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Clinical Pharmacology

P450 Drug Interaction Table: Abbreviated "Clinically Relevant" Table

 

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