Name: | Penbutolol |
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PubChem Compound ID: | 190541 |
Description: | A nonselective beta-blocker used as an antihypertensive and an antianginal agent. |
Molecular formula: | C36H60N2O8S |
Molecular weight: | 680.936 g/mol |
Synonyms: |
103437-28-1
|
Name: | Penbutolol |
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Name (isomeric): | DB01359 |
Drug Type: | small molecule |
Description: | A nonselective beta-blocker used as an antihypertensive and an antianginal agent. |
Synonyms: |
Penbutolol sulfate
|
Brand: | Levatolol, Paginol, Betapressin, Levatol, Lobeta |
Category: | Adrenergic beta-Antagonists, Antihypertensive Agents |
CAS number: | 36507-48-9 |
Indication: | Used in the treatment of high blood pressure. |
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Pharmacology: | Penbutolol is a non-selective beta blocker. Beta-blockers work by affecting the response to some nerve impulses in certain parts of the body. As a result, they decrease the heart's need for blood and oxygen by reducing its workload. They also help the heart to beat more regularly. |
Mechanism of Action: |
Penbutolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle and beta(2)-receptors in the bronchial and vascular smooth muscle. Beta(1)-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both ...
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Absorption: | Oral bioavailability is 90%. |
Protein binding: | 80-98% bound to plasma proteins. |
Biotransformation: | Metabolized in the liver by hydroxylation and glucuroconjugation forming a glucuronide metabolite and a semi-active 4-hydroxy metabolite. |
Route of elimination: | The metabolites are excreted principally in the urine. |
Half Life: | Phase 1: 2.5 hours; phase 2: 24 hours |
Toxicity: | Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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