Indications

Carvedilol is used in combination with digitalis, diuretics, and ACE inhibitors to treat ischemic heart failure or mild, moderate, or severe cardiomyopathy to reduce disease progression, such as cardiovascular death, cardiovascular hospitalization, or the need to adjust other medications for heart failure. Carvedilol can be used in patients who cannot tolerate ACE inhibitors. Carvedilol can be used in patients not receiving treatment with digitalis, hydralazine, or nitrate.

Pharmaceutical Name

Incepta Pharmaceuticals Ltd.

Pharmacology

Carvedilol is a cardiovascular drug whose main pharmacological action is to non-selectively antagonize β-adrenergic receptors, but it also has obvious adrenergic antagonist activity. It also has antiproliferative properties and is an active free radical scavenger. It is used to treat hypertension, angina pectoris, and congestive heart failure.

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: In normal healthy volunteers, a single dose of carvedilol and a single dose of digoxin will cause a significant increase in digoxin levels after 24 hours. Carvedilol was also administered to patients with stable congestive heart failure with digoxin without adverse reactions. When initiating, adjusting, or stopping the carvedilol dose, increased digoxin monitoring is recommended. 

Rifampin: Pretreatment with rifampin causes Cmax and AUC to increase 60 °. 

Warfarin: Carvedilol does not change the binding of warfarin to plasma proteins in vitro. 

Clonidine: β-receptor antagonists can enhance the pressure increase that may occur after abrupt cessation of clonidine treatment, although theoretically the blocking effect of carvedilol should change the increase in pressure.

Contraindications

Carvedilol is contraindicated for decompensated heart failure, bronchial asthma or related bronchospasm, second- or third-degree atrioventricular block, sick sinus syndrome (unless it has been placed permanently). Pacemaker), cardiogenic shock or severe patients with bradycardia.

Side Effects

Orthostatic hypotension, dizziness, headache, fatigue, gastrointestinal disorders, bradycardia; occasionally reduced peripheral circulation, peripheral edema and pain in the limbs, dry mouth, dry eyes, eye irritation or impaired vision, impotence, urinary disorders, flu -Like symptoms, rare angina, atrioventricular block, intermittent claudication or worsening Raynaud’s phenomenon, skin allergic reactions, worsening psoriasis, nasal congestion, wheezing, low mood, sleep disturbance, paresthesia, heart failure, liver enzyme changes, thrombocytopenia , Leukopenia has also been reported.

Pregnancy & Lactation

Carvedilol should not be used during lactation because it has not been studied in breastfeeding women and animal studies have shown that carvedilol is excreted in human milk. The safety and efficacy of carvedilol in children have not been established. Carvedilol should not be used during pregnancy as it has not been studied in this group. Animal studies have shown that carvedilol can cross the placental barrier. There is no information on the safety and efficacy of carvedilol in newborns.

Precautions & Warnings

Be careful in liver failure and heart failure, monitor the clinical status for 23 hours after the start and after each dose increase. Before increasing the dose, make sure that kidney function and heart failure have not worsened.

Therapeutic Class

Alpha-adrenergic receptor blockers, β-adrenergic receptor blockers, β-adrenergic blockers

Storage Conditions

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.