Abstract

To review the pharmacology, pharmacokinetics, and clinical experience with bisoprolol and make recommendations regarding its potential clinical usefulness, as well as considerations for formulary inclusion. Reference citations were sought from Index Medicus and Science Citation Index. Data were collected from abstracts and articles describing experimental studies or blind clinical trials. Studies designed in a randomized, blind, and placebo-controlled manner were emphasized. Studies also were included if bisoprolol was evaluated comparatively with other agents in a randomized, blind fashion. Data from human studies published in English were evaluated. Studies were assessed by sample size and the clarity of descriptions of methods and results. Bisoprolol reduces systolic and diastolic blood pressures in patients with hypertension for a 24-hour dosing interval and is associated with beneficial hemodynamic effects in patients with myocardial ischemia. It is devoid of intrinsic sympathomimetic activity and membrane-stabilizing effects at therapeutic dosages. In patients with hypertension, bisoprolol diminishes plasma renin activity, platelet aggregation, effective renal plasma flow, and creatinine clearance. Bisoprolol has minimal effects on glucose tolerance and plasma lipid profiles. Monotherapy with bisoprolol is as effective as with atenolol, nitrendipine, or nifedipine. Low-dose combination therapy with hydrochlorothiazide is at least as effective as either bisoprolol or hydrochlorothiazide alone. Preliminary experience in the management of angina pectoris suggests that bisoprolol is at least as efficacious as atenolol or verapamil. Thus far, reported adverse effects are similar to those of other beta-blockers. No clinically important drug interactions have been reported at this time.

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