Summary
The importance of cardioselectivity and partial agonist activity (PAA) of β-blockers in controlling blood pressure is under debate. This study was designed to compare the anti-hypertensive effect of a long-acting β1-selective β-blocker (atenolol) with 2 non-selective drugs with different PAA (pindolol and oxprenolol). The double-blind, randomised, crossover study involved 18 moderately hypertensive patients. The drugs were given at the following doses: atenolol (100mg once daily); pindolol (10mg bid); oxprenolol (80mg bid), all being given for 1 month. All 3 agents were associated with a similar fall in exercise tachycardia (i.e. same degree of β1-blockade) but atenolol induced a significantly greater fall of both resting and exercise blood pressure at 2 hours and 24 hours (12 hours in the case of oxprenolol and pindolol) after long term dosing. The difference in blood pressure control at 12–24 hours after administration was 12/12mm Hg (p < 0.01). The antihypertensive efficacy of atenolol, in contrast to oxprenolol, appears not to be increased by raising the plasma levels of the drug. Myocardial oxygen consumption (systolic blood pressure × heart rate) was reduced by all 3 agents both at rest and exercise, the greatest reduction being induced by atenolol. The overall incidence of side effects was less during atenolol, particularly those relating to the central nervous system (e.g. insomnia and dreaming).
It is concluded that atenolol (once daily) is a more effective antihypertensive agent than either oxprenolol or pindolol (both twice daily) when all 3 drugs are given at a dose causing the same degree of β1-blockade. Moreover, fewer side effects (particularly those related to the central nervous system) were associated with atenolol.
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Ambrosioni, E., Costa, F.V., Montebugnoli, L. et al. Comparison of Antihypertensive Efficacy of Atenolol, Oxprenolol and Pindolol at Rest and during Exercise. Drugs 25 (Suppl 2), 30–36 (1983). https://doi.org/10.2165/00003495-198300252-00007
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DOI: https://doi.org/10.2165/00003495-198300252-00007