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Nadolol

Name: Nadolol
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) 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. Mechanism of action: Like other beta-adrenergic antagonists, nadolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, nadolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively. Drug type: Approved. Small Molecule. Drug category: Adrenergic beta-Antagonists. Anti-Arrhythmia Agents. Antihypertensive Agents. Sympatholytics
Synonym(s): Anabet, Corgard, Solgol
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB01203
Id: CHEBI:7444
Related to: Beta-1 adrenergic receptor, Beta-2 adrenergic receptor
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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB01203  +
DefinitionA non-selective beta-adrenergic antagonist 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) 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. Mechanism of action: Like other beta-adrenergic antagonists, nadolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, nadolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively. Drug type: Approved. Small Molecule. Drug category: Adrenergic beta-Antagonists. Anti-Arrhythmia Agents. Antihypertensive Agents. Sympatholytics s. Antihypertensive Agents. Sympatholytics
Has roleDrug  +
IdCHEBI:7444  +
LabelNadolol  +
ModifiedDate12 August 2014  +
RelatedToBeta-1 adrenergic receptor  +, and Beta-2 adrenergic receptor  +
SuperCategoryMolecular entity  +
SynonymAnabet  +, Corgard  +, and Solgol  +