Karvedilol

Karvedilol – alpha and beta adrenoblocker without internal sympathomimetic activity with anti-anginal, vazodilatiruyushchy and antiarrhytmic action.

Form of release and structure

Dosage form – tablets: a ploskotsilindrichesky form, white color, with a facet and dividing risky (in a blister strip packaging: on 10 pieces, in a cardboard pack 3 packagings, on 30 pieces, in a cardboard pack 1 packaging).

Active agent – карведилол, in 1 tablet – 12,5 or 25 mg.

Auxiliary components: sucrose, methyl cellulose, поливидон K25, lactose, кросповидон, sodium of a kroskarmelloz.

Indications to use

• Stable stenocardia;
• Chronic heart failure (combination therapy);
• Arterial hypertension.

Contraindications

• The expressed bradycardia (heart rate less than 50 beats per minute);
• Sick Sinus Syndrome (SSS);
• Chronic heart failure in a decompensation stage;
• Atrioventricular block (AV blockade) of II and III degrees (except patients with an artificial pacemaker);
• Acute heart failure;
• Arterial hypotension (the systolic arterial pressure (AP) is below 85 mm рт.ст);
• Cardiogenic shock;
• Heavy liver failure;
• Age up to 18 years;
• Period of pregnancy and breastfeeding;
• Hypersensitivity to drug components.

With care apply Karvedilol at AV blockade of the I degree, Printsmetal's stenocardia, occlusal diseases of peripheral vessels, a thyrotoxicosis, a pheochromocytoma, a renal failure, psoriasis, a bronkhospastichesky syndrome, emphysema of lungs, chronic bronchitis, the general anesthesia during the carrying out extensive surgeries, a myasthenia, a hypoglycemia, at a diabetes mellitus, a depression.

Route of administration and dosage

Pill is taken inside, after food, washing down with a small amount of water.

The doctor appoints a drug dose individually taking into account clinical indications.

The recommended dosing:

• Stable stenocardia: an initial dose – on 12,5 mg 2 times a day. At good tolerance and insufficient efficiency the first increase in a dose can be carried out in 7-14 days of therapy on 12,5 mg, the second increase in 14 days, without changing frequency rate of reception. The daily dose of drug has to be no more than 50 mg and be accepted 2 times a day;
• Chronic heart failure: an initial dose (the first 2 weeks) – on 3,125 mg 2 times a day. Selection of a dose needs to be made strictly individually, under observation of the attending physician. The patient with good tolerance of Karvedilol the dose is increased multiply 1 time in 2 weeks and brought within 6 weeks to 25 mg 2 times a day. Increase the target daily dose – 50 mg is recommended to produce to the most tolerable dose the patient, for patients with body weight to 85 kg, more than 85 kg – 75-100 mg;
• Arterial hypertension: the first 7-14 days – on 12,5 mg a day. Frequency rate of reception can make 1 time (in the morning after a breakfast) or 2 times a day, having divided a daily dose in half. Then the daily dose is increased to 25 mg, it should be accepted according to already developed scheme. The last increase in a dose is made in 14 days.

If administration of drug is interrupted for more than 2 weeks, then treatment should be resumed from an initial dose according to the recommended scheme.

For patients of advanced age (70 years are more senior) drug is appointed in a daily dose not higher than 25 mg with frequency rate of reception 2 times a day.

Drug withdrawal is made by gradual (1-2 weeks) decrease in the accepted dose.

In case of the admission of the next reception the pill should be taken at once as soon as remembered, but it is impossible to double a dose at the following reception.

