71.2 ð åèçïŒé«åž«åè / PGY OSCEïŒ
71.2.0.1 ð Cram Sheet
71.2.0.1.1 ð¥ é« yield 12
- PK = ADME
- F = AUC PO / AUC IVïŒIV F = 100%ïŒ
- VdïŒlipophilic 倧ãhydrophilic å°
- tœ = 0.693 à Vd / Cl
- 5 åè¡°æ é steady state
- CYP3A4 æ¶ 50% è¥ + grapefruit
- Codeine â morphine é CYP2D6
- Warfarin = CYP2C9 (sulfa, metronidazole, fluconazole å INR)
- Clopidogrel = CYP2C19 (omeprazole éæ)
- TDM 6 è¥: vanco, aminoglycoside, Li, digoxin, phenytoin, theophylline
- Beers Criteria = è人é¿çšè¥
- Cockcroft-Gault 䌰 CrCl
71.2.0.2 â é« yield
71.2.0.2.1 Bioavailability Variants
- IV: F = 100%
- Sublingual: bypass first-pass (nitroglycerin)
- Rectal: partial bypass first-pass
- Oral: full first-pass
71.2.0.2.2 Order Kinetics
- Zero-order: constant amount cleared per timeïŒalcohol, phenytoin (high dose), aspirin (high dose)ïŒ
- First-order: constant fraction cleared per timeïŒå€æžè¥ç©ïŒ
71.2.0.2.3 Loading Dose vs Maintenance
- Loading = Vd à target Css / FïŒé quick steady stateïŒ
- Maintenance = Cl à target Css / F
71.2.0.2.4 Drug Disposition Special
- Hepatic high extraction (flow-limited): lidocaine, propranolol, morphine (è hepatic blood flow çžé)
- Hepatic low extraction (capacity-limited): warfarin, phenytoin (èé ¶æŽ»æ§çžé)
- Severe liver dysfunction â low extraction drugs 圱é¿å€§
71.2.0.2.5 Beers Criteria ç¯äŸ
- BZDïŒfall riskïŒ
- Anticholinergic (diphenhydramine, oxybutynin, TCA)
- Long-acting sulfonylurea (glyburide)
- Muscle relaxant
- Long-acting NSAID (avoid > 2 week)
71.2.0.2.6 Pregnancy Categories (PLLR 2015)
- æ¹çº narrative summary
- 8.1 Pregnancy + 8.2 Lactation + 8.3 Females and Males of Reproductive Potential
71.2.0.3 ð¯ èªææª¢æž¬
- F definition? â AUC PO / AUC IV
- Vd lipophilic vs hydrophilic? â Lipo 倧, hydro å°
- tœ formula? â 0.693 à Vd / Cl
- 5 half-lives? â Steady state (~97%)
- Zero-order kinetics 3 drugs? â Alcohol, phenytoin (high), aspirin (high)
- Codeine activation? â CYP2D6
- Warfarin CYP? â 2C9
- Clopidogrel CYP? â 2C19
- CYP3A4 inducer 6? â Carbamazepine, rifampin, phenytoin, phenobarbital, St. Johnâs, alcohol chronic
- CYP3A4 inhibitor 6? â Grapefruit, azole, macrolide, ritonavir, cimetidine, metronidazole
- Vancomycin trough? â 15-20 severe
- Beers Criteria avoid in elderly? â Long BZD, anticholinergic, glyburide, long NSAID
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