Tacrolimus oral bioavailability doubles with coadministration of ketoconazole

Clinical Pharmacology and Therapeutics

Volumn 62, Issue 1, 1997, Pages 41-49

  Floren, Leslie C ^b   Bekersky, Ihor ^b   Benet, Leslie Z ^b   Mekki, Qais ^b   Dressier, Dawna ^b   Lee, Jean W ^b   Roberts, John P ^b   Hebert, Mary F ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

ANTIFUNGAL AGENT; KETOCONAZOLE; PYRROLE; TACROLIMUS;

ADULT; ARTICLE; BIOAVAILABILITY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG ELIMINATION; ENZYME LINKED IMMUNOSORBENT ASSAY; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; PRIORITY JOURNAL; VOLUNTEER;

ADMINISTRATION, ORAL; ADULT; ANTIFUNGAL AGENTS; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 ENZYME SYSTEM; FEMALE; HUMANS; IMMUNOSUPPRESSIVE AGENTS; KETOCONAZOLE; MALE; MIXED FUNCTION OXYGENASES; P-GLYCOPROTEIN; TACROLIMUS;

EID: 0030742705     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(97)90150-8     Document Type: Article

References (38)

1. Venkataramanan R, Swaminathan A, Prasad T, Jain A, Zuckerman S, Warty V, et al. Clinical pharmacokinetics of tacrolimus. Clin Pharmacokinet 1995;29: 404-30.
2. Kelly PA, Burckart GJ, Venkataramanan R. Tacrolimus: a new immunosuppressive agent. Am J Health Syst Pharm 1995;52:1521-35.
3. Jensen C, Jordan M, Shapiro R, Scantlebury V, Hakala T, Fung J, et al. Interaction between tacrolimus and erythromycin [letter]. Lancet 1994;344:825.
4. Manez R, Martin M, Raman D, Silverman D, Jain A, Warty V, et al. Fluconazole therapy in transplant recipients receiving FK506. Transplantation 1994;57: 1521-3.
5. Hebert MF, Roberts JP, Prueksaritanont T, Benet LZ. Unavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction. Clin Pharmacol Ther 1992;52:453-7.
6. Gomez DY, Wacher VJ, Tomlanovich SJ, Hebert MF, Benet LZ. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin Pharmacol Ther 1995;58:15-9.
7. Wu CY, Benet LZ, Hebert MF, Gupta SK, Rowland M, Gomez DY, et al. Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine. Clin Pharmacol Ther 1995; 58:492-7.
8. Wacher VJ, Wu CY, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P-450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinog 1995;13:129-34.
9. Siegsmund MJ, Cardarelli C, Aksentijevich I, Sugimoto Y, Pastan I, Gottesman MM. Ketoconazole effectively reverses multi-drug resistance in highly resistant KB cells. J Urol 1994;151:485-91.
10. Arceci RJ, Stieglitz K, Bierer BE. Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype. Blood 1992;80:1528-36.
11. Subrahmanyeswara Rao U, Scarborough GA. Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein. Mol Pharmacol 1994;45:773-6.
12. Naito M, Oh-hara T, Yamazaki A, Danki T, Tsuruo T. Reversal of multidrug resistance by an immunosuppressive agent FK-506. Cancer Chemother Pharmacol 1992;29:195-200.
13. Mekki Q, Lee C, Carrier S, Klintmalm G, Schaefer M, Burke P, et al. The effect of food on oral bioavailability of tacrolimus (FK506) in liver transplant patients [abstract]. Clin Pharmacol Ther 1993;53:229.
14. Dressier D, Bekersky I, Lee J, Tracewell WG, Kisicki J, Mekki Q. Effect of meal time on tacrolimus bioavailability [abstract]. Clin Pharmacol Ther 1996;59: 151.
15. Lee JW, Sukovaty RL, Farmen RH, Dressler DE, Alak A, Bekersky I. Tacrolimus (FK506): validation of a sensitive enzyme-linked immunosorbent assay kit for and application to a clinical pharmacokinetic study. Ther Drug Monit 1997;19:201-7.
16. Pascucci VL, Bennett J, Narang PK, Chatterji DC. Quantitation of ketoconazole in biological fluids using high-performance liquid chromatography. J Pharm Sci 1983;72:1467-9.
17. Benet LZ, Galeazzi RL. Noncompartmental determination of the steady-state volume of distribution. J Pharm Sci 1979;68:1071-4.
18. Sattler M, Guengerich FP, Yun CH, Christians U, Sewing KF. Cytochrome P450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Drug Metab Dispos 1992;20: 753-61.
