Each film coated tablet contains Carvedilol 6.25 mg.
Carvedilol is a nonselective beta-adrenergic blocking agent with alpha-1 blocking activity. It is a potent antihypertensive agent. It has the advantage that it is not associated with an increase of the heart rate as observed with other vasodilators. Carvedilol is used to control high blood pressure and to treat patients with mild or moderate congestive heart failure.
Pharmacology: Pharmacokinetics: Carvedilol is well absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism in the liver, the absolute bioavailability is about 25%. Peak plasma concentrations occur 1 to 2 hours after an oral dose. It has high lipid solubility. Carvedilol is more than 98% bound to plasma proteins. It is extensively metabolized in the liver, primarily by the cytochrome P450 isoenzymes CYP2D6 and CYP2C9, and the metabolites are excreted mainly in the bile. The elimination half-life is about 6 to 10 hours. Carvedilol has been shown to accumulate in breast milk in animals.
Carvedilol is a non-cardioselective beta-blocker. It has vasodilating properties, which are attributed mainly to its blocking activity at alpha-1 receptors; at higher doses calcium-channel blocking activity may contribute. It has also antioxidant properties. Carvedilol is reported to have intrinsic sympathomimetic activity and only weak membrane-stabilising activity.
Carvedilol is used in the management of hypertension and angina pectoris, and as an adjunct to standard therapy in sympathomimetic heart failure. It is also used to reduce mortality in patients with left ventricular dysfunction after myocardial infarction.
Hypertension: Initial dose is 12.5 mg once daily, which should be increased to 25 mg once daily after 2 days. If necessary, it may be further increased to maximum 50 mg in single or divided doses at intervals of at least 2 weeks.
Angina: Initial dose is 12.5 mg twice daily which should be increased after 2 days to 25 mg twice daily.
Heart failure: Initial dose is 3.125 mg with food twice daily which should be increased after 2 weeks to 6.25 mg twice daily, then to maximum 25 mg twice daily in patients less than 85 kg body weight and maximum 50 mg twice daily in patients over 85 kg.
Left Ventricular Dysfunction after myocardial infarction: The initial dose is 6.25 mg twice daily, increased after 3 to 10 days, if tolerated, to 12.5 mg twice daily and then to a target dose of 25 mg twice daily. A lower initial dose may be used in symptomatic patients.
Or as prescribed by a physician.
Patients with NYHA class IV decompensated cardiac failure. It is also contraindicated in bronchial asthma, second or third degree AV block, sick sinus syndrome, cardiogenic shock or severe bradycardia. Use of Carvedilol in patients with clinically manifest hepatic impairment is not recommended. Therapy is not to be initiated in severe heart failure.
Beta blockers should not be given to patients with bronchospasm or asthma or to those with a history of obstructive airways disease. This contra-indication generally applies even to those beta-blockers considered to be cardioselective. However, cardioselective beta-blockers may be used with extreme caution when there is no alternative treatment. Other contra-indications include metabolic acidosis, cardiogenic shock, hypotension, severe peripheral arterial disease, sinus bradycardia, and second or third degree AV 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 begun with great care, starting with a low dose and cautiously titrating upwards. Patients with phaeochromocytoma should not be given beta blockers without alpha-adrenoreceptor blocking therapy as well.
Beta blockers may block the symptoms of hyperthyroidism and of hypoglycaemia. They may unmask myasthenia gravis. Psoriasis may be aggravated. Beta blockers may increase the number of attacks of chest pain in patients with Prinzmetal's angina; this occurs especially with non-cardioselective beta blockers, which should be avoided. Beta blockers increase sensitivity to allergens and also the severity of anaphylactoid reactions; patients with a history of anaphylaxis to an antigen while taking beta blockers.
After withdrawal of beta blockers has sometimes resulted in angina, myocardial infarction, ventricular arrythmias and death. Patients on long term treatment with a beta blocker should have their medication stopped gradually over a period of 1 to 2 weeks. In patients undergoing surgery,
beta blockers may reduce the risk of hypotension, the decision to withdraw or continue therapy depends on individual patient risk. If beta blockers are withdrawn, this should take place at least 24 to 48 hours before surgery; if they are continued, atropine may be given to counter increases in vagal tone and anaesthetics causing myocardial depression, such as ether, cyclopropane, and trichloroethylene, are best avoided. It is of greatest importance that the anaesthetist is aware that beta blockers are being given.
Use of beta blockers in pregnancy shortly before delivery has occasionally resulted in bradycardia and other adverse effects such as hypoglycaemia and hypotension in the neonate. Many beta blockers are distributed into breast milk.
Similar precautions apply when beta blockers are used as eye drops since systemic absorption can occur.
Special care should be taken in patients whose cardiac reserve is poor. Heart failure should be satisfactorily controlled before started carvedilol. Carvedilol has beta-blocking activity, so withdrawal should be gradual in patients with ischaemic heart disease. As with other beta-blockers, carvedilol may mask the symptoms of hyperthyroidism and early signs of acute hypoglycemia may be masked in patients with diabetes mellitus; so be careful in using Carvedilol.
Patients taking carvedilol should be warned not to drive or operate machinery if they experience dizziness.
Carvedilol is in the FDA pregnancy category C. This means that it is not known whether Carvedilol will be harmful to an unborn baby. It is not known whether Carvedilol passes into breast milk. Do not take Carvedilol without first talking to a doctor if the patient is pregnant or have a
breast-feeding baby.
Carvedilol is usually well tolerated, although symptomatic postural hypertension may occur mainly on the initiation of therapy or when increasing the dose. Dizziness, headache, fatigue, dry mouth, dry eyes, sleep disturbances, eye irritation or disturbed vision, thrombocytopenia, leucopenia and bradycardia have also been reported.
Beta blockers are generally well tolerated and most adverse effects are mild and transient. Reactions may be more severe after intravenous than oral doses; ocular use has also been associated with systemic adverse effects. The most frequent and serious adverse effects are related to their beta-adrenergic blocking activity. Among the most serious adverse effects are heart failure, heart block, and bronchospasm. Troublesome subjected effects include fatigue and coldness of the extremities; when beta-blockers are used for long-term treatment of asymptomatic diseases such as hypertension, such effects may be an important determinant of patient compliance. Cardiovascular effects include bradycardia and hypotension; heart failure or heart block may be precipitated or worsened in patients with underlying cardiac disorders. Abrupt withdrawal of beta blockers may exacerbate angina and may lead to sudden death.
As with other beta-blockers, Carvedilol may potentiate the effect of other concomitantly administered anti-hypertensive. Pre-treatment with rifampicin resulted in 60% decrease in Cmax and AUG receptor antagonists (e.g. clonidine) potentiate the pressor reaction which may follow sudden withdrawal of treatment with clonidine. Carvedilol, taken together with digoxin results significantly increased digoxin level. Hence, the level of digoxin should be monitored when the dose of carvedilol is initiating or adjusting or discontinuing.
Store at a temperature not exceeding 30°C.
Keep in a dry place away from light and heat.
C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
Carvida 6.25 tab 6.25 mg
30's
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