Penbutolol; Indications/Uses, Dosage, Side Effects, Drug Interaction ,Pregnancy

Penbutolol; Indications/Uses, Dosage, Side Effects, Drug Interaction ,Pregnancy

Penbutolol is a lipophilic, nonselective beta-adrenergic receptor antagonist with anti-anginal and antihypertensive activities. Penbutolol competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. In addition, penbutolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels.

Penbutolol is a medication in the class of beta blockers, used in the treatment of high blood pressure. Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. Penbutolol binds both beta-1 and beta-2 adrenergic receptors, rendering it a non-selective beta-blocker. Penbutolol can act as a partial agonist at beta-adrenergic receptors since it is a sympathomimetic drug. Penbutolol also demonstrates the high binding affinity to the 5-hydroxytryptamine receptor 1A with antagonistic effects.

Mechanism of Action of Penbutolol

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 the heart muscle and increases the heart rate. Penbutolol blocks the catecholamine activation of β1 adrenergic receptors and decreases heart rate, which lowers blood pressure.

Indications of Penbutolol

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Contra-Indications of Penbutolol

Dosage of Penbutolol

Strength:  20 mg

Hypertension

  • Initial dose: 20 mg orally once a day.
  • Maintenance dose: 20 to 40 mg orally once a day.

Angina Pectoris 

  • Initial dose: 20 mg orally once a day.
  • Maintenance dose: 20 to 40 mg orally once a day.

Side Effects of Penbutolol

The most common

More common

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Rare

Drug Interactions of Penbutolol

Penbutolol may interact with the following drug, supplements, & may change the efficacy of the drug

Pregnancy Catagory of Penbutolol

FDA Pregnancy Category C

Pregnancy

There are no reports of the use of penbutolol during pregnancy. As with other beta-blockers, it is recommended that newborns of mothers who were exposed to penbutolol near term or delivery be monitored for signs or symptoms of beta-blockade (bradycardia, hypotension, hypoglycemia) for at least 48 hours.

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Lactation

Based on its physicochemical properties, penbutolol appears to present a low-risk to the breastfed infant. Because there is no published experience with penbutolol during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

References

  1. 9d3b-3b00f655cbc2.xml
    https://www.fda.gov/ForIndustry/DataStandards/StructuredProductLabeling/ucm162549.htm

  2. https://www.webmd.com/drugs/2/drug-11467/Penbutolol/details/list-contraindications
  3. https://pubchem.ncbi.nlm.nih.gov

  4. https://www.drugs.com/cdi/penbutolol.html

Penbutolol

 

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