Concomitant use of cytochrome P450 3A4 inhibitors and simvastatin

American Journal of Cardiology

Volumn 84, Issue 7, 1999, Pages 811-815

  Gruer, Peter J K ^a   Vega, Jose M ^a   Mercuri, Michele F ^a   Dobrinska, Michael R ^a   Tobert, Jonathan A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; CYCLOSPORIN; CYTOCHROME P450 3A4; CYTOCHROME P450 INHIBITOR; CYTOCHROME P450 ISOENZYME; DILTIAZEM; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; PRAVASTATIN; SIMVASTATIN; UNCLASSIFIED DRUG; VERAPAMIL;

ARTICLE; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG METABOLISM; DRUG POTENCY; DRUG POTENTIATION; DRUG RESEARCH; DRUG SAFETY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; MAJOR CLINICAL STUDY; METABOLIC INHIBITION; MYOPATHY; PRIORITY JOURNAL;

ADVERSE DRUG REACTION REPORTING SYSTEMS; CALCIUM CHANNEL BLOCKERS; DRUG INTERACTIONS; HUMANS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; RHABDOMYOLYSIS; SIMVASTATIN;

EID: 0032886788     PISSN: 00029149     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0002-9149(99)00442-7     Document Type: Article

References (25)

1. Thummel K.E., Wilkinson G.R. In vitro and in vivo drug interactions involving human CYP3A. Annu Rev Pharmacol Toxicol. 38:1998;389-430.
2. US Product Circular Zocor (simvastatin) tablets . 1998;Merck & Co., Inc, West Point, PA.
3. Kantola T., Kivisto K., Neuvonen P. Erythromycin and verapamil considerably increase simvastatin and simvastatin acid concentrations. Clin Pharmacol Ther. 64:1998;177-182.
4. Azie N.E., Brater C., Becker P.A., Jones D.R., Hall S.D. The interaction of diltiazem with lovastatin and pravastatin. Clin Pharmacol Ther. 64:1998;369-377.
5. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease the Scandinavian Simvastatin Survival Study (4S) . Lancet. 344:1994;1383-1389.
6. Pedersen T.R., Berg K., Cook T.J., Faergeman O., Haghfelt T., Kjekshus J., Musliner T.A., Olsson A.G., Pyorala K., Thorgeirsson G., Tobert J.A., Wedel H., Wilhelmsen L. Safety and tolerability of cholesterol lowering with simvastatin during 5 years in the Scandinavian Simvastatin Survival Study. Arch Intern Med. 156:1996;2085-2092.
7. MRC/BHF Heart Protection Study of cholesterol-lowering therapy and of antioxidant vitamin supplementation in a wide range of patients at increased risk of coronary heart disease death early safety and efficacy experience . Eur Heart J. 20:1999;725-741.
8. Evans SJW, Waller P, Davis S. Proportional reporting ratios: the uses of epidemiological methods for signal generation. Pharmacoepidemol Drug Saf 1998(suppl 2):5102.
9. Davis S, Evans S, Wark S, Wood S. Signal generation: procedures for identification evaluation and tracking (abstr). Pharmacoepidemiol Drug Saf 1998;(suppl 2):S97.
10. Vickers S., Duncan C.A., Chen I.-W., Rosegay A., Duggan D.E. Metabolic disposition studies on simvastatin, a cholesterol-lowering prodrug. Drug Metab Dispos. 18:1990;138-145.
11. Pentikainen P.J., Saraheimo M., Schwartz J.I., Amin R.D., Schwartz M.S., Brunner Ferber F., Rogers J.D. Comparative pharmacokinetics of lovastatin, simvastatin and pravastatin in humans. J Clin Pharmacol. 32:1992;136-140.
12. Prueksaritanont T., Gorham L.M., Ma B., Liu L., Yu X., Zhao J.J., Slaughter D.E., Arison B.H., Vyas K.P. In vitro metabolism of simvastatin in humans identification of metabolizing enzymes and effect of the drug on hepatic P450s . Drug Metab Dispos. 25:1997;1191-1199.
