acebutolol

Mechanism of action

A beta-adrenergic receptor blocker (beta-blocker) blocks the binding of norepinephrine and epinephrine to beta-adrenergic receptors in the heart and blood vessels. This reduces heart rate, contractility (force of heart muscle contraction), cardiac output, and decreased blood pressure

Spectrum

It has a limited spectrum of activity and is primarily indicated for the treatment of hypertension (high blood pressure), angina pectoris (chest pain due to reduced blood flow to the heart), and prophylaxis after myocardial infarction (heart attack). It can also treat irregular heartbeats (arrhythmias), such as supraventricular tachycardia

 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined:

>10%

Fatigue

1-10%

Headache

Diarrhea

Dyspepsia

Flatulence

Abdominal pain

Chest pain

Edema

Hypotension

Myalgia

Pruritis

Vomiting

Dizziness

Constipation

Dyspnea

Nausea

Insomnia

Bradycardia

Dysuria

Heart failure

Impotence

Pharyngitis

<1%

Hepatotoxicity

Frequency not defined

Depression

Raynaud’s phenomenon

Bronchospasm

 

 

 

 

Contraindications

• Bronchial asthma: Beta-blockers can worsen bronchospasm in patients with asthma or other bronchospastic diseases.
• Heart block: It should be used with caution in patients with heart block, as it can worsen the condition.
• Cardiogenic shock: Beta-blockers are contraindicated in patients with cardiogenic shock, as they can reduce cardiac output and worsen the condition.
• Severe bradycardia: It should not be used in patients with a prolonged heart rate (less than 50 beats per minute) as it can slow the heart rate further.
• Severe peripheral arterial circulatory disorders: Beta-blockers can reduce blood flow to the extremities and should be used with caution in patients with severe peripheral arterial circulatory disorders.
• Anaphylaxis: Beta-blockers can mask the symptoms of anaphylaxis, such as rapid heartbeat, and should not be used in patients with a history of anaphylaxis

Caution

• Heart failure: Beta-blockers can reduce cardiac output and worsen heart failure and should be used with caution in patients with heart failure.
• Diabetes: Beta-blockers can mask symptoms of hypoglycemia (low blood sugar) in diabetic patients and may also interfere with the patient’s ability to detect hypoglycemia.
• Pheochromocytoma: Beta-blockers can worsen the symptoms of pheochromocytoma, an adrenal gland tumor that produces excess amounts of catecholamines.
• Thyrotoxicosis: Beta-blockers can mask symptoms of thyrotoxicosis (overactive thyroid) and may also interfere with the effectiveness of antithyroid drugs used to treat the condition.
• Kidney function is eliminated from the body primarily by the kidneys, and its effects may be increased in patients with reduced kidney function.
• Liver function: Beta-blockers can affect liver function and should be used cautiously in patients with liver disease.
• Electrolyte imbalances: Beta-blockers can alter the levels of electrolytes (such as potassium) in the blood and should be used with caution in patients with electrolyte imbalances.
• Depression: Beta-blockers can cause or worsen depression and should be used with caution in patients with a history of depression.
• Interaction with other drugs: It can interact with other medications, including other beta-blockers, calcium channel blockers, digitalis, and antiarrhythmic drugs, among others

 

Pregnancy consideration: It should not be used during pregnancy, as it can cross the placenta and cause harm to the foetus

Lactation: Excretion of the drug in human breast milk is unknown

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

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

It is a beta-adrenergic receptor blocker (beta-blocker) that belongs to the non-selective beta-blocker class of drugs. It works by blocking the binding of norepinephrine and epinephrine to beta-adrenergic receptors in the heart and blood vessels. This reduces heart rate, contractility (force of heart muscle contraction), and cardiac output and decreases blood pressure

Pharmacodynamics

The pharmacodynamic effects of acebutolol include a reduction in heart rate, contractility (force of heart muscle contraction), cardiac output, and a decrease in blood pressure. These effects inhibit the sympathetic nervous system, which usually stimulates the heart and blood vessels.

In addition to its effects on the cardiovascular system, acebutolol can also have other pharmacodynamic effects, including a reduction in insulin release and an increase in the release of glucose from the liver. The drug may also have some broncho-dilating effects, although these effects are generally not as pronounced as those seen with selective beta-2 adrenergic receptor blockers

Pharmacokinetics

• Absorption: It is well absorbed from the gastrointestinal tract after oral administration and has a bioavailability of about 60-80%. The drug is rapidly absorbed, with peak plasma concentrations occurring within 1-3 hours after oral dosing.
• Distribution: It is widely distributed in the body, with a volume of distribution of about 0.5-0.8 L/kg. The drug is highly protein-bound, with a binding affinity for alpha-1-acid glycoprotein, which may affect its distribution to different tissues.
• Metabolism: It is metabolized primarily in the liver, with the central metabolic pathways being hydroxylation and N-dealkylation. The drug is metabolized by the cytochrome P450 system, primarily CYP2D6, with minor contributions from CYP1A2 and CYP3A4.
• Elimination/Excretion: It is primarily eliminated from the body by the kidneys, with about 50% of the dose being excreted unchanged in the urine and the remainder excreted as metabolites. The half-life of acebutolol is about 5-10 hours

 

Administration

• The dose should be taken each day simultaneously, with or without food.
• The tablet should be swallowed whole, not crushed, chewed, or broken.
• The dose may gradually increase over time to achieve the desired effect, as directed by a doctor or healthcare professional.
• If a dose is missed, it should be taken as soon as possible. If it is almost time for the next dose, the missed dose should be skipped, and the next dose should be taken regularly

 

Patient information leaflet

Generic Name: acebutolol

Pronounced: [ A-se-BUE-toe-lol ]

Why do we use acebutolol?

It is a medication that is used for the treatment of several conditions, including:

• Hypertension (high blood pressure): It is used to treat high blood pressure alone or in combination with other medications. The drug works by reducing the force of heart contractions and dilating blood vessels, which decreases blood pressure.
• Angina pectoris (chest pain): It is used to treat angina (chest pain) caused by narrowing the coronary arteries, which supply blood to the heart. The drug works by reducing the heart’s workload and dilating blood vessels, which helps reduce the frequency and severity of angina attacks.
• Arrhythmias (abnormal heart rhythms): It is used to treat certain arrhythmias, such as supraventricular tachycardia, resulting from an overactive sympathetic nervous system. The drug works by blocking the binding of norepinephrine and epinephrine to beta-adrenergic receptors in the heart, which reduces the stimulation of the heart and helps to regulate its rhythm