Carveshin
Carvedilol 3.125/ 6.25/ 12.5 Indication
Carvedilol is indicated for the management of essential hypertension. It can be used alone or in combination with other antihypertensive agents. Carvedilol is indicated for the treatment of mild or moderate congestive heart failure in conjunction with digitalis, diuretics or ACE inhibitors.
Dosage & Administration
Adults:
Essential Hypertension
Initially 12.5 mg once daily for 2 days, then increased to 25 mg once daily; increased if necessary up to 50 mg daily, dose to be increased at intervals of at least 2 weeks and can be given as a single dose or in divided doses.
Angina
Initially 12.5 mg twice daily for 2 days, then in-creased to 25 mg twice daily.
Heart Failure
Initially 3.125 mg twice daily, dose to be taken with food, then increased to 6.25 mg twice daily, then increased to 12.5 mg twice daily, then increased to 25 mg twice daily, dose should be increased at intervals of at least 2 weeks up to the highest tolerated dose, maximum of 25 mg twice daily in p...
Elderly:
Essential Hypertension
Initially 12.5 mg twice daily, initial dose may provide satisfactory control.
Composition
Each film-coated tablet contains:
Carvedilol B.P ... 3.125 mg/ 6.25 mg/ 12.5 mg.
Description
Carvedilol is a non-selective β-adrenergic blocking agent with α1 - blocking activity. Chemically it is (2RS)-1-(9H-Carbazol-4-yloxy)-3-[(2-(2-methoxy- phenoxy)ethyl]amino]propan-2-ol. Carvedilol is a racemic mixture. Carvedilol is a white to off-white powder with a molecular weight of 406.5 and mol...
Clinical Pharmacology
Carvedilol has both α1 selective & β antagonistic effects. Carvedilol antagonizes the actions of catecholamines more potently at β receptors than α1 receptors.
Carvedilol is racemic mixture in which non-selective β adrenoreceptor blocking activity is present in S(-) enantiomers & α-adrenoreceptor blocking activity is present in both R (+) & S (-) enantiomers at equal potency.
Carvedilol is cardiovascular agent with β blocking & vasodilating properties. The beta blockade is non-cardioselective & is devoid of intrinsic sympathomimetic activity. Vasodilation is predominantly mediated through α1 receptor antagonism.
Pharmacokinetics
Carvedilol is rapidly & extensively absorbed after oral administration with peak plasma concentration achieved after approximately 1 hour. The absolute oral bioavailability is approximately 25-35%. The apparent mean terminal elimination half-life of carvedilol ranges from 6-8 hours. Carvedilol is ex...
Contraindication
Carvedilol is contraindicated in patients with acute or decompensated heart failure, second & third degree heart block, severe bradycardia, cardiogenic shock, uncontrolled heart failure, history of asthma or bronchospasm, hepatic impairment and hypersensitivity to carvedilol.
Precaution
Use with caution in patients with heart failure who also have renal impairment, low blood pressure, ischaemic heart disease, or diffuse vascular disease. It should not be administered during pregnancy or lactation. It is not recommended for children.
Adverse Effects
Carvedilol is generally well tolerated. It rarely causes dry eyes, rashes and hypersensitivity reaction. Headache, dizziness, fatigue, postural hypotension, gastrointestinal upset and brady-cardia have been observed.
Drug Interaction
Many drugs interfere or worsen side effects. Therefore, carvedilol should not be taken together or within 2 weeks of taking MAO inhibitors. Carvedilol can enhance the blood sugar-reducing effects of insulin & oral hypoglycemic agents & therefore, in such patients, regular monitoring of blood glucose...
Concomitant administration of clonidine & calcium channel blockers (verapamil or diltiazem) potentiated blood pressure & heart lowering effects of carvedilol. Plasma digoxin levels may be increase-d in patient co-administered carvedilol & digoxin. Increased monitoring of digoxin level is recommended...
Storage
Store below 30OC in cool and dry place. Protect from light and moisture. Keep out of reach and sight of children.
Presentation
10 x 10’s Alu-Alu Blisters.