Multiple-dose pharmacokinetics of nilvadipine in healthy volunteers

J Clin Pharmacol. 1988 Apr;28(4):350-5. doi: 10.1002/j.1552-4604.1988.tb03157.x.

Abstract

Nilvadipine, a new antihypertensive and antianginal drug, was studied in six healthy male volunteers to evaluate its steady-state pharmacokinetics after oral dosing. The subjects were given a single dose of 4 mg, followed by 4 mg every 12 hours for six days after a washout period of more than 3 days. The pharmacokinetics of nilvadipine were well described by a linear model of triexponential equation with zero-order absorption. The steady state was reached by the fourth day of multiple dosing, with a twofold accumulation of trough plasma concentration and no accumulation of peak concentration. The mean plasma concentration at steady state was 1.0 ng/mL. The optical enantiomers of nilvadipine were also determined in the plasma. The plasma concentration of (+)-nilvadipine was about two and a half times higher than that of (-)-nilvadipine, and this ratio was unaffected by multiple dosing.

MeSH terms

  • Administration, Oral
  • Adult
  • Humans
  • Male
  • Nifedipine / administration & dosage
  • Nifedipine / analogs & derivatives*
  • Nifedipine / blood
  • Nifedipine / pharmacokinetics
  • Stereoisomerism
  • Time Factors

Substances

  • nilvadipine
  • Nifedipine