P450 Table

Version 4.0 released on Aug 20, 2007.

In this version you will find new literature references, which describe whether an inhibitor is strong, moderate or weak (see below for criteria specified by the FDA).
You will also encounter new data about FDA preferred and acceptable substrates for in vitro experiments.

Below the list of drugs that are metabolized by a specific cytochrome P450 isoform are the published inhibitors, inducers and genetic influences on that isoform. Drug names are hyperlinks to specific literature references, most of which now include a link to the abstract of the article in the NLM's PubMed database. Also, you can click on the PubMed link after the drug name to perform a live MedLINE search of articles possibly related to that drug and Cytochrome P450. Enzymes denoted with a colored bullet or with either a superscript number 1 or 2 are taken from the FDA Drug Development and Drug Ineractions: Table of Substrates, Inhibitors and Inducers (May 2006).*

:: View clinically relevant table ::

Please use the following reference:
Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). http://medicine.iupui.edu/flockhart/table.htm. Accessed [date].

Use Ctrl-F to find all or part of the word for which you are searching.

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SUBSTRATES

FDA preferred¹ and acceptable² substrates for in vitro experiments.*

amitriptyline
caffeine²
clomipramine
clozapine
cyclobenzaprine
estradiol
fluvoxamine
haloperidol
imipramine N-DeMe
mexiletine
naproxen
olanzapine
ondansetron
phenacetin¹ =>
acetaminophen=>NAPQI
propranolol
riluzole
ropivacaine
tacrine²
theophylline²
tizanidine
verapamil
(R)warfarin
zileuton
zolmitriptan

bupropion¹
cyclophosphamide
efavirenz¹
ifosfamide
methadone

paclitaxel
torsemide
amodiaquine²
cerivastatin
repaglinide

Proton Pump Inhibitors:
lansoprazole
omeprazole²
pantoprazole
rabeprazole
E-3810

Anti-epileptics:
diazepam=>Nor
phenytoin(O)
S-mephenytoin¹
phenobarbitone

amitriptyline
carisoprodol
citalopram
chloramphenicol
clomipramine
clopidogrel
cyclophosphamide
hexobarbital
imipramine N-DeME
indomethacin
R-mephobarbital
moclobemide
nelfinavir
nilutamide
primidone
progesterone
proguanil
propranolol
teniposide
R-warfarin=>8-OH

NSAIDs:
diclofenac¹
ibuprofen
lornoxicam
meloxicam
S-naproxen=>Nor
piroxicam
suprofen

Oral Hypoglycemic Agents:
tolbutamide¹
glipizide

Angiotensin II Blockers:
losartan
irbesartan

Sulfonylureas:
glyburide/
glibenclamide
glipizide
glimepiride
tolbutamide

amitriptyline
celecoxib
fluoxetine
fluvastatin
glyburide
nateglinide
phenytoin-4-OH²
rosiglitazone
tamoxifen
torsemide
S-warfarin¹

Beta Blockers:
carvedilol
S-metoprolol
timolol

Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine

Antipsychotics:
haloperidol
perphenazine
risperidone=>9OH
thioridazine
zuclopenthixol

alprenolol
amphetamine
aripiprazole
atomoxetine
bufuralol¹
chlorpheniramine
chlorpromazine
codeine (=>O-desMe)
debrisoquine²
dexfenfluramine
dextromethorphan¹
duloxetine
encainide
flecainide
fluoxetine
fluvoxamine
lidocaine
metoclopramide
methoxyamphetamine
mexilletine
minaprine
nebivolol
nortriptyline
ondansetron
oxycodone
perhexiline
phenacetin
phenformin
promethazine
propafenone
propranolol
sparteine
tamoxifen
tramadol
venlafaxine

Anesthetics:
enflurane
halothane
isoflurane
methoxyflurane
sevoflurane

acetaminophen
=>NAPQI
aniline²
benzene
chlorzoxazone¹
ethanol
N,N-dimethyl formamide
theophylline
=>8-OH

Macrolide antibiotics:
clarithromycin
erythromycin² (not 3A5)
NOT azithromycin
telithromycin

Anti-arrhythmics:
quinidine=>3-OH (not 3A5)

