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Active ingredient: Propranolol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Vasodilator Agents
  • Anti-anxiety Agents
  • Antihypertensive Agents
  • Antiarrhythmic Agents
  • Adrenergic Agents

Dosage Forms

  • Tablet

Brands / Synonyms

Angilol; Apsolol; Avlocardyl; Bedranol; Beprane; Berkolol; Beta-Neg; Beta-Propranolol; Beta-Tablinen; Beta-Timelets; Betachron; Betalong; Cardinol; Caridolol; Corpendol; Deralin; Dl-Propranolol Hydrochloride; Dociton; Duranol; Efektolol; Elbrol; Etalong; Euprovasin; Frekven; Inderal; Inderal LA; Inderide; Indobloc; Innopran XL; Intermigran; Kemi S; Obsidan; Oposim; Prano-Puren; Propanalol; Propanix; Propanolol; Prophylux; Propranalol; Propranolol; Propranolol Hcl; Propranolol Hcl Intensol; Propranolol Hydrochloride; Propranur; Proprasylyt; Pylapron; R,S-Propranolol Hydrochloride; Rapynogen; Reducor; Reducor Line; Sagittol; Servanolol; Sloprolol; Sumial; Tesnol

Indications

For the prophylaxis of migraine.

Pharmacology

Propranolol, the prototype of the beta-adrenergic receptor antagonists, is a competitive, nonselective beta-blocker similar to nadolol without intrinsic sympathomimetic activity. Propanolol is a racemic compound; the l-isomer is responsible for adrenergic blocking activity.

Mechanism of Action

Like atenolol and metoprolol, propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles.

Absorption

Propranolol is almost completely absorbed from the GI tract; however, plasma concentrations attained are quite variable among individuals.

Toxicity

Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm. LD50=565 mg/kg (orally in mice).

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Propranolol HCl is contraindicated in 1) cardiogenic shock, 2) sinus bradycardia and greater than first degree block, 3) bronchial asthma, 4) congestive heart failure unless the failure is secondary to a tachyarrhythmia treatable with Propranolol HCl.

Drug Interactions

Patients receiving catecholamine-depleting drugs such as reserpine should be closely observed if Propranolol HCl is administered. The added catecholamine-blocking action may produce an excessive reduction of resting sympathetic nervous activity, which may result in hypotension, marked bradycardia, vertigo, syncopal attacks, or orthostatic hypotension.

Caution should be exercised when patients receiving a beta blocker are administered a calcium-channel blocking drug, especially intravenous verapamil, for both agents may depress myocardial contractility or atrioventricular conduction. On rare occasions, the concomitant intravenous use of a beta blocker and verapamil has resulted in serious adverse reactions, especially in patients with severe cardiomyopathy, congestive heart failure, or recent myocardial infarction.

Blunting of the antihypertensive effect of beta-adrenoceptor blocking agents by nonsteroidal anti-inflammatory drugs has been reported.

Hypotension and cardiac arrest have been reported with the concomitant use of propranolol and haloperidol.

Aluminum hydroxide gel: Greatly reduces intestinal absorption of propranolol.

Ethanol: Slows the rate of absorption of propranolol.

Phenytoin, phenobarbitone: and rifampin accelerate propranolol clearance.

Chlorpromazine: When used concomitantly with propranolol, results in increased plasma levels of both drugs.

Antipyrine: and lidocaine have reduced clearance when used concomitantly with propranolol.

Thyroxine: May result in a lower than expected T3 concentration when used concomitantly with propranolol.

Cimetidine Decreases the hepatic metabolism of propranolol, delaying elimination and incre:asing blood levels.

Theophylline: Clearance is reduced when used concomitantly with propranolol.

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