Inhibitory effects of propafenone on the pharmacokinetics of caffeine in humans

Therapeutic Drug Monitoring

Volumn 28, Issue 6, 2006, Pages 779-783

  Michaud, Véronique ^a   Mouksassi, Mohamad Samer ^a   Labbé, Line ^a   Bélanger, Pierre Maxime ^b   Ferron, Liliane Ayotte ^c   Gilbert, Marcel ^b,c   Grech Bélanger, Odette ^b   Turgeon, Jacques ^a  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b UNIVERSITÉ LAVAL   (Canada)

^c LAVAL UNIVERSITY   (Canada)

Author keywords

Caffeine; CYP1A2; Drug drug interaction; Pharmacokinetics; Propafenone

Indexed keywords

ANTIARRHYTHMIC AGENT; CAFFEINE; CYTOCHROME P450 1A2; CYTOCHROME P450 2D6; PROPAFENONE; RHYTMOL;

ADULT; BLOOD SAMPLING; CLINICAL TRIAL; COMPETITIVE INHIBITION; CONFERENCE PAPER; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFECT; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG METABOLISM; ENZYME INHIBITION; HEART PROARRHYTHMIA; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PHARMACOLOGICAL PARAMETERS; PRIORITY JOURNAL; SINGLE DRUG DOSE; VOLUNTEER;

ADOLESCENT; ADULT; ANTI-ARRHYTHMIA AGENTS; CAFFEINE; CYTOCHROME P-450 CYP1A2; DRUG INTERACTIONS; HUMANS; MALE; PROPAFENONE;

EID: 33845714202     PISSN: 01634356     EISSN: None     Source Type: Journal    
DOI: 10.1097/01.ftd.0000249945.64978.33     Document Type: Conference Paper

References (47)

