Intravenous and oral administration of molsidomine, a pharmacodynamic and pharmacokinetic study.
In 12 healthy male volunteers, molsidomine 1, 2 and 4 mg i.v. increased resting heart rate and decreased systolic blood pressure, the latter still being affected after 8 hours. After single oral doses of 1 and 2 mg, systolic pressure tended to be reduced for 90 minutes and exercise heart rate tended to be increased. After oral treatment with 2 mg molsidomine three times daily for 1 week, the pharmacokinetic parameters and the effects on heart rate and blood pressure after the final dose were not different from those after the first dose. The terminal half-life was independent of dose and route of administration. Clearance and distribution volume were not dose-dependent. The bioavailability of a 2 mg oral dose of molsidomine was 44%. Inter-individual variation in heart rate, blood pressure and pharmacokinetics was observed.
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008981:Molsidomine; D010069:Oxadiazoles / Q000378:metabolism*; D005082:Physical Exertion; D013558:Sydnones / Q000008:administration & dosage / Q000378:metabolism* / Q000494:pharmacology
D010069:Oxadiazoles; D013558:Sydnones; D008981:Molsidomine