Side effects

Karvedilol's use can cause undesirable effects:

• From cardiovascular system: stenocardia, bradycardia, AV blockade, orthostatic hypotension; seldom – progressing of heart failure, the alternating lameness, disturbances of peripheric circulation;
• From a nervous system: muscular weakness (is more often in an initiation of treatment), a headache, dizziness, sleep disorders, syncopal states, paresthesias, a depression;
• From the alimentary system: nausea, dryness in a mouth, vomiting, diarrhea or a lock, abdominal pains, increase in activity of liver enzymes;
• From an urinary system: hypostases, heavy renal failures;
• From system of a hemopoiesis: leukopenia, thrombocytopenia;
• Allergic reactions: sneezing, skin reactions (an itch, a dieback, rash, urticaria), an exacerbation of psoriasis, a bronchospasm, a nose congestion, an asthma (at predisposed patients);
• Others: extremity pains, grippopodobny syndrome, increase in body weight, reduction of a slezootdeleniye.

Special instructions

It is impossible to use drug for treatment of patients with the low ABP.

At the beginning of use and when building a dose orthostatic reactions and sharp decrease in the ABP are possible. Patients with heart failure, especially advanced age, at use of a combination therapy or at a concomitant use of diuretics have severe dizzinesses up to faints.

Sharp drug withdrawal is not recommended, especially at stenocardia not to allow a sharp aggravation of symptoms, the dose decline has to proceed 1-2 weeks.

Treatment of patients with coronary heart disease, a renal failure, arterial hypotension, diseases of peripheral vessels, heart failure has to take place under regular control of function of kidneys, at deterioration in laboratory indicators Karvedilol it is necessary to cancel.

At patients with psoriasis, diseases of peripheral vessels, anaphylactic reactions in the anamnesis effect of drug can lead to an aggravation of symptoms, with Printsmetal's stenocardia – to provoke emergence of retrosternal pains. Use of drug reduces sensitivity at allergy tests.

Against the background of administration of drug with care it is recommended to carry out the general anesthesia by medicines with negative inotropic effect, such as cyclopropane, ether, trichloroethylene. The patient has to report to the doctor about Karvedilol's reception. Before planned extensive surgeries it is necessary to carry out gradual drug withdrawal.

Drug can mask symptoms of a hyperglycemia and a thyrotoxicosis. Treatment of patients with a diabetes mellitus is recommended to be accompanied with regular control of level of glucose in blood, in case of need to adjust hypoglycemic therapy.

It is necessary to observe extra care at purpose of drug the patient with the expressed metabolic acidosis.

Treatment of patients with a pheochromocytoma is begun with purpose of alpha adrenoblockers, and then passed to drug use.

Carrying contact lenses during therapy as drug reduces a slezootdeleniye is not recommended.

During treatment alcohol intake is contraindicated.

At cancellation of a combination therapy of Karvedilol and a clonidine, the first should cancel gradually карведилол, and some days later to begin a clonidine dose decline.

In an initiation of treatment and at increase in a dose drug can cause dizziness and excessive decrease in the ABP therefore during its use it is recommended to abstain from all potentially dangerous types of activity which performance depends on the high speed of psychomotor reactions and special attention.

Medicinal interaction

Against the background of administration of drug it is impossible to appoint intravenous administration of diltiazem and verapamil because of risk of strong decrease in the ABP and reduction of heart rate.

Action of a karvedilol strengthens a combination to anti-anginal, anti-hypertensive, some antiarrhytmic drugs, anesthetics, other beta adrenoblockers (including in the form of eye drops), cardiac glycosides, monoamine oxidase inhibitors, sympatholytics (Reserpinum).

At simultaneous use of Karvedilol:

• Phenobarbital, rifampicin and other inductors of liver enzymes can reduce concentration of a karvedilol in a blood plasma;
• Alkaloids of an ergot worsen peripheric circulation;
• Cimetidinum and other inhibitors of liver enzymes can increase the level of concentration of a karvedilol in a blood plasma;
• Digoxin increases the concentration in a blood plasma.

Drug can strengthen action of hypoglycemic means and mask development of a hypoglycemia.

Terms and storage conditions

To store in the dry, protected from light place at a temperature up to 25 °C. To protect from children.

Period of validity – 3 years.