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Atenolol

Systems	Cardiovascular and Peripheral Vascular System
Category	Selective B1 Blocker

Pharmacokinetics

Atenolol is well absorbed after oral administration, it undergoes extensive hepatic (first pass) metabolism. Its bioavailability is 40%. It has a large volume of distribution and is less completely metabolised before its excretion via urine. Because of hepatic metabolism, a part of the oral dose may not reach the peripheral circulation, so the plasma half-life doesn't correlate with the duration of the therapeutic effects, which is relatively long lasting. This is because the plasma 1/2 life decreases exponentially, following first order kinetics while the effect decreases linearly following zero order kinetics.

Indications

Atenolol 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 need for blood and oxygen by reducing its workload. They also help to maintain the cardiac rhythm.

Routes of Administration and Dosage

Oral dose : For angina : Adults = 50 to 100 mg once a day. For hypertension: Adults: 25 to 100 mg once a day. Children : Dose must be determined For treatment after a MI : Adults: 50 mg ten minutes after the last intravenous dose, followed by another 50 mg twelve hours later. Then 100 mg once a day or 50 mg two times a day for six to nine days or until discharge from hospital. For injection dosage form: For treatment of MI : Adults : 5 mg given over 5 minutes. The dose is repeated ten minutes later.

Contra Indications

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

Precautions

Allergies : Allergic reaction to the beta-blocker. Pregnancy : Use of beta-blockers during pregnancy has been associated with hypoglycaemia, dyspnoea, bradycardia, and hypotension in the newborn infant. Breast-feeding : Atenolol may pass into breast milk. Problems such as bradycardia, hypotension, and dyspnoea have been reported in nursing babies. Older adults : Some side 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

Atenolol sometimes increases 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 increases in pulse rate and hypertension, and may prolong the hypoglycemia. Calcium channel blockers (bepridil, diltiazem, felodipine, flunarizine, 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. With Monoamine oxidase (MAO) inhibitors : taking beta-blockers within 2 weeks of taking monoamine oxidase (MAO) inhibitors may cause severe hypertension.

Brand Names

Aloten (Core), Altol ( Indoco ), Angitol ( Ind-Swift ), Antipress (Saga Labs ), Atcardil (Sun Pharma ), AteCard (Dabur), Atecor (Win-Medicare), Atelol (Themis Pharma), Aten (Kopran), Atenex (Recon), Atenova (Lupin), Atormin (PCI), Atpark (Parke Davis), Beta (Stadmed), Betacard (Torrent), Betanol (Unisearch), beten (Sigma Labs), Biduten (Croydon), BP-NOL (Elder), Catenol (Alidac), Eucard (Malladi Drugs), Hipres (Cipla), Lakten-50 (Shalaks), Lonol (Khandelwal), Normolol (Pace, SOL), Pertenol (Karnataka Antibiotics), Telol (Max), Tenase (Jenburkt), Tenolol (IPCA), Tensicard (Troikaa), Tensimin (Unique).