13. Stubbs R.J., Schwartz M.S., Gerson R.J., Thornton T.J., Bayne W.F. Comparison of plasma profiles of lovastatin (mevinolin), simvastatin (epistatin), and pravastatin (eptastatin) in the dog. Drug Invest. 2:(suppl. 2):1990;18-28.
14. Christians U., Jacobsen W., Floren L.C. Metabolism and drug interactions of 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors in transplant patients are the statins mechanistically similar? Pharmacol Therap. 80:1998;1-34.
15. Neuvonen P.J., Kantola T., Kivisto K.T. Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole. Clin Pharmacol Ther. 63:1998;332-341.
16. Wang R.W., Kari P.H., Lu A.Y.H., Thomas P.E., Guengerich F.P., Vyas K.P. Biotransformation of lovastatin. IV. Identification of cytochrome P450 3A proteins as the major enzymes responsible for the oxidative metabolism of lovastatin in rat and human liver microsomes. Arch Biochem Biophys. 290:1991;355-361.
17. Yang B.-B., Siedlik P.H., Smithers J.A., Sedman A.J., Stern R.H. Atorvastatin pharmacokinetic interactions with other cyp3a4 sustrates; erythromycin and ethinyl estradiol. (abstr) Pharmaceut Res. 13:1996;S437.
18. Boberg M., Angerbauer R., Fey P., Kanhai W.K., Karl W., Kern A., Ploschke J., Radtke M. Metabolism of cerivastatin by human liver microsomes in vitro characterization of primary metabolic pathways and of cytochrome P450 isozymes involved . Drug Metab Dispos. 25:1997;321-331.
19. Vega JM, Prueksaritanont T, Rogers JD, Gagliano K, Greenberg H, Osborne B, Brucker MJ, McLoughlin D, Wong PH, Waldman SA. Simvastatin does not inhibit CYP3A4, quantified by the oral midazolam hydroxylation test, in healthy male volunteers (abstr). Abstracts of the 13th International Symposium on Drugs Affecting Lipid Metabolism, Florence, Italy, May 30-June 3, 1998, 1998:128.
20. Vega J.M., Gagliano K., Gillen L., Greenberg H., Osborne B., Wong P.H., Waldman S.A. Simvastatin does not inhibit CYP3A4, quantified by the erythromycin breath test (EBT), in healthy male volunteers. (abstr) Clin Pharmacol Ther. 63:1998;11-21.
21. Regazzi M.B., Iacona I., Campana C., Raddato V., Lesi C., Perani G., Gavazzi A., Vigano M. Altered disposition of pravastatin following concomitant drug therapy with cyclosporin A in transplant recipients. Transplant Proc. 25:1993;2732-2734.
22. Olbricht C., Wanner C., Eisenhauer T., Kliem V., Doll R., Boddaert M., O'Grady P., Krekler M., Mangold B., Christians U. Accumulation of lovastatin, but not pravastatin, in the blood of cyclosporine-treated kidney graft patients after multiple doses. Clin Pharmacol Ther. 62:1997;311-321.
23. Barbir M., Rose M., Kushwaha S., Akl S., Mitchell A., Yacoub M. Low-dose simvastatin for the treatment of hypercholesterolaemia in recipients of cardiac transplantation. Int J Cardiol. 33:1991;241-246.
24. Vanhaecke J., Van Cleemput J., Van Lierde J., Daenen W., De Geest H. Safety and efficacy of low dose simvastatin in cardiac transplant recipients treated with cyclosporine. Transplantation. 58:1994;42-45.
25. Pflugfelder P.W., Huff M., Oskalns R., Rudas L., Kostuk W.J. Cholesterol-lowering therapy after heart transplantation a 12-month randomized trial . J Heart Lung Transplant. 14:1995;613-622.