CYP3A4 and P-glycoprotein activity in healthy controls and transplant patients on cyclosporin vs. tacrolimus vs. sirolimus

American Journal of Transplantation

Volumn 4, Issue 9, 2004, Pages 1514-1522

  Lemahieu, W P D ^a   Maes, B D ^a   Verbeke, K ^a   Vanrenterghem, Y ^a  

^a UNIVERSITY HOSPITALS LEUVEN   (Belgium)

Author keywords

Calcineurin inhibitors; CYP3A4; P glycoprotein; Sirolimus

Indexed keywords

ACETYLSALICYLIC ACID; AMINOPHENAZONE; AMLODIPINE; ATENOLOL; ATORVASTATIN; BISOPROLOL; CANDESARTAN; CIMETIDINE; CORTICOSTEROID; CYCLOSPORIN; CYCLOSPORIN A; CYTOCHROME P450 3A4; ENALAPRIL; ERYTHROMYCIN; ETHINYLESTRADIOL; GLYCOPROTEIN P; HYDRALAZINE; INTESTINE ENZYME; LISINOPRIL; LIVER ENZYME; LOSARTAN; MYCOPHENOLIC ACID 2 MORPHOLINOETHYL ESTER; OMEPRAZOLE; PERINDOPRIL; RANITIDINE; RAPAMYCIN; TACROLIMUS; TERAZOSIN; UNINDEXED DRUG; WARFARIN;

ADULT; AMINOPYRIN BREATH TEST; ARTICLE; BREATH ANALYSIS; CLINICAL ARTICLE; CONTROL GROUP; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG INTERACTION; ENZYME ACTIVITY; ERYTHROMYCIN BREATH TEST; ERYTHROMYCIN URINE TEST; FEMALE; HUMAN; IMMUNOSUPPRESSIVE TREATMENT; KIDNEY TRANSPLANTATION; MAINTENANCE THERAPY; MALE; NORMAL HUMAN; PRIORITY JOURNAL; URINALYSIS;

CYCLOSPORINE; CYTOCHROME P-450 ENZYME SYSTEM; FEMALE; HUMANS; IMMUNOSUPPRESSIVE AGENTS; KIDNEY TRANSPLANTATION; LIVER; MALE; MIDDLE AGED; P-GLYCOPROTEIN; REFERENCE VALUES; SIROLIMUS; TACROLIMUS;

EID: 4344656740     PISSN: 16006135     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1600-6143.2004.00539.x     Document Type: Article

References (30)

