Pharmacokinetics and bioavailability of drotaverine in humans.

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Bolaji OO, Onyeji CO, Ogundaini AO, Olugbade TA, Ogunbona FA

Pharmacokinetics and bioavailability of drotaverine in humans.

Eur J Drug Metab Pharmacokinet. 1996 Jul-Sep;21(3):217-21.

PubMed ID
8980918 [ View in PubMed
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Abstract

The pharmacokinetics and bioavailability of drotaverine was studied in 10 healthy volunteers after administration of single 80 mg oral and intravenous doses of the HCl salt of the drug, in a crossover fashion. Plasma and urine samples were analyzed for the unchanged drug by HPLC. The pharmacokinetic parameters, such as elimination half-life, plasma clearance, renal clearance and apparent volume of distribution, were not influenced by the route of drug administration. The drug was mainly eliminated by non-renal routes since renal clearance accounted for only 0.31 +/- 0.13% of the total plasma clearance. The absolute bioavailability was variable and ranged from 24.5-91% with a mean of 58.2 +/- 18.2% (mean +/- SD). It is suggested that the high variation in the bioavailability of drotaverine HCl after oral administration may result in significant interindividual differences in therapeutic response.

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