The bioavailability of intramuscularly administered nicomorphine (Vilan) with its metabolites and their glucuronide conjugates in surgical patients

Int J Clin Pharmacol Ther. 1995 Aug;33(8):442-8.

Abstract

The kinetics of 20 mg nicomorphine intramuscularly were described in 8 patients under combined general and epidural anesthesia. The half-life of nicomorphine was 0.32 +/- 0.20 h (mean +/- SD) and is governed by the absorption-rather than the elimination rate. The half-life of 6-mononicotinoylmorphine (0.39 +/- 0.09 h) was identical to that of the parent compound (p = 0.29), suggesting it is directly related to the absorption rate of nicomorphine. Morphine had a half-life of 1.38 +/- 0.31 h. Morphine is subsequently metabolized into morphine-3-glucuronide and morphine-6-glucuronide. The half-life of these 2 glucuronide conjugates was about 2.6 h (p = 0.07). A glucuronide conjugate of 6-mononicotinoylmorphine was not detected. In urine only morphine and its glucuronides are found, with renal clearance values of 214 ml.min-1 for morphine and 132 ml.min-1 for the glucuronides. The bioavailability of this pharmaceutical formulation after intramuscular administration equals that of intravenous administration in surgical patients (at the same dose).

Publication types

  • Clinical Trial

MeSH terms

  • Adult
  • Biological Availability
  • Calibration
  • Chromatography, High Pressure Liquid
  • Female
  • Half-Life
  • Humans
  • Injections, Intramuscular
  • Middle Aged
  • Morphine / administration & dosage
  • Morphine / blood
  • Morphine / pharmacokinetics*
  • Morphine Derivatives / administration & dosage
  • Morphine Derivatives / blood
  • Morphine Derivatives / pharmacokinetics*
  • Morphine Derivatives / urine
  • Nicotinic Acids / administration & dosage
  • Nicotinic Acids / blood
  • Nicotinic Acids / pharmacokinetics
  • Nicotinic Acids / urine
  • Reproducibility of Results

Substances

  • Morphine Derivatives
  • Nicotinic Acids
  • morphine-6-glucuronide
  • morphine 6-nicotinate
  • Morphine
  • morphine 3-nicotinate
  • morphine-3-glucuronide
  • nicomorphine