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QuickView for Penbutolol (compound)

Name: Penbutolol
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
Name: Penbutolol
Name (isomeric): DB01359
Drug Type: small molecule
Description: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.
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.
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:
IbuprofenRisk of inhibition of renal prostaglandins
MethyldopaPossible hypertensive crisis
ErgotamineIschemia with risk of gangrene
InsulinThe beta-blocker, penbutolol, may decrease symptoms of hypoglycemia.
EpinephrineHypertension, then bradycardia
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