Description
Indications |
Listed in Dosage. |
Dosage |
Adult : PO Hypertension Initially, 12.5 mg once daily for 2 days, increased to 25 mg once daily. May gradually increase further at intervals of at least 2 weeks, if necessary. Max: 50 mg daily. Chronic stable angina Initially, 12.5 mg bid for 2 days, increased to 25 mg bid. May gradually increase further at intervals of at least 2 weeks, if necessary. Max: 100 mg/day in 2 divided doses. Heart failure Mild to severe: Initially, 3.125 mg bid for 2 weeks. If tolerated, increase gradually to 6.25 mg bid at intervals of at least 2 weeks, followed by 12.5 mg bid, then 25 mg bid. Max: <85 kg: 25 mg bid. >85 kg: 50 mg bid, if condition is not severe. Left ventricular dysfunction post myocardial infarction Initially, 6.25 mg bid, increased after 3-10 days (based on tolerability) to 12.5 mg bid, and up to target dose of 25 mg bid. Lower initial dose of 3.125 mg bid may be used in symptomatic patients and rate of up-titration may be slowed if clinically indicated. |
Dosage Details |
Oral Left ventricular dysfunction post myocardial infarctionAdult: Initially, 6.25 mg bid, increased after 3-10 days (based on tolerability) to 12.5 mg bid, and up to target dose of 25 mg bid. Lower initial dose of 3.125 mg bid may be used in symptomatic patients and rate of up-titration may be slowed if clinically indicated.Oral Hypertension Adult: Initially, 12.5 mg once daily for 2 days, increased to 25 mg once daily. May gradually increase further at intervals of at least 2 weeks, if necessary. Max: 50 mg daily. Oral Adult: Mild to severe: Initially, 3.125 mg bid for 2 weeks. If tolerated, increase gradually to 6.25 mg bid at intervals of at least 2 weeks, followed by 12.5 mg bid, then 25 mg bid. Max: <85 kg: 25 mg bid. >85 kg: 50 mg bid, if condition is not severe. Oral Adult: Initially, 12.5 mg bid for 2 days, increased to 25 mg bid. May gradually increase further at intervals of at least 2 weeks, if necessary. Max: 100 mg daily in 2 divided doses. |
Hepatic Impairment |
Severe: Contraindicated. |
Administration |
Should be taken with food. |
Contraindications |
Patient with decompensated heart failure requiring IV inotropic treatment, bronchial asthma or related bronchospastic conditions, 2nd- or 3rd-degree AV block without permanent pacemaker, severe bradycardia (<50 bpm), sick sinus syndrome, cardiogenic shock, untreated phaeochromocytoma, Severe hepatic impairment. |
Special Precautions |
Patient with salt and volume depletion, hypotension; ischaemic heart disease, Prinzmetal’s variant angina, diabetes mellitus, thyrotoxicosis, peripheral vascular disease, psoriasis. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation. |
Adverse Drug Reactions |
Significant: Hypotension with or without syncope, bradycardia. Blood and lymphatic system disorders: Anaemia. Cardiac disorders: Dyspnoea, pulmonary oedema. Eye disorders: Visual impairment, eye irritation, dry eye. Gastrointestinal disorders: Nausea, diarrhoea, vomiting, dyspepsia, abdominal pain. General disorders and admin site conditions: Asthenia, fatigue. Infections and infestations: Bronchitis. Metabolism and nutrition disorders: Oedema, hypervolaemia, weight gain, hypercholesterolaemia, hyperglycaemia, hypoglycaemia. Musculoskeletal and connective tissue disorders: Pain in extremities, arthralgia. Nervous system disorders: Dizziness, headache. Psychiatric disorders: Depression. Renal and urinary disorders: Micturition disorders, abnormal renal function, renal failure. Vascular disorders: Orthostatic hypotension, peripheral vascular disease. |
Pregnancy Category (US FDA) |
PO: C |
Patient Counselling |
This drug may cause syncope during initial therapy, if affected, do not drive or operate machinery. |
Monitoring Parameters |
Monitor blood pressure, heart rate, BUN, blood glucose (diabetics), renal and liver function. |
Overdosage |
Symptoms: Severe hypotension, bradycardia, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, vomiting, disturbed consciousness and generalised seizures. Management: Initiate supportive treatment. Monitor vital parameters. Administer atropine IV for excessive bradycardia. In the case of drug resistant bradycardia, initiate pacemaker therapy. To support ventricular function, administer glucagon IV or sympathomimetics (e.g. dobutamine, isoprenaline). For peripheral vasodilation, administer norepinephrine with continuous monitoring of the circulation. For bronchospasm, administer β-sympathomimetics (aerosol or IV) or aminophylline via slow IV inj or infusion. Slow IV inj of diazepam or clonazepam may be given for seizures. |
Drug Interactions |
Additive effect with Ca channel blockers (e.g. diltiazem, verapamil), amiodarone, MAO inhibitors, reserpine, guanfacine, methyldopa. May increase atrioventricular conduction time and decrease heart rate with digitalis glycosides. Increased serum concentrations of ciclosporin. Increased hypoglycaemic effect of insulin and oral antidiabetics. May cause synergistic, negative inotropic and hypotensive effect with anaesthetics. Serum concentration may be reduced by CYP450 inducers (e.g. rifampicin, barbiturates) or increased by CYP450 inhibitors (e.g. ketoconazole, cimetidine, fluoxetine, haloperidol, erythromycin). Increased vasoconstriction effect with ergotamine. |
Food Interaction |
Decreased rate of absorption and risk of orthostatic hypotension with food. |
Mechanism of Action |
Description: Carvedilol is a non-selective β-blocker. It reduces peripheral vascular resistance by selective α1 receptor blockade and suppresses renin-angiotensin system through non-selective β-blockade. Carvedilol has weak membrane stabilising properties and has no intrinsic sympathomimetic activity. Onset: Antihypertensive: Within 30 minutes (α-blockade); within 1 hour (β-blockade). Pharmacokinetics: Absorption: Rapidly and extensively absorbed from the gastrointestinal tract, undergoes first pass effect. Rate of absorption is delayed with food. Absolute bioavailability: Approx 25-35% (immediate release). Time to peak plasma concentration: Approx 1 hour (immediate release); approx 5 hours (extended release). Distribution: Distributed into extravascular tissues and is highly lipophilic. Plasma protein binding: >98% primarily to albumin. Volume of distribution: 115 L. Metabolism: Extensively metabolised in the liver via CYPD2D6 and CYP2C9 enzymes by glucuronidation and aromatic ring oxidation, oxidative metabolites are further metabolised by conjugation via glucuronidation and sulfation. Excretion: Primarily via faeces; urine (<2%, unchanged). Elimination half-life: 7-10 hours. |
Storage |
Store below 30°C. Protect from moisture. |
MIMS Class |
Beta-Blockers |
ATC Classification |
C07AG02 – carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases. |
