Generic

Carvedilol

Indications

Carvedilol is used to treat mild, moderate, or severe ischemic or cardiomyopathic heart failure in combination with digitalis, diuretics, and an ACE inhibitor to slow disease progression as proven by cardiovascular mortality, hospitalization, or the need to change other heart failure drugs. In patients who are unable to tolerate an ACE inhibitor, carvedilol may be utilized. Patients who are not undergoing digitalis, hydralazine, or nitrate treatment may be given carvedilol.

Pharmacology

Carvedilol is a cardiovascular medication that has non-selective antagonism of -adrenergic receptors as its main pharmacological action, but also has some a-adrenergic antagonistic activity. It also acts as an antiproliferator and a scavenger of reactive free oxidant radicals. Hypertension, angina pectoris, and congestive heart failure are all treated with it.

Dosage & Administration

In hypertension: initially, 12.5 mg once daily, increased after 2 days to the usual dose of 25 mg once daily; if necessary the dose may be further increased at intervals of at least 2 weeks to maximum 50 mg daily in single or divided doses. In elderly patients, the initial dose of 12.5 mg daily may provide satisfactory control.

In angina pectoris: the recommended dose for initiation of therapy is 12.5 mg twice daily for the first 2 days. Thereafter, the recommended dosage is 25 mg twice daily. For elderly patients, the maximum daily dose is 50 mg daily in divided doses.

In heart failure: initially, 3.125 mg twice daily (with food) may be given, the dose may be increased at intervals of at least 2 weeks to 6.25 mg twice daily, then to 12.5 mg twice daily, then to 25 mg twice daily. The dose may be increased to the highest dose tolerated, maximum 25 mg twice daily in patients less than 85 kg body-weight and 50 mg twice daily in patients over 85 kg.

Interaction

Digoxin: A single dose of carvedilol combined with a single dose of digoxin resulted in considerably higher levels of digoxin 24 hours later in normal healthy participants. Patients with congestive heart failure who had been stabilized on digoxin were given carvedilol at the same time with no negative side effects. When starting, changing, or stopping carvedilol, it's important to keep a close eye on your digoxin levels.

Rifampin: Rifampin pretreatment resulted in a 60% reduction in Cmax and AUC.

Carvedilol had no effect on warfarin's in vitro plasma protein binding.

Contraindications

Patients with decompensated heart failure requiring intravenous inotropic therapy, bronchial asthma or related bronchospastic conditions, second or third-degree AV block, sick sinus syndrome (unless a permanent pacemaker is in place), cardiogenic shock, or severe bradycardia are all contraindicated for carvedilol.

Side Effects

Postural hypotension, dizziness, headache, fatigue, gastro-intestinal disturbances, bradycardia; occasionally diminished peripheral circulation, peripheral oedema and painful extremities, dry mouth, dry eyes, eye irritation or disturbed vision, impotence, disturbances of micturition, influenza-like symptoms, rarely angina, AV block, exacerbation of intermittent claudication or Raynaud's phenomenon, allergic skin reactions, exacerbation of psoriasis, nasal stuffiness, wheezing, depressed mood, sleep disturbances, paresthesia, heart failure, changes in liver enzymes, thrombocytopenia, leukopenia are also reported.

Pregnancy & Lactation

Because no studies have been done in nursing women and animal studies have demonstrated that carvedilol is excreted in breast milk, carvedilol should not be used while breastfeeding. Carvedilol's safety and efficacy in youngsters have yet to be determined. Because no studies have been done in this category, carvedilol should not be used during pregnancy. Carvedilol has been found to penetrate the placental barrier in animal tests. There is no information on the safety and efficacy of Carvedilol in newborns.

Precautions & Warnings

In the case of hepatic impairment or heart failure, exercise caution. After beginning and after each dose increase, keep a close eye on your clinical status over the next 2-3 hours. Before raising the dose, be sure your kidney function and heart failure aren't getting worse.

Therapeutic Class

Alpha adrenoceptor blocking drugs, Beta-adrenoceptor blocking drugs, Beta-blockers

Storage Conditions

Keep the temperature below 30°C and away from light and moisture. Keep out of children's reach.

Pharmaceutical Name

Incepta Pharmaceuticals Ltd.