Comparative pharmacokinetics of lovastatin, simvastatin and pravastatin in humans

Twelve healthy male volunteers received single market-image 40-mg oral doses of lovastatin and simvastatin (both lactone prodrugs), or pravastatin (a beta-hydroxyacid) at 1 week intervals in a three-way crossover study to quantify HMG-CoA reductase inhibitors in plasma. Multiple plasma samples were...

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Bibliographic Details
Published inJournal of clinical pharmacology Vol. 32; no. 2; p. 136
Main Authors Pentikainen, P J, Saraheimo, M, Schwartz, J I, Amin, R D, Schwartz, M S, Brunner-Ferber, F, Rogers, J D
Format Journal Article
LanguageEnglish
Published England 01.02.1992
Subjects
Administration, Oral
Adult
Drug Administration Schedule
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors
Lovastatin - analogs & derivatives
Lovastatin - pharmacokinetics
Male
Pravastatin - pharmacokinetics
Simvastatin
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Summary:Twelve healthy male volunteers received single market-image 40-mg oral doses of lovastatin and simvastatin (both lactone prodrugs), or pravastatin (a beta-hydroxyacid) at 1 week intervals in a three-way crossover study to quantify HMG-CoA reductase inhibitors in plasma. Multiple plasma samples were collected up to 24 hours after the dose and assayed for active and total HMG-CoA reductase inhibitors. After equal oral doses, higher plasma concentrations of HMG-CoA reductase inhibitory activity after pravastatin than after either lovastatin of simvastatin (2-3 fold greater area under the concentration-time curve) suggest a greater potential availability of pravastatin-related inhibitory activity to peripheral tissues.
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1992.tb03818.x