a single dose. Max=1g. Repeat in 2w. OTH: Full name pyrantel pamoate.
Antifungals
fluconazole: IND: Candidiasis (esophageal, peritoneal, UT, vaginal) infections, pneumonia. MOA: Interferes w/ fungal CYP 450 enzymes decreasing ergosterol synthesis and inhibiting membrane formation. ADM: AE: Naus2-7%, Vom2-5%, Diar2-3%, abdominal pain2-6%, Headache2-13%, skin rash2%, dizziness1%, increased liver enzymes. Increases QT interval. PK: t1/2=30h (20-50h). F=90%. PB=11-12%. Inhibits: 2C19 (strong), 2C9 (mod), 3A4 (mod), 1A2 (weak). Food doesn’t affect F. OTH: 6 months of weekly Tx did not show increased resistance.Antimalarial
Malarone=(250mg atovaquone + 100mg proguanil): IND: Malaria (Tx and prophylaxis). AE: Naus11%, Vom12%, Dia8%, anorexia5%, fever11%, abdominal pain15%. CI: CrCl<30. DI: Tetracycline, metoclopramide, rifabutin and rifampicin (increased Cl). PK: t1/2=1-3d depending on weight. PB>99%.Antiparasitics
ivermectin=Stromectol: AVL: PO (tab3mg) IND: Tx of intestinal strongyloidiasis and onchocerciasis (river blindness). MOA: Broad spectrum antiparasitic that affects invertebrate nerve and muscle cells, resulting in paralysis and death of parasite. EVD: ADM: Take on empty stomach w/ water. AE: Dizziness1-3%, pruritus1-3%, diar1-3%, naus1-3%, anorexia<1%, vom<1%, const<1%, fatigue<1%, abdominal pain<1%, somnolence<1%, vertigo<1%, tremor<1%, rash<1%, urticaria<1%, arthralgia/synovitis, axillary/cervical/inguinal lymph node enlargement and tenderness, skin edema, rash, fever, orthostatic hypotension, tachycardia, headache, abnormal sensation in the eyes, eyelid edema, anterior uveitis, conjunctivitis, limbitis, keratitis, chorioretinitis. CI: No safety/efficacy data in children <15kg. DI: Possible increased INR when used w/ warfarin. MON: Stool examination after dose to verify eradication. DOS: STRONGYLODIASIS: Single oral dose ~200μg/kg. Typical=1-5 tabs. If inefective, repeat course at 2 week intervals. ONCHOCERCIASIS: Single oral dose of ~150 μg/kg. Can retreat at 3 month intervals if necessary.Antivirals
abacavir (ABC)=Ziagen: IND: HIV. ADM: T once/d w/ or without food. No food restrictions. AE: Naus,Vom, increased lipids, liver toxicity, bone loss, lactic acidosis, lipoatrophy, hypersensitivity rxn, MI risk. CI: HLA-B*5701(+) (abacavir allergy). OTH: Triumeq=(DTG+ABC+3TC) 1 tab daily. Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs)acyclovir=Zovirax: AVL: PO, topical and IV. IND: Genital HSV, shingles, and chickenpox. MOA: Inhibits DNA polymerase. EVD: IV 25% more effective than PO. AE: Naus,can crystalize in kidneys. PK: t1/2=3h. PB:9-23%. DOS:Depends on indication (first treatment, suppression, recurrent). Adjust for renal fxn.
adefovir: IND: chronic Hep B with cirrhosis. OTH: Drug Class: Nucleotide Reverse Transcriptase Inhibitors (NRTIs/NtRTIs).
atazanvir (ATV)=Reyataz: IND: HIV. ADM: T w/ food (requires gastric acidity for F). AE: Gallstones, kidney stones, dyslipidemia, insulin resistance, MI/stroke?, hepatitis. Can affect BG levels. DI: PPI, H2RA (need acidity for F). OTH: Drug class: Protease Inhibitors (PI).
darunavir (DRV)=Presista: IND: HIV. ADM: T w/ food. AE: Naus, headache, rash, sulfa allergy, dyslipidemia, insulin resistance, MI/stroke?, hepatitis. Can affect BG levels. OTH: Drug class: Protease Inhibitors (PI).
delavirdine (DLV)=Rescriptor: IND: HIV. AE: Headache, rash, increased liver enzymes. OTH: Drug Class: Non-Nucleosides/Nucleotide Revers Transcriptase Inhibitors (NNRTIs)
didanosine (DDL)=Videx: IND: HIV. AE: GI intolerance, pancreatitis, increased uric acid and lactic acid, reversible peripheral neuropathy, hepatic steatosis. DI: tenofovir (increased DDL). OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
dolutegravir (DTG)=Tivicay: IND: HIV. MOA: Integrase Strand Transfer Inhibitor. EVD: Found superior vs other ARV drugs because of tolerabilility. ADM: T once/d w/ or without food. AE: Headache, insomnia. DI: Ca, Fe (decreased F). DOS: 1 tab once daily. OTH: Triumeq=(DTG+ABC+3TC). Drug class: Integrase Strand Transfer Inhibitors (INSTIs)
efavirenz (EFV)=Sustiva: IND: HIV. EVD: Preferred NNRTI ADM: T once/D without food. AE: Lipoatrophy, increased lipids, rash, psychiatric effects. PRG: CI - avoid if childbearing potential. OTH: Drug Class: Non-Nucleosides/Nucleotide Revers Transcriptase Inhibitors (NNRTIs)
elvitegravir (EVG): IND: HIV. MOA: Integrase Strand Transfer Inhibitor. ADM: T OD w/ or without food. AE: Naus, Diar, Headache, Upper Respiratory Tract Infection (URTI), insomnia, increased lipids. DI: Ca, Fe (decreased F). OTH: Drug class: Integrase Strand Transfer Inhibitors (INSTIs)
emtricitabine (FTC): IND: HIV (PEP and PrEP). ADM: T once/d w/ or without food. AE: Naus, Vom, increased lipids, liver toxicity, bone loss, lactic acidosis, lipoatrophy, hyperpigmentation. OTH: Don’t use w/ 3TC since similar resistance. Truvada=(FTC+TDF). Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
enfuvirtide=Fuzeon: AVL: SubQ. IND: HIV (2nd line). MOA: Inhibits gp41 mediated viral fusion to CD4 cells. AE: rash/site rxn. PK: t1/2=3.8h. PB=92%. DOS: 90mg=1mL BID SubQ. No adjustment for renal fxn or dialysis.
entecavir=Baraclude: AVL: PO (tab or soln). IND: Hep B. OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
etravirdine=Intelence: IND: HIV. ADM: T w/ food. AE: Naus, rash. OTH: Drug Class: Non-Nucleosides/Nucleotide Revers Transcriptase Inhibitors (NNRTIs).
famciclovir=Famvir: AVL: PO,SubQ. IND: Genital HSV, shingles. MOA: Inhibits DNA polymerase. AE: Same as placebo. DI: Preobenecid may decrease Cl. PK: Hepatically converted to active drug penciclovir (famciclovir has no activity). famciclovir F=77%, penciclovir t1/2=2.3h. PB<20%. COS: DOS: Adj for renal fxn. OTH: Tabs contain lactose.
fosamprenavir=Telzir: IND: HIV. EVD: Not preferred PI. Can affect BG levels. AE: Rash, GI upset, hyperlipidemia OTH: Used with ritonavir. Drug class: Protease Inhibitors (PI).
Harvoni=ledipasvir90mg + sofosbuvir400mg): AVL: PO. IND: Chronic Hep C MOA: Both target proteins involved in viral replication. EVD: Sustained Virologic Response (SVR) at 12w=90%. ADM: T once/d w/ or without food. AE: ~=placebo: Headache4%, fatigue5%. DI: P-gp inducers ex. rifampin, SJW: decreased plasma concentrations of both. Separate antacids by 4h (need acidity for F). PK: sofobuvir is metabolized to GS-331007. ledipasvir t1/2=47h. GS-331007 t1/2=27h. ledipasvir PB >99%. GS-331007 PB minimal. OTH: Often given with ribavirin. Contains lactose.
Holkira Pak=(12.5mg ombitasvir + 75mg paritaprevir + 50mg ritonavir + 250mg dasabuvir): AVL: PO (Combination pill (ombitasvir+paritaprevir+ritonavir) w/ desbuvir in a separate tab). IND: Chronic Hep C. EVD: Sustained Virologic Response (SVR) at 12w >d90%. AE: Naus3%, fatigue4%, HA4.5%. Mild QT prolongation (3.2msec). PK: ritonavir is strong 3A4 inhibitor. All drugs >97% PB. DOS: 2 combo tabs (ombitasvir/paritaprevir/ritonavir) in am and 1 dasabuvir BID. No adj for renal fxn. OTH: dasabuvir contains lactose.
indinavir=Crixivan: IND: HIV. AE: Nephrolithiasis, chronic interstitial nephritis, liver enzyme elevations, hyperlipidemia. Can affect BG levels. PK: t1/2=2h. PB=60% (lowest in class). OTH: Drug class: Protease Inhibitors (PI).
lamivudine (3TC): IND: Chronic Hep B and HIV. MOA: T once/d w/ or without food. AE: Naus,Vom, increased lipids, liver toxicity, bone loss, lactic acidosis, lipoatrophy. OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs). Don’t use w/ FTC (similar resistance). Triumeq=(DTG+ABC+3TC) T 1 tab OD w/ or without food.
lopinavir (LPV)=Kaletra: IND: HIV. EVD: Not preferred PI. ADM: T w/ or without food. AE: GI upset, QT prolongation, liver enzyme increase, dyslipidemia, insulin resistance, MI/ stroke?, hepatitis. Can affect BG levels. OTH: Used with ritonavir. Drug class: Protease Inhibitors (PI).
maraviroc=Celsentri: IND: HIV (not 1st line). MOA: CCR5 antagonist. ADM: T w/ or without food. AE: hepatotoxicity, cough, fever, rash, abdominal pain. DOS: BID. Dose depends on other antiretrovirals (150mg BID if w/ 3A inhibitors like PI). OTH: Tropism assay will determine if CCR5 receptor positive.
nelfinavir=Viracept: IND: HIV. AE: Diar, hyperlipidemia. Can affect BG levels. OTH: Drug class: Protease Inhibitors (PI).
nevirapine (NVP)=Viramune: IND: HIV. AE: Rash, increased liver enzymes. OTH: Drug Class: Non-Nucleosides/Nucleotide Revers Transcriptase Inhibitors (NNRTIs).
raltegravir (RAL)=Isentress: IND: HIV. MOA: Integrase Strand Transfer Inhibitor. ADM: T w/ or without food. AE: Elevated CK, myositis, rhabdomyolysis, skin rxn, insomnia. DI: Ca, Fe (decreased F). DOS: BID OTH: Drug class: Integrase Strand Transfer Inhibitors (INSTIs).
ribavirin=Moderiba: AVL: PO (tab). IND: Chronic Hep C. AE: fatigue4%, headache5%, naus3%, itch, insomnia. PRG: CI. PK: t1/2=300h. OTH: Often used with Harvoni or Holkira Pak.
rilpivirene (RPV)=Edurant: IND: HIV. ADM: T OD w/ food. AE: Lipoatrophy, increased lipids, rash. Less psychiatric effects vs EFV. OTH: Drug Class: Non-Nucleosides/Nucleotide Revers Transcriptase Inhibitors (NNRTIs).
