Multiple dose pharmacokinetic study of cicletanine in healthy volunteers

Eur J Drug Metab Pharmacokinet. 1991:Spec No 3:173-7.

Abstract

Cicletanine hydrochloride, a furopyridine derivative, is a new type of antihypertensive drug. A pharmacokinetic study was performed in 8 non-patient subjects who were given 50 mg oral daily doses for 7 days. Cicletanine plasma levels were measured by HPLC. An open bicompartmental model was fitted to the experimental data using an extended non-linear regression method. Additionally plasma levels obtained after the first administration were used to determine pharmacokinetic parameters, which were considered as representative of a single dose administration. The results showed no significant differences between parameters estimated after the first dose and repeated dosing. Mean half-life values were 7.3 and 7.9 hours respectively. The mean peak and trough concentration values in the last interval studied were 1730 and 44 ng/mL respectively. The accumulation index was negligible (1.15). The similarity in the values obtained after the first and repeated administration suggests that cicletanine displays a linear pharmacokinetic behaviour at a dose of 50 mg.

MeSH terms

  • Adult
  • Antihypertensive Agents / administration & dosage
  • Antihypertensive Agents / pharmacokinetics*
  • Capsules
  • Chromatography, High Pressure Liquid
  • Diuretics / administration & dosage
  • Diuretics / pharmacokinetics*
  • Half-Life
  • Humans
  • Male
  • Models, Biological
  • Pyridines*
  • Spectrophotometry, Ultraviolet

Substances

  • Antihypertensive Agents
  • Capsules
  • Diuretics
  • Pyridines
  • cicletanine