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Pharmacokinetics: Substrates, Inhibitors and Inducers of CYP 450 


CYP450 SUBSTRATES
         
1A2 2B6 2C19 2D6 3A4


chlorpromazine
fluphenazine
haloperidol
perphenazine

clozapine
olanzapine
ziprasidone

ropinirole

ALL methylxanthines

Caffeine (cup of coffee)




phenytoin
phenobarbital

citalopram
escitalopram
fluoxetine
sertraline

venlafaxine

PPIs
tranylcypromine
meclobemide

amitriptyline
clomipramine
desipramine
doxepin
imipramine
nortriptyline

citalopram
fluoxetine
escitalopram
paroxetine

nefazodone
trazodone

duloxetine
venlafaxine

chlorpromazine
fluphenazine
haloperidol
thioridazine
perphenazine

aripiprazole
clozapine
quetiapine
risperidone 

metoprolol
most beta blockers

codeine
hydrocodone prodrug
dextromethorphan
tramadol prodrug

tamoxifen prodrug

ondansetron

amitriptyline
clomipramine
doxepin
imipramine

buspirone
citalopram
escitalopram
paroxetine
sertraline
mirtazapine
nefazodone
trazodone
venlafaxine

chlorpromazine
haloperidol
perphenazine
pimozide
aripiprazole
clozapine
quetiapine
risperidone
ziprasidone

triazolo-
benzodiazepines

zaleplon
zolpidem
zoplicone

carbamazepine
valproic acid

buprenorphine
codeine
fentanyl
hydrocodone prodrug
meperidine
methadone
tramadol prodrug

statins
exceptions pravastatin
 and rosuvastatin

antiarrhythmics

CCBs
beta blockers

macrolide
azithromycin

oral contraceptives

CYP450 INHIBITORS   back to top
1A2 2B6 2C19 2D6 3A4
amitriptyline
imipramine

fluvoxamine duloxetine

ciprofloxacin
norfloxacin
ofloxacin

cimetidine

fluvoxamine

clopidogrel
ticlopidine

amitriptyline
imipramine

fluoxetine
fluvoxamine
paroxetine

ketoconazole







lansoprazole is the most potent in vitro
   inhibitor of 2C19

All TCAs

fluoxetine
paroxetine
bupropion

sertraline > 100-150mg
duloxetine
fluvoxamine
citalopram


chlorpromazine
fluphenazine
haloperidol
perphenazine
thioridazine

aripiprazole
clozapine
risperidone

methadone

valproic acid mild

*quinidine*
ritonavir
cimetidine
diphenhydramine
Vistaril

metoclopramide

nefazodone
norfluoxetine
fluoxetine
fluvoxamine

haloperidol
pimozide

ciprofloxacin
norfloxacin

keto- and itraazole

diltiazem
verapamil

cimetidine
protease inhibitors
NNRTIs


grapefruit
CYP450 INDUCERS   back to top
1A2 2B6 2C19 2D6 3A4

modafinil

cruciferous vegetables
charbroiled foods

tobacco
phenobarbital

cyclophosphamide


phenobarbital
phenytoin

rifampin

No Inducers!
phenobarbital
phenytoin

rifampin
ritonavir
efavirenz
St. John's Wort
modafinil


UGT Table
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