Carvedilol

Indications
 Oral
Hypertension
Adult: Initially, 12.5 mg once daily increased to 25 mg once daily after 2 days. Alternatively, initial dose of 6.25 mg bid increased to 12.5 mg bid after 1-2 wk, increased further if necessary to 50 mg once daily or in divided doses.
Elderly: 12.5 mg once daily.
Oral
Angina pectoris
Adult: Initially, 12.5 mg bid increased to 25 mg bid after 2 days.
Oral
Heart failure
Adult: Initially, 3.125 mg bid, doubled to 6.25 mg bid after 2 wk if tolerated, then gradually increased to the max dose the patient can tolerate at intervals of not <2 wk. Max dose: >85 kg: 50 mg bid; <85 kg: 25 mg bid.
Oral
Left ventricular dysfunction post myocardial infarction
Adult: Initially: 6.25 mg bid, if tolerated, after 3-10 days, increase to 12.5 mg bid and then to a target dose of 25 mg bid.
Contraindications
 Hypersensitivity; severe chronic heart failure, bronchial asthma or related bronchospastic conditions; severe hepatic impairment. Patients with NYHA class IV cardiac failure, 2nd or 3rd ° AV block, sick sinus syndrome (unless a permanent pacemaker is in place), cardiogenic shock or severe bradycardia. Lactation.
Warnings / Precautions
 Avoid abrupt withdrawal as it may precipitate thyroid storm or exacerbate hyperthyroidism. Liver injury; vascular disease, renal failures, suspected phaeochromocytoma and prinzmetal's variable angina; worsening cardiac failure or fluid retention during increase in dosage of carvedilol; diabetic patients. Pregnancy.
Adverse Reactions
 Bradycardia, AV block, angina pectoris, hypervolaemia, leucopenia, hypotension, peripheral oedema, allergy, malaise, fluid overload, melena, periodontitis, hyperuricaemia, hyponatraemia, increased alkaline phosphatase, glycosuria, prothrombin time, SGPT and SGOT levels, purpura, somnolence, impotence, albuminuria, hypokinesia, nervousness, sleep disorder, skin reaction, tinnitus, dry mouth, anaemia, sweating, fatigue, arthralgia, aggravation, dizziness. Diarrhoea, nausea, vomiting, insomnia, hypercholesterolaemia, weight gain, abnormal vision, rhinitis, pharyngitis and hypertriglyceridaemia.
Overdose Reactions
 Symptoms include severe hypotension, bradycardia, cardiac insufficiency, cardiogenic shock and cardiac arrest. Respiratory problems, bronchospasms, vomiting, lapses of consciousness and generalised seizures may also occur. Place the patient in a supine position. Gastric lavage or pharmacologically induced emesis may be used shortly after ingestion.
Drug Interactions
 Potentiates insulin-induced hypoglycaemic action. Concurrent use with catecholamine-depleting agents and β-receptor blockers may cause marked hypotension. Serum levels may be increased by fluoxetine. May increase serum levels of ciclosporin and digoxin.
Potentially Fatal: Rifampin pretreatment results in a decreased Cmax and AUC. Combination with verapamil can lead to severe bradycardia and myocardial depression.
See Below for More carvedilol Drug Interactions
Food Interactions
 Food reduces rate of absorption and risk of hypotension.
Mechanism of Actions
 Carvedilol causes vasodilation by blocking the activity of α-blockers, mainly at alpha-1 receptors. It exerts antihypertensive effect partly by reducing total peripheral resistance and vasodilation. It is used in patients with renal impairment, NIDDM or IDDM.
Absorption: Absorbed well from the GI tract (oral); peak plasma concentrations after 1-2 hr.
Distribution: Enters breast milk. Protein-binding: >98%.
Metabolism: Hepatic: Considerable first-pass effect.
Excretion: Via bile (as metabolites); 6-10 hr (elimination half-life).
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store below 30°C.
ATC Classification
 C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
Storage
 Oral: Store below 30°C.
Available As
  • Carvedilol 10 mg
  • Carvedilol 12.5 mg
  • Carvedilol 20 mg
  • Carvedilol 25 mg
  • Carvedilol 3.125 mg
  • Carvedilol 6.25 mg
  • Carvedilol 6.5 mg

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