ritonavir (RTV)=Norvir: IND: HIV. AE: Diar, GI upset, liver enzyme elevation. Can affect BG levels. PK: t1/2=3h. PB>96%. PK booster by inhibiting 3A4, 2D6, and 2C9. OTH: Drug class: Protease Inhibitors (PI).
saquinavir=Invirase: AE: Increased liver enzymes, GI upset, hyperlipidemia. Possible QT. Can affect BG levels. PK: t1/2=10h. PB>96%. F doubles with heavy breakfast. OTH: Used with RTV. Drug class: Protease Inhibitors (PI).
stavudine(D4T)=Zerit: AE: Reversible peripheral neuropathy, increased lactic acid, hepatic steatosis, pancreatitis, lipoatrophy, dyslipidemia. OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
telbivudine: IND: Chronic Hep B with cirrhosis. OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
tenofovir alafenamide (TAF): IND: HIV, Hep B. ADM: T once/d w/ or without food. AE: N,V, increased lipids, liver and renal toxicity, bone loss, lactic acidosis, lipoatrophy. Less renal and bone toxicity vs TDF. OTH: Drug Class: Nucleotide Reverse Transcriptase Inhibitors (NRTIs/NtRTIs)
tenofovir disoproxil fumarate (TDF)=Viread: IND: HIV (PEP and PrEP). ADM: T once/d w/ or without food. AE: Naus,Vom, increased lipids, liver toxicity, bone loss, lactic acidosis, lipoatrophy. OTH: Drug Class: Nucleotide Reverse Transcriptase Inhibitors (NRTIs/NtRTIs). Truvada=(emtricitabine+TDF).
tipranavir=Aptivus: IND: HIV. AE: Hepatotoxicity, rash. Can affect BG levels. OTH: Use w/ RTV. Drug class: Protease Inhibitors (PI).
valacyclovir=Valtrex IND: Genital and oral HSV, shingles. AE: =placebo. PK: valcyclovir is a prodrug to acyclovir. DOS: Adj for renal fxn.
zidovudine (AZT)=Retrovir: AE: Naus, Headache, malaise, fatigue, rash, myositis, myocarditis, anemia, leukopenia, hepatic steatosis, elevated liver enzymes, lactic acid and CK, peripheral lipoatrophy. OTH: Drug Class: Nucleoside Reverse Transcriptase Inhibitors (NRTIs).
Carbapenems
IND: Meningitis, complicated UTI, pneumonia, gram (-), Pseudomonas. MOA: Inhibits cell wall cross-linking. CI: Beta lactam allergy. DI: Decreases valproic acid levels 6-100% within 2d. PK: Beta lactam structure (beta lactamase resistant). OTH: Bactericidal. Time dependent killers.ertapenem=Invanz: AVL: IV/IM. IND: Covers MSSA (+), Strep (+), H. influenza, M. catarrhalis, GNR, anaerobes. AE: Dia, Headache, anaphylaxis, seizure risk. PK: t1/2=4h. No CYP interactions. DOS: Adj for renal fxn. IV: 1g once/d.
imipenem=Primaxin: AVL: IV. IND: Covers MSSA (+), Strep (+), some enterococcus (+), GNR, Pseudomonas (-), anaerobes. AE: Naus, hypotension, seizure (w/ high serum levels). PRG: CI. LAC: CI. DOS: Adj for renal fxn. Std=500mg q6h. OTH: Given w/ cilastatin which inhibits dehydropeptidase-I (renal enzyme which metabolizes imipenem).
meropenem=Merrem: AVL: IV. IND: Meningitis, CAP, complicated UTI. Covers MSSA (+), Strep (+), some enterococcus (+), GNR, Pseudomonas (-), anaerobes. AE: Naus, Diar, hypotention, seizures (lower risk vs imipenem). PRG: CI. LAC: CI. PK: t1/2=1h. DOS: Adj for renal fxn. Std=1g q8h.
Carboxypenicillins
ticarcillin: AVL: IV. IND: Covers Pseudomonas (-). OTH: Often given in combo w/ clavulin: Timentin=clavulin+ticarcillin.Cephalosporins
MOA: Blocks cross linking of NAG-NAM in cell wall. EVD: More resistant to acid breakdown and beta lactamases vs penicillins. CI: Anaphylaxis with penicillin (<0.1% will cross react). Cross reactivity is mostly based on the similarity of side chains. OTH: Bactericidal. Time dependent killers. Later generation cephalosporins have better gram (-) activity. Chemical structure: beta lactam conected to six membered ring.1st Generation
cefadroxil: AVL: PO.
cefazolin: AVL: IV. IND: CAP. Covers MSSA (+), Strep (+), some GNR. AE: Anaphylaxis, rash, GI upset, renal and hepatic dysfunction. DOS: Adj for renal fxn. Std=1-2g q8h.
cephalexin=Keflex: AVL: PO (tab250,500mg or liquid (good taste)). IND: Non-purulent cellulitis, respiratory infections, sinusitis, otitis media, prostatitis, skin infection. Less effective for OM or CAP. Covers Beta-haemolytic Strep, Staph, Strep pneumoniae, E coli, Proteus mirabilis, Klebsiella. PRG: Safe. FDA cat A. DI: Probenecid inhibits the renal excretion. DOS: Adult: Std=250mg q6h. Range=1-4g in divided doses. Children: Std=25-50mg/kg/d in divided doses. OM=75-100mg/kg/d divided QID. OTH: Store reconstituted liquid in fridge. Stable for 14d.
cephradine: AVL: PO.
2nd Generation
cefaclor=Ceclor: AVL: PO. IND: CAP. AE: Anaphylaxis, rash, GI upset, renal and hepatic dysfunction. DOS: Adj for renal fxn. Std= 250mg TID.
cefotetan: AVL: IV.
cefoxitin: AVL: IV.
cefprozil=Cefzil: AVL: PO. IND: CAP. AE: Diar3%, anaphylaxis, rash, GI upset, renal and hepatic dysfunction. DOS: Adj for renal fxn. Std=500mg BID.
cefuroxime=Ceftin: AVL: PO (cefuroxime axetil - liquid has bad taste), IV (cefuroxime sodium). IND: Covers some MSSA (+), some Strep, GNR. AE: Anaphylaxis, rash, GI upset, renal and hepatic dysfunction. PK: Food increases F. DOS: Adj for renal fxn. PO: Std=500mg BID. IV: Std=750mg q8h.
3rd Generation
cefdinir: AVL:PO.
cefditoren: AVL: PO.
cefixime=Suprax: IND: Gonorrhea. AE: Diar16%, Naus7%, indigestion3%.
cefotaxime=Claforan: AVL: IV. IND: Meningitis, CAP. AE: Diar, Vom, rash2%, fever, leukopenia, neutropenia, eosinophilia, thrombocytopenia, seizure, nephrotoxicity. DOS: Adj for kidney fxn. Std=1-2g q8h.
ceftazidime=Fortaz: AVL: IV. IND: CAP. Covers GNR and Pseudomonas (-). AE: D, leukopenia, neutropenia, eosinophilia, thrombocytopenia, seizure, nephrotoxicity. DOS: Adj for kidney fxn. Std=1-2g q8h.
cefpodoxime: AVL: PO.
ceftazidime: AVL: IV. IND: Covers Pseudomonas.
ceftibuten: AVL: PO.
ceftriaxone=Rocephin: AVL: IV and IM. IND: Gonorrhea, otitis media, meningitis, CAP, UTI, PID, post variceal bleed. Covers some MSSA (+), Strep (+), GNR. AE: Diar3%, rash2%, leukopenia, neutropenia, eosinophilia, thrombocytopenia, seizure, nephrotoxicity. CI: Neonates. DI: Don’t mix with Ca (precipitants form). PK: t1/2~7h. DOS: No adj for renal/hepatic. IV: Std=1-2g q24h.
4th Generation
cefepime: AVL: IV. IND: CAP. Covers some MSSA (+), Strep (+), GNR, Pseudomonas (-). ADM: AE: Anaphylaxis, rash, GI upset, renal and hepatic dysfunction, seizures (especially if renal dysfunction). DOS: Adj for renal fxn. Std=1-2g q12h.
5th Generation
ceftolozane: IND: Covers Pseudomonas. OTH: Given in combo w/ tazobatem.
ceftaroline=Teflaro: AVL: IV. IND: Covers Staph (+) including MRSA, Strep (+), Enterococcus (+), GNR, minimal Pseudomonas (-).
Cyclic Lipopeptides
daptomycin=Cubist: AVL: IND: Covers all Staph (+) including MRSA, Strep (+), Enteroccoccus (+). MRSA skin infections. MOA: Links and breaks the bacterial cell membrane. OTH: Bactericidal.Fluoroquinolones
MOA: Inhibits DNA gyrase (enzyme bacteria use for DNA replication, transcription, repair, and recombination). ADM: Can T w/ food but avoid milk. Black Box Warning: QT prolongation, hypersensitivity/anaphylaxis, tendonitis (especially >60yo), muscle weakness (pts w/ myasthenia gravis), seizure risk, hepatotoxic. DI: Chelates with Al, Ca (including milk), Fe (space 2h before or 6h after if XR). Can inhibit elimination of warfarin, theophylline (serious) and cyclosporine. PK: Inhibits 1A2. OTH: Bactericidal. Concentration dependent killers. Has post Antibiotic effect against gram (-). Respiratory fluoroquinolones are levofloxacin and moxifloxacin.ciprofloxacin=Cipro: AVL: PO (IR tabs, XR tabs500,1000mg + suspension), IV. IND: UTI (2nd line), CAP (2nd line), secondary prophylaxis post variceal bleed, traveller’s Diar. Covers some MSSA (+), GNR, Psudomonas (-), some atypicals. AE: GI upset, HA, dizziness, photosensitivity, hepatitis, cartilage toxicity, C. diff. CI: Children (cartilage damage). PK: t1/2=6h. F=56%. PB=20-40%. Vd=3.5L/kg. Moderate inhibitor of 1A2. Mostly excreted unchanged in the urine. MW=385.8. DOS: Adj for renal fxn. PO: IR: Std=500-750mg BID. XR: Uncomplicated UTI=500mg once/d x 3d. Complicated UTI & uncomplicated pyelonephritis=1g once/d x 7-14d. IV: Std=400mg q12h.
levofloxacin=Levaquin: AVL: PO, IV. IND: Used 2nd line for UTI, CAP. Covers MSSA (+), Strep (+), GNR, partial Pseudomonas (-), atypicals. AE: GI upset, HA, dizziness, photosensitivity, hepatitis/liver injury, cartilage toxicity, QT prolongation. PK: t1/2=7h. F=99%. DOS: Adj for renal fxn. PO: 500mg q24h x10d or 750mg q24h x 5d. IV: Std=500mg once/d.
moxifloxacin=Avelox: AVL: IV, PO. IND: CAP, prostatitis. Covers MSSA (+), Strep (+), some GNR, anaerobes, atypicals. AE: GI upset, HA, dizziness, photosensitivity, hepatitis, cartilage toxicity, prolonged QT. PK: t1/2=13h. Best prostate fluid penetration vs. other quinolones. DOS: No adj for renal/hepatic fxn. PO/IV: Std=400mg q24h.
norfloxacin=Noroxin: IND: Prophylaxis after variceal bleed.
