Relationships among timolol doses, plasma concentrations and beta- adrenoceptor blocking activity.

Autor: Ferguson, RK, Vlasses, PH, Koplin, J.R., Holmes, GI, Huber, P., Demetriades, J., Abrams, WB
Zdroj: British Journal of Clinical Pharmacology; 1982, Vol. 14 Issue 5, p719-725, 7p
Abstrakt: 1 We investigated the relationships among dose, plasma concentration and beta-adrenoceptor blockade after single and repeated doses (0.5-20 mg) of timolol and placebo in six normal men. 2 Maximal suppression of exercise-induced tachycardia (bicycle ergometry) was dose-dependent and greater at 2 than at 6 h after dosing; activity up to 12 h was evident on the last dosing day. 3 Attenuation of exercise-induced tachycardia was strongly correlated with the timolol dosage over the 0.5 to 5-10 mg range. 4 A plasma timolol concentration of 27 ng/ml was associated with maximal suppression of exercise-induced tachycardia. 5 Suppression of exercise-induced tachycardia and areas under the plasma concentration- time curves did not differ significantly on the first and last dosing days. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index