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57 Cards in this Set
- Front
- Back
CYP 450 is involve w/ _____ rxns
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phase 1 (oxidation, reduction, and hydrolysis)
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Nomenclature CYP3A4
3=? A=? 4=? |
3=gene family
A=gene-sub-family 4=ind. gene |
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Competitive interactions=?
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drugs compete with binding sites of the same metabolizing enzymes
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Onset of compeptitive interactions depend on??
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half life of the inhibitor
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rifampin induction (dec. conc.) can be apparent when? bc?
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w/i 24 hours because of short 1/2L
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Phenobarbital induction is?? bc?
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gradual, can take abt. 1 week bc of longer 1/2 l
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induction of drugs decreases with?
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age, and hepatic disease
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substates for CYP-1A2
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theophylline, caffeine, clozapine, fluvoxamine, amitriptylline, propranolol
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inh. of CYP-1A2
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Fluvoxamine (use escitalopram), ciprofloxacin (use another quinolone), clarithromycin, e-mycin, cimetidine
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inducers of CYP1A2
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rifampin, st. John's wort
carmabazepine, phenytoin, primidone, phenobarbital cigarette smoke (nicotine patch won't affect substrates, charcoal-broiled foods |
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CYP2C9 substrates
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phenytoin, warfarin, fluoxetine, voriconazole, fluvastatin
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CYP-2C9 inhibitors
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Omeprazole, cimetidine (use lansopazole or famotidine)
amiodarone (use sotalol) fluconazole (use voriconazole) ibuprofen metronidazole |
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CYP-2C9 inducers
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rifampin, st. johns wort
carbamezepine, phenytoin, primidone, phenobarbital |
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CYP2D6 substrates
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codeine-morphine
hydrocodone-methadone oxycodone dextromethorphan tramadol haloperidol, thioridazine risperdone propranolol, metroprolol tricyclic antidepressants, SSRI antidepressants |
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CYP2D6 inh.
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quinidine, amiodarone
fluoxetine, paroxetine (use escitalopram) sertraline ritonavir cimetidine |
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CYP2D6 inducers
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rifampin, st. johns wort
carbamezepine, phenytoin, phenobarb. |
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quinidine + metoprolol
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85% inc. in metoprolol serum conc.
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PIs
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CYP3A4 substate
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Oral contraceptives
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CYP3A4 substate
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alprazolam, triazolam, diazepam, and midazolam
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CYP3A4 substate
Use lorazepam or oxazepam |
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ergot alkaloids
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CYP3A4 substate
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atorvastatin, lovastatin, simvastatin
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use pravastatin, or rosuvastatin
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warfarin, cilostazol
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CYP3A4 substate
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sildenafil, verdenafil, tadalafil
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CYP3A4 substate
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carbamezepine
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CYP3A4 substate
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cyclosporine, tacrolimus
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CYP3A4 substate
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Cimetidine
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inh. of CYP3A4
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Ritonavir
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inh. of CYP3A4
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e-mycin, clarithromycin
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inh. of CYP3A4
for e-mcyin, use azithromycin |
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itraconazole, ketoconazole, fluconazole, voriconazole
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inh. of CYP3A4
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metronidazole
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inh. of CYP3A4
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grapefruit juice
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inh. of CYP3A4
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rifampin
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inducer of CYP3A4
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antiepileptic drugs
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inducer of CYP3A4
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st. john's wort
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inducer of CYP3A4
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ritonavir
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mixed inducer and inh.
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indinavir, saquinavir, amprenavir, atazanavir
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inh. 3YP3A4
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Delavirdine
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inh. 3YP3A4
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Nevirapine
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inh. 3YP3A4
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efavirenz
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inh. and inducer of 3YP3A4
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5-10% of caucasians
1-3% of a.a and asians |
poor met. (may completely lack the enzyme, or may have enzymes with low activitiy) of CYP2D6
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90% of caucasians
>98% of asians and native americans |
extensive met. of CYP2D6
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20% of a.a. and asians
3-5% of caucasians |
pm of CYP 2C19
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CYP3A4 and CYP1A2
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no data available
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probenecid dec. clearance of pencillin, methotrexate and zidovudine bc.
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elimination rxns:
inh. of renal tubular secretion |
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quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
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dig.; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half) |
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cimetidine and ranatidine dec. clearance of ________ bc.
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procainamide; elimination rxns:
inh. of renal tubular secretion |
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
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inh. of enterohepatic recirculation.
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines inc. CL of ?
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oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.
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quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
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digoxin; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half) |
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cimetidine and ranatidine dec. clearance of ________ bc.
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procainamide; elimination rxns:
inh. of renal tubular secretion |
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
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inh. of enterohepatic recirculation.
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines dec. CL of ?
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oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.
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quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
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dig.; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half) |
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cimetidine and ranatidine dec. clearance of ________ bc.
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procainamide; elimination rxns:
inh. of renal tubular secretion |
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
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inh. of enterohepatic recirculation.
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ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines dec. CL of ?
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oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.
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