PMID: 3758142Jan 1, 1986Paper

Pharmacodynamics and pharmacokinetics of three different doses of urapidil infused in hypertensive patients

European Journal of Clinical Pharmacology
R KirstenH W Radtke

Abstract

The study was designed to follow the haemodynamic effects and pharmacokinetics under steady-state conditions of three different doses of urapidil infused continuously. Nine male hypertensive patients received three randomly assigned intravenous infusions of 32.5, 65 and 130 mg urapidil, over 14 h during 6 consecutive days, in a change-over fashion. Blood pressure and heart rate were measured over a period of 28 h after the infusion began and were compared with a reference profile obtained prior to the treatment periods. Urapidil and its main metabolite, parahydroxylated urapidil, were also determined for 28 h after the infusion began using HPLC. The 32.5 mg dose of urapidil caused a maximum decrease in systolic blood pressure of 33 +/- 8 mmHg, the 65 mg dose a maximum decrease of 39 +/- mmHg and the 130 mg dose a maximum decrease of 50 +/- 12 mmHg. The 32.5 and 65 mg doses resulted in similar serum urapidil concentrations, with maximum levels in the 100 to 200 ng/ml range, and the 130 mg dose caused a maximum level approximately four times that achieved with the 32.5 mg dose. The serum concentration of parahydroxy urapidil was proportional to the corresponding dose of urapidil. Four patients reported mild headache, fatigue, wea...Continue Reading

References

Jan 1, 1985·Clinical Pharmacology and Therapeutics·G G BelzD Palm

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Citations

Mar 14, 1992·Lancet·A P JonvilleE Autret
Aug 15, 1989·The American Journal of Cardiology·B N PrichardJ C Renondin

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