First-pass metabolism of diltiazem in anesthetized rabbits: Role of extrahepatic organs

Pharmaceutical Research

Volumn 13, Issue 1, 1996, Pages 124-128

  Lefebvre, Marc ^b   Homsy, Walid ^b   Caillé, Gilles ^b   Du Souich, Patrick ^a  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b NONE

Author keywords

Diltiazem; First pass metabolism; Intestine; Liver; Lungs

Indexed keywords

DEACETYLDILTIAZEM; DILTIAZEM; DRUG METABOLIZING ENZYME;

ANESTHESIA; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BIOAVAILABILITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG METABOLISM; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; RABBIT;

ANESTHETICS; ANIMALS; ANTIHYPERTENSIVE AGENTS; CALCIUM CHANNEL BLOCKERS; DILTIAZEM; INJECTIONS, INTRAVENOUS; INTESTINE, SMALL; LUNG; MALE; RABBITS;

EID: 0029931772     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1016097805003     Document Type: Article

References (21)

1. M.M.T. Buckley, S. Grant, K.L. Goa, D. McTavish and E.M. Sorkin. Diltiazem; a reappraisal of its pharmacological properties and therapeutic use. Drugs 39:757-806 (1990).
2. M.S. Smith, C.P. Verghese, D.G. Shand and E.L.C. Pritchet. Pharmacokinetic and pharmacodynamic effects of diltiazem. Am. J. Cardiol. 51:1369-1374 (1983).
3. P.K.F. Yeung, S.J. Mosher, M.A. Quillam and T.J. Montague. Species comparison of pharmacokinetics and metabolism of diltiazem in humans, dogs, rabbits and rats. Drug Metab. Dispos. 18:1055-1059 (1990).
4. P.K.F. Yeung, S.J. Mosher and P.T. Pollak, Pharmacokinetics and metabolism of diltiazem in rabbits after a single intravenous or single oral administration. Eur. J. Drug Metab. Pharmacokin. 16:69-74 (1991).
5. J. Sugihara, Y. Sugawara, H. Ando, S. Harigaya, A. Etoh and K. Kohno. Studies on the metabolism of diltiazem in man. J. Pharmacobiodyn. 7:24-32 (1984).
6. J.R. Bend and C.J. Serabjit-Singh. Xenobiotic metabolism by extrahepatic tissues: relationship to target organ and cell toxicity, In JR. Mitchell and MG. Horning (eds.), Drug Metabolism and Drug Toxicity, Raven Press, New York, 1984, pp. 99-136.
7. M. Mistry and J.B. Houston. Quantitation of extrahepatic metabolism. Drug Metab. Dispos. 13:740-745 (1985).
8. H. Vainio and E. Hietanen. Role of extrahepatic metabolism in drug disposition and toxicity. In P. Jenner and B. Testa (eds.), Concepts in Drug Metabolism, part A, Marcel Dekker, New York, 1980, pp. 251-284.
9. M.K. Cassidy and J.B. Houston. In vivo capacity of hepatic and extrahepatic enzymes to conjugate phenol. Drug Metab. Dispos. 12:619-624 (1984).
10. L. Pichard, G. Gillet, I. Fabre, I. Dalet-Beluche, C. Bonfils, J.P. Thenot and P. Maurel. Identification of the rabbit and human cytochromes P-450IIIA as the major enzymes involved in the N-demethylation of diltiazem. Drug Metab. Dispos. 18:711-719 (1990).
11. D.R. Krishna and U. Klotz. Extrahepatic metabolism of drugs in humans. Clin. Pharmacokin. 26:144-160 (1994).
12. G. Caillé, L. Dubé, Y. Théorêt, F. Varin, N. Mousseau and I. McGilveray. Stability study of diltiazem and two of its metabolites using a high performance liquid chromatographic method. Biopharm. Drug Dispos. 10:107-114 (1989).
13. K.F. Ilett, L.B.G. Tee, PT. Reeves and R.F. Minchin. Metabolism of drugs and other xenobiotics in the gut lumen and wall. Pharmac. Ther. 46:67-93 (1990).
14. A.S.J. Koster, G.A. Hofman, A.C. Frankhuijzen-Sierevogel and J. Noordhoek. Presystemic and systemic intestinal metabolism of fenoterol in the conscious rat. Drug Metab. Dispos. 13:464-470 (1985).
15. S. Perreault, L. Dumont, V. Villière, H. Ong, A. Adam and P. du Souich. Hepatic and extrahepatic metabolism of salbutamol in anesthetized rabbits. Drug Metab. Dispos. 21:485-491 (1993).
16. G.M. Pacifici, M. Franchi, P.G. Gervasi, V. Longo, P. di Simplico, A. Temellini, and L. Giuliani. Profile of drug-metabolizing enzymes in human ileum and colon. Pharmacology 38:137-145 (1989).
17. W. Homsy, M. Lefebvre, G. Caillé and P. du Souich. Metabolism of diltiazem in hepatic and extrahepatic tissues of rabbits: in vitro studies. Pharmac. Res. 12:609-614 (1995).
18. 14C propranolol by the lung. Thorax 34:810-813 (1979).
19. D.L. Roerig, K.J. Kotrly, E.J. Vucins, S.B. Ahlf, C.A. Dawson, and J.P. Kampine. First-pass uptake of fentanyl, meperidine and morphine in the human lung. Anesthesiology 67:466-472 (1987).
20. A.G.E. Wilson, R.D. Pickett, T.E. Eling and M.W. Anderson. Studies on the persistence of basic amines in the rabbit lung. Drug Metab. Dispos. 7:420-424 (1979).
21. U.S. Ryan and C.J. Grantham. Metabolism of endogenous and xenobiotic substances by pulmonary vascular endothelial cells. Pharmac. Ther. 42:235-250 (1989).