Glycopeptides
vancomycin=Vancocin: AVL: IV, PO. IND: Meningitis, skin or blood infections, pneumonia. MRSA, C. difficile. Only (+) coverage. MOA: Blocks NAG/NAM cross linking in cell wall construction (gram + only). AE: Flushing, hypotension>10%, nephrotoxicity, ototoxicity, allergic rxn. PRG: Safe. DI: Coadministration w/ AGs increases risk of nephrotoxicity. PK: t1/2=4-6h. PB~55%. Vd=0.7L/kg. 75-90% renal elimination. F=0 so oral used for GI C. difficile infection. DOS: Adj for renal fxn. Std~1g q12h. Consider 20-25mg/kg (using ABW) for very ill pts. Draw trough pre 4th dose. Goal: trough level=5-15mg/L. 15–20 mg/L if life-threatening infection or MRSA. Peak: 20-40mg/L (1h after end of 1h infusion). OTH: aka Vanco. Bactericidal. Time dependent killer. Red man syndrome (max 10mg/min),Glycylcyclines
tigecycline=Tygacil: AVL: IV. IND: CAP. AE: Naus, Diar, acute pancreatitisrare. OTH: Structurally similar to tetracyclines.Lincosamides
clindamycin=Dalacin C: AVL: PO (cap, topical, liquid-room temp), IV. IND: Acne, pneumocystis jiroveci, vaginosis. Covers Staph (+) (increasing MRSA resistance), Strep (+), some GNR, anaerobes. Can be used to block toxin production. MOA: Binds 50S subunit of ribososmes. ADM: T w/ or without food. AE: Diar1%, Naus, abdominal pain, C difficile, LFT abnormalities4%, rash1%. PRG: Safe. LAC: Safe. PK: t1/2=2.4h. F=90%. PB=60-94%. Met mainly by 3A4. Doesn’t cross BBB. DOS: Unaffected by renal or hepatic fxn. PO: Std=300-450mg q6h. IV: 600mg q8h. OTH: BacteriostaticMacrolides
IND: Used for gram (-). Increasing S pneumonia resistance (~20%). MOA: Binds 50S ribosomal subunit. AE: Increases QT (all). OTH: Bacteriostatic.azithromycin=Zithromax=Z-PAK: AVL: PO (tab, liquidbrand tastes better), IV. IND: Chlamydia, gonorrhea, otitis media, strep throat, CAP, travellers D in Asia. Covers some MSSA (+), Strep (+), some GNR, atypicals. MOA: EVD: Better tolerated vs erythromycin. 5d Tx ~= efficacy vs 10d Tx. ADM: T w/ food. Repeat dose if vomiting <1h after dose. AE: Naus3%, Diar5%, Vom5%, stomach pain4%, allergic reaction4%, Headache5%, abnormal vision5%. PRG: Safe in 2nd and 3rd trimester. LAC: Safe. DI: Can increase digoxin levels. PK: t1/2=68h. DOS: No adj for renal/hepatic fxn. PO: Std=500mg day 1 then 250mg x 4d. IV: 500mg once/d x 7-10d.
clarithromycin=Biaxin: AVL: PO (tab or liquid). IND: H.pylori, CAP. AE: GI upset, rash, cholestatic hepatitis. PRG: Safe in 2nd and 3rd trimester. LAC: Safe. DOS: IR: Std=500mg BID. XR: Std=1000mg once/d. OTH: Suspension: Shake well. Store at Room Temp. Stable for 14d.
erythromycin=Eryc: AVL: PO. IND: Acne, chlamydia, pneumonia/RTI, syphilis, whooping cough. Poor H. influenzae coverage. EVD: Alternative to azithromycin but rarely used due to increased GI AE, dosed BID-QID, and more DIs. AE: GI upset, rash, cholestatic hepatitis. PRG: Safe. LAC: Safe. PK: t1/2=0.8-3h. PB=75-95%. Inhibits 3A4. DOS: Std=250mg q6h, 333mg q8h, 500mg BID. Children: 30-50mg/kg*d in divided doses
Nitrofuran Antibacterial
nitrofurantoin=MacroBID: AVL: PO. IND: UTI.Covers some Enterococcus, some GNR. Inactive vs. proteus, pseudomonas, enterobacter, klebsiella. ADM: T w/ food to increase F. AE: Naus, flatulence, loss of appetite, Headache, neuropathy, pulmonary/hepatic toxicity, rash/SJS. CI: CrCl<60 or 30 if using Beers criteria. PRG: CI in 3rd trimester. DI: Antacids can decrease F. PK: t1/2=45min. F~30%. 100% renal elim. t1/2=45min. AUX: May discolor urine/feces, T w/ food. DOS: UTI: 100mg BID x 5d.Nitroimidazoles
metronidazole=Flagyl: AVL: PO (cap500mg), IV, topical. IND: Giardiasis, trichomoniasis, vaginosis, protozoans. Covers anaerobes, C. difficile, H. pylori. Often used to treat giardia in dogs and cats. MOA: Inhibits nucleic acid synthesis. Only occurs if metronidazole is partially reduced which only happens in anaerobic cells. AE: Naus10%, Diar4%, metallic taste9%, decreased appetite, vertigo, HA18%, seizure, ataxia allergic rxn. PRG: CI in first trimester. Safe in 2nd and 3rd. DI: Disulfram vomiting rxn with alcohol. Avoid EtOH 24h after last dose. PK: t1/2=7-8h. PB<20%. Inhibits 2C9 and 3A4. Tastes awful. DOS: IV and PO: 500mg q8h. OTH: Bactericidal. Tastes terrible.Novel Antibacterials
fosfomycin=Monurol: IND: UTI (women>18yo). MOA: Irreversibly inhibits enolpyruvate transferase, which form NAM part of cell wall and decreases bacterial adhesion. EVD: Cure rate~70%. ADM: T without food in 125mL of water. AE: Diar10%, Headache10% Naus5.2%, vaginitis8% abdominal pain2%, indigestion2%, rash1%. PK: t1/2=5.7h. F=35%. DOS: 3g sachet once.methenamine mandelate=Mandelamine: IND: UTI. MOA: Metabolized to formaldehyde in bladder. ADM: Needs acidified urine so often given w/ ascorbic acid. AE: GI upset, rash. CI: Gout.
Oxazolidinones
linezolid=Zyvoxam: AVL: PO (tab, susp), IV. IND: Pneumonia, skin infections, resistance/intolerance to vancomycin. Covers Staph (+) including MRSA, Strep, Enterococcus. Bacteriostatic vs S. aureus but bactericidal vs S. pneumoniae. MOA: Binds 50S subunit of ribosomes and prevents formation of functional 70S initiation complex. AE: Diar7%, headache5%, Naus7%, dose and time dependent bone marrow suppression, peripheral neuropathy, optic neuritisrare. DI: MAOIs/SSRI (linezolid is a mild MAOI). PK: t1/2=5h. F~100%. PB=31%. DOS: No adj for renal/hepatic fxn. PO and IV: 600mg q12h.Penicillins
MOA: Inhibits cell wall crosslinking. OTH: Bactericidal.amoxicillin=Amoxil: AVL: PO (chewable, tab, liquid). IND: CAP, chlamydia (2nd line), otitis media, sinusitis. AE: Rash, GI upset. PRG: Safe in 2nd and 3rd trimester. LAC: Safe. DI: Could decrease COC efficacy. DOS: Adj for renal fxn. Std=500mg TID. High dosed=1g TID. OTH: Can be w/ clavulanate=Clavulin at 4:1 or 7:1 ratio to cover S.pneumonia.
ampicillin: AVL: IV. IND: CAP, meningitis. EVD: Better than amoxicillin against shigella, citrobacter, enterobacter, listeria. AE: Diar, Vom, rash, hypersensitivity, seizure. DI: Increased risk of rash while using allopurinol.Decreased birth control efficacy. PK: t1/2=1.25h. F=62%. DOS: Adj for renal fxn. Std=1g q6h.
cloxacillin: AVL: PO (cap, liquidbad taste). IND: CAP. Covers MSSA (+), Strep (+) AE: Rash, GI upset, hemolytic anemia, nephritis. PRG: Safe. DOS: No adj for renal/hepatic fxn.
penicillin G=Crystapen: AVL: IV. IND: Covers Strep (+) and some enterococcus (+). AE: Rash, GI upset, hemolytic anemia, nephritis, seizures. DI: Tetracycline may decrease efficacy. DOS: Adj for renal fxn. Std=2 million units q4h.
penicillin V=Pen VK AVL: PO. IND: Pharyngitis, CAP. AE: Rash, GI upset, interstitial nephritis. PRG: Safe. LAC: Safe. DOS: Adj for renal fxn. Std=300-400mg TID or QID.
piperacillin/tazobactam: AVL: IV. IND: Covers MSSA (+), Strep (+), Enterococcus(+), GNR, Pseudomonas (-), anaerobes. DOS: Adj for renal fxn. Std=3.375g q6h.
Rifamycins
rifampin=Rifadin=Rofact AVL: PO. IND: CAP (not monotherapy), meningitis (Tx + prophylaxis), tuberculosis. MOA: Inhibits DNA-dependent RNA polymerase. AE: GI upset, flu like symptoms, heartburn, liver toxicity, thrombocytopenia. Changes fluids reddish orange color (tears, urine, contact lenses, saliva). CI: Jaundice. PRG: CI. LAC: CI. DI: Decreased COC efficacy, alcohol. Potent inducer of 3A4, 1A2, 2C9, 2C19. PK: t1/2= 3-5h. PB=80%. Potent inducer of 3A4, 1A2, 2C9, 2C19. DOS: No adj for renal/hepatic fxn. Std=300mg BID.Sulfa Antibiotics
sulfamethoxazole+trimethoprim(SMX/TMP)=Bactrim=Septra AVL: PO. IND: Meningitis, UTI, traveller’s D. Covers MSSA (+), some MRSA (+), some GNR. AE: Naus, Vom, Diar, rash/itch, false Cr increase, renal impairment, anemia, bone marrow suppression, increased K. CI: Sulfa allergy. PRG: CI in 1st and 3rd trimester. LAC: Safe. DI: Increased phenytoin, increased warfarin, hypoglycemia with sulfonylureas, increased nephrotoxicity with cyclosporine. PK: Both F=100%. t1/2= 8-11h. Inhibits 2C9. OTH: Septra DS= Septra at double strength.Tetracyclines
MOA: Binds 30S subunit of bacterial ribosomes. ADM: Stay upright for 30min after swallowing. PRG: CI. DI: Ca, Fe, decreased efficacy of COCs and penicillins. OTH: Bacteriostatic. Time dependent killers.doxycycline: AVL: PO. IND: CAP, chlamydia. Covers some MSSA (+), some Strep (+), some GNR, atypicals. ADM: T w/ food. AE: Diar5%, GI upset, photosensitivity. PRG: CI. DOS: No adj for renal/hepatic fxn. Std=100mg BID day 1 then 100mg once/d.
minocycline=Minocin: IND: Acne. AE: Lupus, vertigo. PRG: CI.
tetracycline: ADM: T without food. Warning: Don’t T if expired. PRG: CI. LAC: Safe.
Vaccines - Coronavirus
Astrazeneca COVID-19 vaccine: AVL: IMref. IND: SARS-CoV-2 in pts >18yoref. MOA: Viral vector uses a adenovirus as a carrier for a double stranded DNA which will get our own cells to make the spike proteinref. EVD: 62% effective after 2 doses (95% CI interval= 39-76% AE: Site tenderness75%, site pain54%, fatigue62.3%, headache57%, muscle pain49%, malaise44%, fever34%, chills32%, arthralgia27%, naus22%ref. CI: <18yo, acute severe febrile illness/acute infectionref. PRG: Safety not establishedref. LAC: Safety not establishedref. MON: Observe for 15min after vaccineref. DOS: 2 doses x 0.5mL given 4-12wks apartref. OTH: AKA ChAdOx1 nCoV-19 or AZD1222. Each vial has 8 or 10 doses. After first opening, use vial within 6hrs at room temp or 48hrs at fridge temp. Limited data on pts >65yo. Non medicinal ingredients: EDTA, ethanol, L-Histidine, MgCl hexahydrate, polysorbate 80, NaCl, waterref.Moderna COVID-19 vaccine:
AVL: IMref.
