Cosmos Pharmaceutical Limited | CARDINOL®
Cosmos Limited is one of the leading manufacturers of pharmaceutical products in Kenya and East Africa. Through our specialized Human Health and Animal Health.
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CARDINOL®

CLINICAL PHARMACOLOGY:

Atenolol is a cardioselective beta blocker. It is reported to lack intrinsic sympathomimetic activity and membrane-stabilising properties. Beta blockers (beta-adrenoceptor blocking drugs or antagonists) are competitive  antagonists of catecholamines at beta-adrenergic receptors in a wide range of tissues. Although they have broadly similar properties they differ in their affinity for beta1 or beta2  receptor subtypes, intrinsic sympathomimetic activity, membrane-stabilising activity, blockade of alpha-adrenergic receptors, and pharmacokinetic properties including differences in lipid solubility. Beta blockers have different affinities for beta1 or  beta2 receptors. Beta1 receptors are found mainly in the heart while beta2 receptors are found in noncardiac tissue including bronchial tissue, peripheral blood vessels , uterus, and pancreas.

Pharmacokinetics:

About 50% of a dose is absorbed following oral administration. Peak plasma concentrations are reached in 2 to 4 hours. Atenolol has low lipid solubility. It crosses the placenta and is distributed into breast milk where concentrations higher than those in maternal plasma have been achieved. Only small amounts are reported to cross the blood-brain barrier, and plasma-protein binding is minimal. The plasma half-life is about 6 to 7 hours. Atenolol undergoes little or no hepatic metabolism and is excreted mainly in the urine.

USES:

Atenolol is used in the management of hypertension, angina pectoris, cardiac arrhythmias and myocardial infarction. It may also be used in the prophylactic treatment of migraine.

DOSAGE   AND   ADMINISTRATION:

Hypertension: Atenolol is given by mouth in a dose of 50 to 100 mg daily as a single dose, although 50mg daily is generally adequate. The full effect is usually evident within 1 to 2 weeks.
Angina Pectoris: 50 to 100 mg daily by mouth, given as single or in divided doses.
Cardiac Arrhythmias: Having controlled the arrhythmia with intravenous Atenolol, a suitable oral maintenance dosage of 50 to 100 mg is given daily as a single dose.
Myocardial infarction: Treatment should be given within 12 hours of the onset of chest pain; Atenolol 5mg should be given by slow intravenous injection at a rate of  1mg per minute and followed after 15 minutes with 50mg by mouth.
Migraine: A dose of 50 to 100mg daily by mouth.

CONTRA-INDICATIONS AND  WARNINGS:
Precautions:

Beta blockers should not be given to patients with bronchospasm or asthma or to those with a history of obstructive airways disease. Other contra-indications include metabolic acidosis, cardiogenic shock, hypotension, severe peripheral arterial disease, sinus bradycardia, second-or third-degree atrioventricular block; caution should be observed in first-degree block. Although beta blockers are used in the management of heart failure, they should not be given to patients with uncontrolled heart failure and treatment should be initiated with great care. Patients with phaeochromocytoma should not receive beta blockers without concomitant alpha-adrenoceptor blocking therapy. Beta blockers may mask the symptoms of hyperthyroidism and of hypoglycaemia. They may unmask myasthenia gravis. Psoriasis may be aggravated. Abrupt withdrawal of beta blockers has sometimes resulted in angina, myocardial infarction, ventricular arrhythmias, and death.

CARDINOL® TABLETS
Paediatric Precaution:

Safety and efficacy of Atenolol in children have not been established.

Pregnancy and Lactation:
Atenolol should be used in pregnancy only when the potential benefits justify the possible risks to the foetus.

Adverse Effects:

Among the most serious adverse effects are heart failure, heart block, and bronchospasm. Troublesome subjective adverse-effects include fatigue and coldness of the extremities. Cardiovascular effects include bradycardia and hypotension; heart failure or heart block may be precipitated in patients with underlying cardiac disorders. Abrupt withdrawal of beta blockers may exacerbate angina and may lead to sudden death. CNS effects include headache, depression, dizziness, hallucinations, confusion, and sleep disturbances including nightmares. Coma and convulsions have been reported following beta-blocker overdosage.

Overdosage:

Many cases of beta-blocker overdosage  are uneventful, but some patients develop severe and occasionally fatal cardiovascular depression. Treatment involves gastric lavage and activated charcoal for patients presenting with a history of recent acute ingestion.

Interactions:

Pharmacodynamic interactions may occur with drugs whose actions enhance or antagonise the various effects of beta blockers at beta1 and beta2 receptors, including their antihypertensive effect, cardiodepressant effect, effect on carbohydrate metabolism, or effect on bronchial beta2 receptors. Drugs that enhance the antihypertensive effects of beta blockers, such as ACE inhibitors, calcium-channel blockers, and clonidine may be useful in controlling hypertension. Drugs that cause hypotension such as aldesleukin and general anaesthetics also enhance the antihypertensive effects of beta blockers while other drugs, for example NSAIDs, antagonise the antihypertensive effects. Use of beta blockers with other cardiac depressants such as antiarrhythmics and rate-limiting calcium-channel blockers can precipitate bradycardia and heart block. In diabetic patients beta blockers can reduce the response to insulin and oral hypoglycaemics through their effects on pancreatic beta receptors. Pharmacokinetic interactions occur with drugs that alter the absorption or metabolism of beta blockers. Drugs that reduce absorption include aluminium salts and bile-acid binding resins such as colestyramine. Metabolism of some beta blockers can be increased by concomitant treatment with drugs such as barbiturates and rifampicin and decreased with drugs such as cimetidine, erythromycin , fluvoxamine and hydralazine. Drugs that alter hepatic blood flow also affect metabolism of some beta blockers. Drugs that influence hepatic metabolism affect beta blockers that are extensively metabolised, such as labetalol, propranolol, and timolol, while beta blockers that are excreted largely unchanged, for example atenolol and nadolol, are unaffected.

PHARMACEUTICAL   PRECAUTIONS:

Store in a dry place below 25ºC. Protect from light. Keep all medicines out of the reach of children.

LEGAL   CATEGORY:
Prescription Only Medicine (POM)
®Regd. TM                                             Ref. No.: INS029/09.06

IMAGES
  • CARDINOL®25 Tablets F/C

    PresentationOrange, circular, biconvex film coated tablet embossed 'COSMOS' on one side and a breakline on the other side. Each film coated tablet contains: Atenolol BP 25mg. Pack size - 28's (2x14's)

  • CARDINOL®50 Tablets F/C

    PresentationOrange, circular, biconvex film coated tablet embossed 'CARDINOL' on one side and '50' on the other side. Each film coated tablet contains: Atenolol BP 50mg. Pack size - 28's (2x14's)

  • CARDINOL®100 Tablets F/C

    PresentationOrange, circular, biconvex film coated tablet embossed 'CARDINOL' on one side and '100' on the other side. Each film coated tablet contains: Atenolol BP 100mg. Pack size - 28's (2x14's)