Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1987 Sep;24(3):329–334. doi: 10.1111/j.1365-2125.1987.tb03177.x

Cyclosporin-phenytoin interaction: re-evaluation using metabolite data.

M Rowland 1, S K Gupta 1
PMCID: PMC1386254  PMID: 3663449

Abstract

1 Freeman et al. (1984) evoked enzyme induction to explain the lower plasma concentration of cyclosporin following phenytoin co-administration in man. 2 We have examined the whole blood concentration data of two metabolites of cyclosporin, as well as unchanged drug, all measured by h.p.l.c., associated with the above mentioned study. 3 Phenytoin produced no significant effect on either the terminal half-life of both metabolites or the ratio of area under the concentration-time curve of metabolite to parent drug. 4 These data strongly suggest that phenytoin reduces the absorption of cyclosporin; they do not generally support the idea that phenytoin induces cyclosporin metabolism.

Full text

PDF
329

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Carstensen H., Jacobsen N., Dieperink H. Interaction between cyclosporin A and phenobarbitone. Br J Clin Pharmacol. 1986 May;21(5):550–551. doi: 10.1111/j.1365-2125.1986.tb02843.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Crow J. W., Gibaldi M., Levy G. Comparative pharmacokinetics of coumarin anticoaglulants XLI: Effect of phenobarbital on systemic availability of orally administered dicumarol in rats. J Pharm Sci. 1979 Aug;68(8):958–962. doi: 10.1002/jps.2600680811. [DOI] [PubMed] [Google Scholar]
  3. Freeman D. J., Laupacis A., Keown P. A., Stiller C. R., Carruthers S. G. Evaluation of cyclosporin-phenytoin interaction with observations on cyclosporin metabolites. Br J Clin Pharmacol. 1984 Dec;18(6):887–893. doi: 10.1111/j.1365-2125.1984.tb02560.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Jamali F., Axelson J. E. Griseofulvin---phenobarbital interaction: a formulation-dependent phenomenon. J Pharm Sci. 1978 Apr;67(4):466–470. doi: 10.1002/jps.2600670406. [DOI] [PubMed] [Google Scholar]
  5. Keown P. A., Laupacis A., Carruthers G., Stawecki M., Koegler J., McKenzie F. N., Wall W., Stiller C. R. Interaction between phenytoin and cyclosporine following organ transplantation. Transplantation. 1984 Sep;38(3):304–306. [PubMed] [Google Scholar]
  6. Klaassen C. D. Studies on the increased biliary flow produced by phenobarbital in rats. J Pharmacol Exp Ther. 1971 Mar;176(3):743–751. [PubMed] [Google Scholar]
  7. Lemaire M., Tillement J. P. Role of lipoproteins and erythrocytes in the in vitro binding and distribution of cyclosporin A in the blood. J Pharm Pharmacol. 1982 Nov;34(11):715–718. doi: 10.1111/j.2042-7158.1982.tb06206.x. [DOI] [PubMed] [Google Scholar]
  8. Maurer G., Loosli H. R., Schreier E., Keller B. Disposition of cyclosporine in several animal species and man. I. Structural elucidation of its metabolites. Drug Metab Dispos. 1984 Jan-Feb;12(1):120–126. [PubMed] [Google Scholar]
  9. Putcha L., Nandiwada P., Feldman S., Bruckner J. V., Kramer W. G. Effect of heptabarbital on bioavailability of bishydroxycoumarin in the rat. Res Commun Chem Pathol Pharmacol. 1978 Jan;19(1):67–74. [PubMed] [Google Scholar]
  10. Riegelman S., Rowland M., Epstein W. L. Griseofulvin-phenobarbital interaction in man. JAMA. 1970 Jul 20;213(3):426–431. [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES