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It is an arylethanolamine non-specific ß-adrenorecptor antagonist with ? -blocking activity. It exerts antihypertensive effect partly by reducing total peripheral resitance and vasodiation by blocking ?1 adrenorecptors and by inhibiting ß-adrenorecptor-mediated compensatory mechanisms.
INDICATIONS: Hypertension and congestive heart failure.
DOSAGE: Hypertension: Initially 6.25 mg twice daily. It tolerated, after 7-14 days, increase to 12.5 mg twice daily if needed again increase the dose up to 25 mg twice daily, after 7-14 days. Max total daily dose 50 mg.
Congestive heart failure: Start with 3.125 mg twice daily for 2 weeks. If tolerated, rise to 6.25 mg twice daily and then double the dose every 2 weeks to the level tolerated by patients. Max dose is 25 mg and 50 mg for patients weighing less than 85 kgs and more than 85 kgs respectively.
CONTRAINDICATIONS: Hypersensitivity, patients with NYHA class IV decompensate cardiac failure requiring IV isotropic therapy, bronchial asthma, second or third-degree AV block, Sick Sinus syndrome, cardiogenic shock or severe bradycardia, severe hepatic impairment, lactation.
SPECIAL PRECAUTIONS: Before starting the treatment, laboratory confirmation of liver injury is very much essential. Abrupt withdrawal of ß -blockers may result in result in exacerbation of the symptoms of hyperthyroidism. During the initiation of therapy, avoid driving or operating machinery.
Pregnancy: Safety not established.
Children: Safety not established.
SIDE-EFFECTS: Increased sweating, fatigue, oedema, bradycardia, hypotension (including postural), hyperglycaemia, hypercholesterolemia, bronchitis, insomnia, impotency, skin reactions, tinnitus, anemia and even sudden death.
DRUG-INTERACTIONS: Rifampicin decreases while cimetidines increase the AUC & Cmax of carvedilol. Increase in Steady-state AUC and trough concentration of digoxin. Catecholamine-depleting agents & beta-receptors blockers results in hypotension or severe bradycardia.