Peer-reviewed Literature References (CYP1A2)
1A2 SUBSTRATES:AMITRIPTYLINEFluvoxamine-tricyclic antidepressant interaction. An accidental finding. [ PMID 1905641 ] Bertschy G, Vandel S, Vandel B, Allers G, Volmat R. Eur J Clin Pharmacol 1991;40(1):119-120. [Letter] CAFFEINE Determination of urinary metabolites of caffeine for the assessment of cytochrome P4501A2, xanthine oxidase, and N-acetyltransferase activity in humans. [ PMID 8738764 ] Rasmussen BB, Brosen K. Ther Drug Monit 1996 Jun;18(3):254-262. Assays for CYP1A2 by testing in vivo metabolism of caffeine in humans. [ PMID 8791769 ] Tang BK, Kalow W. Methods Enzymol 1996;272:124-131. CLOMIPRAMINE Fluvoxamine-tricyclic antidepressant interaction. An accidental finding. [ PMID 1905641 ] Bertschy G, Vandel S, Vandel B, Allers G, Volmat R. Eur J Clin Pharmacol 1991;40(1):119-120. [Letter] CLOZAPINE Metabolism and bioactivation of clozapine by human liver in vitro. [ PMID 7891353 ] Pirmohamed M, Williams D, Madden S, Templeton E, Park BK. J Pharmacol Exp Ther 272(3):984-990, 1995. Clozapine disposition covaries with CYP1A2 activity determined by a caffeine test. [ PMID 7893591 ] Bertilsson L, Carrillo JA, Dahl ML, Llerena A, Alm C, Bondesson U, Lindström L, Rodriguez de la Rubia I, Ramos S, Benitez J. Br J Clin Pharmacol 38:471-473, 1994. CYCLOBENZAPRINE Identification of Human Liver Cytochrome P450 Isoforms involved in the in vitro metabolism of cyclobenzaprine. [ PMID 8818577 ] Wang RW, Liu L, Cheng H. Drug Metab Dispos 1996;24(7):786-791. FLUVOXAMINE Disposition of fluvoxamine in humans is determined by the polymorphic CYP2D6 and also by the CYP1A2 activity. [ PMID 8823236 ] Carillo JA, Dahl ML, Svennson JO, Alm C, Rodriguez I, Bertillson L. Clin Pharmacol Ther 1996;60:183-190. ESTRADIOL Differences in the cytochrome P-450 isoenzymes involved in the 2-hydroxylation of oestradiol and 17alpha-ethinyloestradiol. [ PMID 2327982 ] Ball SE, Forrester LM, Wolf CR, Back DJ. Biochem J 267:221-226, 1990. HALOPERIDOL Coadministration of fluvoxamine increases serum concentrations of haloperidol. [ PMID 7806690 ] Daniel DG, Randolph C, Jaskiw G, Handel S, Williams T, Abi-Dargham A, Shoaf S, Egan M, Elkashef A, Liboff S, Linnoila M. J Clin Psychopharmacol 14:340-343, 1994. IMIPRAMINE Reappraisal of human CYP isoforms involved in imipramine N-demethylation and 2-hydroxylation: a study using microsomes obtained from putative extensive and poor metabolizers of S-mephenytoin and eleven recombinant human CYPs. [ PMID 9190854 ] Koyama E, Chiba K, Tani M, Ishizaki T J Pharmacol Exp Ther 1997 Jun;281(3):1199-1210 Major pathway of imipramine metabolism is catalyzed by cytochromes P-450 1A2 and P-450 3A4 in human liver. [ PMID 8502233 ] Lemoine A, Gautier JC, Azoulay D, Kiffel L, Belloc C, Guengerich FP, Maurel P, Beaune P, Leroux JP Mol Pharmacol 1993 May;43(5):827-832 MEXILETINE Role of specific cytochrome P450 enzymes in the N-oxidation of the antiarrhythmic agent mexiletine. [ PMID 12519691 ] Labbé L, Abolfathi Z, Lessard E, Pakdel H, Beaune P, Turgeon J. Xenobiotica. 2003 Jan;33(1):13-25. Inhibition of human liver cytochrome P-450 1A2 by the class IB antiarrhythmics mexiletine, lidocaine, and tocainide. [ PMID 10215663 ] Wei X, Dai R, Zhai S, Thummel KE, Friedman FK, Vestal RE. J Pharmacol Exp Ther. 1999 May;289(2):853-8. NAPROXEN Cytochromes P450, 1A2, and 2C9 are responsible for the human hepatic O-demethylation of R- and S-naproxen. [ PMID 8866821 ] Miners JO, Coulter S, Tukey RH, Veronese ME, Birkett DJ Biochem Pharmacol 1996 Apr 26;51(8):1003-1008 OLANZAPINE Dose-dependent alternations in the pharmacokinetics of olanzapine during coadministration of fluvoxamine in patients with schizophrenia. [ PMID 15545309 ] Chiu CC, Lane HY, Huang MC, Liu HC, Jann MW, Hon YY, Chang WH, Lu ML. J Clin Pharmacol. 