Description
Release form
Tablets.
Packing
30 pcs.
Pharmacological action
Has a combined non-selective beta-adrenergic blocking, alpha1-blocking and antioxidant effect. The vasodilating effect is mainly associated with the blockade of alpha1 receptors. Due to vasodilation, it reduces the total peripheral vascular resistance. It has no internal sympathomimetic activity and, like propranolol, has a membrane stabilizing effect.
A powerful antioxidant that eliminates free oxygen radicals.
The combination of the vasodilating effect and beta-adrenergic blocking properties of carvedilol leads to the fact that in patients with arterial hypertension, a decrease in blood pressure is not accompanied by a simultaneous increase in total peripheral resistance, which is noted when taking beta-blockers, carvedilol slightly reduces heart rate, while maintaining renal blood flow and kidney function. Since peripheral blood flow persists, cooling of the extremities is very rare.
Antihypertensive effect develops rapidly – after 2 3 hours after a single dose and lasts for 24 hours. With prolonged treatment, the maximum effect is observed after 3-4 weeks.
In patients with coronary artery disease, carvedilol has anti-ischemic and antianginal effects. Reduces pre- and afterload on the heart. It does not have a pronounced effect on lipid metabolism and the content of potassium, sodium, magnesium ions in blood plasma.
In patients with impaired left ventricular function and / or circulatory failure, carvedilol has a beneficial effect on hemodynamic parameters: it increases the ejection function of the left ventricle and reduces its size.
Favorable effect of carvedilol on the hemodynamics of the heart, the ejection fraction of the left ventricle is observed both in dilated cardiomyopathy and in ischemic form of heart failure. In heart failure, carvedilol reduces end-systolic and end-diastolic volume, as well as peripheral and pulmonary vascular resistance. The ejection fraction and cardiac index do not change with normal heart function.
The effect of carvedilol is more pronounced in patients with tachycardia (heart rate more than 82 beats / min) and low ejection fraction (less than 23%).
During treatment with carvedilol, the ratio of high density lipoprotein cholesterol / low density lipoprotein does not change.
Contraindications
hypersensitivity to carvedilol or other components of the
preparation heart failure in the stage of decompensation
sinus node weakness syndrome, AV block II ² III degree (with the exception of patients with artificial pacemaker), severe bradycardia (heart rate less than 50 min ), cardiogenic shock
bronchial asthma, severe hepatic dysfunction
metabolic acidosis
pregnancy
lactation
children and adolescents under 18 years of age (efficacy and safety are not established)
joint intravenous administration of verapamil, diltiazem or other antiarrhythmic drugs (especially class I antiarrhythmic drugs).
With care and control to treat:
patients with diabetes
hypoglycemia, thyrotoxicosis, pheochromocytoma (only in combination with the appointment of alpha-adrenergic blockers)
occlusive peripheral vascular disease
grade I angina pectoris, prmetmetal
COPD
psoriasis
renalgia kidney disease
rena alpine depression use with digitalis preparations, diuretics and / or MAO inhibitors
elderly
extensive surgery and general anesthesia.
Special instructions
Therapy should be carried out for a long time and should not stop abruptly, especially in patients with coronary artery disease. this can lead to a deterioration in the course of the underlying disease. If necessary, the dose reduction should be gradual, within 1-2 weeks.
At the beginning of Karvetrend therapy or with an increase in the dose of the drug in patients, especially the elderly, an excessive decrease in blood pressure may occur, mainly upon rising (dose adjustment is necessary). In patients with chronic heart failure, dose selection may increase symptoms of heart failure, the appearance of edema. In this case, you should not increase the dose of Carvetrend, the appointment of large doses of diuretics is recommended, up to the stabilization of the patient’s condition.
Recommended continuous monitoring of ECG and blood pressure while prescribing Carvetrend and blockers of “slow” calcium channels, phenylalkylamine derivatives (verapamil) and benzothiazepine (diltiazem), as well as class I antiarrhythmic drugs.
It is recommended that kidney function be monitored in patients with chronic renal failure, hypotension, and chronic heart failure.
In the event of surgery using general anesthesia, the anesthetist should be warned of prior therapy with carvedilol. Carvetrend does not affect blood glucose concentration and does not cause changes in glucose tolerance test parameters in patients with non-insulin-dependent diabetes mellitus.
Avoid ethanol during treatment.
Patients with pheochromocytoma must be prescribed alpha-blockers before starting therapy.
Patients wearing contact lenses should be aware that the drug may cause a decrease in lacrimation.
If heart rate drops to 55 bpm, the drug should be discontinued.
In individuals who are allergic or undergoing desensitization, carvedilol may increase allergy sensitivity.
It is not recommended to drive a car at the beginning of therapy and when increasing the dose of Karvetrend. You should refrain from other activities associated with the need for a high concentration of attention and quick psychomotor reactions.
Tablets should be stored in a cardboard box, as when stored in the light, the color of the tablets may change.
Composition
1 tab. contains carvedilol 25 mg.
Excipients: MCC lactose monohydrate hydroxypropyl cellulose starch corn talcum silica colloidal magnesium dioxide stearate
Dosage and administration
Inside, with plenty of fluids.
Arterial hypertension. Adults: the initial dose is 12.5 mg once a day for the first 2 days. Then – 25 mg once a day. If necessary, increase the dose. The maximum dose is 50 mg / day once or in 2 divided doses (morning and evening). Dosage increase should be carried out gradually with an interval of at least 2 weeks.
In elderly patients, in some cases, a dose of 12.5 mg may be effective.
