化合物信息

Drug Groups

approved

Description

A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for migraine disorders and for tremor. [PubChem]

Indication

Used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension.

Pharmacology

Nadolol is a nonselective beta-adrenergic receptor antagonist with a long half-life, and is structurally similar to propranolol. Clinical pharmacology studies have demonstrated beta-blocking activity by showing (1) reduction in heart rate and cardiac output at rest and on exercise, (2) reduction of systolic and diastolic blood pressure at rest and on exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. Nadolol has no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, nadolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.

Toxicity

Oral, mouse: LD₅₀ = 4500mg/kg. Symptoms of overdose include abdominal irritation, central nervous system depression, coma, extremely slow heartbeat, heart failure, lethargy, low blood pressure, and wheezing.

Affected Organisms

Biotransformation

Not metabolized by the liver and excreted unchanged primarily by the kidneys.

Absorption

Absorption of nadolol after oral dosing is variable, averaging about 30 percent.

Half Life

14-24 hours

Protein Binding

30%

Elimination

Unlike many other beta-adrenergic blocking agents, nadolol is not metabolized by the liver and is excreted unchanged, principally by the kidneys. Nadolol is excreted predominantly in the urine.

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