Summary of Major CYP Isoforms and their Substrates, Inhibitors and Inducers (Human Drug Metabolism)

This is not an exhaustive list and many drugs are metabolized by several CYP isoforms to varying degrees.

CYP

Substrates

Inhibitors

Inducers

1A1

Polycyclic aromatic hydrocarbons (PAHs), organochlorine insecticides

α-naphthoflavone

PAHs,

organochlorines

1A2

Amitriptyline, imipramine, caffeine, fluvoxamine, clozapine, haloperidol, mexiletine, ondansetron, propranolol, tacrine, theophylline, verapamil,

R – warfarin, zolmitriptan Polycyclic aromatic amines

Amiodarone, cimetidine, furafylline, fluvoximine, ticlopidine ciprofloxacin

PAH amines in

barbecued/

flame – broiled meat,

Brussels sprouts,

broccoli, insulin,

tobacco, omeprazole,

phenytoin

1B1

Tamoxifen, polycyclic aromatics Aromatic amines, aflatoxins, oestrogens.

PCBs (e.g. pyrene) some flavonoids & coumarins, resveratrol, mitoxantrone, flutamide, taxols

PAHs,

ß-naphthoflavone tobacco PAHs

2A6

Coumarins, aflatoxins 1,3, butadiene, letrozole, valproate

Tranylcypramine, methoxsalen, grapefruit juice


Phenobarbitone,

rifampicin

2B6

bupropion, coumarins, cyclophosphamide, mephenytoin, methadone, methoxychor (pesticide), PCP, ketamine, efavirenz

Tranylcypramine, thiotepa, ticlopidine

Phenobarbitone, rifampicin, efavirenz

2C8

Amodiaquine, cerivastatin, paclitaxel, tolbutamide

Quercetin, glitazone drugs, gemfibrozil efavirenz, montelukast

Phenobarbitone

Rifampicin,

CYP

Substrates

Inhibitors

Inducers

2C9

Amitriptyline, dapsone, fluoxetine, fluvastatin, NSAIDS, phenytoin, sulphonyl ureas, tamoxifen, S-warfarin

Isoniazid, fluvastatin, fluvoxamine, lovastatin, sulphafenazole diclofenac

Secobarbitone,

Rifampicin

2C19

Barbiturates, citalopram, mephenytoin, proton pump inhibitors e.g. omeprazole, phenytoin, proguanil, R – warfarin voriconazole.

Tranylcypramine, cimetidine, fluoxetine, ketoconazole, ticlopidine

Carbamazepine,

norethindrone,

prednisone,

rifampicin

2D6

TCAs, antipsychotics (haloperidol, etc.), anti – arrhythmics: flecainide, mexiletine, beta-blockers (e.g. timolol, S-metoprolol, bufuralol), MDMA, SSRIs, opiates (e.g. tramadol, codeine), venlafaxine

Amiodarone, cimetidine, ranitidine, histamine H-1 receptor antagonists (e.g. chlorpheniramine), quinidine, SSRIs (e.g. fluoxetine), St John’s Wort

Not conventionally induced

2E1

Benzene, chlorzoxazone, ethanol, flurane anaesthetics (e.g. halothane), paracetamol

Sulphides (e.g. DDC, diallyl sulphide, disulfiram)

Ethanol, acetone isoniazid

3A4/5

Aflatoxin B1, antihistamines (terfenadine, astemizole), calcium channel blockers (e.g. felodipine), cannabinoids, cyclosporine, macrolides (e.g. erythromycin), opiates (buprenorphine), protease inhibitors (e.g. ritonavir), statins (except pravastatin), tacrolimus, paclitaxel THCs midazolam, nefazodone, dasatinib.

Amiodarone, azoles (ketoconazole fluconazole, voriconazole) cimetidine, grapefruit juice, macrolides, steroids, protease inhibitors

Barbiturates, carbamazepine, glucocorticoids, glitazones, nevirapine, phenytoin, rifampicin, St John’s Wort

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