ASSESSMENT OF BETA-BLOCKING ACTIVITY OF TRIMEPRANOL IN MAN

  • 1 January 1978
    • journal article
    • research article
    • Vol. 16  (6) , 279-284
Abstract
The .beta.-blocking potency and the duration of action of trimepranol were measured in healthy volunteers using isoprenaline antagonism and reduction in exercise tachycardia. Based on isoprenaline antagonism, trimepranol was 4 times as potent as propranolol on a weight basis. The degree of .beta.-blockade increased linearly with dose from 5 mg to 20 mg, excluding a dose-dependent 1st-pass metabolism in this dose range. There was a significant correlation between plasma concentration and the effect of 14C-trimepranol on isoprenaline and exercise tests. The elimination half-life of trimepranol, calculated both on the basis of its effects and plasma concentrations, was approximatedly 3-4 h. The .beta.-blockade due to 10 to 20 mg of trimepranol was extended at least up to 12 h following oral administration, based both on isoprenaline and exercise tests and on the effect of resting heart rate. Twice-a day administration seems sufficient to provide a continuous .beta.-blockade in the clinical use of trimepranol.

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