penbutolol

Action and Spectrum: 

The action of penbutolol is primarily on the beta-1 receptors in the heart, which decreases the heart rate and the force of heart contractions. It also has some effect on the beta-2 receptors, which can cause relaxation of the smooth muscles in the airways, blood vessels, and uterus. 

The spectrum of penbutolol is relatively narrow, meaning it is most effective in treating conditions that involve the heart and blood vessels. It may not be effective for treating conditions that involve other organ systems or areas of the body. 

 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency Not Defined 

Fatigue 

Depression 

Mask symptoms of hypoglycemia 

Decrease HDL 

Aggravate CHF 

May increase triglyceride levels 

Bronchospasm 

Raynaud’s phenomenon 

Decreased exercise tolerance 

Black Box Warning: 

The black box warning for penbutolol relates to its use in patients with certain heart conditions, particularly those with heart failure. 

Contraindication / Caution: 

• Hypersensitivity: penbutolol should not be used in patients who have had an allergic reaction to the drug or any of its components. 
• Heart conditions: penbutolol should be used with caution in patients with heart block, heart failure, or bradycardia (slow heart rate) as it can exacerbate these conditions. 
• Lung conditions: Penbutolol should be used with caution in patients with asthma or chronic obstructive pulmonary disease (COPD) as it can cause bronchospasm (constriction of the airways). 
• Diabetes: penbutolol can mask the symptoms of hypoglycemia (low blood sugar) in patients with diabetes. Therefore, caution should be exercised when using this medication in diabetic patients. 
• Thyroid disorders: penbutolol can mask the symptoms of hyperthyroidism (overactive thyroid) and should be used with caution in patients with this condition. 
• Pregnancy and breastfeeding: penbutolol should be used with caution in pregnant or breastfeeding women as its effects on the fetus or infant are not fully known. 

Pregnancy warnings:   

Pregnancy category: C

Lactation: Excreted into human milk is unknown

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology: 

penbutolol is a beta-blocker medication used to treat high blood pressure, angina (chest pain), and other cardiovascular conditions. It works by blocking the effects of adrenaline and other stress hormones on the heart, reducing the workload on the heart and lowering blood pressure. 

Pharmacodynamics: 

Mechanism of action:  

penbutolol is a non-selective beta-blocker, meaning it blocks both beta-1 and beta-2 adrenergic receptors. By blocking these receptors, penbutolol reduces the effects of sympathetic nervous system activity, which can cause an increase in heart rate, cardiac output, and blood pressure.  

Pharmacokinetics: 

Absorption 

penbutolol is well absorbed after oral administration and reaches peak blood levels within 1-2 hours. 

Distribution 

penbutolol is widely distributed throughout the body, including the heart, lungs, liver, and kidneys. It crosses the blood-brain barrier, but only to a limited extent. 

Metabolism 

penbutolol is metabolized primarily by the liver, with a half-life of about 4-6 hours. 

Elimination and Excretion 

The metabolites are excreted in the urine and feces. 

Administration: 

penbutolol is a beta-blocker medication that is typically used to treat high blood pressure and other heart-related conditions. The administration of penbutolol should always be done under the guidance and supervision of a qualified healthcare professional. 

The dosage of penbutolol can vary depending on a number of factors, such as the patient’s age, medical condition, and response to treatment. Generally, the medication is taken orally once a day, with or without food. It is important to take penbutolol regularly to achieve the best results. 

Patient information leaflet 

Generic Name: penbutolol 

Why do we use penbutolol? 

penbutolol is a medication that belongs to a class of drugs called beta-blockers. It is primarily used to treat hypertension (high blood pressure), angina (chest pain), and other cardiovascular conditions such as arrhythmias (irregular heartbeats) and congestive heart failure.