Tolerance and pharmacokinetics of propacetamol, a paracetamol formulation for intravenous use

Fundam Clin Pharmacol. 1992;6(6):259-62. doi: 10.1111/j.1472-8206.1992.tb00119.x.

Abstract

In 12 healthy volunteers, paracetamol pharmacokinetics were compared following administration of 1 g propacetamol HCl given intravenously over a 15-min period and 500 mg paracetamol given orally. Mean +/- SD total AUC (microgram/ml.h) following the iv formulation was significantly (P < 0.01) greater than following oral paracetamol (25.53 +/- 4.27 vs 21.04 +/- 4.49) corresponding to a mean oral bioavailability of paracetamol of 82.2 +/- 9.4%. Between 1 and 2 h after administration, paracetamol plasma concentrations became very similar following both formulations. In another study, 2 g propacetamol HCl was given both as a 15-min infusion and as a 2-min bolus injection to six healthy volunteers. Contrary to mild to moderate local discomfort experienced during the 2-min bolus injection, the 15-min infusion was well tolerated without any complaints reported.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Acetaminophen / administration & dosage
  • Acetaminophen / adverse effects
  • Acetaminophen / analogs & derivatives*
  • Acetaminophen / blood
  • Acetaminophen / pharmacokinetics
  • Administration, Oral
  • Adult
  • Biological Availability
  • Double-Blind Method
  • Drug Tolerance
  • Humans
  • Infusions, Intravenous
  • Injections, Intravenous
  • Male
  • Prodrugs / administration & dosage*
  • Prodrugs / adverse effects
  • Prodrugs / pharmacokinetics

Substances

  • Prodrugs
  • Acetaminophen
  • propacetamol