IND: SARS-CoV-2 in pts >18yoref.
MOA: mRNA vaccine - RNA goes into host cells which make the SARS-CoV-2 spike antigen. The immune system then sends neutralizing antibodies and cellular immune cells to this antigenref.
EVD: 94.1% effective (95% CI=89-97%. ~80% effective after 1 doseref.
ADM: No dilution needed. 0.5mL IM (deltoid)ref.
AE: Pain at site85%, fatigue51%, headache46%,muscle pain40%, joint pain38%, chills26%, naus/vom14%, axillary swelling12%, arm swelling9%, fever8%,redness6% ref.
CI: <1yo, allergy to a component, symptoms that could be COVIDref.
PRG: No safety data. May consider if high risk for COVIDref.
LAC: No safety data. May consider if high risk for COVIDref.
DOS: 0.5mL IM 1 month apartref.
OTH: Store between -25 to-15oC. Thaw in fridge for 2.5hrs then room temp for 15min before admin. Or, thaw at room temp for 1hr. Don't re-freeze. Discard vial 6hrs after puncture. Each vial=5mL=10 doses. Refrigerated vials can be stored <30days. Unpunctured room temp vials can be stored <12hrsref.
Pfizer-BioNTech COVID-19 vaccine:
AVL: IMref.
IND: SARS-CoV-2 in pts >16yoref.
MOA: mRNA vaccine - RNA goes into host cells which make the SARS-CoV-2 spike antigen. The immune system then sends neutralizing antibodies and cellular immune
cells to this antigenref.
EVD: Efficacy=94.6% (95% CI=89.9-97.3%). 52% effective after 1 doseref.
ADM: Deltoid muscle onlyref.
AE: Pain at injection75%, fatigue46%, headache38%, muscle pain26%, fever8%, joint pain15%, enlarged lymph nodes1%ref.
CI: <16yo, allergy to ingredient, S/Sx of COVIDref.
PRG: No safety data. May consider if high risk for COVIDref.
LAC: No safety data. May consider if high risk for COVIDref.
DOS: 0.3mL x 2 IM injections 21days apartref.
OTH: Vials are stored frozen -80°C to -60°C and protected from light. Can thaw in fridge or room temp. Thaw for 30min at
room temperature before diluting. Room temp vials must be diluted in
<2hrs. Vials can be refrigerated < 5 days. Before and after dilution invert vial gently 10 times to
mix. 
. Dilute vial w/ 1.8mL of 0.9% NaCl. Vial contains 5 doses of 0.3 mL. Discard unused vaccine 6hrs after dilutionref.
. Dilute vial w/ 1.8mL of 0.9% NaCl. Vial contains 5 doses of 0.3 mL. Discard unused vaccine 6hrs after dilutionref.
Vaccines
FLU/INFLUENZAinfluenza vaccine (aka flu shot)=Fluzone: AVL: Nasal spray (Flumist=live attenuated), IM (inactivated). Recombinant egg-free vaccine available. EVD: Antibodies form after 2w. Efficacy by year according to CDC: 10% 2004-05, 21%2005-06, 52% 2006-07, 41%2008-09 , 56%2009-10 , 60%2010-11 , 47% 2011-12 49%2012-13, 52%2013-14 , 19%2014-2015, 48% 2015-16 , 40%2016-17 , 36% 2017-18 . AE: Site pain24.3%, muscle pain18.3% headache14.4%, malaise14%, redness10.8%, swelling5.8%, fever2.3%. CI: < 6months old, fever. PRG: Safe and recommended. LAC: Safe and recommended. DOS: 0.5mL yearly. Fluad Pediatric used for 6-24 months old (0.25mL). Children 6months-9yo getting the flu shot for the fist time should have a second dose in the same year. (>4w apart). The high dose vaccine is indicated if >65yo. OTH: Can’t cause flu.
Fluzone High-Dose: AVL: Comes in packs of 5 x 0.5mL single dose syringes. IND: Flu protection pts >65yo. MOA: Same as standard flu shot but older people have a weaker immune system that is less responsive to the standard vaccine. EVD: ~30% more effective vs standard dose for those >65yo. ADM: IM injection (not in the buttocks. AE: Slightly More AE vs std dose - site pain35.6%, muscle pain21.4%, malaise18%, headache16.8%, redness14.9%, swelling8.9%, fever3.6% CI: Severe egg allergy, Guilain-Barre syndrome (GBS). Postposne if fever. DI: Use caution w/ pts on anticoagulants (more bleeding). DOS: 0.5mL IM yearly. Contains 60ug hemagglutinin (HA) (4 times the std dose). OTH: Trivalent inactivated vaccine. Latex free.
HEPATITIS
Havrix=hepatitis A vaccine: AVL: IM. Havrix=1mL (>19yo). Havrix Junior=0.5mL (1-18yo). EVD: Efficacy=99% at 1 month. Projected to last 20y. AE: headache 10%, site pain/redness>10%, irritability >10%, diar/naus/vom<10%, site rxn<10%, fever<10%, malaise<10%. CI: <1yo, neomycin allergy (trace amount). DOS: Can give single dose but booster recommended 6-12m later for long term protection.
Twinrix=hepatitis A (inactivated) + B (recombinant) vaccine: AVL: Avail IM. Twinrix=1mL (>19yo). Twinrix Junior=0.5mL (1-18yo). Lasts at least 15y in adults, 10y in children. Protection starts after 2-4w. EVD: Efficacy after 3 doses: A=98% B=99.9%. AE: Headache>10%, site pain/redness>10%, diar<10%, naus<10%, vom<10%, site rxn<10%, malaise<10%. CI: <1yo, neomycin allergy (trace amounts), fever. COS: ~$75/dose. DOS: Standard schedule: 0,1m,6m. Rapid 4 dose: 0,7d, 21d,12m. OTH: Hep A part=inactivated. Hep B=recombinant.
HPV
Gardasil 9=HPV vaccine: IND: Protects against HPV types 6,11, 16, 18, 31, 33, 45, 52, 58. Prevents genital warts and cervical cancer. AE: Pain90%, swelling40%, redness34%, headache15%, itch5%, fever5%, naus4%, dizziness3%, bruising2%, fatigue2%. DOS: 0.5mL at 0, 2m, 6m. If alternate schedule necessary, 2nddose >1 month after 1stdose and 3rd> 3 months after 2nd. 2 doses found to be non-inferior to 3 dose. No booster later in life recommended. OTH: Recombinant vaccine. Avail for Males and Females 9-26yo.
OTHER
tetanus + diphtheria vaccine=Td Adsorbed: AVL: IM. IND: Protects against Chlostridium tetani (toxins cause rigidity ex. lockjaw). AE: redness8%, swelling16%, pain81%, fever4%, sore/swollen joints5%. COS: Free at clinic. DOS: 0.5mL. Children get a few doses starting at birth then q10y. OTH: Sometimes given w/ pertussis (Adacel).
PNEUMOCOCCAL
Prevnar 13=PCV13: AVL: IM. IND: Protects against 13 strains of Strep pneumoniae (36% of pneumonias). Indicated in infants (regular schedule) and adults >65yo (>19yo if immunocompromised, smoker). EVD: Immunosuppressed pts may have less benefit. COS: $95/dose. DOS: 0.5mL IM once. Given 8w before Pneumovax. If after, separate by 1y. OTH: Conjugate vaccine. Suspension needs to be shaken vigorously. Store in refrigerator.
Pneumovax 23=PPSV23: AVL: IM, SubQ. IND: Recommended for immunocompromized people >2yo, adults > 65yo, people in nursing homes, alcoholics, smokers, homeless, IVDU. DOS: 0.5mL IM. Typically given 8w or 1y after Prevnar.
SHINGLES VACCINE
Shingrix=shingles vaccine: AVL: IM. IND: Prevent shingles 50yo and older. Can be used in immunocompromised. EVD: Higher incidence of local and systemic AE vs Zostavax. AE: Pain77%, redness38%, swelling at injection site25%, muscle pain45%, fatigue42%, headache37%, shivering27%, fever20% GI symptoms16%. DOS: 0.5mL (2 vials combined entire vial) given IM. Schedule: 2 doses 2-6 months apart. OTH: Inactivated adjuvented vaccine.
TRAVELLER'S DIARRHEA/CHOLERA
Dukoral: AVL: PO (oral susp). IND: Traveller’s Diar from E.coli and Cholera from Vibrio cholera. EVD: Travellers Diar protection for 3y. Cholera protection 2y. AE: Headache, Diar, stomach pain, gas. CI: <2yo. PRG: Safe. LAC:Safe. DOS: 2 dose vaccine. Separate by >1w. Last dose >1w before trip. 2-6yo should receive 3 half doses. 1 dose booster if more than 3 months since last dose. 2 dose booster if more than 5y since last dose. OTH: Inactivated vaccine.
Cation-Exchange Resins
sodium polystyrene sulfonate=Kayexalate: AVL: PO, rectal. IND: Hyperkalemia. ADM: Mixed in water (avoid K containing juices). AE: Hypokalemia, fecal impaction (high dose). CI: K1+<5, obstructive bowel disease. DI: sorbitol. PK: F=0 DOS: 15-60g (30g typical) OTH: Can bind 3.1mM of K1+ for every gram of kayexalate. 1 mol of Na released for every mol of K. Can also bind Ca, Li and Mg. Most action in Large intestine.CoEnzymes
CoEnzyme Q10: IND: Replaces enzyme lost w/ statin use, HF (possibly effective), HTN (possibly effective).Diets
DASH diet=Dietary Approach to Stop Hypertension: EVD: Many trials have shown that it reduces BP (~5/3) for various pts w/ HTN or preHTN. OTH: Emphasizes foods high in: protein, fiber, K, Mg, and Ca (ex fruits, vegetables, nuts, beans, whole grain, low-fat dairy). Limit sugar and saturated fats. Doesn’t talk about Na. <1% of Americans conform to the DASH diet.ketogenic diet:
Echinacea
Echinacea: AVL: Tablets, tinctures, fluid extracts, juices. DOS: Dried root equivalent: E angustifolia=1-3g/d. E purpurea=0.9-4.5g/d. E pallida=0.36-3g/d. OTH: Echinacea is a genus of plant that has a few different species used (ex. E. angustifolia, E. purpurea, E. pallida).Elements - Iron (Fe2+)
iron isomaltoside=Monoferric: AVL: IV (100mg elemental/mL in 1mL, 5mL and 10mL single-dose vials). IND: Iron deficiency in adults intolerant or unresponsive to oral iron. ADM: Administered as IV bolus, IV infusion or as direct injection into venous limb of a dialyzer during hemodialysis. MON: Monitor for hypersensitivity rxns during and at least 30min following each dose. DOS: Individualized for pts hemoglobin target level and iron stores.iron (general)=ferrous sulphate, Feramax: AVL: PO (tab: ferous sulphate=300mg (60mg elemental), liquid). MOA: Body uses Fe in Hgb to transport O2. EVD: XR ferrous sulphate preparations are ineffective and expensive. ADM: T without food for better F. AE: Naus, dyspepsia, const, diar, dark stools. Liquid preparations can stain teeth. DOS: Start at low dose. OTH: Foods rich in heme iron: clams, liver, pork, chicken, beef. Foods rich in non-heme iron: enriched oatmeal, pumpkin seeds, molasses, lentils, kidney beans. Eating foods w/ Vit C like cantaloupe, honey duw, grapefruit etc w/ non-heme iron containing foods increases the F.