Angina pectoris. Adults: the initial dose is 12.5 mg 2 times a day for the first 2 days. Then – 25 mg 2 times (morning and evening) per day. If necessary, the dose is increased with an interval of 2 weeks to a maximum of 100 mg / day, divided into 2 doses.
For elderly patients, the maximum daily dose is 50 mg, in 2 divided doses.
Chronic heart failure. The dose is selected individually. With increasing doses, careful monitoring is carried out. You should monitor the condition of the patient during the first 2-3 hours after the first dose or after the first increased dose. The additional use of Karvetrend requires a stable clinical condition. The dose and purpose of other drugs, such as digoxin, diuretics and ACE inhibitors, should be fixed before the appointment of Karvetrend.
Recommended starting dose is 3.125 mg 2 times a day for 14 days. With good tolerability of the drug and the need to increase the dosage, the drug is prescribed at a dose of 6.25 mg 2 times a day, then 12.5 mg and then 25 mg 2 times a day. Patients are prescribed the maximum tolerated dose. The maximum recommended dose is 25 mg 2 times a day for patients weighing up to 85 kg and 50 mg 2 times a day for patients weighing more than 85 kg. Patients with heart failure in order to prevent orthostatic hypotension are recommended to take the drug with meals. At the beginning of treatment and before increasing each dose, the condition of patients should be monitored, because may worsen the course of heart failure. Fluid retention may develop, and in connection with a vasodilating effect, arterial hypotension and lethargy. With fluid retention, doses of diuretics should be increased, in addition, a temporary dose reduction of Carvetrend may be required. In some cases, treatment with Karvetrend should be temporarily suspended.
Side effects of
At recommended doses, the drug is well tolerated, but in some cases, side effects are possible.
From the digestive system: nausea, dry mouth, abdominal pain, diarrhea or constipation, vomiting, increased activity of liver transaminases.
From the side of the central nervous system: headache, dizziness, feeling tired, unconsciousness, muscle weakness (usually at the beginning of treatment), sleep disturbance, depression, paresthesia.
From the side of hematopoiesis: leukopenia, thrombocytopenia.
Allergic reactions: exanthema, urticaria, pruritus, rash, the appearance and / or exacerbation of psoriasis, sneezing, nasal congestion, very rarely – anaphylactoid reaction.
From the respiratory system: shortness of breath, bronchospasm (in predisposed patients).
From the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, atrioventricular block, progression of circulatory failure (cold extremities), progression of heart failure, edema of the lower extremities.
From the side of metabolism: weight gain, impaired carbohydrate metabolism.
Other: occasionally – exacerbation of the syndrome of “intermittent” claudication, Raynaud’s syndrome, pain in the extremities, impaired urination, impaired renal function, flu-like syndrome, decreased tear production.
As with other drugs with alpha-blocking action, latent current diabetes mellitus may appear or its symptoms may intensify.
Drug interaction
Carvedilol may potentiate the effects of other simultaneously taken antihypertensive drugs or drugs that have a hypotensive effect (nitrates).
With the combined use of carvedilol and diltiazem, cardiac conduction disturbances and hemodynamic disturbances may develop.
With the simultaneous administration of carvedilol and digoxin, the concentration of the latter increases and the time of AV administration may increase.
Carvedilol can potentiate the effects of insulin and oral hypoglycemic agents, while the symptoms of hypoglycemia (especially tachycardia) can be masked, therefore, in patients with diabetes, regular monitoring of blood sugar levels is recommended.
Microsomal oxidation inhibitors (cimetidine) enhance, and inducers (phenobarbital, rifampicin) weaken the hypotensive effect of carvedilol.
Catecholamine-lowering drugs (reserpine, MAO inhibitors) increase the risk of hypotension and severe bradycardia.
With the simultaneous use of cyclosporine, the concentration of the latter increases (correction of the daily dose of cyclosporine is recommended).
Concomitant administration of clonidine can potentiate the antihypertensive and heart-rate-reducing effects of carvedilol.
General anesthetics enhance the negative inotropic and hypotensive effect of carvedilol.
Overdose
Symptoms: marked decrease in blood pressure (systolic pressure 80 mmHg or lower), bradycardia (less than 50 beats / min), respiratory dysfunction (bronchospasm), chronic circulatory failure, cardiogenic shock, cardiac arrest.
Treatment: during the first hours – induction of vomiting and gastric lavage. An overdose requires intensive treatment. The antagonist of beta-adrenergic blocking action is orciprenaline or isoprenaline 0.5 1 mg iv and / or glucagon in a dose of 1 5 mg (maximum dose – 10 mg).
With severe bradycardia, iv atropine is prescribed at a dose of 0.5 2 mg.
Glucagon is administered intravenously (within 30 s) to maintain cardiac activity after which a long infusion is carried out at the rate of 2 5 mg / h.
If peripheral vasodilating action predominates (warm limbs, in addition to significant arterial hypotension), norepinephrine should be prescribed in repeated doses of 5-10 μg or as an infusion – 5 μg / min.
For relief of bronchospasm, beta-adrenergic agonists are prescribed (in the form of an aerosol or iv) or aminophylline iv.
If convulsions develop, slow administration of diazepam or clonazepam is recommended.
In severe cases of intoxication, when shock symptoms dominate, treatment should continue until the patient’s condition stabilizes, taking into account T1 / 2 carvedilol of 6 10 hours.
Monitoring and correction of vital signs is recommended in the intensive care unit.
Storage Conditions
At a temperature not exceeding 25 ° C.
Keep out of the reach and sight of children.
Term hodnosty
3 years
Terms leave through pharmacies
In retseptu
Dosage form
tablet
Teva Pharmaceutical Enterprises Co., Ltd., Israel
