Effect of diltiazem on cyclosporine metabolites through blood concentrations after Sandimmun® and Neoral® in renal transplant patients;DER EINFLUSS VON DILTIAZEM AUF DIE KONZENTRATION VON CYCLOSPORIN-METABOLITEN BEI MIT SANDIMMUN UND NEORAL BEHANDELTEN NIERENTRANSPLANTIERTEN PATIENTEN

Medizinische Klinik

Volumn 92, Issue 10, 1997, Pages 589-596

  Sperschneider, Heide ^a   Wagner, Constanze ^a   Korn, Alexander ^b   Christians, Uwe ^c  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

^b Novartis AG   (Germany)

^c UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

Cyclosporin Metabolism; Diltiazem; Neoral ; Renal transplantation; Sandimmun

Indexed keywords

CALCIUM ANTAGONIST; CALCIUM CHANNEL BLOCKING AGENT; CYCLOSPORIN; CYCLOSPORIN A; DILTIAZEM; DRUG METABOLITE; NIFEDIPINE;

ARTICLE; BLOOD; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG METABOLISM; FEMALE; GRAFT REJECTION; HUMAN; KIDNEY TRANSPLANTATION; MAJOR CLINICAL STUDY; MALE; RANDOMIZED CONTROLLED TRIAL;

EID: 0030859616     PISSN: 07235003     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF03044784     Document Type: Article

References (37)