Elements - Other
calcium (Ca2+): PRG: RDA=1000mg. LAC: RDA=1000mg. DOS: RDA=1000-1200 mg. TUL=2500mg/d.potassium (K1+): OTH: Foods high in K: avocado, bananas, beans, bran, cantaloupe, carrots, chocolate, figs, nuts, juices (carrot, grapefruit, orange, prune & vegetable), milk, raisins, potatoes, pumpkins, salt substitutes, spinach, tomatoes & yogurt.
sodium (Na1+): DOS: FDA recommends <2.3g/d. WHO <2g/d. AHA <1.5g/d.
zinc (Zn2+): PRG: RDA when pregnant=11mg. LAC: RDA when lactating=12mg. DOS: RDA=8-12 mg. TUL=40mg/d.
Garlic
Garlic: EVD: Ineffective for hyperlipidemia. Possibly effective for HTN.Ginseng:
Ginseng: OTH: Cold Fx=North American Ginseng.Omega-3 Fatty Acids:
IND: hypertriglyceridemia. MOA: EPA and DHA are the active ingredients. EVD: Increases HDL 5-10%. decreases TG 25-30%. AE: Naus, GI upset, fishy burbs, bleed riskwhen dose >3g/d. DI: Antithrombotics or anticoagulants can increase bleeds. DOS: 2-4g/d. OTH: Sources: fatty fish, krill oil, microalgae oil, marine lipid concentrate, phytoplankton.Fish Oil: EVD: Effective at reducing Triglyceride levels 20-50%.
Other
grapefruit juice: DI: Will increase levels of amiodarone, cyclosporine, erythromycin, felodipine, lovastatin, nifedipine. PK: Non-reversible inhibitor of the intestinal enzyme CYP 3A4.hawthorn: IND: Traditionally used for HF, angina, HTN, arrhythmias. EVD: Safe and possibly effective for mild forms of HF.
nicotinic acid/niacin=Niaspan: IND: Hyperlipidemia (lacks evidence). MOA: Inhibits liver VLDL synthesis and secretion. EVD: decreases LDL 5-25%, increases HDL 15-35%, decreases TG 20-50%. ADM: T w/ food. AE: Naus, Diar, skin flushing, hyperglycemia, gout, liver toxicity, increased ALT 1%. CI: Gout, peptic ulcer, and liver disease. DOS: IR: Start 50-100mg bid. Double every 3-7d up to 1.5g bid. Max 4.5 g/d. ER: Start 0.5g hs titrate up 0.5g/d each every w to 2 g/d. Max 3g/d).
Saint John’s Wort: DI: COCs, antiretrovirals, antiepileptics, CCBs, cyclosporine, fentanyl, ABs, warfarin. Digoxin levels decrease 25% from PGP induction. PK: Induces 3A4, 1A2, PGP.
Phosphate Binder
lanthanum=Fosrenol: IND: End stage renal disease. EVD: Doesn’t affect Vit/cholesterol absorption like sevelamer. ADM: T w/ meals, chew or crush. AE: Naus10%,vom9%, abdominal pain5%. CI: Bowel obstruction. DOS: Std=750-1500mg/d divided TID. Max=4500mg/d.sevelamer=Renagel=Renvela: IND: Used in ESRD. ADM: T w/ meals, don’t crush. AE: Naus, vom, diar, const, dyspepsia. CI: Bowel obstruction. DI: ciprofloxacin (decreased F by 50%), synthroid, doxycycline. Inhibits absorption of Vit A,D,K and cholesterol. DOS: 2.4g if phosphate between 1.8-2.4mM. If phosphate is >2.4mM then give 4.8g.
Probiotics
AVL: PO (powder, capsule, dairy products). MOA: May suppress growth of pathogenic bacteria, block attachment/invasion, enhance mucosal function and change host immune response. EVD: EFFECTIVE FOR: Antibiotic associated diarrhea in children (2w-17yo). Cochrane 2015 found RR=0.46 and NNT=10. Dose: Lactobacillus rhamnosus or Saccharomyces boulardii at 5-40 billion colony forming units/d. Also effective at preventing antibiotic associated C.difficile. Cochrane 2013 found RRR=64%. Dose: strain + dose not specified POSSIBLY EFFECTIVE FOR: Hepatic encephalopathy (no mortality benefit) Cochrane 2016, VAP preventionCochrane 2014, URTI preventionCochrane 2015, NOT EFFECTIVE FOR: UTI preventionCochrane 2015, UC remission maintenanceCochrane 2011. ADM: T at same time as antibiotics AE: Gas. OTH: Probiotic resource: clinical guide to probiotic supplements (app and site): http://www.probioticchart.ca/#/Vitamins
Vitamin A: PRG: RDA=2500IUs. LAC: RDA=4333IUs. DOS: Adult RDA=2333-3000IUs. TUL=10,000IUs. OTH: RDA=2333-3000IUs.Vitamin B1=thiamin: DOS: RDA Adult=1.1-1.4mg. OTH: Alcoholics are often deficient.
Vitamin B2=riboflavin: PRG: RDA=1.4mg. LAC: RDA=1.4mg. DOS: Adult RDA=1.1–1.6mg.
Vitamin B3=niacin: PRG: RDA=18mg. LAC: RDA=17mg. DOS: Adult RDA=14-18mg. TUL=35mg/d.
Vitamin B5=pantothenic acid: PRG: RDA=1.9mg. LAC: RDA=2mg. DOS: Adult RDA=1.3-2mg.
Vitamin B6=pyridoxine: PRG: RDA=1.9mg. LAC: RDA=2mg. DOS: Adult RDA=1.3-2mg. TUL=100mg/d.
Vitamin B7=biotin: PRG: RDA=30µg. LAC: RDA=35µg. DOS: Adult RDA=30-35µg.
Vitamin B9=folate: PRG: RDA=600µg. Recommended supplement=400µg/d. Should start supplementing 3 months before conception. LAC: RDA=500µg. DOS: Adult RDA=400-600µg. TUL=1000µg/d. Supplemental dose for disease prevention=200ug/d. Supplemental dose for folate replacement=1-5mg/d. OTH: Water-soluble vitamin. Found in leafy green vegetables, liver, legumes. Folic acid is a form of Vitamin B9 that needs to be activated.
Vitamin B12=cyanocolbalamin: IND: Macrocytic anemia. PRG: RDA=30µg. LAC: RDA=35µg. DOS: Adult RDA=30-35µg. Pernicious anemia: Oral or SL=1mg-2mg/d. SubQ/IM: 800-1000µg/d for 1-2w (to saturate stores) then 100-1000ug/w until Hgb, Hct are normal then 100-1000ug/month to maintain normal RBCs. OTH: Only dietary source is milk and meat.
Vitamin C: PRG: RDA=85mg. LAC: RDA=120mg. DOS: Adult RDA=75-120mg. TUL=2g/d.
Vitamin D: PRG: RDA=600IUs. LAC: RDA=600IUs. DOS: Adult RDA=600-800IU. TUL=4000IU/d.
Vitamin E: PRG: RDA=15mg. LAC: RDA=19mg. DOS: RDA=15-19mg. TUL=1000mg/d.
Vitamin K: PRG: RDA=90µg. LAC: RDA=90µg. DOS: Adult RDA=90-120µg.
Anticholinergics
scopolamine=Hyoscine, Transderm Scop: AVL: Skin patch, IM, IV, SubQ. IND: Injection used to reduce respiratory secretions at end of life. Patch used for motion sickness, postoperative naus/vom, hypersalivation. MOA: CNS depressant by antagonizing muscarinic receptors. AE: Dry mouth29%, drowsiness17%. CI: Children. PK: Patch: Onset=4-12h. Priming dose of 140ug is released from the adhesive layer. Then 5µg/h for 72h via controlled release membrane. After removal of patch, excretion from the skin site continues for up to 12h w/ effects lasting up to 24h. SubQ: t1/2=3.5h. IM:t1/2=1h. Onset=15-20min IV: t1/2=1h. Onset=5-10min. Metabolized hepatically and excreted in urine. <10% of parent drug excreted unchanged in urine. DOS: Motion sickness: Apply 1 patch to dry, hairless skin behind the ear ~12h before antiemetic effect is required. Can be left up to 72h prn but should be removed when travel is complete. Hypersalivation: (not HC-approved use): 1 patch applied q72h (change application side each time). Postoperative N/V: 1 patch applied the evening before surgery or 4h before end of surgery. OTH: Schedule II.Anti-Gout
colchicine: IND: Gout. DOS: Acute gout Tx: 1.2mg initially. Then 0.6 mg 1h later (total=1.8mg colchicine). Gout prophylaxis=0.6mg once/d or BID. Can start prophylaxis 12h after the last treatment dose. OTH: Not recommended if presenting 36h after onset of symptoms.Cannabinoids
cannabis=marijuana: EVD: Effective for: chronic pain in adults, naus and vom in Cancer pts. Likely improves: MS spasticity symptoms, sleep in the short term. ADM: AE: Drowsiness/fatigue, dizziness, dry mouth, cough/phlegm/bronchitis (smoking only), anxiety, naus, cognitive effects, euphoria, blurred vision, euphoria, blured vision, headache, orthostatic hypotension, toxic psychosis/paranoia, depression, ataxia/dyscoordination, tachycardia, diar. Lower level of memory and attention. PRG: Lowers birth weight. PK: VAPORIZATION/SMOKING: Onset=5-10min. Duration=1-4hrs. ORAL: Onset=60-180min. Duration=6-8hrs. OTH: Possible link to testicular cancer. Not linked with lung cancer.nabilone=Cesamet: AVL: PO. IND: Chemo induced N + V. AE: Drowsiness, dizziness, dry mouth, euphoria/high, HA, insomnia, anxiety, depression, memory loss. PRG: CI. LAC: CI. DOS: Std= 1-2mg BID. Taken 1-3h before chemo. OTH: May be addictive. Don’t drive while taking.
Dihydrofolate Reductase Inhibitor
methotrexate=Metoject: IND: CD. MOA: Inhibits dihidrofolate reductase. EVD: Effective at maintenance of remission. Possibly effective for induction. AE: Naus, flu-like aches, HA, oral ulcers, bone marrow and liver toxicity, pneumonitis, immunosuppression, lymphoma. PK: Time to effect=4w. DOS: 25mg injection q1w. OTH: Can be used w/ 20mg prednisone.EPO Receptor Agonist
epoetin alpha=Eprex: AVL: IV and SubQ. OTH: SubQ has longer half life (more efficient use of drug).darbopoetin alpha=Aranesp: AVL: IV and SubQ. PK: t1/2: IV & SubQ=30h.