Benzodiazepines:
alprazolam
diazepam=>3OH
midazolam¹
triazolam²

Immune Modulators:
cyclosporine
tacrolimus (FK506)

HIV Antivirals:
indinavir
nelfinavir
ritonavir
saquinavir

Prokinetic:
cisapride

Antihistamines:
astemizole
chlorpheniramine
terfenadine²

Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
lercanidipine
nifedipine²
nisoldipine
nitrendipine
verapamil

HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin

Steroid 6beta-OH:
estradiol
hydrocortisone
progesterone
testosterone¹

Miscellaneous:
alfentanyl
aprepitant
aripiprazole
buspirone
cafergot
caffeine=>TMU
cilostazol
cinacalcet
cocaine
codeine- N-demethylation
dapsone
dexamethasone
dextromethorphan²
docetaxel
domperidone
eplerenone
fentanyl
finasteride
gleevec
haloperidol
irinotecan
LAAM
lapatinib
lidocaine
methadone
nateglinide
ondansetron
pimozide
propranolol
quetiapine
quinine
risperidone
NOT rosuvastatin
salmeterol
sildenafil
sirolimus
tamoxifen
taxol
terfenadine
trazodone
vincristine
zaleplon
ziprasidone
zolpidem

INHIBITORS

Inhibitors compete with other drugs for a particular enzyme thus affecting the optimal level of metabolism of the substrate drug which in many cases affect the individual's response to that particular medication, e.g. making it ineffective.

A Strong inhibitor is one that cause a > 5-fold increase in the plasma AUC values or more than 80% decrease in clearance.
A Moderate inhibitor is one that cause a > 2-fold increase in the plasma AUC values or 50-80% decrease in clearance.
A Weak inhibitor is one that cause a > 1.25-fold but < 2-fold increase in the plasma AUC values or 20-50% decrease in clearance.
All other inhibitors.

FDA preferred¹ and acceptable² inhibitors for in vitro experiments.*

fluvoxamine

ciprofloxacin

cimetidine

amiodarone

fluoroquinolones

furafylline¹

interferon

methoxsalen

mibefradil

thiotepa

ticlopidine²

gemfibrozil²

trimethoprim²

glitazones

montelukast¹

quercetin¹

PPIs:
lansoprazole
omeprazole²
pantoprazole
rabeprazole

chloramphenicol

cimetidine

felbamate

fluoxetine

fluvoxamine

indomethacin

ketoconazole

modafinil

oxcarbazepine

probenicid

ticlopidine²

topiramate

fluconazole²

amiodarone

fenofibrate

fluvastatin

fluvoxamine²

isoniazid

lovastatin

phenylbutazone

probenicid

sertraline

sulfamethoxazole

sulfaphenazole¹

teniposide

voriconazole

zafirlukast

bupropion

fluoxetine

paroxetine

quinidine¹

duloxetine

terbinafine

amiodarone

cimetidine

sertraline

celecoxib

chlorpheniramine

chlorpromazine

cinacalcet

citalopram

clemastine

clomipramine

cocaine

diphenhydramine

doxepin

doxorubicin

escitalopram

goldenseal

halofantrine

histamine H1 receptor antagonists

hydroxyzine

levomepromazine

methadone

metoclopramide

mibefradil

midodrine

moclobemide

perphenazine

ranitidine

red-haloperidol

ritonavir

ticlopidine

tripelennamine

diethyl-dithiocarbamate²

disulfiram

HIV Antivirals:

indinavir

nelfinavir

ritonavir

clarithromycin

itraconazole¹

ketoconazole¹

nefazodone

saquinavir

telithromycin

aprepitant

erythromycin

fluconazole

grapefruit juice

verapamil²

diltiazem

cimetidine

amiodarone

NOT azithromycin

chloramphenicol

delaviridine

diethyl-dithiocarbamate

fluvoxamine

gestodene

imatinib

mibefradil

mifepristone

norfloxacin

norfluoxetine

star fruit

voriconazole

INDUCERS

Inducers stimulate the production of the enzyme thus increasing the rate of metabolism causing the substrate drug to clear out of the system faster. This will also affect the individual's response to the medication, i.e. making he drug ineffective because it has not been in the system long enough to have an effect.

FDA preferred¹ and acceptable² inducers for in vitro experiments.*