Labetalol

Information about Labetalol

Labetalol is an antihypertensive agent with both alpha- and beta-adrenergic receptor blocking activity.

Liver safety of Labetalol

Labetalol has been linked to several cases of clinically apparent drug induced liver disease, some of which have been severe and even fatal.

Mechanism of action of Labetalol

Labetalol (la bayt' a lol) is a unique antihypertensive agent that has both alpha- and beta-adrenergic receptor blocking activity. The beta-blockade is nonselective, acting on both beta-1 and beta-2 adrenergic receptors. Beta-1 adrenergic blockade reduces the heart rate and myocardial contractility by slowing the AV conduction and suppressing automaticity. Beta-2 blockade affects peripheral vascular resistance and can cause bronchospasm and hypoglycemia. The alpha blockade is largely directed at the alpha-1 receptors and leads to relaxation of arterial smooth muscle and vasodilation.

FDA approval information for Labetalol

Labetalol was approved for use in the United States in 1984 and currently more than 2 million prescriptions are filled yearly.

Current indications for labetalol are in the therapy of hypertension alone or in combination with other agents. Parenteral forms of labetalol are indicated for therapy of hypertensive emergencies, severe hypertension and pheochromocytoma.

Dosage and administration for Labetalol

Labetalol is available in tablets of 100, 200 and 300 mg in generic formulations and under the trade name Trandate. Parenteral formulations for intravenous administration are also available. The typical oral dose of labetalol in adults is 100 mg twice daily initially with subsequent dose adjustments based upon clinical response and tolerance to a range of 200 to 1200 mg daily.

Side effects of Labetalol

Common side effects include bradycardia, hypotension, fatigue, dizziness, orthostatic hypotension, depression, memory loss, incontinence, weight gain and diarrhea. As with all beta-blockers, sudden withdrawal can trigger rebound hypertension.

Antihypertensive agents

• Dailymed label info on Labetalol
• FDA Labetalol

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  (RR)-Labetalol Structural Formula

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  (RS)-Labetalol Structural Formula

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  (SR)-Labetalol Structural Formula