betaxolol

Actions and Spectrum 

The action of this drug is to block the beta-1 receptors in the heart and kidneys, This helps lower blood pressure and lessens the burden on the heart. By reducing the heart rate and the force of contractions, betaxolol also reduces the heart’s demand for oxygen, making it useful in the treatment of angina (chest pain) and other heart-related conditions. 

The spectrum of this drug is selective, meaning that it primarily blocks beta-1 receptors in the heart and kidneys, while having little or no effect on beta-2 receptors located in the lungs and other parts of the body. This drug’s selectivity can be beneficial for individuals with asthma or other lung conditions since it does not impede their breathing 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined  

2-10% 

Pharyngitis (2%) 

Fatigue (2-10%) 

Palpitation (2%) 

Dyspepsia (2-5%) 

Diarrhea (2%) 

Edema (2%) 

Lethargy (3%) 

Bradycardia (6-8%) 

Chest pain (2-7%)  

<2% 

Hyperlipidemia 

Diabetes 

Anemia 

Malaise 

Hyperglycemia 

Arrhythmia 

Hypercholesterolemia 

Neuropathy 

Depression 

Rash  

Frequency Not Defined 

decrease HDL levels 

Raynaud’s phenomenon 

May increase triglyceride levels and insulin resistance 

Decreased exercise tolerance 

Black Box Warning:  

Abrupt discontinuation of this drug may lead to an exacerbation of angina symptoms or the occurrence of myocardial infarction (heart attack), arrhythmias (irregular heartbeat), or sudden death. Individuals with coronary artery disease who are taking this medication should be cautioned against stopping or interrupting treatment without first consulting their doctor. When discontinuing therapy, the dosage should be tapered gradually over one to two weeks. 

Patients with bronchospastic disease, such as asthma or chronic obstructive pulmonary disease (COPD), should use this drug with caution. It can cause bronchospasm, which can be life-threatening in some cases. Individuals with these conditions should be carefully monitored for signs of respiratory distress, and their treatment should be stopped if needed 

Contraindication/Caution:  

Hypersensitivity: Patients who are known to be hypersensitive should not take this drug. 

Cardiogenic shock: this should not be used in patients with cardiogenic shock. 

 Sinus bradycardia and heart block greater than first degree: This should not be used in patients with sinus bradycardia (slow heart rate) or heart block greater than first degree (an electrical conduction abnormality in the heart). 

 Severe pulmonary disease: This is contraindicated in patients with severe pulmonary disease, such as bronchial asthma or chronic obstructive pulmonary disease (COPD), which beta-blockers can worsen.  

Cardiac failure: This drug should not be used in patients with severe cardiac failure.  

Diabetes: Patients with diabetes taking this medication may have trouble recognizing and treating hypoglycemia (low blood sugar) as the drug could mask its symptoms 

Pregnancy warnings:     

Pregnancy category: N/A 

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 a lack of studies on pregnant women and no evidence of risk to the fetus 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 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: The drug is a selective beta-1 adrenergic receptor blocker. This medication is prescribed as an anti-hypertensive agent to reduce high blood pressure in individuals diagnosed with hypertension. It also treats certain heart conditions, such as angina pectoris and arrhythmias. 

Pharmacodynamics: The pharmacodynamics of this drug involves its selective blockade of beta-1 adrenergic receptors in the heart, which leads to a reduction in heart rate and force of contraction, and ultimately, a decrease in blood pressure.  

MOA: The drug is a beta-adrenergic receptor antagonist that is primarily used as a cardioselective beta-blocker. It works by blocking the beta-1 receptors in the heart, which decreases the sympathetic nervous system’s effects and reduces the heart’s workload. This ultimately leads to a decrease in heart rate and blood pressure. 

Pharmacokinetics: 

Absorption 

The drug is absorbed quickly and almost completely from the gastrointestinal tract after oral administration. The bioavailability of betaxolol is approximately 90% when taken orally. 

Distribution 

The distribution of betaxolol is relatively uniform throughout the body, with no significant accumulation in any particular tissue. 

Metabolism 

The cytochrome P450 enzyme system primarily metabolizes the drug in the liver. The main metabolite of betaxolol is inactive, and there are no known active metabolites. 

Excretion and elimination 

 The drug is eliminated primarily in the urine, with approximately 50% of the dose excreted unchanged. The half-life of this drug is approximately 14-22 hours, and steady-state concentrations are reached within 5-7 days of regular dosing. 

Administration:  

The recommended dosage of this medication varies depending on the patient’s medical history and the condition being treated. 

The frequency of the medication is usually once or twice daily, depending on the prescribed medication. It’s essential to take the medication at the same time every day to ensure consistent blood levels.   

The drug is typically taken orally in tablet or capsule form and should be swallowed whole with a glass of water. Do not crush or chew the medication. 

Patient information leaflet 

Generic Name: betaxolol 

Why do we use betaxolol ?   

This medication is classified as a beta-blocker and used for high blood pressure. 

Aside from hypertension, this medication may also be prescribed for other conditions including chest pain (angina), heart failure, and irregular heartbeat (arrhythmia). Additionally, it may be used as a preventative measure for migraines or to reduce their frequency and severity.