Table 1

Examples of central nervous system–acting substrates for 3 drug-metabolizing cytochromes P450 (5), (13) (18)

EnzymeCNS-acting drugsEndogenousOther drugs and toxins
CYP2B6Bupropion, diazepam, ketamine, methadone, meperidine, nicotine, pentobarbital, phencyclidine, propofol, sertraline selegiline, tramadol17-β estradiol, anandamide, arachidonic acid, estrone, serotonin, testosterone3,4-methylenedioxy-amphetamine (ecstasy), chlorpyrifos, cyclophosphamide, DEET, efavirenz, ifosphamide, malathion, paraquat, parathion
CYP2D6Amyltriptyline, brofaromine, clomipramine, codeine, citalopram, clozapine, desipramine, dextromethorphan, ethylmorphine, fluoxetine, fluvoxamine, haloperidol, hydrocodone, imipramine, mianserin, mirtazapine, nicergoline, nortryptaline, oxycodone, paroxetine, perphenazine, risperidone, tramadol, tranylcypromine, venlafaxine, zuclopenthixol5-methoxytryptamine, anandamide, progesterone, tyramineMPTP, parathion, tamoxifen
CYP2E1Enflurane, felbamate, halothane, isoflurane, sevoflurane, trimethadione17-β estradiol, arachidonic acid, estrone, prostaglandinAcetaminophen, acetone, aniline, benzene, carbon tetrachloride, chloroform, chlozoxazone, ethanol, NNK, phenol, theophylline, trichloroethane
  • CNS = central nervous system; DEET = N,N-diethyl-m-toluamide; MPTP = 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine; NNK = 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.