Variable bioavailability of papaverine

The plasma concentration curves of papaverine have been studied in nine healthy males and seven patients after administration of single intravenous (80 mg) and oral (80 mg) doses. The bioavailability of the drug was highly variable with a mean of 28% (range 5-99%) but reproducible within the same individual (4 of the volunteers) after a repeated (80 mg) oral dose. The calculated half-life after intravenous administration ranged between 1.2-6.6 hours (mean 3.0). The mean apparent volume of distribution was 3.1 l/kg and the mean total plasma clearance was 836 ml/min. It is concluded that papaverine shows an unacceptable inter-individual variation in the bioavailability after oral administration of 80 mg tablets.