2004 Dec;44(12):1385-90. ONDANSETRON (in part) Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. [ PMID 8591723 ] Dixon CM, Colthup PV, Serabjit-Singh CJ, Kerr BM, Boehlert CC, Park GR, Tarbit MH Drug Metab Dispos 1995 Nov;23(11):1225-1230 PHENACETIN Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2. [ PMID 8474022 ] Tassaneeyakul W, Birkett DJ, Veronese ME, McManus ME, Tukey RH, Quattrochi LC, Gelboin HV, Miners JO. J Pharmacol Exp Ther 1993 Apr;265(1):401-407. Acetaminophen bioactivation by human cytochrome P450 enzymes and animal microsomes. [ PMID 19219744 ] Laine JE, Auriola S, Pasanen M, Juvonen RO. Xenobiotica. 2009 Jan;39(1):11-21. PROPRANOLOL Selective induction of propranolol metabolism by smoking: Additional effects on renal clearance of metabolites. [ PMID 3598909 ] Walle, U.K., Walle, T., Cowart, T.D., Conradi, E.C., and Gaffney, T.E. J. of Pharm. & Exp. Ther. 241:928-933, 1987. Fluvoxamine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. [ PMID 3096686 ] Benfield, P and Ward A Drugs 1986;32:313-334 [Fluvoxamine is a potent inhibitor of propranolol metabolism in vivo.] RILUZOLE Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitro. [ PMID 9316860 ] Sanderink GJ, Bournique B, Stevens J, Petry M, Martinet M J Pharmacol Exp Ther 1997 Sep;282(3):1465-1472 ROPIVACAINE Metabolism of ropivacaine in humans is mediated by CYP1A2 and to a minor extent by CYP3A4: an interaction study with fluvoxamine and ketoconazole as in vivo inhibitors. [ PMID 9834040 ] Arlander E, Ekstrom G, Alm C, Carrillo JA, Bielenstein M, Bottiger Y, Bertilsson L, Gustafsson LL Clin Pharmacol Ther 1998 Nov;64(5):484-91 TACRINE Determination of human hepatic cytochrome P450 1A2 activity in vitro: use of tacrine as an isozyme-specific probe. [ PMID 8565783 ] Spaldin V, Madden S, Adams DA, Edwards RJ, Davies DS, Park BK Drug Metab Dispos 1995;23(9):929-934 THEOPHYLLINE Metabolism of theophylline by cDNA-expressed human cytochromes P450. [ PMID 7619675 ] Ha HR, Chen J, Freiburghaus AU, Follath F Br J Clin Pharmacol 1995;39:321-326 TIZANIDINE Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism. [ PMID 15592331 ] Granfors MT, Backman JT, Neuvonen M, Neuvonen PJ. Clin Pharmacol Ther. 2004 Dec;76(6):598-606 Fluvoxamine drastically increases concentrations and effects of tizanidine: a potentially hazardous interaction. [ PMID 15060511 ] Granfors MT, Backman JT, Neuvonen M, Ahonen J, Neuvonen PJ. Clin Pharmacol Ther. 2004 Apr;75(4):331-41 VERAPAMIL The effect of three different oral doses of verapamil on the disposition of theophylline. [ PMID 1505606 ] Stringer KA, Mallet J, Clarke M, Lindenfeld JA Eur J Clin Pharmacol 1992;43(1):35-38 Verapamil-induced inhibition of theophylline elimination in healthy humans. [ PMID 2315261 ] Nielsen-Kudsk JE, Buhl JS, Johannessen AC Pharmacol Toxicol 1990 Feb;66(2):101-103 WARFARIN Possible antiretroviral therapy-warfarin drug interaction. [ PMID 18576910 ] Fulco PP, Zingone MM, Higginson RT. Pharmacotherapy. 2008 Jul;28(7):945-9. ZILEUTON Identification of the human liver cytochrome P450 enzymes involved in the metabolism of zileuton (ABT-077) and its N-dehydroxylated metabolite, Abbott-66193. [ PMID 8654206 ] Machinist JM, Mayer MD, Shet MS, Ferrero JL, Rodrigues AD Drug Metab Dispos. 