Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia

Bull Exp Biol Med. 2020 Feb;168(4):465-469. doi: 10.1007/s10517-020-04732-w. Epub 2020 Mar 7.

Abstract

We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiorthostatic hypokinesia, a tendency to a decrease in half-elimination period, mean retention time, and volume of distribution and an increase in the rate of absorption, ratio of maximum concentrations, and relative rate of absorption of verapamil and propranolol were revealed. For ethacizine, a statistically significant increase in the time of attaining maximum concentration and volume of distribution and a decrease in the maximum concentration, rate of absorption, ratio of maximum concentrations, and relative rate of absorption under conditions of antiorthostatic hypokinesia were found.

Keywords: antiorthostatic hypokinesia; ethacizine; pharmacokinetics; propranolol; verapamil.

MeSH terms

  • Adult
  • Area Under Curve
  • Biological Availability
  • Cardiovascular Agents / blood
  • Cardiovascular Agents / pharmacokinetics*
  • Half-Life
  • Humans
  • Hypokinesia / blood*
  • Hypokinesia / drug therapy
  • Male
  • Middle Aged
  • Phenothiazines / blood
  • Phenothiazines / pharmacokinetics*
  • Propranolol / blood
  • Propranolol / pharmacokinetics*
  • Verapamil / blood
  • Verapamil / pharmacokinetics*
  • Weightlessness Simulation / methods*

Substances

  • Cardiovascular Agents
  • Phenothiazines
  • Propranolol
  • Verapamil
  • ethacizine