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57 Cards in this Set

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CYP 450 is involve w/ _____ rxns
phase 1 (oxidation, reduction, and hydrolysis)
Nomenclature CYP3A4
3=?
A=?
4=?
3=gene family
A=gene-sub-family
4=ind. gene
Competitive interactions=?
drugs compete with binding sites of the same metabolizing enzymes
Onset of compeptitive interactions depend on??
half life of the inhibitor
rifampin induction (dec. conc.) can be apparent when? bc?
w/i 24 hours because of short 1/2L
Phenobarbital induction is?? bc?
gradual, can take abt. 1 week bc of longer 1/2 l
induction of drugs decreases with?
age, and hepatic disease
substates for CYP-1A2
theophylline, caffeine, clozapine, fluvoxamine, amitriptylline, propranolol
inh. of CYP-1A2
Fluvoxamine (use escitalopram), ciprofloxacin (use another quinolone), clarithromycin, e-mycin, cimetidine
inducers of CYP1A2
rifampin, st. John's wort

carmabazepine, phenytoin, primidone, phenobarbital

cigarette smoke (nicotine patch won't affect substrates, charcoal-broiled foods
CYP2C9 substrates
phenytoin, warfarin, fluoxetine, voriconazole, fluvastatin
CYP-2C9 inhibitors
Omeprazole, cimetidine (use lansopazole or famotidine)

amiodarone (use sotalol)

fluconazole (use voriconazole)

ibuprofen

metronidazole
CYP-2C9 inducers
rifampin, st. johns wort

carbamezepine, phenytoin, primidone, phenobarbital
CYP2D6 substrates
codeine-morphine
hydrocodone-methadone
oxycodone
dextromethorphan
tramadol
haloperidol, thioridazine
risperdone
propranolol, metroprolol
tricyclic antidepressants,
SSRI antidepressants
CYP2D6 inh.
quinidine, amiodarone

fluoxetine, paroxetine (use escitalopram)

sertraline

ritonavir

cimetidine
CYP2D6 inducers
rifampin, st. johns wort

carbamezepine, phenytoin, phenobarb.
quinidine + metoprolol
85% inc. in metoprolol serum conc.
PIs
CYP3A4 substate
Oral contraceptives
CYP3A4 substate
alprazolam, triazolam, diazepam, and midazolam
CYP3A4 substate

Use lorazepam or oxazepam
ergot alkaloids
CYP3A4 substate
atorvastatin, lovastatin, simvastatin
use pravastatin, or rosuvastatin
warfarin, cilostazol
CYP3A4 substate
sildenafil, verdenafil, tadalafil
CYP3A4 substate
carbamezepine
CYP3A4 substate
cyclosporine, tacrolimus
CYP3A4 substate
Cimetidine
inh. of CYP3A4
Ritonavir
inh. of CYP3A4
e-mycin, clarithromycin
inh. of CYP3A4
for e-mcyin, use azithromycin
itraconazole, ketoconazole, fluconazole, voriconazole
inh. of CYP3A4
metronidazole
inh. of CYP3A4
grapefruit juice
inh. of CYP3A4
rifampin
inducer of CYP3A4
antiepileptic drugs
inducer of CYP3A4
st. john's wort
inducer of CYP3A4
ritonavir
mixed inducer and inh.
indinavir, saquinavir, amprenavir, atazanavir
inh. 3YP3A4
Delavirdine
inh. 3YP3A4
Nevirapine
inh. 3YP3A4
efavirenz
inh. and inducer of 3YP3A4
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
90% of caucasians
>98% of asians and native americans
extensive met. of CYP2D6
20% of a.a. and asians
3-5% of caucasians
pm of CYP 2C19
CYP3A4 and CYP1A2
no data available
probenecid dec. clearance of pencillin, methotrexate and zidovudine bc.
elimination rxns:
inh. of renal tubular secretion
quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
dig.; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half)
cimetidine and ranatidine dec. clearance of ________ bc.
procainamide; elimination rxns:
inh. of renal tubular secretion
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
inh. of enterohepatic recirculation.
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines inc. CL of ?
oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.
quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
digoxin; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half)
cimetidine and ranatidine dec. clearance of ________ bc.
procainamide; elimination rxns:
inh. of renal tubular secretion
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
inh. of enterohepatic recirculation.
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines dec. CL of ?
oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.
quinidine , amiodarone, and bactrim dec. clearnace of _______ bc?
dig.; elimination rxns:
inh. of renal tubular secretion (may need to dec. dose of digoxin by half)
cimetidine and ranatidine dec. clearance of ________ bc.
procainamide; elimination rxns:
inh. of renal tubular secretion
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines are?
inh. of enterohepatic recirculation.
ampicillin, penacillin, nitrofurantoin, sulfonamides, and tetracyclines dec. CL of ?
oral contraceptives bc of dec. absorption due to dec. enterohepatic circulation.