1. Aoyama, T , S. Yamano, D. J. Waxman, D. P. Lapenson, U. A. Meyer, V. Fischer, R. Tyndale, T. Inaba, W. Kalow, H. V. Gelboin, F. J. Gonzalez: Cytochrome P-450hPCN3, a novel cytochrome P-450IIIA gene product that is differentially expressed in adult human liver J biol Chem. 264 (1989), 10388-10395.
2. Benet, L. Z., C. Y. Wu, M F Herbert, V. J. Wacher: Intestinal drug metabolism and antitransport processes: a potential paradigm shift in oral drug delivery. J. contr. Release 39 (1996), 139-143.
3. Brockmöller, J., H.-H. Neumayer, K. Wagner, W. Weber, G Heinemeyer, H. Kewitz, I Roots: Pharmacokinetic interaction between cyclosporin and diltiazem. Europ. J clin Pharmacol. 38 (1990), 237-242
4. Chang, T , L Z. Benet, M. F Herbert The effect of water soluble vitamine E on cyclosporine pharmacokinetics in healthy volunteers Clin Pharmacol. Ther 59 (1996), 297-303.
5. Christians, U , K O. Zimmer, K Womgeit, G. Maurer, K F. Sewing: Liquid-chromatographic measurement of cyclosporin A and its metabolites in blood, bile and urine Clin. Chem 34 (1988), 34-39
6. Christians, U., K. Kohlhaw, J. Budniak, J. S, Bleck, R. Schottmann, H. J. Schlitt, V. M. F. Almeida, M. Deters, K. Wonigeit, R. Pichlmayr, K. F. Sewing: Ciclosporin metabolite pattern in blood and urine of liver graft recipients. I. Association of ciclosporin metabolites with nephrotoxicity. Europ. J. clin. Pharmacol. 41 (1991), 285-290.
7. Christians, U., J. S. Bleck, A. Lampen, A. Bader, C. Thiesemann, V. Kliem, H, Repp, M. Westhoff-Bleck, M. Manns, K. F. Sewing: Are cytochrome P450 enzymes in the small intestine responsible for different cyclosporine metabolite patterns in stable male and female renal allograft recipients after co-administration of Diltiazem? Transplant. Proc. 28 (1996), 2159-2216.
8. Christians, U., L. C. Floren, G. Kirchner, K. F. Sewing: The clinical pharmacokinetics of macrolide immunosuppressants and its impact on the clinical management of organ transplantation. Transplantationsmedizin (im Druck).
9. Combalbert, J., I. Fabre, G. Fabre, I. Dalet, J. Derancourt, J. P. Cano, P. Mautel: Metabolism of cyclosporin A: IV. Purification and identification of the rifampicin inducible human liver cytochrome P-450 (cyclosporin A oxidase) as a product of P-450 IIIA gene subfamily. Drug Metab. Dispos. 17 (1989), 197-207.
10. Consensus Document: Hawk's Cay Meeting on Therapeutic Drug Monitoring of Cyclosporine Transplant. Proc. 22 (1990), 1357-1361.
11. Copeland, K. R., R. W. Yatscoff, R. M. McKenna: Immunosuppressive activity of cyclosporine metabolites compared and characterized by mass spectroscopy and nuclear magnetic resonance. Clin. Chem. 36 (1990), 225-229.
12. Fahr, A., P. Hiestand, B. Ryffel: Studies on the biologic activities of sandimmun metabolites in humans and in animal models: review and original experiments. Transplant. Proc. 22 (1990), 1116-1124
13. Ferguson, C. J., J. D. Williams, A. N. Hillis, D. Parry-Jones, J. R. Salaman: Effects of the calcium channel blocker diltiazem on cyclosporine nephrotoxicity in renal transplant patients. Clin. Transplant. 6 (1992), 391-398.
14. Freed, B. M., T. G. Rosano, N. Lempert: In vitro immunosuppressive properties of cyclosporine metabolites. Transplantation 43 (1987), 123-127.
15. Freed, B. M., J. A Bennett, T. G. Rosano, C. A. Brooks, S. M. Cramer, N. Lempert: Assessment of the in vivo immunosuppressive activity of the major cyclosporine metabolite by leukemia allograft rejection. Transplantation 53 (1992), 456-460.
16. Guengerich, F. P., M. V Martin, P. H. Beaune, P. Kremers, T. Wolff, D. J Waxman: Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. J. biol. Chem. 261 (1986), 5051-5060.
17. Hebert, M. F., J. P. Roberts, T. Prueksaritanont, L. Benet: Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction. Clin. Pharmacol. Ther. 52 (1992), 453-457.
18. Kolars, J. C , W. M. Awni, R. M. Merion, P. B. Watkins: First-pass metabolism of cyclosporin by the gut. Lancet 338 (1991), 1488-1490.
19. Kolars, J. C., K. S. Lown, P. Schmiedlin-Ren, M. Ghosh, C. Fang, S. A. Wrighton, R. M Merion, P. B. Watkins: CYP3A gene expression in human gut epithelium. Pharmacogenetics 4 (1994), 247-259.
20. Kovarik, J. M , L Vernillet, E. A. Müller, R. Freiburghaus, W Niederberger, K. Kutz: Cyclosporine disposition and metabolite profiles in renal transplant patients recerving a microemulsion formulation. Ther. Drug Monit. 16 (1994), 519-525.
21. Kovarik, J. M., E. A. Müller, J. B. van Bree, W. Tetzloff, K. Kutz. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J. pharm. Sci. 83 (1994), 444-446.
22. Kunzendorf, U., J. Brockmöller, F. Jochimsen, I. Roots, G. Offermann: Activity of cyclosporin metabolites M17 and M1. Transplant. Proc 22 (1990), 1697-1699.
23. Kunzendorf, U., G. Walz, J. Brockmöller, H.-H. Neumayer, F. Jochimsen, I. Roots, G Offermann, T. B. Strom. Effects of diltiazem upon metabolism and immuno-suppressive action of cyclosporine in kidney graft recipients Transplantation 52 (1991), 280-284.
24. Lampen, A., U. Christians, A. Bader, I. Hackbarth, K. F. Sewing: Drug interactions and interindividual variability of ciclosporin metabolism in the small intestine. Pharmacology 52 (1996), 159-168.
25. Lucey, M. R., J. C. Kolars, R. M. Merion, D. A Campbell, M. Aldrich, P. B. Watkins: Cyclosporin toxicity at therapeutic blood levels and cytochrome P450IIIA. Lancet 335 (1990), 11-15
26. Macdonald, P , A. Keogh, J Connell, A, Harvison, D. Richens, P Spratt Diltiazem co-administration reduces cyclosporine toxicity after heart transplantation: a prospective randomised study Transplant. Proc. 24 (1992), 2259-2262.
27. Morales, J. M., A. Andres, E. Rodriguez-Paternina, J. M. Alcazar, C Montoyo, L. Rodicio Calcium antagonist therapy prevents chronic cyclosporine nephrotoxicity after renal transplantation: a prospective study. Transplant. Proc 24 (1992), 89-91.
28. Muller, E. A., J. M. Kovarik, J B. van Bree, W. Tezloff, J. Grevel, K Kutz: Improved dose-linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharrn. Res. 11 (1994), 301-304.
29. Nagineni, C N , B. C. Misra, D B. N. Lee, N. Yanagawa. Cyclosporine A-calcium channels interaction : a possible mechanism for nephrotoxicity. Transplant Proc. 19 (1987), 1358-1362.
30. Neumayer, H.-H., Prävention des akuten Transplantatversagens nach Nierentransplantation durch Calciumantagonisten und Prostaglandine Mitt. Arbeitsgemeinsch. klin Nephrol 18 (1989), 1-35.
31. Pichard, L , I. Fabre, G. Fabre, J. Domergue, B. S Aubert, G. Mourad, P, Maurel: Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. Drug Metab. Dispos 18 (1990), 595-606.
32. Pichard, L , G. Gillet, I. Fabre, I. Dalet-Beluche, C. Bonfils, J -P. Thenot, P Maurel: Identification of the rabbit and human cytochromes P-450IIIA as the major enzymes involved in the N-demethylation of diltiazem Drug Metab. Dispos 18 (1990), 711-719.
33. Schlitt, H. J , U. Christians, K. Wonigeit, K. F. Sewing, R Pichlmayr. Immuno-suppressive activity of cyclosporine metabolites in vitro. Transplant. Proc. 19 (1987), 4248-4251.
34. Thiesemann, C.: Emfluß von Diltiazem auf die Metabolisterung und Elimination von Ciclosporin bei nieren-transplantierten Patienten. Inaug.-Dissertarion, Med. Hochschule Hannover 1996.
35. Wacher, V. J , C Y. Wu, L. Z Benet Overlapping substrate specifities and tissue distribution of cytochrome P450 3A and p-glycoprotein. Implications for drug delivery and activity in cancer chemotherapy. Molec. Carcinogen, 13 (1995), 129-134.
36. Wagner, K., M Henkel, G. Heinemeyer, H.-H Neumayer Interaction of calcium blockers and cyclosporine. Transplant. Proc 20 (1988), 561-568
37. Wagner, K , T. Philipp, G Heinemeyer, F. Brockmüller, I Roots, H.-H. Neumayer. Interaction of cyclosporin and calcium antagonists Transplant. Proc. 21 (1989), 1453-1456.