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Variable bioavailability of papaverine.

G Berg1, K A Jönsson, M Hammar

  • 1Department of Obstetrics and Gynaecology, Linköping University, Sweden.

Pharmacology & Toxicology
|May 1, 1988
PubMed
Summary
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Papaverine bioavailability varies greatly between individuals after oral administration, despite being reproducible within the same person. This high inter-individual variability in papaverine absorption impacts its effectiveness.

Area of Science:

  • Pharmacokinetics
  • Drug Metabolism and Disposition

Background:

  • Papaverine is an alkaloid used for smooth muscle relaxation.
  • Understanding papaverine's pharmacokinetic profile is crucial for optimizing its therapeutic use.

Purpose of the Study:

  • To investigate the plasma concentration curves of papaverine following intravenous and oral administration.
  • To assess the bioavailability and variability of papaverine after oral dosing.

Main Methods:

  • Single intravenous (80 mg) and oral (80 mg) doses of papaverine were administered to healthy males and patients.
  • Plasma papaverine concentrations were measured to determine pharmacokinetic parameters.
  • Repeated oral dosing was used to assess intra-individual reproducibility.

Main Results:

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  • Oral papaverine bioavailability was highly variable (mean 28%, range 5-99%).
  • Intra-individual bioavailability was reproducible in 4 volunteers after repeated oral doses.
  • Intravenous administration yielded a half-life of 1.2-6.6 hours (mean 3.0), volume of distribution of 3.1 L/kg, and clearance of 836 mL/min.

Conclusions:

  • Oral administration of 80 mg papaverine tablets exhibits unacceptable inter-individual variability in bioavailability.
  • The significant variability in papaverine absorption may necessitate dose individualization or alternative formulations.