Document Detail


Pharmacokinetics of cerivastatin when administered under fasted and fed conditions in the morning or evening.
MedLine Citation:
PMID:  10890578     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
OBJECTIVE: The influence of food and time of drug dosing on the pharmacokinetics of cerivastatin, a potent HMG-CoA reductase inhibitor, was evaluated in 24 healthy male subjects between 21 and 44 years of age. METHODS: A single-dose, four-way crossover design was employed, with each subject receiving cerivastatin 0.8 mg at weekly intervals under each of four conditions: 8 a.m. dosing after an overnight fast (reference), 8 a.m. dosing with a high-fat breakfast (test), 6 p.m. dosing with the evening meal (low-fat; test), and 10 p.m. dosing 4 h after dinner (reference). Plasma concentrations of the parent compound and its active metabolites were measured by high performance liquid chromatography with fluorescence detection subsequent to post-column derivatization. RESULTS: The calculated 90% confidence intervals for cerivastatin AUC and Cmax were completely contained within the range 0.8 to 1.25. Thus, no relevant influence of food could be detected, although the presence of food increased the Cmax of cerivastatin on average by 12% (90% confidence interval: 1.04 - 1.21) under morning, but not evening dosing. With respect to the effect of daytime on cerivastatin pharmacokinetics, AUCs were bioequivalent for all treatment conditions, with Cmax values slightly lower (8 - 19%) following evening dosing, irrespective of food intake. Cerivastatin was well tolerated by the subjects in the study. CONCLUSION: Food effect bioequivalence according to current guidelines could be demonstrated. Cerivastatin can be administered independent of meal intake at dinner or at bedtime, the preferred time of dosing for statins because the rate of hepatic cholesterol synthesis is greatest at night.
Authors:
W Mück; R Frey; S Unger; B Voith
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Publication Detail:
Type:  Clinical Trial; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  International journal of clinical pharmacology and therapeutics     Volume:  38     ISSN:  0946-1965     ISO Abbreviation:  Int J Clin Pharmacol Ther     Publication Date:  2000 Jun 
Date Detail:
Created Date:  2000-10-19     Completed Date:  2000-10-19     Revised Date:  2004-12-18    
Medline Journal Info:
Nlm Unique ID:  9423309     Medline TA:  Int J Clin Pharmacol Ther     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  298-303     Citation Subset:  IM    
Affiliation:
Institute of Clinical Pharmacology, Bayer AG, Wuppertal, Germany.
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MeSH Terms
Descriptor/Qualifier:
Adult
Area Under Curve
Cross-Over Studies
Fasting
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics*
Male
Pyridines / adverse effects,  pharmacokinetics*
Chemical
Reg. No./Substance:
0/Hydroxymethylglutaryl-CoA Reductase Inhibitors; 0/Pyridines; 0/cerivastatin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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