Labetalol is a competitive antagonist of alpha 1-, beta 1-, and beta 2-adrenergic receptors. The hemodynamic effects of the drug include reduced blood pressure, heart rate, and peripheral resistance, with little change in resting cardiac output or stroke volume. In open trials and controlled studies, labetalol was an effective antihypertensive. Labetalol compared favorably with beta-blockers alone or in combination with vasodilators, for the treatment of hypertension. Reductions in heart rate are less pronounced with labetalol as compared with propranolol. Labetalol produces rapid reductions in blood pressure when administered intravenously for severe hypertension. The most frequent adverse reactions to the drug include fatigue, postural symptoms, headache, and gastrointestinal complaints. Labetalol may prove advantageous when vasodilation in addition to beta-blockade is desired, or for selected patients experiencing adverse effects attributable to beta-blockade. Until the clinical profile of labetalol is better defined, the use of the drug should be limited.