Concomitant clotrimazole therapy more than doubles the relative oral bioavailability of tacrolimus

Therapeutic Drug Monitoring

Volumn 27, Issue 5, 2005, Pages 587-591

  Vasquez, Eva M ^a   Shin, Grace P ^a   Sifontis, Nicole ^a   Benedetti, Enrico ^a  

^a UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

Author keywords

Clotrimazole; Drug interaction; Tacrolimus

Indexed keywords

CLOTRIMAZOLE; CYTOCHROME P450 3A4; TACROLIMUS;

ADULT; ANTIFUNGAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL ARTICLE; CONCENTRATION RESPONSE; CREATININE BLOOD LEVEL; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG CROSS REACTIVITY; DRUG INDUCED HEADACHE; FEMALE; GRAFT REJECTION; HUMAN; IMMUNOSUPPRESSIVE TREATMENT; KIDNEY GRAFT; KIDNEY TRANSPLANTATION; MALE; PRECIPITATION; PRIORITY JOURNAL;

ADULT; ANTI-INFECTIVE AGENTS, LOCAL; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CLOTRIMAZOLE; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; DRUG MONITORING; FEMALE; HUMANS; IMMUNOSUPPRESSIVE AGENTS; KIDNEY TRANSPLANTATION; MALE; MIDDLE AGED; TACROLIMUS;

EID: 26444597593     PISSN: 01634356     EISSN: None     Source Type: Journal    
DOI: 10.1097/01.ftd.0000151186.91464.7c     Document Type: Article

References (28)

1. Sattler M, Guengerich FP, Yun CH, et al. Cytochrome P4503A enzymes are responsible for biotransformation of FK 506 and rapamycin in man and rat. Drug Metab Dispos. 1992;20:753-761.
2. Vincent SH, Karanam BV, Painter SK, et al. In vitro metabolism of FK-506 in rat, rabbit, and human liver microsomes: identification of major metabolites and of cytochrome P450 3A as the major enzymes responsible for its metabolism. Arch Biochem Biophys. 1992;294:454-460.
3. Saeki T, Ueda K, Tanigawara Y, et al. Human P-glycoprotein transports cyclosporine and FK506. J Biol Chem. 1993;268:6077-6080.
4. Jenson C, Jordan M, Shapiro R, et al. Interaction between tacrolimus and erythromycin (letter). Lancet. 1994;28:280-281.
5. Shaeffer MS, Collier D, Sorrell MF. Interaction between FK 506 and clarithromycin in a renal transplant patient. Eur J Clin Pharmacol. 1994;47:207-208.
6. Furlan V, Perello L, Jacquemin E, et al. Interactions between FK 506 and rifamycin or erythromycin in pediatric liver recipients. Transplantation. 1995;59:1217-1218.
7. Assa R, Fredi G, Larger E, et al. FK 506/fluconazole interaction enhances FK 506 nephrotoxicity. Diabete Metab. 1994;20:49-52.
8. Furlan V, Parquin F, Penaud J, et al. Interaction between tacrolimus and itraconazole in a heart-lung transplant recipient. Transplant Proc. 1998;30:187-188.
9. Osowski CL, Dix SP, Lin LS, et al. Evaluation of the drug interaction between intravenous high-dose fluconazole and cyclosporine or tacrolimus in bone marrow transplant patients. Transplantation. 1996;61:1268-1272.
10. Paterson DL, Singh N. Interactions between tacrolimus and antimicrobial agents. Clin Infect Dis. 1997;25:1430-1440.
11. Mieles L, Venkataramanan R, Yokoyama I, et al. Interaction between FK 506 and clotrimazole in a liver transplant recipient. Transplantation. 1991;52:1086-1087.
12. Vasquez EM, Pollak R, Benedetti E. Clotrimazole increases tacrolimus blood levels: a drug interaction in kidney transplant recipients. Clin Transplant. 2001;15:95-99.
13. Spatzenegger M, Jaeger W. Clinical importance of hepatic cytochrome P450 in drug metabolism. Drug Metab Rev. 1995;27:397-417.
14. Jusko WJ, Piekoszewski W, Klintmalm GB, et al. Pharmacokinetics of tacrolimus in liver transplant patients. Clin Pharmacol Ther. 1995;57:281-290.
15. Gruber SA, Hewitt JM, Sorenson AL, et al. Pharmacokinetics of FK506 after intravenous and oral administration in patients awaiting renal transplantation. J Clin Pharmacol. 1994;34:859-864.
16. Venkataramanan R, Swaminathan A, Prasad T, et al. Clinical pharmacokinetics of tacrolimus. Clin Pharmacokinet. 1995;29:404-430.
17. Gibbs MA, Kunze KL, Howald WN, et al. Effect of inhibitor depletion on inhibitory potency: tight binding inhibition of CYP3A by clotrimazole. Drug Metab Dispos. 1999;27:596-599.
18. 1 values and impact of CYP3A5 expression. Drug Metab Dispos. 1999;27:180-187.
19. Pichard L, Fabre I, Fabre G, et al. Cyclosporin A drug interactions: screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and liver microsomes. Drug Metab Dispos. 1990;18:595-606.
20. Seo M, Iida H, Miura Y. Basic experiments with clotrimazole administered orally. Curr Med Res Opin. 1977;5:169-178.
21. Floren LC, Bekersky I, Benet LZ, et al. Tacrolimus oral bioavailability doubles with coadministration of ketoconazole. Clin Pharmacol Ther. 1997;62:41-49.
22. Watkins PB. Drug metabolism by cytochrome P450 in the liver and small bowel. Gastroenterol Clin North Am. 1992;21:511-526.
23. Gomez DY, Wacher VJ, Tomlanovich SJ, et al. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin Pharmacol Ther. 1995;58:15-19.
24. Kolars JC, Stetson PL, Rush BD, et al. Cyclosporine metabolism by P450IIIA in rat enterocytes-another determinant of oral bioavailability? Transplantation. 1992;53:596-602.
25. Kolars JC, Awni WM, Merion RM, et al. First-pass metabolism of cyclosporin by the gut. Lancet. 1991;338:1488-1490.
26. Lampen A, Christians U, Gonschior A, et al. Metabolism of the macrolide immunosuppressant tacrolimus by the pig gut mucosa in the Ussing chamber. Br J Pharmacol. 1996;117:1730-1734.
27. Kaplan B, Lown K, Craig R, et al. Low bioavailability of cyclosporine microemulsion and tacrolimus in a small bowel transplant recipient. Transplantation. 1999;67:333-338.
28. Lown KS, Mayo RR, Leichtman AB, et al. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther. 1997;62:248-260.