19. Vincent SH, Karanam BV, Painter SK, Chiu SH. In vitro metabolism of FK506 in rat, rabbit, and human liver microsomes: identification of a major metabolite and of cytochrome P450 3A as the major enzymes responsible for its metabolism. Arch Biochem Biophys 1992;294:454-60.
20. Benet LZ, Wu CY, Hebert MF, Wacher VJ. Intestinal drug metabolism and antitransport processes: a potential paradigm shift in oral drug delivery. J Control Rel 1996;39:139-43.
21. Christians U, Kruse C, Kowanatzki R, Schiebel HM, Schwinzer R, Sattler M, et al. Measurement of FK506 by HPLC and isolation and characterization of its metabolites. Transplant Proc 1991;23:940-1.
22. Christians U, Radeke HH, Kownatzki R, Schiebel HM, Schottmann R, Sewing KF. Isolation of an immunosuppressive metabolite of FK506 generated by human microsome preparations. Clin Biochem 1991; 24:271-5.
23. Kolars JC, Lown KS, Schmiedlin-Ren P, Ghosh M, Fang C, Wrighton SA, et al. CYP3A gene expression in human gut epithelium. Pharmacogenetics 1994;4: 247-59.
24. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT, Guzelian PS. Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J Clin Invest 1987;80:1029-36.
25. Iwasaki K, Matsuda H, Nagase K, Shiraga T, Tokuma Y, Uchida K. Effects of twenty-three drugs on the metabolism of FK506 by human liver microsomes. Res Commun Chem Pathol Pharmacol 1993;82:209-16.
26. Lampen A, Christians U, Gonschior A, Bader A, Hackbarth I, von Engelhardt W, et al. Metabolism of the macrolide immunosuppressant tacrolimus by the pig gut mucosa in the Ussing chamber. Br Pharmacol 1996;117:1730-4.
27. Leveque D, Jehl F. P-glycoprotein and pharmacokinetics. Anticancer Res 1995;15:331-6.
28. Sugawara I, Kataoka I, Morishita Y, Hamada H, Tsuruo T, Itoyama S, et al. Tissue distribution of P-glycoprotein encoded by multidrug-resistant gene as revealed by a monoclonal antibody, MRK16. Cancer Res 1988;48:1926-9.
29. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, Willingham MC. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc Natl Acad Sci USA 1987; 84:7735-8.
30. Saeki T, Ueda K, Tanigawara Y, Hori R, Komano T. Human P-glycoprotein transports cyclosporine and FK506. J Biol Chem 1993;268:6077-80.
31. Kolars JC, Stetson PL, Rush BD, Ruwart MJ, Schmiedlin-Ren P, Duell EA, et al. Cyclosporine metabolism by P450IIIA in rat enterocytes - another determinant of bioavailability? Transplantation 1992;53: 596-602.
32. Labroo RB, Thummel KE, Kunze KL, Podoll T, Trager WF, Kharasch ED. Catalytic role of cytochrome P450 3A4 in multiple pathways of alfentanil metabolism. Drug Metab Dispos 1995;23:490-6.
33. Newton DJ, Wang RW, Lu AYH. Cytochrome P450 inhibitors: evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab Dispos 1995;23:154-8.
34. Jusko WJ, Piekoszewski W, Klintmalm GB, Shaefer MS, Hebert MF, Piergies AA, et al. Pharmacokinetics of tacrolimus in liver transplant patients. Clin Pharmacol Ther 1995;57:281-90.
35. Gruber SA, Hewitt JM, Sorenson AL, Barber DL, Bowers L, Rynders G, et al. Pharmacokinetics of FK506 after intravenous and oral administration in patients awaiting renal transplantation. J Clin Pharmacol 1994;34:859-64.
36. Osowski CL, Dix SP, Lin LS, Mullins RE, Geller RB, Wingard JR. Evaluation of the drug interaction between intravenous high-dose fluconazole and cyclosporine or tacrolimus in bone marrow transplant patients. Transplantation 1996;61:1268-72.
37. Gonschior AK, Christians U, Winkler M, Schiebel HM, Linck A, Sewing KF. Simplified high-performance liquid chromatography-mass spectrometry assay for measurement of tacrolimus and its metabolites and cross-validation with microparticulate enzyme immunoassay. Ther Drug Monit 1995;17:504-10.
38. Tokunaga Y, Alak AM. FK506 (tacrolimus) and its immunoreactive metabolites in whole blood of liver transplant patients and subjects with mild hepatic dysfunction. Pharm Res 1996;13:137-40.