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Pharmacokinetic and pharmacological studies with tolamolol in man.
Author(s) -
Faulkner JK,
Stopher DA,
Walden R
Publication year - 1975
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.1365-2125.1975.tb00551.x
Subject(s) - pharmacokinetics , oral administration , volume of distribution , half life , tachycardia , plasma concentration , medicine , heart rate , clearance , volunteer , plasma clearance , distribution (mathematics) , anesthesia , pharmacology , blood pressure , urology , biology , mathematical analysis , mathematics , agronomy
Pharmacokinetic and physiological variables were measured in six healthy subjects after intravenous and oral administration of tolamolol. 2. After intravenous injection of tolamolol (20 mg), there was a biphasic decline both in plasma concentration and attenuation of maximum exercise tachycardia. First and second phase half‐lives of plasma concentration were 7 min and 2.5 h respectively. WReduction of maximum exercise tachycardia declined from 32 beats/min at 2 h to 19 beats/min at 8 hours. Clearance of tolamolol from blood ranged from 0.8‐ 1.41 min‐1. 3. After the oral administration of tolamolol (100 mg), the average volume of distribution was 220.1 and plasma concentration half‐ life 1.8 hours. After ten eight‐hourly doses of 100 mg there was no accumulation of tolamolol and the half‐life of plasma clearance was unchanged. 4. Hydroxytolamolol was detected in plasma in two of six subjects after oral tolamolol. 5. There was a significant positive correlation between reduction in maximum exercise heart rate and logarithm of plasma concentration of tolamolol after both oral and intravenous administration.