Anabet - General Information
A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Anabet is also used for migraine disorders and for tremor.
Pharmacology of Anabet
Anabet 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. Anabet 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.
Anabet for patients
Patients, especially those with evidence of coronary artery insufficiency, should be warned against interruption or discontinuation of nadolol therapy without the physician's advice. Although cardiac failure rarely occurs in properly selected patients, patients being treated with beta-adrenergic blocking agents should be advised to consult the physician at the first sign or symptom of impending failure. The patient should also be advised of a proper course in the event of an inadvertently missed dose.
When administered concurrently, the following drugs may interact with beta-adrenergic receptor blocking agents:
Anesthetics, general: exaggeration of the hypotension induced by general anesthetics.
Antidiabetic drugs (oral agents and insulin): hypoglycemia or hyperglycemia; adjust dosage of antidiabetic drug accordingly.
Catecholamine-depleting drugs (e.g., reserpine): additive effect; monitor closely for evidence of hypotension and/or excessive bradycardia (e.g., vertigo, syncope, postural hypotension).
Response to Treatment for Anaphylactic Reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.
Nadolol is contraindicated in bronchial asthma, sinus bradycardia and greater than first degree conduction block, cardiogenic shock, and overt cardiac failure.
Additional information about Anabet
Anabet Indication: Used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension.
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. Anabet therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
Drug Interactions: Acetohexamide The beta-blocker decreases the symptoms of hypoglycemia
Chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia
Disopyramide The beta-blocker increases toxicity of disopyramide
Gliclazide The beta-blocker decreases the symptoms of hypoglycemia
Glipizide The beta-blocker decreases the symptoms of hypoglycemia
Glisoxepide The beta-blocker decreases the symptoms of hypoglycemia
Glibenclamide The beta-blocker decreases the symptoms of hypoglycemia
Glycodiazine The beta-blocker decreases the symptoms of hypoglycemia
Insulin The beta-blocker decreases the symptoms of hypoglycemia
Lidocaine The beta-blocker decreases the symptoms of hypoglycemia
Repaglinide The beta-blocker decreases the symptoms of hypoglycemia
Tolazamide The beta-blocker decreases the symptoms of hypoglycemia
Tolbutamide The beta-blocker decreases the symptoms of hypoglycemia
Verapamil Increased effect of both drugs
Clonidine Increased hypertension when clonidine stopped
Theophylline Antagonism of action and increased effect of theophylline
Aminophylline Antagonism of action and increased effect of theophylline
Dyphylline Antagonism of action and increased effect of theophylline
Oxtriphylline Antagonism of action and increased effect of theophylline
Dihydroergotamine Ischemia with risk of gangrene
Dihydroergotoxine Ischemia with risk of gangrene
Ergonovine Ischemia with risk of gangrene
Ergotamine Ischemia with risk of gangrene
Methysergide Ischemia with risk of gangrene
Prazosin Risk of hypotension at the beginning of therapy
Epinephrine Hypertension, then bradycardia
Methyldopa Possible hypertensive crisis
Ibuprofen Risk of inhibition of renal prostaglandins
Indomethacin Risk of inhibition of renal prostaglandins
Piroxicam Risk of inhibition of renal prostaglandins
Food Interactions: Avoid alcohol.
Avoid natural licorice.
Generic Name: Nadolol
Synonyms: Not Available
Drug Category: Sympatholytics; Antihypertensive Agents; Anti-Arrhythmia Agents; Adrenergic beta-Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Nadolol: Anabet; Corgard; Solgol;
Absorption: Absorption of nadolol after oral dosing is variable, averaging about 30 percent.
Toxicity (Overdose): 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.
Protein Binding: 30%
Biotransformation: Not metabolized by the liver and excreted unchanged primarily by the kidneys.
Half Life: 14-24 hours
Dosage Forms of Anabet: Tablet Oral
Chemical IUPAC Name: (2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
Chemical Formula: C17H27NO4
Nadolol on Wikipedia: http://en.wikipedia.org/wiki/Nadolol
Organisms Affected: Humans and other mammals