The pharmacokinetics and pharmacodynamics of sulfinalol hydrochloride in dogs after intravenous administration.

ABSTRACT

The pharmacokinetic behavior of sulfinalol hydrochloride, an antihypertensive agent with vasodilator and beta-adrenergic blocking activity, was determined in dogs after intravenous administration. The plasma concentrations of sulfinalol HCl were fit to an open two-compartment body model. The mean values for the alpha- and beta-phase constants were 33.3 hr-1 and 0.52 hr-1, respectively. The mean plasma clearance was 2.30 L/kg X hr. The steady-state volume of distribution was approximately four times the body weight of the animals. The urine data gave renal clearance rates approximately equal to the normal glomerular filtration rate in the dog. About 7.5% of the administered dose was excreted in the urine as free sulfinalol hydrochloride. The time course of the hypotensive effect of sulfinalol appears to be better correlated with calculated tissue levels of drug than with observed plasma levels.