References for Cytochrome P450 Drug Interaction Table: 1A2

These pages contain all the literature citations referenced in the Cytochrome P450 Drug Interaction Tables (both the extensive research-oriented table and the concise clinical table). Most of these citations are hyperlinks, which bring up the abstract in the NLM's PubMed database.

Click on the [ PubMed ] link after the drug name to perform a live MedLINE search of articles possibly related to that drug and Cytochrome P450.

Entries are organized by mode of activity (substrate, inhibitor, inducer) within specific isoform. You can quickly branch to a section by clicking on the appropriate link here:

1A2 | 2B6 | 2C8 | 2C19 | 2C9 | 2D6 | 2E1 | 3A457

Use Ctrl-F to find all or part of the name or word for which you are searching.




1A2 SUBSTRATES



» AMITRIPTYLINE [ PubMed ]
ArticleFluvoxamine-tricyclic antidepressant interaction. An accidental finding.
AuthorsBertschy G, Vandel S, Vandel B, Allers G, Volmat R
Link to AbstractEur J Clin Pharmacol 1991;40(1):119-120.
Infowww.rxlist.com

amitriptyline: PubMed

Fluvoxamine-tricyclic antidepressant interaction. An accidental finding.
Bertschy G, Vandel S, Vandel B, Allers G, Volmat R
Eur J Clin Pharmacol 1991;40(1):119-120. [Letter]

caffeine: PubMed

Determination of urinary metabolites of caffeine for the assessment of cytochrome P4501A2, xanthine oxidase, and N-acetyltransferase activity in humans.
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.
Tang BK, Kalow W
Methods Enzymol 1996;272:124-131

clomipramine: PubMed

Fluvoxamine-tricyclic antidepressant interaction. An accidental finding.
Bertschy G, Vandel S, Vandel B, Allers G, Volmat R
Eur J Clin Pharmacol 1991;40(1):119-120. [Letter]

clozapine: PubMed

Metabolism and bioactivation of clozapine by human liver in vitro.
Pirmohamed, M., Williams, D., Madden, S., Templeton, E., and Park, B.K
J Pharmacol Exp Ther 272(3):984-990, 1995

Clozapine disposition covaries with CYP1A2 activity determined by a caffeine test.
Bertilsson, L., Carrillo, J.A., Dahl, M.-L., Llerena, A., Alm, C., Bondesson, U., Lindstrom, L., de la Rubia, I.R., Ramos, S., and Benitez, J
Br J Clin Pharmacol 38:471-473, 1994

cyclobenzaprine: PubMed

Identification of Human Liver Cytochrome P450 Isoforms involved in the in vitro metabolism of cyclobenzaprine.
Wang RW, Liu L, Cheng H
Drug Metab Dispos 1996;24(7):786-791

fluvoxamine: PubMed

Disposition of fluvoxamine in humans is determined by the polymorphic CYP2D6 and also by the CYP1A2 activity.
Carillo JA, Dahl M-L, Svennson J-O, Alm C, Rodriguez I, Bertillson L
Clin Pharmacol Ther 1996;60:183-190

estradiol: PubMed

Differences in the cytochrome P-450 isoenzymes involved in the 2-hydroxylation of oestradiol and 17alpha-ethinyloestradiol.
Ball, S.E., Forrester, L.M., Wolf, C.R., and Back, D.J
Biochem J 267:221-226, 1990

haloperidol: PubMed

Coadministration of fluvoxamine increases serum concentrations of haloperidol.
Daniel, D.G., Randolph, C., Jaskiw, G., Handel, S., Williams, T., Abi-Dargham, A., Shoaf, S., Egan, M., Elkashef, A., Liboff, S., and Linnoila, M
J Clin Psychopharmacol 14:340-343, 1994

imipramine: PubMed

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.
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.
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: PubMed

CYP1A2 is the major enzyme involved in the metabolism of mexillitene in man.
Abolfathi Z, Pakdel H, Beaune P, Turgeon J
Clin Pharmacol Ther 1995;57(2):215 Abst.

