Original Article
You have full text access to this OnlineOpen article
Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin
Article first published online: 30 DEC 2003
DOI: 10.1002/hep.510240407
Copyright © 1996 by the American Association for the Study of Liver Diseases
Additional Information
How to Cite
Fromm, M. F., Busse, D., Kroemer, H. K. and Eichelbaum, M. (1996), Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin. Hepatology, 24: 796–801. doi: 10.1002/hep.510240407
Publication History
- Issue published online: 30 DEC 2003
- Article first published online: 30 DEC 2003
References
- 1, , , , . Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J Clin Invest 1987; 80: 1029–1036.
- 2, , , , . Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J Clin Invest 1992; 90: 1871–1878.
- 3, , , , , , . et al. CYP3A gene expression in human gut epithelium. Pharmacogenetics 1994; 4: 247–259.
- 4, , , , , , . Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Drug Metab Dispos 1994; 22: 947–955.
- 5, , , , . Cytochrome P 450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues. J Pharmacol Exp Ther 1990; 253: 387–394.
- 6, . Extrahepatic metabolism of drugs in humans. Clin Pharmacokinet 1994; 26: 144–160.
- 7, , , . First-pass metabolism of cyclosporin by the gut. Lancet 1991; 338: 1488–1490.
- 8, , , . Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction. Clin Pharmacol Ther 1992; 52: 453–457.
- 9, , , , . The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin Pharmacol Ther 1995; 58: 15–19.
- 10, , , . Superiority of stable isotope techniques in the assessment of the bioavailability of drugs undergoing extensive first pass elimination. Eur J Clin Pharmacol 1981; 19: 127–131.
- 11, , , . Predictability of the in vivo metabolism of verapamil from in vitro data: contribution of individual metabolic pathways and stereoselective aspects. J Pharmacol Exp Ther 1992; 260: 1052–1057.
- 12, , , , , . Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol 1993; 348: 332–337.
- 13, , , , . Cytochromes of the P450 20 subfamily are the major enzymes involved in the O-demeth-ylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol 1995; 353: 116–121.
- 14, , , , . The effect of dextro-, levo-, and racemic verapamil on atrioventricular conduction in humans. Am Heart J 1985; 109: 210–217.
- 15, , . Effects of d, l-verapamil on atrioventricular conduction in relation to its stereoselective first-pass metabolism. Clin Pharmacol Ther 1985; 38: 71–76.
- 16, , . Update on rifampin drug interactions II. Arch Int Med 1992; 152: 711–716.
- 17, , , , . Tuberculosis in the United States. JAMA 1989; 262: 385–389.
- 18, , , . Reduction of bioavailability of verapamil by rifampin. N Engl J Med 1985; 312: 920–921.
- 19. Verapamil-rifampin interaction. Drug Intell Clin Pharm 1985; 19: 559–560.
- 20, , , , . Near-total reduction in verapamil bioavailability by rifampin. Chest 1988; 94: 954–959.
- 21, , , , . Simultaneous assessment of the intravenous and oral disposition of the enantiomers of racemic nimodipine by chiral stationary-phase high-performance liquid chromatography and gas chromatography-mass spectroscopy combined with a stable isotope technique. J Pharm Sci 1993; 82: 244–250.Direct Link:
- 22, , , , , . Interaction of verapamil and cimetidine: stereochemical aspects of drug metabolism, drug disposition and drug action. J Pharmacol Exp Ther 1990; 253: 1042–1048.
- 23, . Clinical Pharmacokinetics. Concepts and applications. Philadelphia: Lea & Febiger, 1995.
- 24, , , . Physiological disposition of verapamil in man. Cardiovasc Res 1976; 10: 1–8.
- 25, , , , , . The effect of age upon liver volume and apparent liver blood flow in healthy man. Hepatology 1989; 9: 297–301.Direct Link:
- 26, , , , . Pharmacokinetics, bioavailability and EGG response of verapamil in patients with liver cirrhosis. Br J Clin Pharmacol 1981; 12: 51–60.
- 27, , . Stereoselective protein binding of verapamil enantiomers. Biochem Pharmacol 1988; 37: 4623–4627.
- 28
- 29, , , . Hepatic blood flow and drug metabolism in patients on enzyme-inducing anticonvulsants. Eur J Clin Pharmacol 1982; 22: 441–445.
- 30, , , , , . Changes in antipyrine and indocyanine green kinetics during nifedipine, verapamil, and diltiazem therapy. Clin Pharmacol Ther 1986; 40: 239–242.
- 31, , , , , . Verapamil pharmacokinetics and apparent hepatic and renal blood flow. Br J Clin Pharmacol 1985; 20: 101–106.
- 32
- 33, , , , , . The effects of oral nifedipine on hepatic blood flow in humans. Clin Pharmacol Ther 1991; 50: 379–384.
- 34, , . Induction of cytochrome P450IA genes (CYP1A) by omeprazole in the human alimentary tract. Gastroenterology 1992; 103: 1509–1516.
- 35, , , , , , . Expression of cytochrome P-450 enzymes in cultured human hepatozytes. Eur J Biochem 1990; 191: 437–444.Direct Link:
- 36, . Biochemistry and molecular biology of the human CYP2C subfamily. Pharmacogenetics 1994; 4: 285–299.
- 37, , , , , . Pharmacokinetics of oral and intravenous rifampicin during chronic administration. Klin Wschr 1985; 63: 1205–1211.
- 38, , . Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 1995; 57: 485–491.
- 39, , , , , , . A potentially hazardous interaction between erythromycin and midazolam. Clin Pharmacol Ther 1993; 53: 298–305.
- 40, , , . Simultaneous determination of the intravenous and oral pharmacokinetic parameters of D,L-verapamil using stable isotope-labelled verapamil. Eur J Clin Pharmacol 1981; 19: 133–137.
- 41, , , . Direct determination of hepatic extraction of verapamil in cardiac patients. Clin Pharmacol Ther 1981; 30: 52–56.
- 42, , , , . Influence of mesocaval shunt surgery on verapamil kinetics, bioavailability and response. Brit J Clin Pharmacol 1980; 10: 527–530.
- 43. Nonchiral, homochiral and composite chiral drugs. Trends Pharmacol Sci 1993; 14: 68–75.
- 44, , , , , . An enantiomer-enantiomer interaction of (S)-and (R)-propafenone modifies the effect of racemic drug therapy. Circulation 1994; 89: 2396–2400.
- 45, , , , . Age-dependent stereoselective increase in the oral clearance of hexobarbitone isomers caused by rifampicin. Br J Clin Pharmacol 1991; 32: 735–739.
- 46, , . Urinary excretion of 6β-hy-droxycortisol and the time course measurement of enzyme induction in man. Eur J Clin Pharmacol 1989; 36: 39–46.
- 47, , , , , . Effect of corticosteroids on the expression of cytochromes P450 and on cyclosporin A oxidase activity in primary cultures of human hepatocytes. Mol Pharmacol 1992; 41: 1047–1055.

1527-3350/asset/olbannerleft.gif?v=1&s=4b2409f9534ed500d3c8da1940a23842e2b9932d)
1527-3350/asset/olbannerright.gif?v=1&s=141b9a8485298533c3e2016e937b0404f7d933e1)
1527-3350/asset/cover.gif?v=1&s=3cd983af6575c8dbfd6b47a63ffa95415ace15f8)