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Pharmacokinetics of propranolol

L Borgström, C G Johansson, H Larsson

Journal of Pharmacokinetics and Biopharmaceutics

|August 1, 1981

Summary

This study investigated propranolol pharmacokinetics in healthy males across various oral and intravenous doses. Results showed consistent drug disposition kinetics, with a 6-hour half-life and 25% bioavailability, indicating no dose-dependent effects.

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Area of Science:

Pharmacology
Clinical Pharmacy
Drug Metabolism

Background:

Propranolol is a widely used beta-blocker with established therapeutic applications.
Understanding its pharmacokinetic profile is crucial for optimizing dosing and predicting patient response.
Variability in propranolol absorption and elimination necessitates detailed pharmacokinetic studies.

Purpose of the Study:

To characterize the pharmacokinetics of propranolol following oral and intravenous administration.
To evaluate potential dose-dependent effects on propranolol disposition.
To determine key pharmacokinetic parameters such as bioavailability, volume of distribution, and half-life.

Main Methods:

A pharmacokinetic study involving nine healthy male volunteers.
Administration of propranolol at oral doses of 40, 80, and 120 mg, and an intravenous dose of 10 mg.
Analysis of propranolol concentrations using gas-liquid chromatography after extraction and derivatization.
Pharmacokinetic analysis employing a multiexponential curve-stripping program.

Main Results:

The mean terminal half-life of propranolol was determined to be approximately 6 hours.
The volume of distribution was calculated to be around 6 L/kg.
Oral bioavailability was found to be approximately 25%.
No evidence of dose-dependent disposition kinetics or an oral threshold dose was observed.
A minor increase in urine volume was noted post-administration.

Conclusions:

Propranolol exhibits predictable pharmacokinetic behavior in healthy males within the studied dose range.
The established bioavailability and half-life provide valuable data for clinical dosing considerations.
The absence of dose-dependent kinetics simplifies therapeutic management of propranolol.

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