Ciprofloxacin decreases mexillitene (mex) clearance in smokers and non-smokers.
Labbe L, Lefez C, Gilbert M, O'Hara G, Turgeon J
Clin Pharmacol Ther 1995;57:210 Abst.

naproxen: PubMed

Cytochromes P450, 1A2, and 2C9 are responsible for the human hepatic O-demethylation of R- and S-naproxen.
Miners JO, Coulter S, Tukey RH, Veronese ME, Birkett DJ
Biochem Pharmacol 1996 Apr 26;51(8):1003-1008

olanzapine PubMed

ondansetron (in part): PubMed

Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans.
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: PubMed

Specificity of substrate and inhibitor probes for human cytochromes P450 1A1 and 1A2.
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

propranolol: PubMed

Selective induction of propranolol metabolism by smoking: Additional effects on renal clearance of metabolites.
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.
Benfield, P and Ward A
Drugs 1986;32:313-334
[Fluvoxamine is a potent inhibitor of propranolol metabolism in vivo.]

riluzole: PubMed

Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitro.
Sanderink GJ, Bournique B, Stevens J, Petry M, Martinet M
J Pharmacol Exp Ther 1997 Sep;282(3):1465-1472

ropivacaine: PubMed

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.
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: PubMed

Determination of human hepatic cytochrome P450 1A2 activity in vitro: use of tacrine as an isozyme-specific probe.
Spaldin V, Madden S, Adams DA, Edwards RJ, Davies DS, Park BK
Drug Metab Dispos 1995;23(9):929-934

theophylline: PubMed

Metabolism of theophylline by cDNA-expressed human cytochromes P450.
Ha HR, Chen J, Freiburghaus AU, Follath F
Br J Clin Pharmacol 1995;39:321-326

tizanidine PubMed

Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism.
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.
Granfors MT, Backman JT, Neuvonen M, Ahonen J, Neuvonen PJ.
Clin Pharmacol Ther. 2004 Apr;75(4):331-41

verapamil: PubMed

The effect of three different oral doses of verapamil on the disposition of theophylline.
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.
Nielsen-Kudsk JE, Buhl JS, Johannessen AC
Pharmacol Toxicol 1990 Feb;66(2):101-103

warfarin: PubMed

zileuton: PubMed

Identification of the human liver cytochrome P450 enzymes involved in the metabolism of zileuton (ABT-077) and its N-dehydroxylated metabolite, Abbott-66193.
Machinist JM, Mayer MD, Shet MS, Ferrero JL, Rodrigues AD
Drug Metab Dispos. 1995 Oct; 23(10): 1163-1174

zolmitriptan: Pubmed

Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan.
Wild MJ, McKillop D, Butters CJ
Xenobiotica. 1999 Aug;29(8):847-57



1A2 INHIBITORS



» AMIODARONE [ PubMed ]
ArticleInhibitory effects of antiarrhythmic drugs on phenacetin O-deethylation catalysed by human CYP1A2.
AuthorsKobayashi K, Nakajima M, Chiba K, Yamamoto T, Tani M, Ishizaki T, Kuroiwa Y.
Link to AbstractBr J Clin Pharmacol 1998 Apr;45(4):361-368.
Infowww.rxlist.com

» CIMETIDINE [ PubMed ]
ArticleThe effect of cimetidine on dextromethorphan O-demethylase activity of human liver microsomes and recombinant CYP2D6.
AuthorsMadeira M, Levine M, Chang TK, Mirfazaelian A, Bellward GD.
Link to AbstractDrug Metab Dispos. 2004 Apr;32(4):460-7.

ArticleComparative in vitro and in vivo inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists.
AuthorsMartínez C, Albet C, Agúndez JA, Herrero E, Carrillo JA, Márquez M, Benítez J, Ortiz JA.
Link to AbstractClin Pharmacol Ther. 1999 Apr;65(4):369-76.

ArticleImipramine-cimetidine interaction: impairment of clearance and enhanced absolute bioavailability.
AuthorsAbernethy DR, Greenblatt DJ, Shader RI.
Link to AbstractJ Pharmacol Exp Ther. 1984 Jun;229(3):702-5.

Infowww.rxlist.com

» CIPROFLOXACIN [ PubMed ]
ArticleCiprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism.
AuthorsGranfors MT, Backman JT, Neuvonen M, Neuvonen PJ.
Link to AbstractClin Pharmacol Ther. 2004 Dec;76(6):598-606.
Infowww.rxlist.com

» FLUOROQUINOLONES [ PubMed ]
ArticleThe effect of ciprofloxacin on theophylline pharmacokinetics in healthy subjects.
AuthorsBatty K, Davis TME, Ilett KF, Dusci LJ, Langton SR.
Link to AbstractBr J Clin Pharmacol 1995;39(3):305-311.
Infowww.rxlist.com

» FLUVOXAMINE [ PubMed ]
ArticleFluvoxamine is a potent inhibitor of cytochrome P4501A2.
AuthorsBrosen K, Skjelbo E, Rasmussen BB, Poulsen HE, Loft S.
Link to AbstractBiochem Pharmacol 1993 Mar 24;45(6):1211-1214.

ArticleVenlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYP1A2.
AuthorsBall SE, Ahern D, Scatina J, Kao J.
Link to AbstractBr J Clin Pharmacol. 1997 Jun;43(6):619-26.

ArticleDose-dependent alternations in the pharmacokinetics of olanzapine during coadministration of fluvoxamine in patients with schizophrenia.
AuthorsChiu CC, Lane HY, Huang MC, Liu HC, Jann MW, Hon YY, Chang WH, Lu ML.
Link to AbstractJ Clin Pharmacol. 2004 Dec;44(12):1385-90.

ArticleCytochrome P450 1A2 is a major determinant of lidocaine metabolism in vivo: effects of liver function.
AuthorsOrlando R, Piccoli P, De Martin S, Padrini R, Floreani M, Palatini P.
Link to AbstractClin Pharmacol Ther. 2004 Jan;75(1):80-8.

ArticleFluvoxamine-theophylline interaction: gap between in vitro and in vivo inhibition constants toward cytochrome P4501A2.
AuthorsYao C, Kunze KL, Kharasch ED, Wang Y, Trager WF, Ragueneau I, Levy RH.
Link to AbstractClin Pharmacol Ther. 2001 Nov;70(5):415-24.

ArticleEffect of fluvoxamine on the pharmacokinetics of mexiletine in healthy Japanese men.
AuthorsKusumoto M, Ueno K, Oda A, Takeda K, Mashimo K, Takaya K, Fujimura Y, Nishihori T, Tanaka K.
Link to AbstractClin Pharmacol Ther. 2001 Mar;69(3):104-7.

ArticleFluvoxamine is a potent inhibitor of tacrine metabolism in vivo.
AuthorsLarsen JT, Hansen LL, Spigset O, Brøsen K.
Link to AbstractEur J Clin Pharmacol. 1999 Jul;55(5):375-82.

ArticleInfluence of the CYP1A2 inhibitor fluvoxamine on tacrine pharmacokinetics in humans.
AuthorsBecquemont L, Ragueneau I, Le Bot MA, Riche C, Funck-Brentano C, Jaillon P.
Link to Abstract Clin Pharmacol Ther. 1997 Jun;61(6):619-27.

Infowww.rxlist.com

furafylline: PubMed

Furafylline is a potent and selective inhibitor of P4501A2 in man.
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: PubMed

Regulation of hepatic cytochrome P-450 during infectious disease
Renton KW, Knickle LC
Can J Physiol Pharmacol 1990 Jun;68(6):777-781

methoxsalen: PubMed

mibefradil: PubMed

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.
Wiltshire HR, Sutton BM, Heeps G, Betty AM, Angus DW, Harris SR, Worth E, Welker HA
Xenobiotica 1997 Jun;27(6):557-571

ticlopidine: PubMed

Ticlopidine-theophylline interaction.
Colli A, Buccino G, Cocciollo M, Parravicini R, Elli GM, Scaltrini G
Clin Pharmacol Ther 1987; 41: 358-362


broccoli: PubMed

brussel sprouts: PubMed

char-grilled meat: PubMed

Effects of a chargrilled meat diet on expression of CYP3A, CYP1A, and P-glycoprotein levels in healthy volunteers.
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: PubMed

Hyperinsulinemia causes a preferential increase in hepatic P4501A2 activity.
Barnett CR, Wilson J, Wolf CR, Flatt PR, Ioannides C
Biochem Pharmacol 1992;43(6):1255-61

methyl cholanthrene: PubMed

modafinil: Info  PubMed

In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil.
Robertson P, DeCory HH, Madan A, Parkinson A.
Drug Metab Dispos 2000 Jun;28(6):664-71

nafcillin: PubMed

beta-naphthoflavone: PubMed

omeprazole: PubMed

tobacco: PubMed

Effect of smoking on caffeine clearance.
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.
Wietholz H, Voegelin M, Arnaud MJ, Bircher J, Preisig R
Eur J Clin Pharmacol 1981;21:53-59

Updated: 09/2003