Effects of intestinal and hepatic metabolism on the bioavailability of tacrolimus in rats

Pharmaceutical Research

Volumn 15, Issue 10, 1998, Pages 1609-1613

  Hashimoto, Yukiya ^a   Sasa, Hiroaki ^a   Shimomura, Masahiro ^a   Inui, Ken Ichi ^a  

^a KYOTO UNIVERSITY   (Japan)

Author keywords

Bioavailability; Intestine; Metabolism; Pharmacokinetics; Tacrolimus

Indexed keywords

IMMUNOSUPPRESSIVE AGENT; TACROLIMUS;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; FIRST PASS EFFECT; GRAFT REJECTION; INTRAVENOUS DRUG ADMINISTRATION; LIVER METABOLISM; MALE; NONHUMAN; PORTAL VEIN; PRIORITY JOURNAL; RAT;

ANIMALS; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 ENZYME SYSTEM; IMMUNOSUPPRESSIVE AGENTS; INTESTINES; LIVER; MALE; MIXED FUNCTION OXYGENASES; P-GLYCOPROTEIN; RATS; RATS, WISTAR; TACROLIMUS;

EID: 0031718440     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1011967519752     Document Type: Article

References (16)

1. R. Venkataramanan, A. Swaminathan, T. Prasad, A. Jain, S. Zuckerman, V. Warty, J. McMichael, J. Lever, G. Burckart, and T. Starzl. Clinical pharmacokinetics of tacrolimus. Clin. Pharmacokinet. 29:404-430 (1995).
2. M. Yasuhara, T. Hashida, M. Toraguchi, Y. Hashimoto, M. Kimura, K. Inui, R. Hori, Y. Inomata, K. Tanaka, and Y. Yamaoka. Pharmacokinetics and pharmacodynamics of FK 506 in pediatric patients receiving living-related donor liver transplantations. Transplant. Proc. 27:1108-1110 (1995).
3. H. Sasa, Y. Hashimoto, T. Shimizu, and K. Inui. Hepatic extraction of tacrolimus in rats with experimental liver diseases. Biol. Pharm. Bull. in press.
4. M. Sattler, F. P. Guengerich, C. Yun, U. Christians, and K. F. Sewing. Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Drug Metab. Dispos. 20:753-761 (1992).
5. J. C. Kolars, P. L. Stetson, B. D. Rush, M. J. Ruwart, P. Schmiedlin-Ren, E. A. Duell, J. J. Voorhees, and P. B. Watkins. Cyclosporine metabolism by P450IIIA in rat enterocytes - another determinant of oral bioavailability? Transplantation 53:596-602 (1992).
6. L. C. Floren, I. Bekersky, L. Z. Benet, Q. Mekki, D. Dressler, J. W. Lee, J. P. Roberts, and M. F. Hebert. Tacrolimus oral bioavailability doubles with coadministration of ketoconazole. Clin. Pharmacol. Ther. 62:41-49 (1997).
7. A. Lampen, U. Christians, A. K. Gonschior, A. Bader, I. Hackbarth, W. von Engelhardt, and K. F. Sewing. Metabolism of the macrolide immunosuppressant, tacrolimus, by the pig gut mucosa in the Ussing chamber. Br. J. Pharmacoi. 117:1730-1734 (1996).
8. T. H. Wilson and G. Wiseman. The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface. J. Physiol. 123:116-125 (1954).
9. F. C. Grenier, J. Luczkiw, M. Bergmann, S. Lunetta, M. Morrison, D. Blonski, K. Shoemaker, and M. Kobayashi. A whole blood FK 506 assay for the IMx® analyzer. Transplant. Proc. 23:2748-2749 (1991).
10. S. L. Beal and L. B. Sheiner. NONMEM Users Guide, University of California, San Francisco, 1992
11. N. Holtbecker, M. F. Fromm, H. K. Kroemer, E. E. Ohnhaus, and H. Heidemann. In vivo assessment of intestinal drug metabolism: Reply. Drug Metab. Dispos. 25:1110-1111 (1997).
12. K. S. Lown, R. R. Mayo, A. B. Leichtman, H. Hsiao, D. K. Turgeon, P. Schmiedlin-Ren, M. B. Brown, W. Guo, S. J. Rossi, L. Z. Benet, and P. B. Watkins. Role of intestinal P-glycoprotein (mdrl) in interpatient variation in the oral bioavailability of cyclosporine. Clin. Pharmacol. Ther. 62:248-260 (1997).
13. D. Y. Gomez, V. J. Wacher, S. J. Tomlanovich, M. F. Hebert, and L. Z. Benet. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin. Pharmacol. Ther. 58:15-19 (1995).
14. K. E. Thummel, D. O'Shea, M. F. Paine, D. D. Shen, K. L. Kunze, J. D. Perkins, and G. R. Wilkinson. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin. Pharmacol. Ther. 59:491-502 (1996).
15. M. F. Fromm, D. Busse, H. K. Kroemer, and M. Eichelbaum. Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin. Hepatology 24:796-801 (1996).
16. P. B. Watkins. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv. Drug Delivery Rev. 27:161-170 (1997).