| Effects of regular consumption of grapefruit juice on the pharmacokinetics of simvastatin. | |
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MedLine Citation:
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PMID: 15206993 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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AIMS: Simvastatin, a substrate for CYP3A4, is extensively metabolized during the first pass. Our aim was to investigate the effect of regular consumption of grapefruit juice on the pharmacokinetics of simvastatin. METHODS: In a randomized cross-over study with two phases, 10 healthy volunteers ingested grapefruit juice 200 ml or water (control) for 3 days. On day 3, a single 40-mg dose of simvastatin was administered with grapefruit juice 200 ml or water. Plasma concentrations of simvastatin and simvastatin acid were determined up to 24 h. RESULTS: Grapefruit juice increased the area under the plasma concentration-time curves from 0 to 24 h [AUC(0-24)] of simvastatin 3.6-fold (range 1.8-6.0-fold; P < 0.01) and that of simvastatin acid 3.3-fold (range 2.1-5.6-fold; P < 0.01), respectively. The peak concentrations (C(max)) of simvastatin and simvastatin acid were increased 3.9-fold (range 2.3-9.3-fold; P < 0.01) and 4.3-fold (range 2.7-7.9-fold; P < 0.01) by grapefruit juice. CONCLUSIONS: Even one glass of grapefruit juice, taken daily, considerably increases the plasma concentrations of simvastatin and simvastatin acid. Grapefruit juice may increase both the cholesterol-lowering effect and the risk of adverse effects of simvastatin. |
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Authors:
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Jari J Lilja; Mikko Neuvonen; Pertti J Neuvonen |
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Publication Detail:
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Type: Clinical Trial; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: British journal of clinical pharmacology Volume: 58 ISSN: 0306-5251 ISO Abbreviation: Br J Clin Pharmacol Publication Date: 2004 Jul |
Date Detail:
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Created Date: 2004-06-21 Completed Date: 2004-10-12 Revised Date: 2009-11-18 |
Medline Journal Info:
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Nlm Unique ID: 7503323 Medline TA: Br J Clin Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 56-60 Citation Subset: IM |
Affiliation:
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Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland. jari.lilja@hus.fi |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adult Anticholesteremic Agents / pharmacokinetics* Citrus* Cross-Over Studies Food-Drug Interactions Humans Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics* Male Simvastatin / analogs & derivatives*, metabolism, pharmacokinetics* |
| Chemical | |
Reg. No./Substance:
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0/Anticholesteremic Agents; 0/Hydroxymethylglutaryl-CoA Reductase Inhibitors; 121009-77-6/simvastatin acid; 79902-63-9/Simvastatin |
| Comments/Corrections | |
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