1995 Oct; 23(10): 1163-1174 ZOLMITRIPTAN Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan. [ PMID 10553725 ] Wild MJ, McKillop D, Butters CJ Xenobiotica. 1999 Aug;29(8):847-57 1A2 INHIBITORS:AMIODARONEInhibitory effects of antiarrhythmic drugs on phenacetin O-deethylation catalysed by human CYP1A2. [ PMID 9578183 ] Kobayashi K, Nakajima M, Chiba K, Yamamoto T, Tani M, Ishizaki T, Kuroiwa Y. Br J Clin Pharmacol 1998 Apr;45(4):361-368. CIMETIDINE The effect of cimetidine on dextromethorphan O-demethylase activity of human liver microsomes and recombinant CYP2D6. [ PMID 16680870 ] Madeira M, Levine M, Chang TK, Mirfazaelian A, Bellward GD. Drug Metab Dispos. 2004 Apr;32(4):460-7. Comparative in vitro and in vivo inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists. [ PMID 10223772 ] Martínez C, Albet C, Agúndez JA, Herrero E, Carrillo JA, Márquez M, Benítez J, Ortiz JA. Clin Pharmacol Ther. 1999 Apr;65(4):369-76. Imipramine-cimetidine interaction: impairment of clearance and enhanced absolute bioavailability. [ PMID 6726654 ] Abernethy DR, Greenblatt DJ, Shader RI. J Pharmacol Exp Ther. 1984 Jun;229(3):702-5. CIPROFLOXACIN Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism. [ PMID 15592331 ] Granfors MT, Backman JT, Neuvonen M, Neuvonen PJ. Clin Pharmacol Ther. 2004 Dec;76(6):598-606. FLUOROQUINOLONES The effect of ciprofloxacin on theophylline pharmacokinetics in healthy subjects. [ PMID 7619673 ] Batty K, Davis TME, Ilett KF, Dusci LJ, Langton SR. Br J Clin Pharmacol 1995;39(3):305-311. FLUVOXAMINE Fluvoxamine is a potent inhibitor of cytochrome P4501A2. [ PMID 8466541 ] Brosen K, Skjelbo E, Rasmussen BB, Poulsen HE, Loft S. Biochem Pharmacol 1993 Mar 24;45(6):1211-1214. Venlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYP1A2. [ PMID 9205822 ] Ball SE, Ahern D, Scatina J, Kao J. Br J Clin Pharmacol. 1997 Jun;43(6):619-26. Dose-dependent alternations in the pharmacokinetics of olanzapine during coadministration of fluvoxamine in patients with schizophrenia. [ PMID 15545309 ] Chiu CC, Lane HY, Huang MC, Liu HC, Jann MW, Hon YY, Chang WH, Lu ML. J Clin Pharmacol. 2004 Dec;44(12):1385-90. Cytochrome P450 1A2 is a major determinant of lidocaine metabolism in vivo: effects of liver function. [ PMID 14749694 ] Orlando R, Piccoli P, De Martin S, Padrini R, Floreani M, Palatini P. Clin Pharmacol Ther. 2004 Jan;75(1):80-8. Fluvoxamine-theophylline interaction: gap between in vitro and in vivo inhibition constants toward cytochrome P4501A2. [ PMID 11719727 ] Yao C, Kunze KL, Kharasch ED, Wang Y, Trager WF, Ragueneau I, Levy RH. Clin Pharmacol Ther. 2001 Nov;70(5):415-24. Effect of fluvoxamine on the pharmacokinetics of mexiletine in healthy Japanese men. [ PMID 11240973 ] Kusumoto M, Ueno K, Oda A, Takeda K, Mashimo K, Takaya K, Fujimura Y, Nishihori T, Tanaka K. Clin Pharmacol Ther. 2001 Mar;69(3):104-7. Fluvoxamine is a potent inhibitor of tacrine metabolism in vivo. [ PMID 10456487 ] Larsen JT, Hansen LL, Spigset O, Brøsen K. Eur J Clin Pharmacol. 