Monoclonal Antibodies (MABs)
adalimumab=Humira: AVL: SubQ (self-injection). IND: Psoriasis. EVD: Best evidence for inducing fistula closure. AE: Naus, injection site rxn, opportunistic infections, reversible lupus-like syndrome, worsening heart failur, lymphoma, CNS demyelinating disorders. DOS: CD: Induction: 4 injections on day 1 (160mg), 2 injections day 15 (80mg), 1 injection day 29 (40mg). Maint=1 injection q2w (40mg).certolizumab pegol=Cimzia: AVL: SubQ (professional injection). IND: Not approved in Canada for CD. AE: Naus, injection site rxn, opportunistic infections, reversible lupus-like syndrome, worsening heart failure, lymphoma, CNS demyelinating disorders. COS: $700/dose. DOS: Injection q4w.
erenumab=Aimovig: AVL: SubQ70mg/mL 1mL single-dose autoinjector. IND: Migraine prevention in adults w/ > 4 migraine days/month. MOA: Competes w/ calcitonin gene-related peptide (CGRP) for binding to CGRP receptors, which antagonizes CGRP receptor function. CGRP, a neuropeptide, modulates nociceptive signalling and causes vasodilation, which has been associated with migraine pathophysiology. ADM: Can be self-administered w/ training. Leave injector at room temp for >30min before injection. Can be injected in abdomen, thigh or upper arm. Rotate injection sites. AE: Site rxns (pain, erythema, pruritus), const, muscle spasms, generalized pruritus/pruritic rash. CI: <18yo. DI: None. PK: Not metabolized or effect on CYPs. AUX: Store in refrigerator. Do not shake. DOS: Std=70 mg SubQ once/month. Max=2 injections (140mg) once/month. OTH: Drug class: CGRP antagonist. Keep in refridgerator. Stable for 14d once reaches room temp (<25C). Don't freeze or shake.
golimumab=Simponi: AVL: SubQ. COS: $1600/50mg dose. DOS: Flare up=200mg then 100mg 2w later. Maint=50mg q4w.
infliximab=Remicade: AVL: IV. IND: Psoriasis. AE: Naus, injection site Rxn, opportunistic infections, reversible lupus-like syndrome, worsening HF, lymphoma, CNS demyelinating disorders. COS: $1000/100mg dose. DOS: Induction=5mg/kg at 0, 2, and 6w. Maint=5mg/kg q8w. If no/partial response, try 10mg/kg.
secukinumab: IND: Psoriasis.
ustekinumab: IND: Psoriasis.
Muscle Relaxers
cyclobenzaprine=Flexeril: IND: Short term (<3 months) treatment of muscle spasms. AE: Drowsiness/fatigue35%, dry mouth25%. CI: MAOI in last 2w. PK: t1/2=18hrs. F=0.4 tmax=7.5hrs OTH: Similar structure and AEs to TCAs.Smoking Cessation - Nicotine Replacement Therapy (NRT)
IND: 1st line for smoking cessation. MOA: Mimics nicotine levels from smoking. EVD: HC recommends trying NRT first. 12 month efficacy=17%. ADM: Can combine w/ smoking to decrease # of cigarettes (could do 2w taper or start on quit day). AE: Headache, naus, insomnia, light headedness, irritability, vivid dreams. DI: Don’t combine with varenicline. DOS: Decrease dose over 3-6 months.PATCHES
Nicoderm=Habitrol: AVL: 7, 14, 21mg/d patches. ADM: Wear for 24h and rotate site. Don’t cut Nicoderm patch. Can take off before bed but not recommended. AE: Skin irritation. CI: Skin disease. PRG: Wear 16h/d to decrease exposure. DOS: 6w of 21mg then 2w of 14mg then 2w of 7mg. If <10cigarettes/d start with 14mg. May need additional NRT for cravings.
GUMS
Nicorette=Thrive: AVL: 2, 4mg gum. ADM: Bite, bite, park on side of cheek for 1min. 1 gum should last 30min. AE: Hiccups, sore jaw, mouth ulcer. CI: Dental diseases. PRG: Safest smoking cessation option in prg. PK: Peak=30min. DOS: Usual=10gums/d. Max=20gums/day. Use 4mg gum if smoking <30min after waking up. OTH:
LOZENGES
Nicorette=Thrive: AVL: 2, 4mg lozenges. ADM: Dissolve over 20-30min. AE: Hiccups, heartburn, mouth/throat irritation. DOS: Based on time of first cigarette. Usual=8/d. Max 15/d. OTH: Delivers more nicotine vs. gum.
SPRAYS
Nicorette QuickMist: AVL: 1mg/spray. AE: Tingling lips, hiccups, bad taste. DOS: 1-2 sprays q30-60min. Max 2 sprays/time, 4sprays/hr, 64 sprays/d.
INHALERS
Nicorette: AVL: 4mg inhaler. MOA: Mimics cigarette. AE: Mouth/throat irritation66%, cough, rhinitis. COS: Most expensive NRT option. DOS: 6-12 cartridges/d. 20min of active puffing (80 deep breaths).
Smoking Cessation (Other)
varenicline=Champix: AVL: PO (tab0.5, 1mg). IND: Smoking cessation. MOA: Bdlocks and partially activates nicotinic receptors. Agonist decreases cravings and withdrawal. Antagonist decreases pleasure from smoking. EVD: Best quit rate vs all smoking cessation options. ADM: T w/ food. AE: Naus30%, vom, insomnia (take 2nd dose w/ supper), vivid dreams18%, mood changes, suicidal ideation. CI: Prg, mood disorders. DI: Don’t combine with NRT. Minimize alcohol as it could lead to depression. PK: t1/2=33h. DOS: 0.5mg OD x 3d then 0.5mg bid x 4d then 1mg BID x12w. Start 1-2w before quit date. OTH: Schedule I (Need Rx).Steroids
dexamethasone=Decadron: AVL: IV, IM, PO. IND: Chemotherapy induced N + V (increases effect of ondansetron.). ADM: T w/ food. AE: fluid retension, thrush, bone loss, cataracts, indigestion, muscle weakness, back pain, bruising, increased glucose, weight gain, insomnia. PRG: FDA cat C. PK: Induces and metabolized by 3A4. Duration=3d.prednisolone: EVD: Used for 4w in alcoholic liver disease. Original study had a short term mortality benefit with a NNT of 5 at 4w. Later studies showed it was less effective short term and had no effect longer term. AE: Infection.
Weight Loss Agents
Contrave=naltrexone+bupropion: AVL: PO (extended release tab containing naltrexone8mg+bupropion90mg. IND: Used w/ diet and exercise to reduce weight in people >18yo >30kg/m2 (obese) or >27kg/m2 (overweight) w/ 1 weight related condition (ex. T2DM, HTN, dyslipidemia). MOA: Thought to act on hypothatlamus which regulates apetite and the mesolymbic dopamine circuit (reward system). EVD: After 56w, people using Contrave lost 5.5kg vs placebo 1.4kg. Doesn't have evidence for cardiovascular, mortaliy or morbidity health. ADM: Should not be taken w/ high-fat meals. AE: Naus32.5%, constipation19.2%, headache17.6%, vomiting10.7%, dizziness9.8%, dry mouth8.1%, seizurerare. CI: Uncontrolled HTN, seizure history, currently using opioids, closed angle glaucoma. PRG: Contraindicated. LAC: Not recommended. DI: MAOIs, thioridazine, tamoxifen. Dose of Contrave should be reduced if using w/ CYP2B6 inhibitors. AUX: Don't crush/chew. MON: BP and pulse measured before starting and at "regular intervals" once started. Assess effectiveness at 12w. If <5% of original weight is lost D/C Tx. DOS: STD ADULT: Taper up to the max dose=2 tabs bid using this schedule: 1 tab am x 7d, then 1 tab bid x7d, then 2 tabs am and 1 in evening x 7d, then 2 tabs bid. PEDIATRIC (<18yo): Not indicated. GERIATRIC (>65yo): Use w/ caution. HEPATIC IMPAIRMENT: Max= 1 tab in am for mild or moderate impairment. RENAL IMPAIRMENT: Max=1 tab BID for mod to severe impairment. OTH: Contains lactose.Xanthine Oxidase Inhibitor
allopurinol=Zyloprim: AVL: PO tab100,200,300mg. IND: Gout, Tx/prevention of uric acid nephropathy. MOA: Reduces uric acid concentrations in both serum and urine by inhibiting the production in the body. AE: Skin rash (SJSrare). PK: t1/2: allopurinol=1-3h. oxypurinol=12–30h. Onset=2-3d. F=80-90%. PB=0. Elimination: Renal: allopurinol=5–7%, oxypurinol=70%. Fecal=20%. Max decreases of uric acid in 1–3w. MON: Serum urate concentrations should be monitored. ULN=430µM for men/postmenopausal women and 345 µM for premenopausal. Can target <300uM in severe gout and <360uM for mild-mod gout. DOS: Adj for renal fxn. Gout: Starting dose=100mg/d. Std=300mg/d titrated to urate conc. Max=800mg/d. For tolerability divide doses >300mg 2–3 times/d. CrCl 10-20mL/min=100mg/d. CrCl<10mL/min=100mg q2–3d. OTH: Both allopurinol and its active metabolite oxypurinol are active.Analgesics (Non-NSAID)
acetaminophen=Tylenol: AVL: PO (tab325,500, 650(ER), liquid). IND: Pain (ex.arthritis, HA, strain/sprains), fever. ADM: Take w/ or without food. AE: Dizziness6%, drowsiness9%, headache5%, diar2%, stomach upset1%, naus3%. AUX: Don’t crush (ER tabs). MON: Kidney and liver fxn if long term Tx. DOS: Pain: Max=4g/d divided TID/QID. OTH: Doesn’t reduce inflammation. Aka paracetamol.Ergotamines
IND: Migraines. EVD: More naus but less chest pain vs triptans. CI: Don’t use within 12h of triptan or 24h of naratriptan.dihydroergotamine (DHE)=Migranal: AVL: IM, IV, SubQ, nasal spray. IND: 1st line for severe/ultra severe attacks. DOS: IV, IM SubQ: 0.5-1mg. May repeat after 1h. Max=4 doses/d. OTH: Give metoclopramide 10mg IV or prochlorperazine 5mg IV before administering DHE.
Janus Kinase (JAK) Inhibitors
baricitinib=Olumiant: AVL: PO (tab2mg). IND: Reducing signs and symptoms of mod-severe rheumatoid arthritis in adults who have inadequate response to >1 DMARD. MOA: Selective and reversible inhibitor of Janus kinases (JAKs), which are enzymes involved in hematopoiesis, inflammation and immune function. This inhibition results in a reduced pro-inflammatory response, as well as modulation of lymphocyte activation/proliferation and cytokine production. ADM: T w/ or without food. AE: Increase in creatine phosphokinase, hypercholesterolemia, pharyngitis, naus, UTI, URTI, HTN, headache, nasopharyngitis, bronchitis, higher risk for developing serious infections (ex active tuberculosis), GI perforation, lymphoma, shingles, liver enzyme elevation, DVT/PE. CI: Shouldn't be started if lymphocyte count <0.5 x 109 cells/L, neutrophil count <1 x 109 cells/L or hemoglobin <80 g/L. Test for TB before starting. DI: Live vaccines not recommended (update immunizations before starting). Not recommended w/ other JAK inhibitors (tofacitinib), DMARDs or potent immunosuppressants. MON: Test for TB periodically. DOS: STD=2mg once/d. No dose adj in mild renal impairment. Not recommended in mod-severe renal impairment (eGFR<60mL/min/1.73 m2). No dose adj in mild-mod hepatic impairment. Not recommended in severe hepatic impairment. OTH: To be used w/ methotrexate, but can be monotherapy if methotrexate not tolerated. Second oral JAK kinase inhibitor in Canada.tofacitinib=Xeljanz OTH: First oral JAK inhibitor in Canada.
