ACEBUTOLOL

 ACEBUTOLOL

BRAND NAME:- SECTRAL 200,400mg tab, 10mg/2ml amp.

ACEBUTOLOL is an other beta blocker, Cardioselectivity agent with significant partial and membrane stabilizing properties . Effect on resting heart rate is less.

CARDIOSELECTIVITY:-

These drug are more potent in blocking cardiac Beta1 than bronchial Beta2 receptors. Selectivity is only relative and is lost at high doses. 

Their features are:-

1. Lower propensity to cause bronchoconstriction,but even these drug should usually be avoided in asthmatic and COPD patients.

2. Less Interference with carbohydrates metabolism and less inhibition of glycogenolysis during hypoglycemia --safer in diabetics.

3. Lower incidence of cold hand and feet ,less chances of precipitation Raynaud's phenomenon.

4.No/less deleterious effects on blood lipid profile.

5. Ineffective in suppression essential tremor.

6. Less liable to impair exercise capacity.

PARTIAL AGONISTIC (INTRINSIC SYMPATHOMIMETICS) ACTION:-

The drug themselves activate Beta1 or Beta2 receptors submaximally . The benefits of this property are controversial.

1. Bradycardia and depression of contractility at rest are not prominent,but exercise tachycardia is blocked; may be preferred in those prone to severe bradycardia (elderly patients;Sick sinus) or with low cardiac reserve.

2. Withdrawal is less likely to exacerbaina  hypertension or angina ; continued agonistic action on beta receptors (of the drug itself) prevent development of supersensitivity .

3. Plasma lipid profile is not/ less worsened.

4. Not effective in migraine prophylaxis —they dilate cerebral vessels.

5. Not suitable for secondary prophylaxis of MI.

MEMBRANE STABILIZING ACTIVITY:-

In ACEBUTOLOL this activity is claimed to contribute to the antiarrhythmic action,but appears to be significant only at high doses.

DOSE:- A single daily dose is sufficient in many patients.

Intravenous dose for arrhythmias 20-40mg.

SIDE EFFECTS:- of ACEBUTOLOL is milder. 

USED:-used in the treatment of Hypertension (high blood pressure), Angina (heart-related chest pain), Arrhythmia and heart attack.