Carvilol

Carvilol

carvedilol

Manufacturer:

Darya-Varia

Marketer:

Darya-Varia
Full Prescribing Info
Contents
Carvedilol.
Description
Each tablet CARVILOL 6.25 contains: Carvedilol 6.25 mg.
Each tablet CARVILOL 25 contains: Carvedilol 25 mg.
Action
Pharmacology: Carvedilol is a β-adrenoceptor antagonist which also causes peripheral vasodilation primarily via α1-adrenergic blockade. Carvedilol produces its antihypertensive effect partly by reducing total peripheral resistance by blocking α1-adrenoceptor and by preventing β-adrenoceptor-mediated compensatory mechanisms.
Dosage adjustment in renal impaired patients is not required. However, peak plasma carvedilol concentrations and bioavailability are significantly increased in patients with severe hepatic impairment (e.g. cirrhosis) and the use of carvedilol in these patients is not recommended.
Indications/Uses
Congestive heart failure: Carvedilol is indicated for the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin, in conjunction with digitalis, diuretics, and ACE inhibitor, to reduce the progression of disease as evidenced by cardiovascular death, cardiovascular hospitalization, or the need to adjust other heart failure medicatiom.
Carvedilol may be used in patients unable to tolerate an ACE inhibitor and in patients who are or not receiving digitalis, hydralazine or nitrate therapy.
Essential hypertension: Carvedilol is indicated for the management of essential hypertension. It can be used alone or in combination with other antihypertensive agents, especially Thiazide-type diuretics.
Dosage/Direction for Use
Congestive heart failure: Dosage must be individualized and closely monitored by a physician during up-titration.
Prior to initiation of carvedilol, the dosing of digitalis, diuretics and ACE inhibitor (if used) should be stabilized. The recommended starting dose of carvedilol is 3.125 mg twice daily for two weeks. If this dose is tolerated, it can be then be increased to 6.25 mg twice daily. Dosing should then be doubled every 2 weeks to the highest level tolerated by the patient. The maximum recommended dose is 25 mg twice daily in patients weighing less than 85 kg and 50 mg twice daily in patients weighing more than 85 kg. Carvedilol should be taken with food to slow the rate of absorption and reduce the incidence of orthostatic effects.
Essential hypertension: Adults: The recommended dose for initiation of therapy is 12.5 mg once a day (or 6.25 mg twice daily) for the first 2 days. Thereafter, the recommended dosage is 25 mg once a day. If necessary, the dosage may subsequently be increased at intervals of at least two weeks up to the recommended maximum daily dose of 50 mg given once a day or in divided doses (twice daily).
Elderly: The recommended dose for initiation of therapy is 12.5 mg once daily, which has provided satisfactory control in some patients. If response is inadequate, the dose may be titrated at intervals of at least two weeks up to the recommended maximum daily dose of 50 mg given once a day or in divided doses.
Contraindications
Carvedilol must not be used in patients with: New York Heart Association (NYHA) Class-IV decompensated heart failure requiring intravenous inotropic support; Bronchial asthma; Chronic obstructive pulmonary disease (COPD) with a bronchospastic component; Clinically manifest liver dysfunction; 2nd and 3rd degree AV-block; Severe bradycardia (< 50 bpm); Shock, including cardiogenic shock and hypovolaemic shock; Sick sinus syndrome (including sino-artrial block); Severe hypotension (systolic blood pressure < 85 mmHg).
Hypersensitivity to the drug. Allergic disorder (including asthma and allergic rhinitis) which may suggest a predisposition to bronchospasm);
Carvedilol should not be used during pregnancy or lactation, or in children younger than 18 years.
Pregnancy and nursing mothers: There is no adequate experience with carvedilol in pregnant women. Animal reproduction studies have revealed no teratogenic potential for carvedilol. Beta blockers reduce placental perfusion, which may result in intrauterine fetal death, immature and premature deliveries. In addition, adverse effects (especially hypoglycemia and bradycardia) may occur in the fetus and neonate. There is increased risk of cardiac and pulmonary complications in the neonate in the postnatal period. Therefore, carvedilol should not be used during pregnancy. Carvedilol and/or its metabolites are excreted in breast milk. Therefore, breast-feeding is not recommended during administration of carvedilol.
Special Precautions
