Indications
Congestive Heart Failure: Carvedilol is indicated for the treatment of mild or moderate heart failure of ischemic or cardiomyopathic origin, in conjunction with digitalis, diuretics and ACE inhibitors, to reduce the progression of disease as evidenced by cardiovascular death, cardiovascular hospitalization, or the need to adjust other heart failure medications. Carvedilol may be used in patients unable to tolerate an ACE inhibitor. Carvedilol may be used in patients who are or are not receiving digitalis, hydralazine or nitrate therapy.Hypertension: Carvedilol is also indicated for the management of essential hypertension. It can be used alone or in combination with other antihypertensive agents especially with thiazide type diuretics.
Pharmacology
Carvedilol is a non selective β-adrenergic blocking agent which causes vasodilation by blocking the activity α-1 receptors. It exerts antihypertensive effect partly by reducing total peripheral resistance and vasodilation.
Dosage & Administration
Essential hypertension
Adults: The initial dosage is 12.5 mg once daily for the first two days. Thereafter a dose of 25 mg once daily is recommended. If the effect is inadequate, the daily dose may be increased after a minimum of two weeks to 50 mg taken as one or two individual doses. The maximum daily dose in hypertension is 50 mg.
Elderly patients: Initially 12.5 mg once daily. In some patients this dose is sufficient for adequate control of blood pressure. If the effect is inadequate, the daily dose may be increased stepwise at intervals of at least two weeks up to a maximum of 50 mg taken as one or two individual doses.
Angina pectoris
The initial dosage is 12.5 mg twice daily for the first two days. Thereafter a dose of 25 mg twice daily is recommended. If the effect is inadequate, the dose may be increased stepwise at intervals of at least two weeks up to a maximum daily dose of 100 mg taken as two individual doses.
Elderly patients: In general a dose of 25 mg twice daily should not be exceeded.
Treatment of mild to severe heart failure (NYHA class II–IV)
The dosage must be individually determined and the patient must be closely monitored during the titration phase. The dose of digitalis, diuretics and ACE inhibitor should have been stabilised before the start of Dilatrend® therapy. The recommended dosage for initiation of therapy is 3.125 mg twice daily (½ a tablet of Dilatrend® 6.25 mg twice daily) for two weeks. If this dose is tolerated, the dose can be increased progressively at intervals of at least two weeks to 6.25 mg twice daily (1 tablet of Dilatrend® 6.25 mg twice daily), then to 12.5 mg twice daily (1 tablet of Dilatrend® 12.5 mg twice daily), and then to 25 mg twice daily (1 tablet of Dilatrend® 25 mg twice daily). The dose should be increased to the highest level that the patient tolerates. The maximum recommended dose is 25 mg twice daily in patients weighing up to 85 kg and 50 mg twice daily in patients weighing more than 85 kg. Before each dose increment, the physician should examine the patient for signs and symptoms of deteriorating heart failure, vasodilation (fall in blood pressure, dizziness) or bradycardia. Transient deterioration of heart failure or fluid retention should be treated with increased doses of diuretics, although it will occasionally be necessary to reduce the dose of Dilatrend® or to interrupt treatment temporarily. If treatment with Dilatrend® is interrupted for more than two weeks, it should be reinitiated with a dose of 3.125 mg; this dose should then be increased at intervals of two weeks, as indicated above. Signs and symptoms of vasodilation should be treated initially with a reduction in the dose of diuretic. If they persist, the dose of the ACE inhibitor should be reduced, after which the dose of Dilatrend® should be reduced. Under these circumstances the dose of Dilatrend® should not be increased until the signs and symptoms of deterioration of heart failure or vasodilatation have improved. The safety and efficacy of Dilatrend® in patients under 18 years of age have not been investigated.
Patients with renal impairment: No reduction in the initial dose is required in patients with renal impairment (see Pharmacokinetics, Pharmacokinetics in special patient populations).
Patients with hepatic impairment: Dilatrend® is contraindicated in patients with clinically manifest liver failure (see Contraindications, Clinically manifest liver failure’ and Pharmacokinetics).
