The synthesis of atenolol resulted from attempts to produce a β-adrenoceptor antagonist that would competitively block β1 (cardiac) receptors but have no effect on β2-receptors. It is classified as a β1 selective (cardioselective) β-adrenergic receptor antagonist with no membranestability activity and no partial agonist activity. It is markedly the most hydrophilic of the currently available β- blockers and thus penetrates the lipid of cell membranes poorly
Apcard is used for: Hypertension, Angina pectoris, Cardiac arrhythmia, Myocardial infarction
Apcard is also used to associated treatment for these conditions: Alcohol Withdrawal Syndrome, Angina Pectoris, Atrial Fibrillation, Heart Failure, High Blood Pressure (Hypertension), Migraine, Myocardial Infarction, Refractory Hypertension, Secondary prevention Myocardial infarction, Supra-ventricular Tachyarrhythmias, Thyrotoxicosis, Ventricular Tachyarrhythmias
|Atenolol Other Names||Atenolol, Atenololum|
6-16% bound in plasma. Atenolol binds to two sites on human serum albumin.
|Therapeutic Class||Beta-adrenoceptor blocking drugs, Beta-blockers|
|Manufacturer||APC Pharma Ltd|
|Last Updated:||June 23, 2021 at 11:16 am|
Hypertension: 50 mg once daily, the daily dose can be raised to 100 to 200 mg.
Angina pectoris: 50 to 100 mg daily.
Cardiac arrhythmia: Apcard in low dose, 25-50 mg once daily, can be used in combination with digoxin to control the ventricular rate in atrial fibration or atrial flutter which is refractory to digoxin alone.
In general, atenolol is well tolerated although in a small number of patients (approximately 2-3%) therapy must be withdrawn because of troublesome symptomatic adverse effects. The commonest of these are cold extrimities, fatigue, vivid dreams, insomnia, diarrhoea, constipation, impotence and paraesthesia. Bronchospasm has been occurred with atenolol although this is very much less common than with the non-selective β-blockers.
Patients already on a β-blocker must be evaluated carefully before Apcard is administered. Apcard may aggravate peripheral arterial circulatory disorders. Impaired Renal Function: Caution should be excised.
Catecholamine-depleting drugs (e.g., Reserpine) and Calcium channel blockers may have an additive effect when given with Apcard. Clonidine and aspirin may have some drug reactions.
Food InteractionNo interactions found.
Volume of Distribution
Total Vd of 63.8-112.5 L. Apcard distributes into a central volume of 12.8-17.5 L along with two peripheral compartments with a combined volume of 51-95 L. Distribution takes about 3 hrs for the central compartment, 4 hrs for the shallower peripheral compartment, and 5-6 hrs for the deeper peripheral compartment.
Total clearance is estimated at 97.3-176.3 mL/min with a renal clearance of 95-168 mL/min.
Pregnancy & Breastfeeding use
Pregnancy Category D. Caution should be exercised when Apcard is administered to a nursing woman.
Apcard is contraindicated for: Second and third degree heart block, Untreated heart failure, Overt cardiac failure, Cardiogenic shock.
Safety and effectiveness in pediatric patients have not been established.
Overdosage with Apcard has been reported with patients surviving acute doses as high as 5 gm. One death was reported in a man who may have taken as much as 10 gm acutely.