Carvedilol should not be used in the case of the following diseases since there is a lack of experience in these situations: markedly reduce performance of the heart, labile or secondary (organically induced) high blood pressure, unstable angina pectoris, impulse conductions disturbances in the heart (complete bundle branch block), final stages of peripheral artery disease, impaired renal function (serum creatinine concentration > 1.8 mg/dl or creatinine clearance < 30 mL/min), recent heart attack (less than 6 months old), tendency to drop in blood-pressure lowering drugs (α1 receptor antagonists). Particularly close medical surveillance is required in diabetes mellitus patients with pronounced fluctuations in blood sugar levels and in the event of strict fasting. In older patients a sharper drop in blood pressure can occur after administration of the first dose of carvedilol. This applies especially to patients already taking diuretics. Diuretics should therefore be discontinued before beginning treatment with carvedilol. Drugs with β-blocking properties may trigger psoriasis vulgaris in isolated cases, cause the symptoms of this disease to deteriorate, or produce rashes resembling psoriasis (psoriasis form). Patients with personal of familiar history of psoriasis should only take drugs with β-blocking properties (e.g. carvedilol) after careful consideration of the benefit to risk ratio.
Treatment with carvedilol should not be stopped abruptly but must be gradually tapered all over a few days. This is particularly important in the case of patients with concomitant coronary artery disease (angina pectoris). Treatment of hypertension requires regular medical surveillance. Individual varying reactions can impair the ability to drive or operate machinery. This applies particularly when beginning the treatment or starting a new preparation and in conjuction with alcohol. During treatment with carvedilol the eyes must be examined regularly at 6-monthly intervals. Patients with mild to moderate occlusive vascular disease should be carefully monitored during initiation of therapy and β-blockers should be avoided in patients with severe occlusive vascular diease, particularly those with rest pain.
Carvedilol should only be used in patients with chronic obstructive pulmonary disease (COPD) with a bronchospastic component not receiving oral or inhaled medication if the potential benefit outweigh the potential risk. In patients with a tendency to bronchospasm, respiratory distress can occur as a result of a possible increase in airway resistance. Patient should be closely monitored during initiation and up-titration of carvedilol and the dose of carvedilol reduced if any evidence of bronchospasm is observed during treatment. Carvedilol, like other agents with beta-blocking properties may obscure the symptoms of thyrotoxicosis. Care should be taken in administering carvedilol to patients with a history of serious hypersensitivity reactions and in those undergoing desensitization therapy as beta-blockers may increase both the sensitivity towards allergens and the serious of anaphylactic reactions. In patients with pheochromocytoma, an alpha-blocking agent should be initiated prior to the use of any beta-blocking agent. Although carvedilol has both alpha and beta-blocking pharmacological activities, there is no experience with its use in this condition. Therefore, caution should be taken in administration of carvedilol to patients suspected of having pheochromocytoma. Agents with non-selective beta-blocking activity may provoke chest pain in patients with Prinzmetal's variant angina. There is no clinical experience with carvedilol in these patients, although the alpha-blocking activity of carvedilol may prevent such symptoms. However, caution should be taken in the administration of carvedilol to patients suspected of having Prinzmetal's variant angina. In patients suffering from peripheral circulatory disorders (Raynaud's phenomenon) there may be exacerbation of symptoms. Caution should be exercised in patients undergoing general surgery, because of the synergistic negative inotropic and hypotensive effects of carvedilol and anesthetic drugs. Carvedilol may induce bradycardia. If the pulse rate decreases to less than 55 beats per minute, the dosage of carvedilol should be reduced. In patients receiving concomitant therapy with calcium channel blockers of the verapamil or diltiazem-type, or other antiarrhythmic drugs, careful monitoring of ECG and blood is necessary.
Carvedilol should be used with caution in patients with labile or secondary hypertension until further clinical experience is available.
Use In Pregnancy & Lactation
Pregnancy and nursing mothers: There is no adequate experience with carvedilol in pregnant women. Animal reproduction studies have revealed no teratogenic potential for carvedilol. Beta blockers reduce placental perfusion, which may result in intrauterine fetal death, immature and premature deliveries. In addition, adverse effects (especially hypoglycemia and bradycardia) may occur in the fetus and neonate. There is increased risk of cardiac and pulmonary complications in the neonate in the postnatal period. Therefore, carvedilol should not be used during pregnancy. Carvedilol and/or its metabolites are excreted in breast milk. Therefore, breast-feeding is not recommended during administration of carvedilol.
