Acebutolol

Oral
Hypertension

Oral
Cardiac arrhythmias

Oral
Angina pectoris

CrCl	Dosage
<25	Reduce dose by 75%.
25-50	Reduce dose by 50%.

May be taken with or without food.

Cardiogenic shock, 2nd and 3rd degree AV block, severe bradycardia, sick sinus syndrome, uncontrolled heart failure, severe asthma or COPD, metabolic acidosis, severe peripheral circulatory disease, untreated phaeochromocytoma.

1st degree AV block. May mask symptoms of hyperthyroidism and hypoglycaemia. Patients w/ myasthenia gravis, DM. May aggravate psoriasis. Avoid abrupt withdrawal as it may precipitate thyroid storm or MI, and may exacerbate angina and ventricular arrhythmias. Patients undergoing surgery involving general anaesth. Hepatic impairment. Pregnancy and lactation.

Fatigue, dizziness, headache, insomnia, mental depression, nightmare, anxiety, hyperesthesia or hypoesthesia. Constipation, diarrhoea, nausea, vomiting, flatulence, dyspepsia, abdominal pain, dry mouth, thirst, epigastric distress, anorexia. Dyspnoea, cough, pharyngitis, rhinitis, shortness of breath, bronchospasm, asthma. Urinary frequency, nocturia, dysuria, impotence. Rash, pruritus, sweating, reversible alopecia. Abnormal vision, sore or gritty eyes, conjunctivitis, tinnitus. Myalgia, arthralgia, lupus erythematosus-like syndrome, hypersensitivity pneumonitis, pulmonary granulomas, pleuropulmonary fibrosis, pleurisy. Reversible alterations in LFT results; dark urine, fever, malaise.

PO: B

May affect ability to drive or engaging in tasks that require alertness.

Monitor BP, heart rate, ECG and blood glucose.

Symptoms: Excessive bradycardia or hypotension, pulmonary oedema, cardiogenic shock, AV block, conduction defects, bronchospasm, depressed level of consciousness, hypoglycaemia and rarely hyperkalaemia. Management: Induce emesis or perform gastric lavage for acute ingestion. Admin IV atropine sulfate for severe bradycardia, followed by slow IV inj of isoprenaline if initial admin of atropine sulfate is insufficient; vasopressors may be used for severe hypotension despite correction of bradycardia, diazepam can be used for seizures; for cardiac failure, a cardiac glycoside and diuretic. Glucagon may also be useful for myocardial depression and hypotension. A β-adrenergic agonist and/or a theophylline derivative may be used for bronchospasm. Haemodialysis may be useful in enhancing elimination.

Additive effect w/ reserpine. Antagonises β-adrenergic stimulating effect of sympathomimetic agents. Additive negative effect on SA or AV nodal conduction w/ cardiac glycosides, nondihydropyridine Ca channel blockers. Reduced hypotensive effect w/ NSAIDs.

Description: Acebutolol is a cardioselective β-blocker w/ little effect on the bronchial receptors. It exhibits some intrinsic sympathomimetic activity and membrane-stabilising properties.
Onset: 1-2 hr.
Duration: 12-24 hr.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Bioavailability: Approx 40%. Time to peak plasma concentration: Approx 2 hr (acebutolol); approx 4 hr (diacetolol).
Distribution: Widely distributed, crosses the placenta, enters breast milk and minute amounts penetrate into CSF. Volume of distribution: 1.2 L/kg. Plasma protein binding: Approx 26%.
Metabolism: Undergoes extensive first-pass effect to diacetolol (active metabolite).
Excretion: Via faeces (50-60%); urine (30-40%). Plasma elimination half-life: 3-4 hr (acebutolol); 8-13 hr (diacetolol).

Store between 20-25°C. Protect from light.

Beta-Blockers

C07AB04 - acebutolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.

Anon. Acebutolol Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/12/2013.

Anon. Acebutolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/12/2013.

Buckingham R (ed). Acebutolol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2013.

Joint Formulary Committee. Acebutolol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2013.

Sectral Tablet. U.S. FDA. https://www.fda.gov/. Accessed 02/12/2013.