Propranolol
Propranolol | |
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INN | |
Drug class | Beta blocker |
Routes of administration | By mouth, rectal, intravenous |
Pregnancy category | |
Bioavailability | 26% |
Metabolism | Liver (extensive) CYP1A2, CYP2D6; minor: CYP2C19, CYP3A4 |
Elimination half-life | 4–5 hours |
Excretion | Kidney (<1%) |
Legal status | |
CAS Number | 525-66-6 |
PubChem | 4946 |
DrugBank | DB00571 |
ChemSpider | 4777 |
KEGG | D08443 |
A medication used to treat high blood pressure ("beta blocker").
Information about Propranolol
Propranolol is a nonselective beta-adrenergic receptor blocker (beta-blocker) that is widely used for the therapy of hypertension, cardiac arrhythmias, angina pectoris and hyperthyroidism.
Liver safety of Propranolol
Propranolol has yet to be convincingly associated with clinically apparent liver injury and is often used in patients with liver disease and cirrhosis.
Mechanism of action of Propranolol
Propranolol (proe pran' oh lol) was the prototype beta-blocker developed for therapy of hypertension and is considered nonselective, acting on both the beta-1 and beta-2 adrenergic receptors. Beta-1 adrenergic blockade reduces the heart rate and myocardial contractility by slowing AV conduction and suppressing automaticity. Beta-2 blockade also affects peripheral vascular resistance and can cause bronchospasm and hypoglycemia. The beta-2 blockade is responsible for the majority of adverse effects associated with propranolol.
FDA approval information for Propranolol
Propranolol was approved for use in the United States in 1967 and is still commonly used, with several million prescriptions filled yearly. Propranolol is indicated for the management of hypertension, myocardial infarction, angina pectoris, idiopathic hypertrophic subaortic stenosis and prevention of migraine and vascular headaches. Propranolol is also used to treat essential tremor, to decrease the heart rate in patients with hyperthyroidism, and to prevent recurrent variceal hemorrhage.
FDA approval information for Propranolol
Propranolol is available in multiple generic forms and under the trade name of Inderal in tablets of 10, 20, 40, 60, 80 and 90 mg, as well as extended or sustained release capsules of 60, 80, 120 and 160 mg. Liquid formulations for oral and parenteral administration are also available. The typical dose of propranolol in adults is 60 to 240 mg daily in 2 divided doses (one with extended release formulations), with subsequent dose modification based upon efficacy and tolerance.
Side effects of Propranolol
Common side effects of propranolol include bradycardia, hypotension, fatigue, dizziness, depression, memory loss, incontinence, cold limbs and less commonly severe hypotension, heart failure and bronchospasm. Sudden withdrawal can trigger rebound hypertension. Beta-blockers are contraindicated in patients with asthma, bradycardia and heart failure and should be used cautiously in the elderly and in patients with diabetes.
Beta blockers (C07) | ||||||||
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