Side Effects
The most common adverse reaction were edema, dizziness, bradycardia, hypotension, nausea, diarrhea, and blurred vision. There may be occasional dizziness, headaches, and tiredness. These symptoms are usually mild and occur particularly at the beginning of treatment. There may also be a considerably slowed pulse rate, gastrointestinal upset (nausea, abdominal pain, diarrhea, constipation and, in isolated cases, vomiting) or flu-like symptoms. As a result of a possible increase in airway resistance, breathing problems can occur in patients with a tendency towards bronchial constriction (bronchospastic reactions). Occasionally, particularly after taking the first dose of carvedilol, also when changing position from lying down to standing up, there can be an excessive drop in blood pressure (postural hypotension), with symptoms such as dizziness, going black before the eyes, or in rare cases fainting (syncope). In rare occasions, there may be angina pectoris or conduction disturbances from the atrium to the ventricle of the heart. Rarely, there can be an exacerbation of symptoms in patients suffering from intermittent claudication or vascular spasms in fingers or toes (Raynaud's phenomenon). Cold hands and feet have only been observed in isolated cases. It is also possible for silent diabetes to manifest, for already existing diabetes to become aggravated or for blood sugar counter-regulation to be inhibited. The signs of low blood sugar (e.g. a rapid heart rate), may be masked. There have been reports of isolated cases of allergic skin reactions (e.g. rashes and itching), depressed moods, sleep disturbances, disturbances of vision, eye irritation, disturbances of sensation (paraesthesia), pain in the limbs, potency disturbances, intensification of existing heart failure, increases in certain liver enzymes in the blood (serum transaminases) and reduced platelets and white blood corpuscles (thrombocytopenia, leukopenia). Users of contact lenses should be aware of the possibly reduced lacrimation.
Drug Interactions
When CARVEDILOL is used at the same time as other drugs, the following must be taken into account: The effect of other blood - pressure - lowering drugs may be intensified.
Simultaneous therapy with reserpine, guanethidine, methyldopa, clonidine or guanfacine may cause and intensified blood - pressure and heart - rate lowering effect.
Rifampicin reduces the systemic availability of carvedilol and thus, possibly its blood pressure lowering action.
Concomitant administration of clonidine with agents with β-blocking properties may potentiate blood pressure and heart rate lowering effect. When concomitant treatment with carvedilol and clonidine is to be terminated, carvedilol should be discontinued first. Clonidine therapy can then be discontinued several days later by gradually decreasing the dosage.
When nifedipine and carvedilol are used simultaneously there may be a more abrupt drop in blood pressure. When calcium channel blockers of the verapamil or diltiazem type of other anti-arrhythmic drugs are used simultaneously, careful monitoring of blood pressure and ECG are indicated since there may be a sharp drop on blood pressure, a reduced heart rate (bradycardia) or other rhythm disturbances of the heart. Calcium channel blockers and anti-arrhythmic drugs should therefore, not be administered intravenously during treatment with carvedilol.
When carvedilol and anesthesia drugs are used simultaneously, attention must be paid to the decreasing in heart rate, the cardiac effects (negative inotropism) of the two drugs, and stimulus conductions in the heart may be delayed. If patient is required to undergo anesthesia, please inform the doctor that patient is taking carvedilol.
Carvedilol can cause clinically relevant elevation of plasma digoxin concentrations.
The effects of insulin or oral blood-sugar-lowering drugs may be intensified. The signs of low blood sugar (hypoglycaemia) may be masked or attenuated (especially the increase in heart rate). Regular monitoring of blood sugar is therefore required with diabetics. Certain sedative (barbiturates, phenothiazines) and drugs for treating depression (cyclic anti-depressants) vasodilating drugs and alcohol may intensify the blood pressure lowering effect.
Storage
Store at temperature below 30°C.
MIMS Class
Beta-Blockers
ATC Classification
C07AG02 - carvedilol ; Belongs to the class of alpha and beta blocking agents. Used in the treatment of cardiovascular diseases.
Presentation/Packing
Tab 6.25 mg x 3 x 10's. 25 mg x 3 x 10's.
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