Acebutolol

Registered South African indications:

• Angina pectoris
• Cardiac arrhythmias
• Hypertension

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Breastfeeding 
• History of hypersensitivity to beta blockers
• Cardiogenic shock
• Severe hypotension (<100/60mmHg)
• 2nd or 3rd degree heart block
• Sick sinus syndrome
• Marked bradycardia (heart rate <50bpm)
• Uncontrolled cardiac failure
• Metabolic acidosis
• Severe peripheral circulatory disorders
• Untreated phaeochromocytoma

Cautions

• Breastfeeding
• Moderate to severe renal impairment
• Hepatic impairment
• Obstructive airway disease
• Prinzmetal's angina
• Thyrotoxicosis
• Diabetes mellitus
• Psoriasis
• History of severe anaphylactic or allergic reactions
• Abrupt withdrawal 
• Ischaemic heart disease
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose-galactose malabsorption
• Bradycardia 

Forms avail. in SA and covered in this monograph: tab, cap

Angina pectoris

• Oral (tab, cap): 400mg/day in 1-2 divided doses; Max: 1200mg/24hrs

Hypertension - mild to moderate

• Oral (tab, cap): Initial: 400mg/day in 1-2 divided doses; Titrate after 2 weeks; Maintenance: 400-800mg/day in 1-2 divided doses; Max: 1200mg/24hrs

At doses of 1200mg/day, suggested dosing regimen is 800mg in the morning and 400mg in the evening

Cardiac arrhythmias (excluding those due to conduction defects)

• Oral (tab, cap): Initial: 200mg, dly; Maintenace: 400-1200mg/day in divided doses; Max: 1200mg/24hrs
  

Not established for use in children

Pregnancy

• Caution; not recommended
• Acebutolol should not be administered to female patients during the first trimester of pregnancy unless the physician considers it essential. In such cases, the lowest possible dose should be used
• Beta-blockers administered in late pregnancy may give rise to bradycardia, hypoglycaemia and cardiac or pulmonary complications in the foetus / neonate
• Beta-blockers can reduce placental perfusion, which may result in intrauterine foetal death, immature and premature deliveries
• Animal studies have shown no teratogenic hazard

Breastfeeding

• Contraindicated 
• Acebutolol and its active metabolites are excreted in human milk and effects have been shown in breastfed newborns / infants of treated mothers
• Acebutolol should not be used during breastfeeding

Renal Impairment

• Moderate to severe: Caution; dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• No dose adjustment recommended

Porphyria Information

• Not porphyrinogenic (NP)

Central Nervous System Disorders

• Depression
• Nightmare
• Psychoses
• Hallucinations
• Confusion
• Sleep disorder
• Fatigue
• Dizziness
• Headache
• Paraesthesia

Cardiovascular Disorders

• Cardiac failure
• Atrioventricular block first degree
• Increase of an existing atrioventricular block
• Bradycardia
• Intermittent claudication
• Raynaud's syndrome
• Cyanosis
• Hypotension

Respiratory Disorders

• Dyspnoea
• Pneumonitis
• Lung infiltration
• Bronchospasm

Gastrointestinal Disorders

• Gastrointestinal disorders
• Nausea and vomiting
• Diarrhoea 

Hepatobiliary Disorders

• Increased hepatic enzymes 
• Hepatocellular liver injury 

Genitourinary Disorders

• Loss of libido

Skin and Subcutaneous Tissue Disorders

• Rash

Immune, Blood and Lymphatic System Disorders

• Antinuclear antibody
• Lupus like syndrome

Sensory Disorders

• Visual impairment
• Dry eye

Others

• Withdrawal syndrome

• Calcium channel blockers
• Class 1 antiarrhythmic agents
• Insulin
• Clonidine
• Sympathomimetic agents
• Xanthine bronchodilators
• Digoxin
• Non-steroidal anti-inflammatory drugs
• Phenothiazines
• Barbituates
• Tricyclic antidepressants
• Antihypertensives
• Monoamine oxidase inhibitors
• Anaesthetic agents
• Fingolimod
• Diltiazem

• Heart rate

Specific cases may require

• Blood glucose
• ECG

Hypertension

• If the hypertension is still not adequately controlled, consideration should be given to adding a second antihypertensive agent such as the calcium channel antagonist nifedipine or small doses of thiazide diuretic

Cardiac Arrhythmias

• It may take up to three hours for the maximal anti-arrhythmic effect to become apparent

Acebutolol is a cardioselective beta-adrenoreceptor antagonist which acts selectively on beta1-adrenergic receptors in the heart. Acebutolol and its active metabolite also have some partial agonist activity (intrinsic sympathomimetic activity). Under conditions of rest this partial agonist activity enures that the negative chronotropic and negative inotropic effects of the drug are balanced out. However, under conditions of effort and emotional induced sympathetic stimulation this agonist activity is overcome and acebutolol is able to protect the heart during times of stress.

Capsule 100mg

• Sectral (Sanofi) orginator

Capsule 200mg 

• Sectral (Sanofi) originator

Tablet 400mg

• Butobloc (Pharmacare)