1. Lo A, Burckart GJ. P-glycoprotein and drug therapy in organ transplantation. J Clin Pharmacol 1999; 39: 995-1005.
2. Lampen A, Christians U, Guengerich FP et al. Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions and interindividual variability. Drug Metab and Dispos 1995; 23: 1315-1324.
3. Sattler M, Guengerich FP, Yun C, Christians U, Sewing KF. Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and Rapa in man and rat. Drug Metab and Dispos 1992; 20: 753-761.
4. Christians U, Jacobsen W, Benet LZ, Lampen A. Mechanisms of Clinically Relevant Drug Interactions Associated with Tacrolimus. Clin Pharmacokinet 2002; 41: 813-851.
5. Kelly PA, Wang H, Napoli BD, Kahan BD, Strobel HW. Metabolism of cyclosporine by cytochromes P450 3A9 and 3A4. Eur J of Drug Metab and Pharmacokinet 1999; 24: 321-328.
6. Plosker GL, Foster RH. Tacrolimus: a further update of its pharmacology and therapeutic use in the management of organ transplantation. Drugs 2000; 59: 323-389.
7. Wandel C, Kim RB, Kajiji S, Guengerich P, Wilkinson GR, Wood AJJ. P-glycoprotein and Cytochrome P-450 Inhibition: Dissociation of Inhibitory Potencies. Cancer Res 1999; 59: 3944-3948.
8. Yacyshyn BR, Bowen-Yacyshyn MB, Pilarski LM. Inhibition by Rapa of P-glycoprotein 170-mediated export from normal lymphocytes. Scand J Immunol 1996; 43: 449-455.
9. Achira M, Suzuki H, Ito K, Sugiyama Y. Comparative Studies to Dermine the Selective Inhibitors for P-Glycoprotein and Cytochrome P4503A4. AAPS PharmSci 2001; 1: 18.
10. Kusus M, Stapleton DD, Lertora JJ, Simon EE, Dreisbach AW. Rhabdomyolysis and acute renal failure in a cardiac transplant recipient due to multiple drug interactions. Am J Med Sci 2000; 320: 394-397.
11. Park JW, Siekmeier R, Lattke P et al. Pharmacokinetics and pharmacodynamics of fluvastatin in heart transplant recipients taking cyclosporin A. J Cardiovasc Pharmacol Ther 2001; 6: 351-361.
12. Fisher GA, Sikic BI. Clinical studies with modulators of multidrug resistance. Hematol/oncol Clin North Am 1995; 9: 363-383.
13. Meerum Terwogt JM, Malingre MM, Beijnen JH et al. Co-administration of oral cyclosporin A enables oral therapy with paclitaxel. Clin Cancer Res 1999; 5: 3379-3384.
14. Lemahieu W, Maes B, Vanrenterghem Y, Rutgeerts P, Verbeke K, Ghoos Y. Measurement of hepatic and intestinal CYP3A4 and P-glycoprotein activity by means of a combined po and iv, C14 Erythromycin breath and urine test. Am J Physiol 2003; 285: 470-482.
15. Ghoos YF, Maes B, Geypens BJ et al. Measurement of gastric emptying rate of solids by means of a carbon labeled octanoic breath test. Gastroenterology 1993; 104: 1640-1647.
16. Maes B, Geypens BJ, Ghoos YF, Hiele MI, Rutgeerts PJ. 13C-Octanoic acid breath test for gastric emptying rate of solids. Gastroenterology 1998; 114: 856-859.
17. Maes BD, Mys G, Geypens BJ, Evenepoel P, Ghoos Y, Rutgeerts PJ. Gastric emptying flow curves separated from carbon-labeled octanoic acid breath test results. Am J Physiol 1998; 275: 169-175.
18. Irving CS, Schoeller DA, Nakamura KI, Baker AL, Klein PD. The aminopyrin breath test as a measure of liver function. J Lab Clin Med 1982; 100: 3563-3573.
19. Mion F, Queneau PE, Rousseau M, Brazier JL. Paliard, Minaire Y. Aminopyrin Breath Test: development of a 13C-breath test for quantitative assessment of liver function in humans. Hepatogastroenterology 1995; 42: 931-938.
20. Lan LB, Dalton JT, Schuetz EG. Mdrl limits CYP3A metabolism in vivo. Mol Pharmacol 2000; 58: 863-869.
21. Xie W, Barwick JL, Downes M et al. Humanized xenobiotic response in mice expressing nuclear receptor SXR. Nature 2000; 406: 435-439.
22. Tanaka E, Breimer DD. In vivo function tests of hepatic drug-oxidizing capacity in patients with liver disease. J Clinical Pharm Ther 1997; 22: 237-249.
23. Watkins PB. Drug metabolism by cytochromes P450 in the liver and small bowel. Gastrointestinal Pharmacol 1992; 23: 511-525.
24. Schmider J, Brockmöller J, Arold G, Bauer S, Roots I. Simultaneous assessment of CYP3A4 and CYP1A2 activity in vivo with alprazolam and caffeine. Pharmacogenetics 1999; 9: 725-734.
25. Ichimaru N, Takahara S, Kokado Y et al. Changes in lipid metabolism and effect of simvastatin in renal transplant recipients induced by cyclosporine or tacrolimus. Atherosclerosis 2001; 158: 417-423.
26. Van Gelder T, Klupp J, Barten MJ, Christians U, Morris RE. Co-administration of tacrolimus and mycophenolate mofetil does not increase mycophenolic acid (MPA) exposure, but co-administration of cyclosporin inhibits the enterohepatic recirculation of MPA, thereby decreasing its exposure. J Heart Lung Transplant 2001; 20: 160-161.
27. McAlister VC, Mahalati K, Peltekian KM, Fraser A, MacDonald AS. A Clinical pharmacokinetic study of tacrolimus and sirolimus combination immunosuppression comparing simultaneous to separated administration. Ther Drug Monit 2002; 24: 346-350.
28. Nielsen FT, Ottosen P, Starklint H et al. Kidney function and morphology after short-term combination therapy with cyclosporine A, tacrolimus and sirolimus in the rat. Nephrol Dial Transplant 2003; 18: 491-496.
29. Maes B, Lemahieu W, Kuypers D et al. Differential effect of diarrhea on FK 506 versus Cyclosporin A trough levels and resultant prevention of allograft rejection in renal transplant recipients. Am J Transplant 2002; 2: 989-992.
30. Chowbay B, Cumaraswamy S, Cheun YB et al. Genetic polymorphisms in MDR1 and CYP3A4 genes in Asians and the influence of MDR1 haplotypes on cylcosporin disposition in heart transplant recipients. Pharmacogenetics 2003; 13: 89-95.