Grapefruit juice-simvastatin interaction: Effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors

Clinical Pharmacology and Therapeutics

Volumn 64, Issue 5, 1998, Pages 477-483

  Lilja, Jari J ^a,b   Kivistö, Kari T ^a,b   Neuvonen, Pertti J ^a,b  

^a Helsinki University Central Hospital ^*

^b UNIVERSITY OF HELSINKI   (Finland)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOSPORIN; CYTOCHROME P450 ISOENZYME; ESTRADIOL; GESTODENE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; ITRACONAZOLE; LEVONORGESTREL; MIBEFRADIL; ORAL CONTRACEPTIVE AGENT; SIMVASTATIN;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG HALF LIFE; FEMALE; FOOD DRUG INTERACTION; FRUIT JUICE; HUMAN; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RADIOENZYMATIC ASSAY; RANDOMIZED CONTROLLED TRIAL;

EID: 0031741901     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(98)90130-8     Document Type: Article

References (20)

1. Bailey DG, Arnold JMO, Munoz C, Spence JD. Grapefruit-felodipine interaction: mechanism, predictability, and effect of naringin. Clin Pharmacol Ther 1993;53:637-42.
2. Bailey DG, Arnold JMO, Strong HA, Munoz C, Spence JD. Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther 1993;54:589-94.
3. Ducharme MP, Provenzano R, Dehoorne-Smith M. Edwards DJ. Trough concentrations of cyclosporine in blood following administration with grapefruit juice. Br J Clin Pharmacol 1993;36:457-9.
4. Kupferschmidt HHT, Ha HR, Ziegler WH, Meier PJ, Krähenbühl S. Interaction between grapefruit juice and midazolam in humans. Clin Pharmacol Ther 1995;58:20-8.
5. Benton RE, Honig PK, Zamani K, Cantilena LR, Woosley RL. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin Pharmacol Ther 1996;59:383-8.
6. Kantola T, Kivistö KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998;63:397-402.
7. Prueksaritanont T, Gorham LM, Ma B, Liu L, Yu X, Zhao JJ, et al. In vitro metabolism of simvastatin in humans: identification of metabolizing enzymes and effect of the drug on hepatic P450s. Drug Metab Dispos 1997;25: 1191-9.
8. Neuvonen PJ, Kantola T, Kivistö KT. Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole. Clin Pharmacol Ther 1998;63:332-41.
9. Manning JA, Swanson BN, Emaus NA, Fry J. A semi-automated, radioenzymatic assay for pravastatin and lovastatin in human serum [abstract]. Pharm Res 1989; 6:S237.
10. Horn M. Coadministration of itraconazole with hypolipidemic agents may induce rhabdomyolysis in healthy individuals [letter]. Arch Dermatol 1996;132:1254.
11. Meier C, Stey B, Brack T, Maggiorini M, Risti B. Krähenbühl S. Rhabdomyolysis in patients treated with simvastatin and cyclosporin: role of the hepatic cytochrome P450 enzyme system. Schweiz Med Wochenschr 1995; 125:1342-6.
12. Segaert MF, De Soete, Vandewiele I, Verbanck J. Drug-interaction-induced rhabdomyolysis. Nephrol Dial Transplant 1996;11:1846-7.
13. [Anonymous]. Worldwide labeled warning for mibefradil. Reactions 1997;681:2.
14. Ameer B, Weintraub RA. Drug interactions with grapefruit juice. Clin Pharmacokinet 1997;33:103-21.
15. Lown KS, Bailey DG, Fontana RJ, Janardan SK, Adair CH, Fortlage LA, et al. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest 1997; 99:2545-53.
16. Lundahl J, Regårdh CG, Edgar B, Johnsson G. Relationship between time of intake of grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy subjects. Eur J Clin Pharmacol 1995;49:61-7.
17. Vickers S, Duncan CA, Chen IW, Rosegay A, Duggan DE. Metabolic disposition studies on simvastatin, a cholesterol-lowering prodrug. Drug Metab Dispos 1990;18: 138-45.
18. Vickers S, Duncan CA, Vyas KP, Kari PH, Arison B, Prakash SR, et al. In vitro and in vivo biotransformation of simvastatin, an inhibitor of HMG CoA reductase. Drug Metab Dispos 1990;18:476-83.
19. Kivistö KT, Bookjans G, Fromm MF, Griese EU, Münzel P, Kroemer HK. Expression of CYP3A4, CYP3A5 and CYP3A7 in human duodenal tissue. Br J Clin Pharmacol 1996;42:387-9.
20. Kivistö KT, Kantola T, Neuvonen PJ. Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin. Br J Clin Pharmacol 1998;46:49-53.