Summary
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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Meszaros S., Szentmiklóski P., Czibula G. (1967): USA patent No. 3,337,539.
McEvoy G.K. (ed.) (1989): AHFS Drug Information, American Society of Hospital Pharmacists Inc., Bethesda, MD, USA, pp 941–942.
Magyar K., Lengyel M., Knoll J. (1978): Absorption, distribution and elimination of drotaverine. Acta Physiol. Acad. Sci. Hung., 51, 401–411.
Vargay Z., Simon G., Winter M., Szüts T. (1980): Qualitative and quantitative determination of drotaverine metabolites in rat bile. Eur. J. Drug Metab. Pharmacokinet., 5, 69–74.
Simon G., Vargay Z., Winter M., Szüts T. (1979): The intestinal absorption and excretion of14C drotaverine in rats. Eur. J. Drug Metab. Pharmacokinet., 4, 213–217.
Rutz-Coudray M.H., Balant L., Revillard C., Buri P., Giust J. (1976): Pharmacokinetique chez l’homme. Pharm. Acta Helv., 51 258–263.
Vargay Z., Deutsch T., Szatmári I. et al. (1984): The fate of drotaverine-acephyllinate in rat and man. II. Human pharmacokinetics. Eur. J. Drug. Metab. Pharmacokinet., 9, 17–21.
Mezei J., Kuttel S., Szentmilklósi P., Marton S., Rácz I. (1984): A new method for high-performance liquid chromatographic determination of drotaverine in plasma. J. Pharm. Sci., 73, 1489–1491.
Lalla J.K. Shah M.U., Jain M.B., Sharma A.H. (1993): Modified high-performance liquid chromatographic method for analysis of drotaverine in human plasma. J. Pharm. Biomed. Anal., 11, 385–388.
Bolaji O.O., Onyeji C.O., Ogungbamila F.O., Ogunbona F.A., Ogunlana E.O. (1993): High-performance liquid chromatographic method for the determination of drotaverine in human plasma and urine. J. Chromatogr., 622, 93–97.
Vargay Z., Szüts T., Bihari V. (1980). In: No-Spa product data: pharmacokinetics and metabolism. Budapest. Chinoin Pharmaceutical & Chemical Work Ltd.
Meyer M.C., Gollanud R., Staughn A. (1979): The influence of dosage form on papaverine bioavailability, J. Clin. Pharmacol., 19, 435–444.
Berg G., Jonsson K., Hammar M., Norlander B. (1988): Variable bioavailability of papaverine. Pharmacol Toxicol., 62, 308–310.
Garret E.R., Roseboon H., Green J.R., Schuermann W. (1978): Pharmacokinetics of papaverine hydrochloride and the biopharmaceutics of its oral dosage forms. Int. J. Clin. Pharmacol., 16, 193–208.
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Bolaji, O.O., Onyeji, C.O., Ogundaini, A.O. et al. Pharmacokinetics and bioavailability of drotaverine in humans. European Journal of Drug Metabolism and Pharmacokinetics 21, 217–221 (1996). https://doi.org/10.1007/BF03189716
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DOI: https://doi.org/10.1007/BF03189716