Around the Beta-Blockers, One More Time

Abstract

We review the pharmacology, pharmacokinetics, and relative costs of beta-blockers, as well as indications for and therapeutic controversies surrounding their use. It is hoped that this discussion will assist clinicians in making informed decisions when choosing a drug for a hospital formulary or a particular patient. Beta-blockers are indicated for a variety of noncardiovascular and cardiovascular conditions, including hypertension, ischemic heart disease, arrhythmias, and prophylaxis of myocardial infarction (MI). These agents compete with catecholamines at beta-adrenoreceptors. They have different ancillary properties, including intrinsic sympathomimetic activity (ISA), cardioselectivity, and membrane stabilizing-activity, and vary in their duration of action, route of elimination, and lipophilicity. Beta-blocking agents decrease oxygen demand by exerting a negative inotropic and chronotropic effect. They also reduce blood pressure and possess antiarrhythmic effects. Beta-blockers penetrate the central nervous system (CNS) to different degrees and can cause a wide variety of CNS adverse effects. Nonselective beta-blockers have been noted to slightly reduce renal blood flow. Nadolol is an exception in that either no change, or even a small increase in renal blood flow, is observed upon initiation of therapy. Beta-blockers also act on the pulmonary bed by preventing beta2-mediated bronchodilation, thereby exacerbating bronchospastic disease in some patients. Beta-adrenergic blocking agents can potentiate both hypoglycemia and hyperglycemia in diabetic patients. Their effects on total peripheral resistance (TPR) are controversial. Initially it appears that beta-blockade increases TPR. After chronic therapy, however, TPR decreases to or below baseline values. These agents appear to be equally efficacious in the treatment of hypertension, arrhythmias, and ischemic heart disease. Agents with ISA should not be used for prevention of secondary MI. Cost may be the most practical differentiating factor when choosing agents for a hospital formulary or a particular patient.