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

Autor: Ferguson RK, Vlasses PH, Koplin JR, Holmes GI, Huber P, Demetriades J, Abrams WB
Jazyk: angličtina
Zdroj: British journal of clinical pharmacology [Br J Clin Pharmacol] 1982 Nov; Vol. 14 (5), pp. 719-25.
DOI: 10.1111/j.1365-2125.1982.tb04963.x
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.
Databáze: MEDLINE