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

British Journal of Clinical Pharmacology
R K FergusonW B Abrams


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.


Jun 1, 1993·Cardiovascular Drugs and Therapy·L Arcavi, N L Benowitz
Jan 1, 1985·Journal of Clinical Pharmacology·R K FergusonW B Abrams
May 1, 1986·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·M S LennardH F Woods
Mar 1, 1985·British Journal of Clinical Pharmacology·R V LewisH F Woods


Feb 1, 1976·Clinical Pharmacology and Therapeutics·M R AchongR I Ogilvie
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Apr 1, 1980·Biopharmaceutics & Drug Disposition·J J MackichanW J Jusko

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Beta-adrenergic receptor
Dose-Response Relationship, Drug
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