Comparative Pharmacokinetics and Pharmacodynamics of Pravastatin and Lovastatin

摘要: The oral bioavailability of two HMG-CoA reductase inhibitors, pravastatin and lovastatin, was investigated in this randomized, two-way crossover study. Twenty healthy men were randomly assigned to treatment with a 40-mg dose or lovastatin once daily for 1 week; steady state kinetics assessed after the last dose. After week washout, each subject received alternate treatment. Serum specimens assayed by gas chromatography/mass spectrometry (GC/MS) intact acid bioassay active inhibitor concentration and, hydrolysis lactones, total concentration. systemic bioavailabilities (active plus potentially active) inhibitors drugs different, mean AUC value being 50% higher than that (mean +/- SEM AUC0-24 values 285 25 189 13 ng-equiv x hr/mL, respectively, P less .0001). Pravastatin, which is administered as monosodium salt, present circulation open acid; lactone, both open-acid metabolites (62%) closed-ring lactone (38%), are active. Based on values, accounted 75% from Lovastatin just 25% dose, remainder due other metabolites. Significant decreases baseline low-density lipoprotein (LDL) cholesterol observed during first leg lovastatin.(ABSTRACT TRUNCATED AT 250 WORDS)