Cytochrome P450 : substrates, inhibitors and inducers

Bulletin ( January - March 2000 Vol.9 No.1)

Cytochrome P450 : substrates, inhibitors and inducers

Cytochrome P450	Substrates	Inhibitors	Inducers	Genetics
CYP1A2	amitriptyline caffeine Clomipramine Cyclobenzapine (Flexeril ^(R)) estradiol Fluvoxamine haloperidol imipramine N-DeMe mexiletine naproxen (in part) ondansetron (in part) phenacetin==>acetaminophen==>NAPQI propanolol riluzole ropivacaine tacrine theophylline varapamil(thoe) (R) warfarin zileuton zomitriotan(/td)	amiodarone cemetidine fluoroquinilones fluvoxamine furafylline interferon? methoxsalen mibefradil ticlopidine	broccoli brussel sprouts? char-grilled meat insulin methyl cholanthrene nafcillin? beta-naphtthoflavone omeprazole tobacco	chromosome 15
CYP2C19	amitriptyline citalopram clomipramine hexobarbital imipramine N-DeMe indomethacin R-mephobarbital moclobemide nefinavir nilutamide primidone? progesterone proguanil propanolol (in part) teniposide R-warfarin==ɴ-OH Proton Pump inhibitors lansoprazole omeprazole pantoprazole E-3810 Antiepileptics diazepam==>Nor phenytoin(O) S-metphenytoin phenobarbitone	cimetidine felbamate fluoxetine indomethacin ketoconazole lansoprazole paroxetine ?probenicid ticlopidine topiramate	carbamazepine? norethindrone Not pentobarbital prednisone rifampin	Chromosome 10 Polymorphic 3-5% Caucasian PMs 15-20% Asian PMs
CYP2C9	NSAIDs diclofenac ibuprofen S-naproxen==>Nor piroxicam Oral Hypoglycemic Agents tobutamide glipizide AngiotensinII Blockers NOT candesartan irbesatan losatan NOT valsartan amitriptyline celecoxib fluoxetine fluvastatin phenytoin==>4-OH rosiglitazole sulfamethoxazole tamoxifen torsemide S-warfarin	amiodarone fluconazole fluvastatin fluvoxamine isoniazid lovastatin paroxetine phenylbutazone ?probenicid sertraline sulfaphenazole teniposide ?trimethoprim zafirlukast	rifampin secobabital	Chromosome 10 Polymorphic 1-3% caucasian PMs
CYP2D6	Beta Blockers carvedilol S-metoprolol propafenone tomolol Antidepressants amitriptylline (in part) clomipramine (in part) desipramine imipramine (in part) paroxetine (in part) Antipsychotics haloperidol perphenazine risperidone==>9-OH thioridazine alprenolol amphetamine bufuralol codeine(==>O-desMe) debrisoquine dexfenfluramine dextromethorphan encainide flecainide fluoxetine fluvoxamine lidocaine (in part) methoxyamphetamine mexiletine minaprine nortriptyline ondansetron perhexilinenortriptyline phenacetin phenformin propranolol (==>4OH) quanoxan spateine tamoxifen tramadol venlafaxine	amiodarone celecoxib chlorpheniramine cimetidine clomipramine cocaine doxorubicin? fluoxetine halofantrine red-haloperidol levomeprazine methadone mibefradil moclobemide paroxetine quinidine ranitidine ritonavir tterbinafine	dexamethasone? rifampin?	Chromosome 22 Polymorphic 5-10% caucasian PMs
CYP2E1	Aneathetic enflurane halothane isoflurane methoxyflurane sevoflurane acetaminophen==>NAPQI aniline benzene chlorzoxazone ethanol N,N-dimethyl formamide theophylline==>8-OH	diethyl-dithiocarbamate disulfiram	ethanol isoniazid	Chromosome 10
CYP3A4,5,7	Macrolide clarithromycin erythromycin(not 3A5) NOTazithromycin Anitiarrhythmics quinidine==> 3-OH Benzodiazepines alprazolam midazolam triazolam Immune Modulators cyclosporine tacrolilimus(FK506) HIV Antivirals indinavir nefinavir ritonavir saquinavir Prokinetic cisapride Antihistamines astemizole chlorpheniramine terfenidine Calcium Channel Blockers amlodipine diltiazem felodepine lercanidipine nifedipine nisoldepine nitrendipine verapamil HMG CoA Reductase Inhibitors atorvastatin cerivastatin lovastatin NOT pravastatin simvastatin Steroid 6Beta-OH estradiol hydrocortisone progesterone testosterone Miscellaneous alfentanyl buspirone caffeine==>N-OH (in part) codeine-N-demethylation dextromethorphan fentanyl finasteride haloperidol (in part) lidocaine (in part) methadone odansetron pimozide propanolol? quinine salmeterol sidenafil tamoxifen taxol (in part) terfenadine trazodone vincristine zalephon zolpidem	HIV Antivirals delaviridine indinavir nelfinavir ritonavir saquinavir amiodarone NOT azithromycin cimetidine ciprofloxacin diethyl-dithiocarbamate dilthiazem erythromycin fluconazole fluvoxamine gestodene grapefruit juice itraconazole ketoconazole mifepristone nefazodone norfluoxetine mibefradil troleandomycin	HIV Antivirals efavirenz nevirapine barbiturates carbamazepine glucocorticoids phenobarbital phenytoin pioglitazone rifampin St. John's wort troglitazone	Chromosome 7