1. Bender AM, Donnerstein RL, Samson RA, et al. Hemodynamic effects of acute caffeine ingestion in young adults. Am J Cardiol. 1997;79:696-699.
2. Donnerstein RL, Zhu D, Samson R, et al. Acute effects of caffeine ingestion on signal-averaged electrocardiograms. Am Heart J. 1998;136:643-646.
3. Chopra A, Morrison L. Resolution of caffeine-induced complex dysrhythmia with procainamide therapy. J Emerg Med. 1995;13:113-117.
4. Zimmerman PM, Pulliam J, Schwengels J, et al. Caffeine intoxication: a near fatality. Ann Emerg Med. 1985;14:1227-1229.
5. Tang-Liu DD, Williams RL, Riegelman S. Disposition of caffeine and its metabolites in man. J Pharmacol Exp Ther. 1983;224:180-185.
6. Berthou F, Flinois JP, Ratanasavanh D, et al. Evidence for the involvement of several cytochromes P-450 in the first steps of caffeine metabolism by human liver microsomes. Drug Metab Dispos. 1991;19:561-567.
7. Grant DM, Tang BK, Kalow W. Polymorphic N-acetylation of a caffeine metabolite. Clin Pharmacol Ther. 1983;33:355-359.
8. Grant DM, Campbell ME, Tang BK, et al. Biotransformation of caffeine by microsomes from human liver. Kinetics and inhibition studies. Biochem Pharmacol. 1987;36:1251-1260.
9. Fuchs P, Haefeli WE, Ledermann HR, et al. Xanthine oxidase inhibition by allopurinol affects the reliability of urinary caffeine metabolic ratios as markers for N-acetyltransferase 2 and CYP1A2 activities. Eur J Clin Pharmacol. 1999;54:869-876.
10. Carrillo JA, Benitez J. Clinically significant pharmacokinetic interactions between dietary caffeine and medications. Clin Pharmacokinet. 2000;39:127-153.
11. Lelo A, Miners JO, Robson RA, et al. Quantitative assessment of caffeine partial clearances in man. Br J Clin Pharmacol. 1986;22:183-186.
12. Lelo A, Birkett DJ, Robson RA, et al. Comparative pharmacokinetics of caffeine and its primary demethylated metabolites paraxanthine, theobromine and theophylline in man. Br J Clin Pharmacol. 1986;22:177-182.
13. Tassaneeyakul W, Birkett DJ, McManus ME, et al. Caffeine metabolism by human hepatic cytochromes P450: contributions of 1A2, 2E1 and 3A isoforms. Biochem Pharmacol. 1994;47:1767-1776.
14. Kalow W, Tang BK. The use of caffeine for enzyme assays: a critical appraisal. Clin Pharmacol Ther. 1993;53:503-514.
15. Gu L, Gonzalez FJ, Kalow W, et al. Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1. Pharmacogenetics. 1992;2:73-77.
16. Tassaneeyakul W, Mohamed Z, Birkett DJ, et al. Caffeine as a probe for human cytochromes P450: validation using cDNA-expression, immunoinhibition and microsomal kinetic and inhibitor techniques. Pharmacogenetics. 1992;2:173-183.
17. Hege HG, Hollmann M, Kaumeier S, et al. The metabolic fate of 2H-labelled propafenone in man. Eur J Drug Metab Pharmacokinet. 1984;9:41-55.
18. Funck-Brentano C, Kroemer HK, Lee JT, et al. Propafenone. N Engl J Med. 1990;322:518-525.
19. Siddoway LA, Roden DM, Woosley RL. Clinical pharmacology of propafenone: pharmacokinetics, metabolism and concentration-response relations. Am J Cardiol. 1984;54:9D-12D.
20. Siddoway LA, Thompson KA, McAllister CB, et al. Polymorphism of propafenone metabolism and disposition in man: clinical and pharmacokinetic consequences. Circulation. 1987;75:785-791.
21. Kroemer HK, Mikus G, Kronbach T, et al. In vitro characterization of the human cytochrome P-450 involved in polymorphic oxidation of propafenone. Clin Pharmacol Ther. 1989;45:28-33.
22. Botsch S, Gautier JC, Beaune P, et al. Identification and characterization of the cytochrome P450 enzymes involved in N-dealkylation of propafenone: molecular base for interaction potential and variable disposition of active metabolites. Mol Pharmacol. 1993;43:120-126.
23. Tang BK, Zubovits T, Kalow W. Determination of acetylated caffeine metabolites by high-performance exclusion chromatography. J Chromatogr. 1986;375:170-173.
24. Campbell ME, Spielberg SP, Kalow W. A urinary metabolite ratio that reflects systemic caffeine clearance. Clin Pharmacol Ther. 1987;42:157-165.
25. Cheng WS, Murphy TL, Smith MT, et al. Dose-dependent pharmacokinetics of caffeine in humans: relevance as a test of quantitative liver function. Clin Pharmacol Ther. 1990;47:516-524.
26. Csajka C, Haller CA, Benowitz NL, et al. Mechanistic pharmacokinetic modelling of ephedrine, norephedrine and caffeine in healthy subjects. Br J Clin Pharmacol. 2005;59:335-345.
27. Joeres R, Klinker H, Heusler H, et al. Influence of smoking on caffeine elimination in healthy volunteers and in patients with alcoholic liver cirrhosis. Hepatology. 1988;8:575-579.
28. Renner E, Wietholtz H, Huguenin P, et al. Caffeine: a model compound for measuring liver function. Hepatology. 1984;4:38-46.
29. Heim M, Meyer UA. Genotyping of poor metabolisers of debrisoquine by allele-specific PCR amplification. Lancet. 1990;336:529-532.
30. Gaedigk A, Blum M, Gaedigk R, et al. Deletion of the entire cytochrome P450 CYP2D6 gene as a cause of impaired drug metabolism in poor metabolizers of the debrisoquine/sparteine polymorphism. Am J Hum Genet. 1991;48:943-950.
31. Mahgoub A, Idle JR, Smith RL. Genetically determined variability in drug metabolism: dual slow acetylation and drug oxidation traits. Lancet. 1979;2:154.
32. Lennard MS, Silas JH, Smith AJ, et al. Determination of debrisoquine and its 4-hydroxy metabolite in biological fluids by gas chromatography with flame-ionization and nitrogen-selective detection. J Chromatogr. 1977;133:161-166.
33. Evans DA, Mahgoub A, Sloan TP, et al. A family and population study of the genetic polymorphism of debrisoquine oxidation in a white British population. J Med Genet. 1980;17:102-105.
34. Christensen M, Tybring G, Mihara K, et al. Low daily 10-mg and 20-mg doses of fluvoxamine inhibit the metabolism of both caffeine (cytochrome P4501A2) and omeprazole (cytochrome P4502C19). Clin Pharmacol Ther. 2002;71:141-152.
35. Kim MK, Nightingale C, Nicolau D. Influence of sex on the pharmacokinetic interaction of fleroxacin and ciprofloxacin with caffeine. Clin Pharmacokinet. 2003;42:985-996.
36. Labbe L, Abolfathi Z, Robitaille NM, et al. Stereoselective disposition of the antiarrhythmic agent mexiletine during the concomitant administration of caffeine. Ther Drug Monit. 1999;21:191-199.
37. Healy DP, Polk RE, Kanawati L, et al. Interaction between oral ciprofloxacin and caffeine in normal volunteers. Antimicrob Agents Chemother. 1989;33:474-478.
38. Joeres R, Klinker H, Heusler H, et al. Influence of mexiletine on caffeine elimination. Pharmacol Ther. 1987;33:163-169.
39. Campbell ME, Grant DM, Inaba T, et al. Biotransformation of caffeine, paraxanthine, theophylline, and theobromine by polycyclic aromatic hydrocarbon-inducible cytochrome(s) P-450 in human liver microsomes. Drug Metab Dispos. 1987;15:237-249.
40. Kobayashi K, Nakajima M, Chiba K, et al. Inhibitory effects of antiarrhythmic drugs on phenacetin O-deethylation catalysed by human CYP1A2. Br J Clin Pharmacol. 1998;45:361-368.
41. Scott NR, Stambuk D, Chakraborty J, et al. The pharmacokinetics of caffeine and its dimethylxanthine metabolites in patients with chronic liver disease. Br J Clin Pharmacol. 1989;27:205-213.
42. Bryson HM, Palmer KJ, Langtry HD, et al. Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias. Drugs. 1993;45:85-130.
43. Shi J, Benowitz NL, Denaro CP, et al. Pharmacokinetic-pharmacodynamic modeling of caffeine: tolerance to pressor effects. Clin Pharmacol Ther. 1993;53:6-14.
44. Vozeh S, Haefeli W, Ha HR, et al. Nonlinear kinetics of propafenone metabolites in healthy man. Eur J Clin Pharmacol. 1990;38:509-513.
45. Labbe L, O'Hara G, Lefebvre M, et al. Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings. Clin Pharmacol Ther. 2000;68:44-57.
46. Cai WM, Chen B, Zhou Y, et al. Fluoxetine impairs the CYP2D6-mediated metabolism of propafenone enantiomers in healthy Chinese volunteers. Clin Pharmacol Ther. 1999;66:516-521.
47. Cai WM, Chen B, Cai MH, et al. The influence of CYP2D6 activity on the kinetics of propafenone enantiomers in Chinese subjects. Br J Clin Pharmacol. 1999;47:553-556.