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QuickView for Labetalol (compound)

Name: Labetalol
PubChem Compound ID: 134043
Description: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.
Molecular formula: C19H24N2O3
Molecular weight: 328.406 g/mol
S,S-Labetalol; Benzamide, 2-hydroxy-5-((1S)-1-hydroxy-2-(((1S)-1-methyl-3-phenylpropyl)amino)ethyl)-; 83167-24-2; 2-Hydroxy-5-((1S)-1-hydroxy-2-(((1S)-1-methyl-3-phenylpropyl)amino)ethyl)benzamide
Name: Labetalol
Name (isomeric): DB00598
Drug Type: small molecule
Description: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.
Labetalolum [INN-Latin]; Labetolol; Labetalol hydrochloride; Labetalol HCL
Brand: Normodyne, Presdate, Albetol, Trandate, Ibidomide
Category: Sympatholytics, Adrenergic beta-Antagonists, Adrenergic alpha-Antagonists, Antihypertensive Agents
CAS number: 36894-69-6
Indication: For the management of hypertension (alone or in combination with other classes of antihypertensive agents), as well as chronic stable angina pectoris and sympathetic overactivity syndrome associated with severe tetanus. Labetalol is used parenterally for immediate reduction in blood pressure in severe hypertension or in hypertensive crises when considered an emergency, for the control of blood pressure in patients with pheochromocytoma and pregnant women with preeclampsia, and to produce controlled hypotension during anesthesia to reduce bleeding resulting from surgical procedures.
Labetalol is an selective alpha-1 and non-selective beta adrenergic blocker used to treat high blood pressure. It works by blocking these adrenergic receptors, which slows sinus heart rate, decreases peripheral vascular resistance, and decreases cardiac output. Labetalol has two asymmetric centers and therefore, exists as a molecular complex of two...
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Mechanism of Action:
Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. The principal phy...
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Absorption: Completely absorbed (100%) from the gastrointestinal tract with peak plasma levels occurring 1 to 2 hours after oral administration. The absolute bioavailability of labetalol is increased when administered with food.
Protein binding: 50%
Biotransformation: Primarily hepatic, undergoes significant first pass metabolism
Route of elimination: These metabolites are present in plasma and are excreted in the urine, and via the bile, into the feces.
Half Life: 6-8 hours
Toxicity: LD50 = 66 mg/kg (Rat, IV). Side effects or adverse reactions include dizziness when standing up, very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals.
Drug interaction:
IbuprofenRisk of inhibition of renal prostaglandins
InsulinThe beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
GlipizideThe beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
ErgonovineIschemia with risk of gangrene
HalothaneMonitor arterial pressure closely
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