Adults: The initial dosage is 12.5 mg once daily for the first two days. Thereafter a dose of 25 mg once daily is recommended. If the effect is inadequate, the daily dose may be increased after a minimum of two weeks to 50 mg taken as one or two individual doses. The maximum daily dose in hypertension is 50 mg.
Elderly patients: Initially 12.5 mg once daily. In some patients this dose is sufficient for adequate control of blood pressure. If the effect is inadequate, the daily dose may be increased stepwise at intervals of at least two weeks up to a maximum of 50 mg taken as one or two individual doses.
Angina pectoris
The initial dosage is 12.5 mg twice daily for the first two days. Thereafter a dose of 25 mg twice daily is recommended. If the effect is inadequate, the dose may be increased stepwise at intervals of at least two weeks up to a maximum daily dose of 100 mg taken as two individual doses.
Elderly patients: In general a dose of 25 mg twice daily should not be exceeded.
Treatment of mild to severe heart failure (NYHA class II–IV)
The dosage must be individually determined and the patient must be closely monitored during the titration phase. The dose of digitalis, diuretics and ACE inhibitor should have been stabilised before the start of Dilatrend® therapy. The recommended dosage for initiation of therapy is 3.125 mg twice daily (½ a tablet of Dilatrend® 6.25 mg twice daily) for two weeks. If this dose is tolerated, the dose can be increased progressively at intervals of at least two weeks to 6.25 mg twice daily (1 tablet of Dilatrend® 6.25 mg twice daily), then to 12.5 mg twice daily (1 tablet of Dilatrend® 12.5 mg twice daily), and then to 25 mg twice daily (1 tablet of Dilatrend® 25 mg twice daily). The dose should be increased to the highest level that the patient tolerates. The maximum recommended dose is 25 mg twice daily in patients weighing up to 85 kg and 50 mg twice daily in patients weighing more than 85 kg. Before each dose increment, the physician should examine the patient for signs and symptoms of deteriorating heart failure, vasodilation (fall in blood pressure, dizziness) or bradycardia. Transient deterioration of heart failure or fluid retention should be treated with increased doses of diuretics, although it will occasionally be necessary to reduce the dose of Dilatrend® or to interrupt treatment temporarily. If treatment with Dilatrend® is interrupted for more than two weeks, it should be reinitiated with a dose of 3.125 mg; this dose should then be increased at intervals of two weeks, as indicated above. Signs and symptoms of vasodilation should be treated initially with a reduction in the dose of diuretic. If they persist, the dose of the ACE inhibitor should be reduced, after which the dose of Dilatrend® should be reduced. Under these circumstances the dose of Dilatrend® should not be increased until the signs and symptoms of deterioration of heart failure or vasodilatation have improved. The safety and efficacy of Dilatrend® in patients under 18 years of age have not been investigated.
Patients with renal impairment: No reduction in the initial dose is required in patients with renal impairment (see Pharmacokinetics, Pharmacokinetics in special patient populations).
Patients with hepatic impairment: Dilatrend® is contraindicated in patients with clinically manifest liver failure (see Contraindications, Clinically manifest liver failure’ and Pharmacokinetics).
Contraindications
Carvedilol is contraindicated in patients with severe chronic cardiac 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. Use of carvedilol in patients with clinically manifested hepatic impairment is not recommended. Carvedilol is contraindicated in patients with hypersensitivity to the drug.
Side Effects
Side effects include dizziness, headache, fatigue, gastrointestinal disturbances, postural hypotension, peripheral oedema, bradycardia, dry mouth, dry eyes, eye irritation or disturbed vision, impotence, disturbances of micturition, and influenza like symptoms. Rarely angina, AV block, exacerbation of intermittent claudication or Raynaud’s phenomenon, allergic skin reactions, nasal stuffiness, wheezing, depressed mood, sleep disturbances, paresthesia, heart failure, changes in liver enzymes, thrombocytopenia, leucopenia are reported.
Pregnancy & Lactation
Animal studies have shown adverse effects on the fetus (see Preclinical data) and no data are available in humans. Dilatrend® has been found in the milk of animals. Therefore Dilatrend® must not be used during pregnancy or lactation.
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