1999 Jul;55(5):375-82. Influence of the CYP1A2 inhibitor fluvoxamine on tacrine pharmacokinetics in humans. [ PMID 9209244 ] Becquemont L, Ragueneau I, Le Bot MA, Riche C, Funck-Brentano C, Jaillon P. Clin Pharmacol Ther. 1997 Jun;61(6):619-27. FURAFYLLINE Furafylline is a potent and selective inhibitor of P4501A2 in man. [ PMID 2378786 ] Sesardic D, Boobis AR, Murray BP, Murray S, Segura J, de la Torre R, Davies DS. Br J Clin Pharmacol 1990;29:651-663 INTERFERON Regulation of hepatic cytochrome P-450 during infectious disease. [ PMID 1695539 ] Renton KW, Knickle LC Can J Physiol Pharmacol 1990 Jun;68(6):777-781 METHOXSALEN Specificity of substrate and inhibitor probes for cytochrome P450s: evaluation of in vitro metabolism using cDNA-expressed human P450s and human liver microsomes. [ PMID 8819299 ] Ono S, Hatanaka T, Hotta H, Satoh T, Gonzalez FJ, Tsutsui M. Xenobiotica. 1996 Jul;26(7):681-93. MIBEFRADIL Metabolism of the calcium antagonist, mibefradil (POSICOR,Ro40-5967). Part III. Comparative pharmacokinetics of mibefradil and its major metabolites in rat, marmoset, cynomolgus monkey and man. [ PMID 9211656 ] Wiltshire HR, Sutton BM, Heeps G, Betty AM, Angus DW, Harris SR, Worth E, Welker HA Xenobiotica 1997 Jun;27(6):557-571 1A2 INDUCERS:BROCCOLIEffects of dietary broccoli on human in vivo caffeine metabolism: a pilot study on a group of Jordanian volunteers. [ PMID 17266520 ] Hakooz N, Hamdan I. Curr Drug Metab. 2007 Jan;8(1):9-15. BRUSSEL SPROUTS 3,3-Diindolylmethane induces CYP1A2 in cultured precision-cut human liver slices. [ PMID 9741959 ] Lake BG, Tredger JM, Renwick AB, Barton PT, Price RJ. Xenobiotica. 1998 Aug;28(8):803-11. CHARGRILLED MEAT Effects of a chargrilled meat diet on expression of CYP3A, CYP1A, and P-glycoprotein levels in healthy volunteers. [ PMID 10381914 ] Fontana RJ, Lown KS, Paine MF, Fortlage L, Santella RM, Felton JS, Knize MG, Greenberg A, Watkins PB Gastroenterology 1999 Jul;117(1):89-98 INSULIN Hyperinsulinemia causes a preferential increase in hepatic P4501A2 activity. [ PMID 1562279 ] Barnett CR, Wilson J, Wolf CR, Flatt PR, Ioannides C Biochem Pharmacol 1992;43(6):1255-61 METHYLCHOLANTHRENE 3-Methylcholanthrene and pyridine effects on CYP1A1 and CYP1A2 expression in rat renal tissue. [ PMID 7493548 ] H Kim, S Reddy, RF Novak Drug Metab Dispos. 1995 Aug;23(8):818-24. Induction of CYP1A1, but not CYP1A2, in adrenals of 3, 3'-methylcholanthrene-treated guinea pigs. [ PMID 9637727] Black VH, Wang AF, Henry M, Shaw PM. Arch Biochem Biophys. 1998 Jun 15;354(2):197-205. MODAFINIL In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. [ PMID 10820139 ] Robertson P, DeCory HH, Madan A, Parkinson A. Drug Metab Dispos 2000 Jun;28(6):664-71 NAFCILLIN Interaction between warfarin and nafcillin: case report and review of the literature. [ PMID 10820139 ] Kim KY, Frey RJ, Epplen K, Foruhari F. Pharmacotherapy. 2007 Oct;27(10):1467-70. BETA-NAPHTHOFLAVONE Involvement of the CYP1A Subfamily in Stereoselective Metabolism of Carvedilol in beta-Naphthoflavone-Treated Caco-2 Cells. [ PMID 19252307 ] Ishida K, Taguchi M, Akao T, Hashimoto Y. Biol Pharm Bull. 2009 Mar;32(3):513-6. OMEPRAZOLE Increase of cytochrome P450IA2 activity by omeprazole: evidence by the 13C-[N-3-methyl]-caffeine breath test in poor and extensive metabolizers of S-mephenytoin. [ PMID 1505152 ] Rost KL, Brösicke H, Brockmöller J, Scheffler M, Helge H, Roots I. Clin Pharmacol Ther. 1992 Aug;52(2):170-80. TOBACCO Effect of smoking on caffeine clearance. [ PMID 657717 ] Parsons WD, Neims AH. Clin pharmacol Ther 1978;24(1):40-45 Assessment of the cytochrome P-448 dependent liver enzyme system by a caffeine breath test. [ PMID 6800827 ] Wietholz H, Voegelin M, Arnaud MJ, Bircher J, Preisig R Eur J Clin Pharmacol 1981;21:53-59 |



