Drug/Small Molecule:
nadolol

2D structure

Overview

Trade Names: Anabet; Corgard; Solgol
Brand Mixtures: Corzide Tab W Nadolol 40mg (Bendroflumethiazide + Nadolol); Corzide Tab W Nadolol 80mg (Bendroflumethiazide + Nadolol)
PharmGKB Accession Id: PA450573

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 (source: Drug Bank)

Indication

Used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. (source: Drug Bank)

ATC Therapeutic Category

  • C07AA:Beta blocking agents, non-selective

Pharmacology, Interactions, and Contraindications

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. (source: Drug Bank)

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. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid natural licorice.
Magnesium, potassium and zinc needs increased.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Not metabolized by the liver and excreted unchanged primarily by the kidneys. (source: Drug Bank)

Protein Binding

30% (source: Drug Bank)

Absorption

Absorption of nadolol after oral dosing is variable, averaging about 30 percent. (source: Drug Bank)

Toxicity

Oral, mouse: LD<sub>50</sub> = 4500mg/kg. Symptoms of overdose include abdominal irritation, central nervous system depression, coma, extremely slow heartbeat, heart failure, lethargy, low blood pressure, and wheezing. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)(C)NCC(COc1cccc2c1C[C@@H]([C@@H](C2)O)O)O (source: Drug Bank)

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ADRB1 Uncurated Annotation (source: Drug Bank)
ADRB2 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
Methyldopa Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
acetohexamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
aminophylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
chlorpropamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
clonidine Uncurated Annotation Increased hypertension when clonidine stopped (source: Drug Bank)
dihydroergotamine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
dihydroergotoxine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
disopyramide Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
dyphylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
epinephrine Uncurated Annotation Hypertension, then bradycardia (source: Drug Bank)
ergonovine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
ergotamine Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
fenoterol Uncurated Annotation Antagonism (source: Drug Bank)
formoterol Uncurated Annotation Antagonism (source: Drug Bank)
glibenclamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
gliclazide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glipizide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glisoxepide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
glycodiazine Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
ibuprofen Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
indomethacin Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
isoproterenol Uncurated Annotation Antagonism (source: Drug Bank)
l-methyldopa Uncurated Annotation Possible hypertensive crisis (source: Drug Bank)
lidocaine Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
methysergide Uncurated Annotation Ischemia with risk of gangrene (source: Drug Bank)
orciprenaline Uncurated Annotation Antagonism (source: Drug Bank)
oxtriphylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
pirbuterol Uncurated Annotation Antagonism (source: Drug Bank)
piroxicam Uncurated Annotation Risk of inhibition of renal prostaglandins (source: Drug Bank)
prazosin Uncurated Annotation Risk of hypotension at the beginning of therapy (source: Drug Bank)
procaterol Uncurated Annotation Antagonism (source: Drug Bank)
repaglinide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
salbutamol Uncurated Annotation Antagonism (source: Drug Bank)
salmeterol Uncurated Annotation Antagonism (source: Drug Bank)
terbutaline Uncurated Annotation Antagonism (source: Drug Bank)
theophylline Uncurated Annotation Antagonism of action and increased effect of theophylline (source: Drug Bank)
tolazamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
tolbutamide Uncurated Annotation The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank)
verapamil Uncurated Annotation Increased effect of both drugs (source: Drug Bank)

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01203
KEGG Drug ID:
D00432
PubChem Compound ID:
39147
PubChem Substance ID:
180211
IUPHAR Ligand ID:
554

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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