Carvedilol

Indications

Carvedilol is used for: Hypertension, Congestive heart failure, Myocardial infarction, Left ventricular dysfunction, Angina pectoris

Adult Dose

Congestive Heart Failure Immediate release 3.125 mg PO q12hr for 2 weeks, then increased every 2 weeks as tolerated to 6.25 mg, 12.5 mg, or 25 mg PO twice daily Maximum recommended dosage (mild-to-moderate heart failure): <85 kg, 25 mg PO q12hr; >85 kg: 50 mg PO twice daily Maximum recommended dosage (severe heart failure): 25 mg PO twice daily Extended release 10 mg/day PO; maintained for 1-2 weeks if tolerated; may be increased to 20 mg/day, 40 mg/day, or 80 mg/day PO if necessary Hypertension Immediate release: 6.25 mg PO twice daily initially; after 7-14 days, increased as tolerated, first to 12.5 mg PO twice daily and then to 25 mg PO twice daily Extended release: 20 mg/day PO; maintained for 1-2 weeks if tolerated; may be increased to 40 mg/day PO if necessary; not to exceed 80 mg/day PO Left Ventricular Dysfunction Following Myocardial Infarction Immediate release: 3.125-6.25 mg PO q12hr initially; after 3-10 days, increased as tolerated, first to 12.5 mg PO q12hr and then to 25 mg PO q12hr (target dosage) Extended release: 10-20 mg/day PO; increased every 3-10 days as tolerated up to 80 mg/day PO (target dosage) Angina pectoris 25-50 mg PO twice daily Hepatic impairment: Contraindicated in severe liver impairment

Child Dose

Safety and efficacy not established

Renal Dose

Renal impairment: No dosage adjustments necessary

Administration

Should be taken with food.

Contra Indications

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.

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. Lactation: Unknown whether drug is excreted in milk; not recommended

Pregnancy-Lactation

Pregnancy category: C; D in 2nd and 3rd trimesters

Interactions

Decreased serum levels w/ rifampicin. Combination w/ Ca channel blockers (e.g. verapamil and diltiazem) can lead to bradycardia and myocardial depression. Potentiates insulin-induced hypoglycaemic action. May increase hypoglycaemic effects of antidiabetic agents. Increased risk of bradycardia w/ digoxin. Increased risk of hypotension and bradycardia w/ reserpine, MAOIs, clonidine. May increase ciclosporin concentrations. Concurrent use w/ ether, cyclopropane, trichloroethylene may increase the risk of hypotension and heart failure.

Adverse Effects

Side effects of Carvedilol : >10% Dizziness (2-32%),Fatigue (4-24%),Hypotension (9-20%),Weight gain (10-12%),Hyperglycemia (5-12%),Diarrhea (1-12%) 1-10% Bradycardia (2-10%),Nausea (2-9%),Cough (5-8%),Headache (5-8%),Atrioventricular block, edema (1-7%),Angina (1-6%),Hpercholesterolemia (1-4%),Hypertriglyceredemia (1%),Vomiting (1-6%),Dyspnea (>3%),Syncope (3%),Rhinitis (2%) Frequency Not Defined Hypertension,Palpitations,Insomnia,Somnolence,Skin rash,Hepatotoxicity,Impotence,Bronchospasm,Rales,Depression,Decreased exercise tolerance,Raynaud phenomenon,Increased triglyceride levels and insulin resistance with decreased high-density lipoprotein (HDL) levels

Mechanism of Action

Carvedilol is a nonselective beta-adrenoreceptor and alpha-adrenergic blocking activity. It exerts antihypertensive effect partly by reducing total peripheral resistance and vasodilation.