Muscle Relaxers
cyclobenzaprine=Flexeril: AVL: PO. IND: Fibromyalgia, muscle spasms/pain. AE: Fatigue35%, dizziness10%, dry mouth25%, urinary retention, increased IOP. May impair driving. CI: Safety <15yo not established. DI: MAOI, serotonergic drugs (serotonin syndrome). PK: t1/2= 18h. F=33-55%. High PB. Met by 1A2 (main), 3A4, and 2D6. DOS: 5mg TID as effective as 10mg TID w/ less sedation. Shouldn’t be used >3 weeks. OTH: Has similar structure and AE as tricyclic antidepressants.Opioids
OTH: Naloxone used in overdose.buprenorphine+naloxone=Suboxone: AVL: SL tabsbuprenorphine/naloxone 8/2 and 2/0.5mg. IND: Opioid dependence Tx. MOA: Buprenorphine is a high affinity partial opioid agonist (at mu and kappa). It can bump other opioids off of the mu receptors leading to abbrupt withdrawl. Naloxone is a high affinity mu antagonist. It has poor oral F but is added to prevent IV use. Because t1/2 is shorter for naloxone than buprenorphine, you can still get high if injected. EVD: Has lower overdose, mortality, toxicity risk vs methadone. Has less sedation vs methadone. Doesn't prolong QTc like methadone. May be less effective vs methadone (especially those w/ heavy dependence). Easier to D/C vs methadone. ADM: Drinking water before dose helps tabs dissolve faster. AE: Headache, insomnia, anxiety, naus, abdominal pain, const, sweating, LFT elevationrare. CI: Opioid intoxication. PRG: Crosses placenta. Associated w/ neonatal abstinence syndrome (NAS) but may be less severe vs methadone. Growing evidence says that buprenorphine has better outcomes for mom and baby however lack of evidence means Suboxone is not approved for use in prg and methadone remains preffered choice. LAC: Compatible. Lacking evidence for naloxone component but not orally bioavaible so should not have effect. DI: 3A4 inducers and inhibitors (less susceptible vs methadone due to ceiling effect). Sedatives/hypnotics could lead to respiratory depression. Anticholinergics can make const worse. PK: Sublingual F=28-51%. Oral F~0%. Onset=30-60min. Peak effect=1-4hrs. Vd=4-5L/kg. t1/2=28-37hrs. Duration=48-72hrs. Time to steady state=5-10d. PB=96%. Met by 3A4 and 2C8. Excreted mainly in feces but also urine. MON: Clinical Opiate Withdrawl Scale (COWS) used to measure withdrawl and adjust dose. DOS: Pt specific depending on degree of tolerance, severity of withdrawl and risk factors (ex. use of benzos). Can be titrated faster than methadone due to increased safety. Start=2-6mg. Second dose on day 1 can be given after prescriber assessment (>3hrs after first dose). If signs of intoxication decrease dose by 2mg. If withdrawal present, increse dose by 2-4mg on day 2 or 3. Should reach optimal dose in 1-2wks. Max=24mg/d. Pts allowed to miss 4 doses but must get new Rx if 5 doses are missed. OTH: If switching from methadone to Suboxone, methadone dose should be decreased to <30mg and should be completely off methadone for 3d to avoid precipitated withdrawal.
buprenorphine implant=Probuphine: AVL: 80mg subdermal implant. IND: Opioid dependence in adults stabilized on <8mg of sublingual buprenorphine. MON: Combine w/ counselling and psychosocial support. DOS: Each dose has 4 implants inserted subdermally in the inner side of the upper arm by a trained professional. Left in for 6 months of Tx and then removed. Can replaced w/ new implants in opposite arm at the time of removal if continued Tx desired. OTH: Drug class=partial opioid agonist. Each implant is a sterile flexible ethylene vinyl acetate rod (length=26mm), diameter=2.5mm).
codeine: AVL: Oral, IM, SubQ.
methadone=Methadose=Metadol-D: AVL: PO (tab, soln1mg/mL and 10mg/mL, powder). IND: Tablets are only indicated for pain management. MOA: EVD: Pts 3X less likely to be "using" while on methadone than without. Mortality rate is 1/3 when taking methadone vs no Tx. Pt retention in rehab programs is increased. Reduced risk of HIV and Hep C. Criminal activity decreases. Methadone is better at retaining pts vs Suboxone. ADM: Morning is preferrable so pt won't sleep during overdose. Space doses by >15hrs. Methadone typically diluted w/ tang (qs to 100mL). Can also use crystal light. AE: Prolonged QT (especially >120mg), constipation. Increased mortality risk early in Tx CI: Severe respiratory problems. PRG: Crosses placenta. Improved pregnancy outcomes vs no Tx. Not terratogenic but associated w/ neonatal abstinence syndrome (NAS). May need increased dose due to increased clearance and Vd. Methadone in apple juice instead of OJ may help w/ naus/vom. LAC: Risk of serious harm (including death) to children exposed through breasmilk. DI: 3A4 inducers or inhibitors. Sedatives/hypnotics could lead to respiratory depression. Anticholinergics can worsen const. PK: t1/2=22-48hrs. Duration=24-36hrs. Onset=30min. F=80%. Peak plasma concentration=2-4hrs. Vd=4-5L/kg. Time to steady state=5-7d. PB=85-90%. Similar potency to morphine. Metabolized by 3A4major, 1A2minor, 2B6minor, 2C8minor, 2C9minor, 2C19minor, 2D6minor. Excreted in urine and feces. COS: NS college requires use of 10mg/mL soln. AUX: Methadone specific label, store in locked box, refrigerate/shake well. MON: ECG before starting is recomended if at risk for Torsades and periodically when dose >150mg. DOS: Start: 30mg/d or less. If abstinent for >7d, starting dose should be <10mg/d. Max dose increase=10mg q3d. If also taking benzos max recommended dose=120mg/d. If dose >150mg/d monitor ECG for QT prolongation. Length of Tx is pt specific. Always once/d unless using for pain. Pts allowed to miss 2 doses but must get new Rx if missed 3. OTH: Methadone decreases likelihood of euphoria if taking other opioids at the same time. Death has happened w/ dose as low as 40mg. If dose is vomited within 15min and vomit is witnessed then a replacement dose (50% of full dose) can be given. Need new Rx.
morphine: IND: During MI.
Selective Serotonin Receptor Agonists
IND: Migraines. MOA: Agonist at 5HT1B/1D. EVD: All triptans equally effective but can have different individual response. Alleviates headache pain, naus, vom, photo/phonophobia. Can combine w/ NSAID for better efficacy. AE: Chest discomfort, fatigue, dizziness, drowsiness, naus, throat symptoms. DI: Don’t use within 24hrs of another triptan or DHE. OTH: Aka Triptansalmotriptan=Axert: AVL: PO. DOS: 6.25-12.5mg at start of headache. Can repeat in 2h. Max=2 doses/d.
eletriptan=Relpax: AVL: PO. DOS: 20-40mg at start of HA. Can T 20mg after 2h. Max=40mg/d. doses/d.
frovatriptan=Frova: AVL: PO. DOS: 20-40mg at start of headache. Can T 20mg after 2h. Max=40mg/d.
naratriptan=Amerge: AVL: PO (D shaped tab). DOS: Adj for renal fxn. 1-2.5mg at start of headache. Can repeat after 4h. Max=5mg/d.
rizatriptan=Maxalt: AVL: PO (tab, oral disintegrating tab). DOS: 5-10mg at start of HA. Can repeat in 2h. Max=20mg/d.
sumatriptan=Imitrex: AVL: PO (tab25, 50, 100mg, dissintegrating film (DF)), intranasal5, 20mg. SubQ6mg. IND: Tx of migraine w/ or without aura. AE: 100mg tabs caused: naus11%,dizziness6%, neck/jaw/throat pressure or pain5%, vom4%, headache3%, throat/tonsil symptoms2.3%, abdominal pain2%. CI: Heart conditions (ex. tachycardia) (can increase BP), liver impairment. MAOI CI if taken within last 2 weeks. DOS: *PO*: 25-100mg at start of headache. Can repeat in 2h. Max=200mg/24h. *SubQ*: 6mg. Can repeat in 1h. Max=2 injections(12mg)/24h. *Intranasal*: 5-20mg. Can repeat in 2h. Max=40mg/24h.
zolmitriptan=Zomig: AVL: PO (tab, oral disintegrating tab), intranasal. DOS: *PO*: 2.5-5mg at start of headache. Can repeat in 2h. Max=10mg/d.
2 Drug Combination Inhalers
Advair: fluticasone (steroid) + salmeterol (LABA). AVL: MDI, diskus.Anoro Ellipta: umeclidinium (LAMA) + vilanterol (LABA). AVL: DPI.
Breo Ellipta: fluticasone (steroid) + vilanterol (LABA). AVL: DPI.
Combivent Respimat: ipratropium (SAMA) + salbutamol (SABA). AVL: Soft mist inhaler, nebules.
Duaklir Genuair: aclidinium (LAMA) + formoterol (LABA). AVL: DPI.
Duovent: ipratropium (SAMA) + fenoterol (SABA).
Inspiolto Respimat: tiotropium (LAMA) + olodaterol (LABA). AVL: Soft mist inhaler.
Symbicort Turbuhaler: budesonide (steroid) + formoterol (LABA). AVL: DPI.
Ultibro Breezhaler : glycopyrronium (LAMA) + indacaterol (LABA). AVL: DPI (white+yellow).
Zenhale: mometasone (steroid) + formoterol (LABA).
Anticholinergics (Inhaled)
AE: Dry mouth, metallic taste, glaucoma if used on eye, urinary retention. Possible increased risk of cardiovascular events. CI: <18yo. OTH: Used for COPD more than asthma.Short Acting Muscarinic Antagonists (SAMAs)
ipratropium=Atrovent: AVL: MDI, nebules. IND: COPD. Sometimes used if tachycardia from SABA. MOA: Short-acting muscarinic antagonist (SAMA). EVD: Slower onset than SABA but longer duration of action. PK: Onset=15-30 min. Duration=3-8h. DOS: *MDI* (20ug/puff): 2-4 puffs q6-8h. Max=12 puffs/d. *Nebules*: 250–500 µg TID–QID.
Long Acting Muscarinic Antagonist (LAMAs)
aclidinium=Tudorza: AVL: DPI. IND: COPD. DOS: DPI (400ug/actuation): 1 actuation BID.
glycopyrronium=Seebri Breezhaler: AVL: DPI. IND: COPD. PK: Rapid Onset LAMA. DOS: DPI (50ug/cap): 1 cap inhaled once/d.
tiotropium=Spiriva: AVL: DPI (Insert pill) and Respimat Soft Mist Inhaler (SMI). DI: Other anticholinergics. PK: Duration=24h. DOS: *DPI* (18ug/cap): 1 cap inhaled once/d. *SMI* (2.5ug/actuation): 2 actuations once/d. Max=4 puffs/d. OTH: Not for acute relief.
umeclidinium=Incruse Ellipta: AVL: DPI. IND: COPD. DOS: DPI (62.5 µg/actuation): 1 actuation once/d.
