Penbutolol

291.4 g/mol

291.43

253-074-3

78W62V43DY

DTXSID8023428|DTXSID5045467

C66336

C - Cardiovascular system

41.5 Ų

4.15 (LogP)|4.15

68-72 °C

438.2

0.02 M|2.12e-02 g/L

Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.

Mild-to-moderate elevations in serum aminotransferase levels occur in less than 2% of patients on penbutolol and are usually transient and asymptomatic, resolving even with continuation of therapy. Despite its wide spread use, penbutolol has not been convincingly linked to instances of clinically apparent liver injury. Other beta-blockers have been linked to rare instances of acute liver injury with a latency to onset of 4 to 24 weeks, a hepatocellular pattern of serum enzyme elevations and a rather mild, self-limiting course without evidence of hypersensitivity or autoimmune reactions.

80-98% bound to plasma proteins. Extensively bound to Alpha-1-acid glycoprotein 1.

Penbutolol is indicated in the treatment of mild to moderate arterial hypertension. It may be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics.Penbutolol is contraindicated in patients with cardiogenic shock, sinus bradycardia, second and third degree atrioventricular conduction block, bronchial asthma, and those with known hypersensitivity.|FDA Label

Penbutolol is a nonselective beta-adrenergic receptor blocker (beta-blocker) used for the therapy of hypertension. Penbutolol has yet to be convincingly associated with clinically apparent liver injury.

Beta-Adrenergic Receptor Antagonists

Penbutolol is a ß-1, ß-2 (nonselective) adrenergic receptor antagonist. Experimental studies showed a dose-dependent increase in heart rate in reserpinized (norepinephrine-depleted) rats given penbutolol intravenously at doses of 0.25 to 1.0 mg/kg, suggesting that penbutolol has some intrinsic sympathomimetic activity. In human studies, however, heart rate decreases have been similar to those seen with propranolol.

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety. (See all compounds classified as Adrenergic beta-Antagonists.)

>90%.|The metabolites are excreted principally in the urine.|Approximately 90% of the metabolites are excreted in the urine.

Metabolized in the liver by hydroxylation and glucuroconjugation forming a glucuronide metabolite and a semi-active 4-hydroxy metabolite.

Plasma= approximately 5h Conjugated= approximately 20h in healthy persons, 25h in healthy elderly persons, and 100h in patients on renal dialysis.

Penbutolol acts on the β1 adrenergic receptors in both the heart and the kidney. When β1 receptors are activated by catecholamines, they stimulate a coupled G protein that leads to the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). The increase in cAMP leads to activation of protein kinase A (PKA), which alters the movement of calcium ions in heart muscle and increases the heart rate. Penbutolol blocks the catecholamine activation of β1 adrenergic receptors and decreases heart rate, which lowers blood pressure.

Betapressin

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals