Bopindolol is a potent and specific beta‐adrenoceptor antagonist with partial agonist activity. In animal experiments it blocks both beta 1‐ and beta 2‐adrenoceptors and possesses a long duration of action. In the present study in healthy volunteers bopindolol was about ten times more potent than pindolol in reducing isoprenaline‐induced and exercise‐ induced tachycardia. In experiments on exercise‐induced tachycardia an oral dose of 2 mg produced a near maximum reduction of exercise heart rate, occurring within 2 to 3 h of administration. With higher doses (up to 12 mg) the maximum effect was reached earlier (between 1 and 2 h). The long duration of action of bopindolol observed in animal studies was confirmed in man. Twenty‐four hours after 4 and 10 mg bopindolol more than 2/3 of the maximum effect was still present. After 48 h 38% of the maximum effect of 4 mg and 50% of that of 12 mg remained. Even at 72 and 96 h exercise‐induced tachycardia was still significantly lowered after both doses of the drug. When bopindolol was administered once daily for 5 days there was a slight increase in the maximum reduction of exercise‐induced tachycardia during treatment with 1 mg/day but not with 4 mg/day, which produced a near maximum effect.
DOI: 10.1111/j.1365-2125.1985.tb02713.x
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