Antihistamines (Intranasal)
levocabastine: EVD: Effective for sneezing, itching, runny nose, inflammation. PK: Onset <15min. DOS: 1 spray in each nostril BID-QID.Antihistamines (Oral)
IND: Allergic rhinitis (sneezing, itching, runny nose, itchy eyes, inflammation). MOA: Competitive antagonist for H1 receptor. Also changes 3 dimensional configuration of the receptor which decreases the affinity for histamine. EVD: Increased efficacy if taken before allergen exposure. Less effective for most allergic rhinitis symptoms vs intranasal corticosteroids. PRG: Safe. LAC: Safe. OTH: Compared to 2nd gen, 1st gen have shorter duration of action, more toxicity, less selective for H1 receptor, and is more lipophilic. 1st gen can cross BBB while 2nd can't.FIRST GENERATION
brompheniramine: AVL:Only avail in combination products. DOS: 4mg q4-6h. Ped (6-11yo): 2mg q4-6h.
chlorpheniramine: DOS: 4mg q4-6h. Ped: 0.35mg/kg/d divided q4-6h.
cyproheptadine: AE: Stimulates appetite. DOS: Adult max=0.5mg/kg*d Ped: max=0.25mg/kg/d. OTH:
diphenhydramine=Benadryl: AVL: PO (tabs or liquid), IV, IM. IND: Allergies, naus, vom. AE: Const, sedation, confusion, dizziness, paradoxical excitement in children, dry mouth, blurred vision, urinary retention. DI: Sedatives (ex. alcohol), anticholinergic agents (scopolamine). DOS: Adult: 25-50mg q4-6h prn. Max=300mg/d. Ped: 2-5yo: max=37.5mg/d. 6-11yo: max= 150mg/d.
SECOND GENERATION
cetirizine=Reactine: AVL: PO (tabs and liquid). AE: Most likely 2nd gen to cause drowsiness (dose dependent). DOS: >5yo: 5-10mg/d. 5mg/d if renal or hepatic impairment. Ped: 6-23months: 2.5mg/d. 2-5yo: 2.5-5mg/d.
desloratadine=Aerius: AVL: PO (tabs, liquid). EVD: Has evidence for nasal congestion. PK: Active metabolite of loratadine. DOS: Adult=5mg/d. Renal or Hepatic impairment=5mg q48h. Ped: 6-11mon=1mg/d. 1-5yo=1.25mg/d. 6-11yo=2.5mg/d.
fexofenadine=Allegra: EVD: Appears non-sedating even at high doses. DOS: 60mg q12h. 60mg/d if renal impairment. Ped: 6-11yo: 30mg q12h.
loratadine=Claritin: AVL: PO (tab, ped rapid dissolve tab). DOS: Adult=10mg/d. Renal or hepatic impairment=10mg q48h. Ped: <30kg=5mg/d. >30kg=10mg/d.
COMBINATIONS
dimenhydrinate=Gravol: DOS: 50-100mg q4-6h prn. OTH: Contains diphenhydramine + mild stimulant 8-chlorotheophylline.
β2 Agonists (Inhaled)
Short-Acting β2-Agonists (SABAs)IND: Asthma (first line) and COPD. MOA: Stimulates β2 receptors which inhibits bronchoconstriction. AE: tremor, nervousness, increased HR, increased insulin secretion, increased glucose, decreased K. Possible increased QT. PRG: Safe. LAC: Safe. OTH: Aka rescue inhaler.
salbutamol=Ventolin: AVL: MDI, diskus, nebules. ADM:Shake MDI before use. Hold air for 10sec. PRG: Preferred SABA in P. PK: t1/2=4.5-6h. Duration=3-6h. Takes a few minutes to work. DOS: *MDI*100ug/puff: 1-2 puffs TID-QID prn. Max=8 puffs/d or 800ug/d. T 2 puffs 15min pre-exercise. *Diskus*200ug/actuation: 1 actuation TID-QID prn. Max=4 actuations/d. *Nebules*: 2.5–5mg QID prn.
terbutaline=Bricanyl: AVL: DPI. IND: Also used to delay labor up to 48h. DOS: DPI0.5 mg/actuation: 1 actuation q4–6h prn. Max=6 actuations/d.
Long-Acting β2-Agonists (LABAs)
MOA: Stimulates β2 receptors which inhibits bronchoconstriction. EVD: Always use as add on to corticosteroid in asthma due to increased asthma (but not COPD) deaths. AE: increased HR, nervousness thrush, URTI, hypokalemia. DOS: Used regularly (not prn).
formoterol=Foradil=Oxeze: AVL: DPI (w/ or without caps). PK: Onset=5min. Duration=12h. DOS:1 cap (12ug) BID. Max=48ug/d. OTH: Should only be used as rescue if combined with budesonide (Symbicort).
indacatrol=Onbrez: AVL: DPI. IND: COPD but not asthma. PK: Duration=24h. DOS: (75 µg/cap): 1 cap inhaled once/d.
olodaterol=Striverdi: AVL: Soft Mist Inhlaer (SMI). IND: COPD. PK:Duration=24h.
salmeterol=Serevent AVL: Diskus. PK: t1/2= 5.5h. Onset=15min. Duration=12h. DOS: Diskus and Diskhaler (50ug/actuation): 1 actuation BID. OTH:Shouldn’t be used as rescue inhaler.
vilanterol: PK: Onset=15min. Duration=24h. OTH: Avail as combo w/ fluticasone (Breo Ellipta).
β2 Agonists (Oral)
orciprenaline=Alupent: AVL: PO (liquid 250mL grape flavor. IND: Asthma, bronchitis, emphysema. ADM: If using an inhaler as well, taking the liquid first can open the lungs making the inhaler more effective. AE: Fine tremor, nervousness, Headache, dizziness, tachycardia, and palpitations, Naus, Vom, sweating, weakness, rashrare. DI: epinephrine, MAOIs, TCAs (β agonist effect enhanced). PK: t1/2: Phase 1=40min. Phase 2=15h. F=40%. Onset=30min. Duration=3-6h. MW= 520.60g/mol. DOS: Syrup concentration=2mg/mL. Adult=20mg/10mL TID-QID. Ped: Age 4-12yo=10mg/5mL TID. Age >12yo=20mg/10mL TID. OTH: Store at room temp. Protect from light.Corticosteroids - Inhaled (ICS)
IND: Treats inflammatory part of asthma. EVD: Some effect in 1w. Full effect in 8w. ADM: Rinse mouth w/ water and use spacer to avoid thrush. AE: thrush, sore mouth/throat, hoarseness, RTIs, cough, growth suppression (1.2cm), decreased BMD.beclomethasone=Qvar: AVL: MDI. CI: < 5yo. DOS: Low: <250ug/d. Mod=251-500ug/d. High=>500ug/d.
budesonide=Pulmicort: AVL: Dry Powder Inhaler (DPI), nebules. CI: <6yo. PRG: Preferred ICS in Prg. DOS: Low=<400ug/d. Mod=401-800ug/d. High=>800ug/d.
ciclesonide=Alvesco: AVL: MDI. CI: <6yo. DOS: Low=<200ug/d. Mod=201-400ug/d. High=>400ug/d.
fluticasone=Flovent: AVL: Dry Powder Inhaler (DPI)diskus, MDI. CI: MDI CI <1yo. PK: Fluticasone furoate more potent and longer lasting vs propionate. DOS: Low=<250ug/d. Mod=251-500ug/d. High=>500ug/d.
mometasone=Asmanex: AVL: DPI (twisthaler). CI: <12yo. DOS: Low=<200ug/d. Mod=400-800ug/d. High=>800ug/d.
Corticosteroids - Intranasal (INCS)
IND : Allergic rhinitis, modest benefit for allergic conjunctivitis. EVD : Similar efficacy between products. Effective for sneezing, itching, runny nose, congestion, eye symptoms, inflammation. ADM : Point away from septum. Small sniff after spray. AE : Nose bleed/irritation, Headache. LAC : Safe. PK : Onset: 1-2d. Max benefit: 2w. DOS : Start at high dose then tapper down. Can take prn but continuous use is more effective. Adults: T at night since inflammation worse then. Children T in am. beclomethasone: PRG : Safe. DOS : >6yo=2 sprays each nostril BID.budesonide: PRG : Safe. DOS : >6yo: Max=400ug/d.
ciclesonide: DOS : &t;12yo: 2 sprays/nostril daily. OTH : Has smaller spray volume.
flunisolide: DOS : >6yo: 1 spray/nostril TID. Adult=2 sprays/nostril BID.
fluticasone propionate: DOS : 4-11yo: 1-2 sprays/nostril daily. >12yo=2 sprays/nostril daily.
fluticasone furoate: DOS : 2-11yo: 1 spray/nostril daily. >12yo: 2 sprays/nostril daily.
mometasone furoate=Nasonex: DOS : 3-11yo=1 spray/nostril daily. >12yo=2 sprays/nostril daily. OTH : has a small spray volume.
triamcinolone=Nasacort: DOS : 4-11yo=1 spray/nostril daily. >12yo:2 sprays/nostril daily.
Decongestants (Intranasal)
EVD: Only effective for congestion. AE: Burning/stinging, sneezing, dryness, brady/tachycardia, hypo/hypertension, rebound congestion if >3d of use. PRG: Safe.oxymetazoline: PK: Onset=5-10min. Duration=12h. DOS: >12yo=2-3 drops or sprays per nostril q12h.
phenylephrine: PK: Onset=5-10min. Duration=4h. DOS: >12yo=2-3 drops or sprays per nostril q4h.
xylometazoline: PK: Onset=5-10min. Duration=12h. DOS: >12yo=2-3 drops or 1-2 sprays per nostril q8h.
Decongestants (Oral)
IND : Allergic rhinitis. AE : Restlessness/excitability, dizziness, weakness, insomnia, tachycardia, palpitations, increased BP, BG deregulation. CI : HTN, <6yo. PRG : Not safe in first trimester. DI : MAOIs (hypertensive crisis).phenylephrine: DOS : > 12yo=10mg q4h. 6-11yo=5mg q4h.
pseudoephedrine=Sudafed: LAC : Safe. DOS : > 12yo: 60mg q4-6h. Max=240mg/d. 6-11yo=30mg q4-6h. Max=120mg/d.
Leukotriene Receptor Antagonists (LTRA)
IND: Allergic rhinitis (not 1st line), asthma (especially if Samter’s triad present). Effective for inflammation. Inconsistent data for sneezing, itching, congestion. Similar efficacy to antihistamines but less effective vs intranasal corticosteroids.montelukast=Singulair: AVL: PO. AE: Headache, abdominal pain, flu-like symptoms. May worsen GERD. CI: <1yo PRG: Safe. DI: Carbamazepine, rifampin, phenobarbital, and phenytoin will reduce montelukast levels. DOS: 10mg qHS.
zafirlukast=Accolate: AVL: PO. ADM: AE: Headache, Naus, Diar. CI: <12yo. DI: Carbamazepine, rifampin, phenobarbital, and phenytoin will reduce zafirlukast levels. DOS: 20mg at least 1h before or 2h after meal.
Mast Cell Stabilizers
cromolyn: AVL: Intranasal, Ophthalmic. IND: Allergic rhinitis. EVD: Effective for itchy eyes and inflammation. Conflicting evidence for sneezing, runny nose, itching, congestion. Less effective vs steroids. AE: Sneezing, nasal stinging/irritation, bad taste, nose bleed. PK: Onset=4-7d. DOS:>2yo: 1 spray in each nostril 3-6 times/d.Methylxanthines
IND: Asthma, COPD. EVD: Less effective vs LABAs. AE: Naus, Vom, abdominal cramps, Headache, palpitations, stimulation. OTH: Uncommon due to toxicity and lack of efficacyoxtryphilline: AVL: Avail as elixir only. DOS: Initial=200mg QID. Maintenance=800-1200mg/d divided TID or QID.
theophylline: AVL: PO. IND: Severe COPD (add on after triple therapy). ADM: T w/ food. DI: Smoking, clarithromycin, many others. MON: Target plasma levels=55-85µM. DOS: Initial=400-600mg/d can be divided BID or TID.