Term
| What is the pharmokinetic modality of the majority of clinical drug interactions? |
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Definition
| induction or inhibition of CYP450 enzymes |
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Term
| What 5 Cytochrome P450 Isoenzymes are involved in drug metabolism? |
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Definition
| CYP's: 1A2, 2C9, 2C19, 2D6, and 3A4 |
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Term
| What is a CYP450 Inducer? |
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Definition
| Drug that increases CYP450 enzyme activity leading to *increase in metabolism of substrate* |
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Term
| What is the time-frame of the onset of CYP Inducer effect? |
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Definition
| onset of effect usually *delayed* and depends on inducer half-life |
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Term
| What is a CYP450 Inhibitor? |
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Definition
| A drug that decreases CYP450 enzyme activity leading to *decrease in metabolism of substrate* |
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Term
| How do the following drugs affect a CYP450 enzyme: caffeine, thephylline, propranolol, TCA's, R-warfarin, clozapine? |
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Definition
| important substrates of the CYP1A2 enzyme |
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Term
| How do the following drugs affect a CYP 450 Enzyme activity: ciprofloxacin, cimetidine, fluvoxamine? |
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Definition
| important inhibitors of the CYP1A2 enzyme |
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Term
| How do the following affect a CYP 450 enzyme: cigarette smoke, charbroiled foods, omeprazole, phenobarbital, rifampin? |
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Definition
| important inducers of the CYP1A2 enzyme |
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Term
| How do beta-blockers, antidepressants, antipsychotics, codeine analogs, and donepezil affect the metabolism of a CYP450 enzyme? |
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Definition
| important *substrates* of CYP2D6 enzyme |
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Term
| What are important modulator mechanisms of the CYP2D6 enzyme? |
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Definition
| important *substrates, inhibitors* *not inducible*. |
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Term
| What are important modulator mechanisms of the CYP2C9 enzyme? |
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Definition
| important *substrates, inhibitors, and inducers* |
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Term
| How do the following drugs affect a CYP450 enzyme: S-warfarin, NSAIDs, sulfonylureas, angiotensin receptor blockers, phenytoin, diazepam, carvediol? |
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Definition
| important *substrates* of the CYP2C9 enzyme |
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Term
| How do the following drugs affect a CYP 450 enzyme: Amiodarone, fluconazole, fluxetine, metronidazole, paroxetine, sulfonamides? |
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Definition
| important *inhibitors* of the CYP2C9 enzyme |
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Term
| How do the following drugs affect a CYP450 enzyme: carbamazepine, phenobarbital, rifampin? |
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Definition
| important *inducers* of the CYP2C9 enzyme |
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Term
| How do the following affect a CYP450 enzyme: amiodarone, fluoxetine, paroxetine, sertraline, quinidine, bupropion, cimetidine, terbinafine? |
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Definition
| important *inhibitors* of the CYP2D6 enzyme |
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Term
| How do the following medications affect a CYP 450 enzyme: benzodiazepines, HIV antivirals, statins, steroids, cyclosporin, R-warfarin, sildenafil, zolpidem, CCBs? |
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Definition
| important *substrates* of the CYP3A4/5 enzymes |
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Term
| How do the following medications affect a CYP 450 enzyme: macrolides, azole, antifungals, verapamil, diltazem, protease inhibitors, grapefruit juice? |
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Definition
| Important *inhibitors* of CYP3A4/5 enzymes |
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Term
| How do the following medications affect a CYP 450 enzyme: carbamazepine, phenytoin, phenobarbital, rifampin, garlic, St. John's wort? |
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Definition
| important *inducers* of the CYP3A4/5 enzymes |
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Term
| How do the following drugs alter CYP450 metabolism: amiodarone, cimetidine, ciprofloxacin, fluvoxamine? |
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Definition
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Term
| How do the following drugs alter CYP450 metabolism: fluvoxamine, isoniazid, ritonavir? |
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Definition
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Term
| How do the following drugs alter CYP450 metabolism: amiodarone, cmetidine, diphenhydramine, fluxetine, paroxetine, quinidine, ritonavir, terbinafine? |
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Definition
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Term
| How do the following drugs alter CYP450 metabolism: clarithromycin, diltiazem, erythromycin, grapefruit juice, itraconazole, ketoconazole, nefazodone, ritonavir, telithromycin, verapamil? |
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Definition
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Term
| How do the following drugs alter CYP450 metabolism: carbamazepine, phenobarbital, rifampin, smoking? |
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Definition
|
|
Term
| How do the following drugs alter CYP450 metabolism: carbamazepine, phenobarbital, rifampin? |
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Definition
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Term
| what unit of CYP450 has no significant enzyme inducers? |
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Definition
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Term
| How do the following drugs alter CYP450 metabolism: Carbamazepine, phenobarbital, phenytoin, St. John's wort, rifampin? |
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Definition
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Term
| What are 3 *substrates* of cyp3a4 affected by rifampin? |
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Definition
| itraconazole, voriconazole, tacrolimus, and sildenafil |
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Term
| What does rifampin induce? |
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Definition
|
|
Term
| What does st. john's wort induce? |
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Definition
|
|
Term
| what does phenobarbital induce? |
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Definition
|
|
Term
| What does phenytoin induce? |
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Definition
|
|
Term
| What does carbamazepine induce? |
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Definition
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|
Term
| How does grapefruit juice interact w/cyp450? Name 4 drug categories with which it interacts. |
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Definition
| *irreversible inhibitor of 3a4; ca2+ channel blockers-100-200% increase in plasma levels. cyclosporine: increase in auc by 55-300%. terfenadine: 7-10 fold increase in msd terfenadine. simvastatin, atorvastatin, lovastatin. |
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Term
| Does grapefruit increase concentration, bioavailability, or half life of substrate? |
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Definition
| increases concentration (bioavailability) but not half-life |
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Term
| Name 3 drug interactions w/paroxetine |
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Definition
| metoprolol, codeine: cyp2d6 inhibition by paroxetine. erythromycin: cyp 3a inhibition of paroxetine |
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Term
| What drugs interact w/cisapride and what is the adr? |
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Definition
| azoles and macrolide (clarithromycin)s- fatal arrhythmias |
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Term
| With what drug does erythromycin interact? |
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Definition
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Term
What drug class has been known to
Increase in plasma levels of
cyclosporine/tacrolimus, carbamazepine,
warfarin, terfenadine/astemizole,
theophylline , triazolam/midazolam,
ergotamine, cisapride, “statins”? How does this drug class affect a cyp450 enzyme? |
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Definition
| macrolydes inhibit cyp 3a4- erythromycin=clarithromycin=telithromycin>azithromycin |
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Term
| What drug class influences metabolism of fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, venlafaxine, nefazodone? |
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Definition
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|
Term
35% of patients on this class of medications and 3 or
more medications have potential for drug-drug
interaction.
Most of the new medications in this class inhibit one or
more of the CYP450 enzymes.
Several have metabolites that are also inhibitors. |
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Definition
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Term
| What drug has decreased absorption with cholestyramine, decreased protein binding with phenytoin, diflunisal (dolobid), and altered metabolism with drugs that affect 1a2, 2c9, 2c19, and 3a4? |
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Definition
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Term
| What drug levels should be monitored if this drug is being taken with theophylline? |
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Definition
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