Carvedilol

Betablocking Agent · Beta-blocker

Indications

Essential hypertension. Angina. Adjunct to diuretics, or ACE inhibitors in symptomatic chronic heart failure. Hypertension of pregnancy, hypertension following MI, hypertensive emergencies.

Dosage

Adults: Essential hypertension: ORAL: Initially, 12.5 mg once daily for two days, then 25 mg once daily. If necessary, titrate at two wk intervals to max 50 mg once daily or in divided doses. Angina: ORAL: Initially 12.5 mg twice daily for 2 days, then increased to 25 mg twice daily. Adjunct to diuretics, or ACE inhibitors in symptomatic chronic heart failure: Initially 3.125 mg twice daily, 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 wks. Patients with severe heart failure or body wt <85 kg: Max 25 mg two times daily; body wt >85 kg: Max 50 mg two times daily. Hypertension of pregnancy: INFUSION: IV: Initially 20 mg/hr, then increased if required to 40 mg/hr after 30 min, then increased if required to 80 mg/hr after 30 min, then increased if required to 160 mg/hr…

Adverse Effects

Postural hypotension, bradycardia, dizziness, headache, fatigue, Gi upset. Reduced peripheral circulation, dry eyes, angina, A-V block, intermittent claudication, skin reaction, hypotension, oedema, headache, visual disturbances, wt gain, asthaenia, fatigue, asthma, dyspnoea, hypercholesterolaemia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: 2nd or 3rd degree A-V block, severe bradycardia, uncontrolled heart failure, asthma, COPD, bronchospasm, cardiogenic shock, sick sinus syndrome, hepatic impairment, severe hypotension, metabolic acidosis, phaeochromocytoma. Marked fluid retention or overload requiring IV inotropic support. Precautions: Poor cardiac reserve. Withdraw gradually in ischaemic heart disease. Hyperthyroidism, diabetes, unstable angina. 1st degree AV block.

Interactions

General anaesthetics, class I antiarrhythmics, verapamil, digoxin, rifampicin, other antihypertensives, cimetidine, clonidine, hypoglycaemics, reserpine, MAOIs, cyclosporin, diltiazem.

Advice to Patient

Take with meals to minimize the risk of orthostatic hypotension. Contact prescriber if there is unrelieved swelling of extremities, difficulty in respiration, fatigue, unusual weight gain (>5 lb per week), unrelieved constipation or diarrhoea or unusual muscle weakness. Check blood pressure and pulse regularly before taking medication. If you have diabetes, regularly check blood glucose level. Change position slowly.

Pharmacokinetics

Onset of action: Antihypertensive effect: Alpha-blockade: Within 30 min. Beta-blockade: Within 1 hr. Peak antihypertensive effect: Approx. 1-2 hrs. Absorption: Oral: Rapid and extensive; but with large first pass effect; delayed with food. Metabolism: Extensively (98%) hepatic. Bioavailability: Immediate release: Approx. 25%-35%. Extended release: Approx. 85% of immediate release. Half-life elimination: Infants and children 6 wks-3.5 yrs: 2.2 hrs. Children and Adolescents 5.5-19 yrs: 3.6 hrs. Adults 7-10 hrs: Some have reported lower values. Adults 24-37 yrs: 5.2 hrs. R(+)-carvedilol: 5-9 hrs. S(-)-carvedilol: 7-11 hrs. Time to peak, plasma: Extended release: Approx. 5 hrs. Excretion: Primarily faeces. Urine (<2%).

Unlicensed Use

Children: Adjunct in heart failure: 2-18 yr initially 50 mcg/kg (max 3.125 mg) twice daily, double dose at intervals of at least 2 wk up to 350 mcg/kg (max 25 mg) twice daily.

Brands with this active ingredient

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.