SUBSTRATES
|
1A2 |
2B6 |
2C8 |
2C9 |
2C19 |
2D6 |
2E1 |
3A4,5,7 |
clozapine
cyclobenzaprine
duloxetine
fluvoxamine
haloperidol
imipramine
mexiletine
nabumetone
naproxen
olanzapine
riluzole
tacrine2
theophylline
tizanidine
triamterene
zileuton
zolmitriptan
|
artemisinin
bupropion1
cyclophosphamide
efavirenz1
ifosfamide
ketamine
meperidine
methadone
nevirapine
propofol
selegiline
|
paclitaxel
torsemide
amodiaquine2
cerivastatin
repaglinide |
NSAIDs:
diclofenac
ibuprofen
naproxen
piroxicam
Oral Hypoglycemics:
tolbutamide
glipizide
glyburide
Angiotensin II Blockers:
losartan
irbesartan
Others:
celecoxib
fluvastatin
phenytoin
rosiglitazone
torsemide
valproic acid
warfarin
zafirlukast |
PPIs:
esomeprazole
lansoprazole
omeprazole
pantoprazole
Anti-epileptics:
diazepam
phenytoin
phenobarbitone
Others:
amitriptyline
carisoprodol
citalopram
clomipramine
clopidogrel
cyclophosphamide
imipramine
labetalol
proguanil
voriconazole |
Beta Blockers:
carvedilol
S-metoprolol
propafenone
timolol
Antidepressants:
amitriptyline
clomipramine
desipramine
duloxetine
fluoxetine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
Others:
aripiprazole
atomoxetine
codeine
dextromethorphan
doxepine
flecainide
mexiletine
ondansetron
oxycodone
risperidone
tamoxifen
TAMOXIFEN GUIDE
tramadol
venlafaxine |
Anesthetics:
enflurane
halothane
isoflurane
methoxyflurane
sevoflurane
Others:
acetaminophen→NAPQI
aniline
benzene
chlorzoxazone
ethanol
N,N-dimethyl formamide
theophylline→8-OH |
Macrolide antibiotics:
clarithromycin
erythromycin (not 3A5)
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine→3-OH (not 3A5)
Benzodiazepines:
alprazolam
diazepam→3OH
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
sirolimus
HIV Antivirals:
indinavir
ritonavir
saquinavir
nevirapine
Prokinetics:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
lovastatin
NOT pravastatin
NOT rosuvastatin
simvastatin
PDE-5 Inhibitors:
sildenafil
tadalafil
vardenafil
Others:
alfentanyl
aripiprazole
boceprevir
buspirone
carbamazepine
gleevec
haloperidol
pimozide
quinine
tamoxifen
telaprevir
trazodone
vincristine |
INHIBITORS
|
A Strong inhibitor is one that causes a > 5-fold increase in the plasma AUC values or more than 80% decrease in clearance.
A Moderate inhibitor is one that causes a > 2-fold increase in the plasma AUC values or 50-80% decrease in clearance.
A Weak inhibitor is one that causes a > 1.25-fold but < 2-fold increase in the plasma AUC values or 20-50% decrease in clearance.
|
1A2 |
2B6 |
2C8 |
2C9 |
2C19 |
2D6 |
2E1 |
3A4,5,7 |
amiodarone
cimetidine
efavirenz
fluoroquinolones
fluvoxamine1
ticlopidine
|
clopidogrel
thiotepa
ticlopidine2
voriconazole
|
gemfibrozil
montelukast1 |
amiodarone
efavirenz
fluconazole2
isoniazid
metronidazole
paroxetine
sulfamethoxazole
voriconazole |
cimetidine
esomeprazole
felbamate
fluoxetine
fluvoxamine
isoniazid
ketoconazole
lansoprazole
omeprazole
oral contraceptives
pantoprazole
ticlopidine2
voriconazole
|
bupropion
fluoxetine
paroxetine
quinidine1
duloxetine
amiodarone
cimetidine
aripiprazole
diphenhydramine
chlorpheniramine
clomipramine
doxepin
haloperidol
methadone
ritonavir
terbinafine |
disulfiram |
HIV Antivirals:
indinavir
nelfinavir
ritonavir
clarithromycin
itraconazole
ketoconazole
nefazodone
erythromycin
grapefruit juice
verapamil2
suboxone
diltiazem
cimetidine
amiodarone
NOT azithromycin
fluvoxamine
troleandomycin
voriconazole
|
INDUCERS
|
1A2 |
2B6 |
2C8 |
2C9 |
2C19 |
2D6 |
2E1 |
3A4,5,7 |
carbamazepine
chargrilled meat
rifampin
tobacco
|
artemisinin
carbamazepine
efavirenz
nevirapine
phenobarbital
phenytoin
rifampin |
|
carbamazepine
nevirapine
phenobarbital
rifampin
St. John's Wort |
efavirenz
rifampin
ritonavir
St. John's Wort |
|
ethanol
isoniazid |
carbamazepine
efavirenz
nevirapine
phenobarbital
phenytoin
pioglitazone
rifabutin
rifampin
St. John's Wort
troglitazone |
GENETICS
|
1A2 |
2B6 |
2C8 |
2C9 |
2C19 |
2D6 |
2E1 |
3A4,5,7 |
Chr |
Chr |
Chr |
Chr |
Chr |
Chr 22 |
Chr |
Chr |
|
|
|
Haplotypes:
*2=PM
*3=PM |
Haplotypes:
*2=PM (99% in Asians)
*3=PM (87% in Whites) |
Haplotypes:
*2=EM (similar to WT)
*3=PM (truncates protein)
*4=PM (non-functional)
*5=PM (whole gene del.)
*6=PM (truncates protein)
*9=IM/EM (reduces func.)
*10=IM (reduces func.)
*17=IM (reduces func.)
*29=IM (reduces func.)
*41=IM (reduces func.) |
|
|
Metabolizer Phenotypes:
PM = Poor
IM = Intermediate
EM = Extensive
UM = Ultrarapid |