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Acebutalol

Systems	Cardiovascular and Peripheral Vascular System
Category	Selective Beta1 Blocker

Pharmacokinetics

Acebutalol is adequately absorbed after oral administration and it undergoes hepatic (first pass) metabolism resulting in 50% bioavailability. It has a large volume of distribution and is not completely metabolised before its excretion via urine.

Indications

Acebutalol is used in the treatment of hypertension, to relieve angina and in IHD patients to help prevent recurrent Myocardial Infarction, to correct cardiac arrhythmias and in hyperthyroidism. It has a membrane stabilising effect in large doses. It causes decreased automaticity, conduction velocity and increases the refractory period to nerve impulses in nerve conduction. As a result, they decrease the heart's requirement for blood and oxygen by reducing its workload. They also help to maintain the cardiac rhythm.

Routes of Administration and Dosage

Oral dose: (capsules and tablets): For angina or Cardiac arrhythmia: Adults: 200 milligrams (mg) twice a day. The dose may be increased up to a total of 1200 mg a day. For high blood pressure: Adults: 200 to 800 mg a day as a single dose daily or divided into two doses.

Contra Indications

Acebutalol is contraindicated in Sinus bradycardia, heart block greater than 2nd degree, untreated cardiac failure,and cardiogenic shock.

Precautions

Allergies : Allergic reaction to the beta-blocker may occur. Pregnancy : Use of beta-blockers during pregnancy has been associated with hypoglycaemia, dyspnoea, bradycardia, and hypotension in the newborn infant. Breast-feeding : Acebutalol may pass into breast milk. Problems such as bradycardia, hypotension, and dyspnoea have been reported in nursing babies. Older adults : Adverse effects are more likely to occur in the elderly, who are usually more sensitive to the effects of beta-blockers. Also, beta-blockers may reduce tolerance to cold temperatures in elderly patients.

Interactions

It may increase the risk of serious allergic reaction to these drugs: Aminophylline, Caffeine, Oxtriphylline or Theophylline (the effects of both these drugs and beta-blockers may be blocked; in addition, theophylline levels in the body may be increased, especially in patients who smoke). Oral Antidiabetics or Insulin: There is an increased risk of hyperglycemia ; beta-blockers may mask certain symptoms of hypoglycemia such as increase in pulse rate and hypertension, and may prolong the hypoglycemia. Calcium channel blockers (bepridil, diltiazem, felodipine, isradipine, nicardipine ), nifedipine, nimodipine, verapamil or Clonidine or Guanabenz : Risk of hypertension may be increased. Cardiac arrhythmias may occur when beta-blockers are used with calcium channel blockers. Cocaine: Cocaine may block the effects of beta-blockers; in addition, there is an increased risk of hypertension, tachycardia, and possibly cardiac arrhythmias if cocaine is used while taking a beta-blocker. Monoamine oxidase (MAO) inhibitors, furazolidone, isocarboxazid, phenelzine, procarbazine, selegiline, tranylcypromine: taking beta-blockers with these drugs may cause severe hypertension.