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
SMZ/TMP
Bactrim®
2C9 inhibitor
Fluvastatin
Lescol®
2C9 inhibitor
2C9 substrate
Isoniazid
2C9 inhibitor
Gemfibrozil
Lopid®
2C9 inhibitor
Fenofibrate
Tricor®
2C9 inhibitor
NSAIDS
2C9 substrates
Glimepiride
Amaryl®
2C9 substrate
Glipizide
Glucotrol®
2C9 substrate
Glyburide®
Diabeta®, Micronase®
2C9 substrate
Warfarin
Coumadin®
2C9 substrate
Posaconazole
Noxafil®
3A4 inhibitor
Empirically, what should be done to the dose of warfarin when amiodarone is initiated? Why?
Decrease dose of warfarin by 30-50%. Amiodarone is a 2C9 inhibitor and warfarin is a 2C9 substrate. Therefore, amiodarone will inhibit the metabolism of warfarin leading to increased concentration and effect and potential risk of bleeding.
If adding warfarin to a patient regimen that already includes amiodarone, initial dose of warfarin should be more conservative.
Choose all of the true statements:
A. Hyperthyroidism increases effects of warfarin from increased catabolism of vit K dependent clotting factors
B. Hyperthyroidism decreases effects of warfarin from increased catabolism of vit K dependent clotting factors
C. Hypothyroidism increases effects of warfarin from decreased catabolism of vit K dependent clotting factors
D. Hypothyroidism decreases effects of warfarin from decreased catabolism of vit K dependent clotting factors
A & D are correct
Digoxin
Lanoxin®
P-gp substrate
Quinidine
Quinidex® (class IA anti-arrhythmic)
2D6 inhibitor
Fluoxetine
Prozac®
2D6 inhibitor
2D6 substrate
2C19 inhibitor
Paroxetine
Paxil®
2D6 inhibitor
2D6 substrate
Duloxetine
Cymbalta®
2D6 inhibitor
Bupropion
Wellbutrin®
2D6 inhibitor
Flecainide
Tambocor® (class IC anti-arrhythmic)
2D6 substrate
Mexiletine
Mexitil® (Class IB anti-arrhythmic)
2D6 substrate
Metoprolol
Lopressor®, Toprol XL®
2D6 substrate
Carvedilol
Coreg®
2D6 substrate
Propranolol
Inderal®
2D6 substrate
Timolol
2D6 substrate
Amitriptyline
Elavil®
2D6 substrate
1A2 substrate
Imipramine
Tofranil®
2D6 substrate
Nortriptyline
Pamelor®
2D6 substrate
1A2 substrate
Venlafaxine
Effexor®
2D6 substrate
Thioridazine
2D6 substrate
Haloperidol
Haldol®
2D6 substrate
Risperidone
Risperdal®
2D6 substrate
Tamoxifen
Nolvadex®
2D6 substrate
Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)
Codeine
2D6 substrate
Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)
Tramadol
Ultram®
2D6 substrate
Prodrug so inhibiting its metabolism will actually DECREASE its effect (since it’s not being metabolized into its active metabolite)
Sertraline
Zoloft®
2D6 inhibitor
Terbinafine
Lamisil®
2D6 inhibitor
Omeprazole
Prilosec®
2C19 inhibitor
2C19 substrate
Esomeprazole
Nexium®
2C19 inhibitor
2C19 substrate
Lansoprazole
Prevacid®
2C19 substrate
Pantoprazole
Protonix®
2C19 substrate
Rabeprazole
Aciphex®
2C19 substrate
Clopidogrel
Plavix®
2C19 substrate
Diazepam
Valium®
2C19 substrate
Escitalopram
Lexapro®
2C19 substrate
Efavirenz
Sustiva®
2C19 inhibitor
Etravirine
Intelence®
2C19 inhibitor
Cimetidine
Tagamet®
2C19 inhibitor
1A2 inhibitor
Fluvoxamine
Faverin®
2C19 inhibitor
1A2 inhibitor
1A2 substrate
Which CYP enzyme does charbroiled foods affect? How does it affect it?
Charbroiled foods induce CYP1A2
Primidone
Mysoline®
1A2 inducer
Which CYP enzyme does smoking affect? How?
Smoking induces CYP1A2
Ciprofloxacin
Cipro®
1A2 inhibitor
Ethinyl estradiol
1A2 inhibitor
Caffeine
1A2 substrate
Theophylline
Theolair®
1A2 substrate XO substrate (if used with allopurinol, a XO inhibitor, decrease dose of theophylline by 25-33%)
Clozapine
Clozaril®
1A2 substrate
Olanzapine
Zyprexa®
1A2 substrate
Zolmitriptan
Zomig®
1A2 substrate
Frovatriptan
Frova®
1A2 substrate
Mirtazapine
Remeron®
1A2 substrate
Tizanidine
Zanaflex®
1A2 substrate
Melatonin
1A2 substrate
Allopurinol (Zyloprim®) and febuxostat (Uloric®) inhibit which enzyme involved in the production of uric acid?
Xanthine oxidase
Azathioprine
Imuran® Prodrug to 6-MP
XO substrate (allopurinol and febuxostat inhibit XO which would increase the active metabolite potentially leading to increased risk of myelosuppression.
(if used with allopurinol, a XO inhibitor, decrease dose of Azathioprine by 25-33%)
Febuxostat
Uloric®
XO inhibitor
CI with Azathioprine (Imuran®) and 6-MP