Quiz #01 Flashcards
Which are the only (3) CYP enzymes that exhibit polymorphisms?
2C9
2C19 (more common in Asians)
2D6 (more common in Caucasians)
Which of the following would have a rapid onset typically within 24 hrs?
A. Enzyme induction
B. Enzyme inhibition
B. Onset of enzyme inhibition is more rapid than enzyme induction.
Enzyme inhibition is faster b/c it involves the drug binding with the enzyme, thereby preventing its function, whereas enzyme induction requires increased synthesis of the enzyme (a slower process).
Carbamazepine
give the brand name, state whether it’s an inducer, inhibitor and/or substrate of any CYP enzyme
Tegretol®
3A4 inducer
2C9 inducer
1A2 inducer
Phenytoin
Dilantin®
3A4 inducer 2C9 inducer 2C9 substrate 2C19 substrate 1A2 inducer
Phenobarbital
Luminal®
3A4 inducer
2C9 inducer
1A2 inducer
Rifampin
Rifadin®
3A4 inducer
2C9 inducer
1A2 inducer
Nafcillin
3A4 inducer
Dexamethasone
3A4 inducer
St. John’s wort
3A4 inducer
1A2 inducer
Itraconazole
Sporanox®
3A4 inhibitor
Ketoconazole
Nizoral®
3A4 inhibitor
2C19 inhibitor
Voriconazole
Vfend®
3A4 inhibitor
2C9 inhibitor
2C19 inhibitor
Fluconazole
Diflucan®
3A4 inhibitor (only at high doses)
2C9 inhibitor
2C19 inhibitor
HIV Protease Inhibitors
Atazanavir
Nelfinavir
Ritonavir
Saquinavir
Atazanavir - Reyataz®
Nelfinavir - Viracept®
Ritonavir - Norvir®
Saquinavir - Invirase®, Fortovase®
3A4 inhibitors 2C9 inhibitor (ritonavir) 2D6 inhibitor (ritonavir) 1A2 inducer (ritonavir) 1A2 inhibitor (atazanavir)
Clarithromycin
Biaxin®
3A4 inhibitor
1A2 inhibitor
Erythromycin
Erythrocin®
3A4 inhibitor
1A2 inhibitor
Diltiazem
Cardizem®
3A4 inhibitor
3A4 substrate
Verapamil
Calan®
3A4 inhibitor
3A4 substrate
Amiodarone
actually the active metabolite of amiodarone - desethylamiodarone
Cordarone®, Pacerone®
3A4 inhibitor
2C9 inhibitor
2D6 inhibitor
P-gp inhibitor
Alprazolam
Xanax®
3A4 substrate
Midazolam
Versed®
3A4 substrate
Felodipine
Plendil®
3A4 substrate
Nifedipine
Procardia®
3A4 substrate
Triazolam
Halcion®
3A4 substrate
Simvastatin
Zocor®
3A4 substrate
2C9 inhibitor
Atorvastatin
Lipitor®
3A4 substrate
Lovastatin
Mevacor®
3A4 substrate
2C9 inhibitor
Cyclosporin
Neoral®, Sandimmune®
3A4 substrate
Tacrolimus
Prograf®
3A4 substrate
Rivaroxaban
Xarelto®
3A4 substrate
Apixaban
Eliquis®
3A4 substrate
Ticagrelor
Brilinta®
3A4 substrate
Which (3) statins are metabolized solely by CYP3A4?
Simvastatin, Atorvastatin, and Lovastatin
Which statin is not metabolized by any CYP enzymes?
Pravastatin (Pravachol®)
What (2) CYP enzymes metabolize Crestor®?
2C9 & 2C19
Which statin is metabolized by both glucuronidation and CYP2C9?
Pitavastatin (Livalo®)
Max dose of simvastatin is limited to 10mg while on which of the following concomitant medications?
A. Amiodarone B. Calan® C. Multaq® D. B & C E. All of the above
D. B & C (Verapamil-Calan® and dronedarone-Multaq®) are both CYP3A4 inhibitors and limit the maximum daily dose of simvastatin to 10mg.
Diltiazem is the 3rd drug that limits Zocor® max dose to 10mg
Concomitant use of which (3) medications while on Zocor® would limit the dose to 20mg?
- Amiodarone
- Norvasc®
- Ranolazine (Ranexa®)
True or False - Clopidogrel is a prodrug?
True - Plavix® is metabolized by several different CYP enzymes into its active metabolite
Prasugrel (Effient®), another antiplatelet prodrug, is also metabolized into an active metabolite by multiple CYP enzymes
Which is the more active enantiomer of warfarin?
A. R-warfarin
B. S-warfarin
B. S-warfarin is the more active enantiomer
True or False - polymorphisms can exist in VKORC1 which would lead to increased warfarin effect?
True - VKORC1 or vitamin K epoxide reductase complex makes activated (reduced) vitamin K-dependent clotting factors. A polymorphism is this enzyme would decrease production of vitamin-K dependent clotting factors thereby indirectly increasing warfarin’s effects which may put the patient at higher risk for bleeding.
Miconazole
Oravig®
2C9 inhibitor
Metronidazole
Flagyl®
2C9 inhibitor