Disposition of pravastatin sodium, a tissue-selective HMG-CoA reductase inhibitor, in healthy subjects

Br J Clin Pharmacol. 1990 Feb;29(2):239-43. doi: 10.1111/j.1365-2125.1990.tb03626.x.


Pravastatin sodium, a competitive inhibitor of HMG-CoA reductase, is a new orally effective hypocholesterolaemic agent. In a two-way crossover study, eight healthy male subjects each received an intravenous and an oral dose of [14C]-pravastatin sodium. The oral absorption of [14C] activity from pravastatin sodium was about 34% and the oral bioavailability was about 18%, suggesting first-pass metabolism of pravastatin. After the intravenous dose, the recovery of radioactivity averaged 60% and 34% in urine and faeces, respectively. Corresponding values were 20% (urine) and 71% (faeces) for the oral dose. The estimated average plasma elimination half-life of pravastatin was 0.8 and 1.8 h for the intravenous and oral routes, respectively. The average values for total and renal clearances were 13.5 and 6.3 ml min-1 kg-1, respectively, and the steady-state volume of distribution averaged 0.51 kg-1. These results suggest that both kidney and liver are important sites of elimination for pravastatin.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Biological Availability
  • Chromatography, Thin Layer
  • Feces / analysis
  • Heptanoic Acids / blood
  • Heptanoic Acids / pharmacokinetics*
  • Heptanoic Acids / urine
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors*
  • Injections, Intravenous
  • Naphthalenes / blood
  • Naphthalenes / pharmacokinetics*
  • Naphthalenes / urine
  • Pravastatin
  • Random Allocation


  • Heptanoic Acids
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Naphthalenes
  • Pravastatin