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Relationships among timolol doses, plasma concentrations and beta‐ adrenoceptor blocking activity.
Author(s) -
Ferguson RK,
Vlasses PH,
Koplin J.R.,
Holmes GI,
Huber P.,
Demetriades J.,
Abrams WB
Publication year - 1982
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1982.tb04963.x
Subject(s) - timolol , adrenergic beta antagonists , beta adrenoceptor , blocking (statistics) , beta (programming language) , pharmacology , plasma concentration , adrenergic receptor , medicine , chemistry , endocrinology , propranolol , receptor , glaucoma , ophthalmology , mathematics , statistics , computer science , programming language
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.