Labetalol
- Atc Codes:C07AG01
- CAS Codes:32780-64-6#36894-69-6
- PHARMGKB ID:32780-64-6#36894-69-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Trandate; Belgium: Trandate; Czech Republic: Trandate; Denmark: Trandate; Estonia: Trandate; Finland: Albetol; France: Trandate; Greece: Narcan, Trandate; Hungary: Trandate; Ireland: Trandate; Italy: Ipolab, Trandate, Trandiur; Luxembourg: Trandate; Malta: Labetalol, Trandate; Netherlands: Labetalol, Trandate; Poland: Pressocard, Trandate; Spain: Trandate; Sweden: Trandate; UK: Trandate.
North America
Canada: Labetalol, Trandate; USA: Labetalol, Trandate.
Latin America
Argentina: Biascol.
Asia
Japan: Adbroal, Amitalol, Ascool, Resporito, Trandate.
Drug combinations
Chemistry
Labetalol Hydrochloride: C~19~H~24~N~2~O~3~ HCl. Mw: 364.87. (1) Benzamide, 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]-, monohydrochloride; (2) 5-[1-Hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]salicylamide monohydrochloride. CAS-32780-64-6; CAS-36894-69-6 (labetalol)(1976).
Pharmacologic Category
Sympatholytic (Adrenergic Blocking) Agents; Selective α-Adrenergic Blocking Agents. Cardiovascular Drugs; α-Adrenergic Blocking Agents; β-Adrenergic Blocking Agents.(ATC-Code: C07AG01).
Mechanism of action
Blocks α-, β~1~-, and β~2~-adrenergic receptor sites. Elevated renins reduced.
Therapeutic use
Treatment of mild to severe hypertension. Used intravenously for hypertensive emergencies.
Pregnancy and lactiation implications
Labetalol crosses placenta. β-Blockers associated with persistent bradycardia, hypotension, and intrauterine growth retardation. β-Blockers generally safe during pregnancy. Cases of neonatal hypoglycemia reported following maternal use of β-blockers at parturition or during breast-feeding.
Unlabeled use
Pediatric hypertension.
Contraindications
Hypersensitivity to labetalol or any component of the formulation. Sinus bradycardia. Heart block greater than first-degree (except in patients with functioning artificial pacemaker). Cardiogenic shock. Bronchial asthma. Uncompensated cardiac failure. Pregnancy (2^nd^ and 3^rd^ trimesters).
Warnings and precautions
Anaphylactic reactions might occur (use caution with history of severe anaphylaxis to allergens). Hepatic injury including some fatalities reported rarely. Symptomatic hypotension with or without syncope may occur. Orthostatic hypotension may occur with I.V. administration. Avoid use in bronchospastic disease. Use with caution in diabetes mellitus (might potentiate hypoglycemia and/or mask signs and symptoms, also reduce release of insulin in response to hyperglycemia). Use with extreme caution in compensated heart failure. Use with caution in hepatic impairment, myasthenia gravis, peripheral vascular disease and Raynaud’s disease (might precipitate or aggravate symptoms of arterial insufficiency), pheochromocytoma. Use with caution in history of psychiatric illness (may cause or exacerbate CNS depression). Use with caution in patients receiving anesthetic agents which decrease myocardial function. Use with caution in patients on concurrent verapamil or diltiazem (bradycardia or heart block can occur). Avoid concurrent use of both agents. Elimination of labetalol reduced in elderly patients. Avoid abrupt withdrawal.