Karvelend

General characteristics. Structure:

Akvtivny substance: 25 mg of a karvedilol.

Excipients: lactose, iron oxide (yellow) (tablets of 12,5 mg and 25 mg), iron oxide (red) (tablets of 25 mg), sucrose, povidone, the water purified кросповидон, colloid silicon dioxide, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Karvelend renders the combined non-selective a1-, b1-b2-blocking and antioxidant action. Its vazodilatiruyushchy effect is mediated, mainly, through the selection blockade of a1 - receptors. Karvelend reduces activity system renin-angiotensin-aldosteronovoy, reducing release of a renin therefore the liquid delay (characteristic of the selection alpha адреноблокатолоров) arises seldom. Karvelend has no own sympathomimetic activity, has membrane stabilizing properties. Karvelend - the powerful antioxidant eliminating free oxygen radicals. The combination of a vazodilatation and b-blockade at use of a karvelend has the following effect: at patients arterial hypertension the lowering of arterial pressure is not followed by simultaneous increase in the general peripheric vascular resistance which is observed at reception of b-blockers; heart rate decreases a little; the renal blood stream, and function of kidneys remain. The peripheral blood stream therefore the cold snap of extremities (which is often arising at treatment by usual b-blockers) is noted seldom does not change.

At patients coronary heart disease карвелэнд has the antiischemic and anti-anginal effect remaining at prolonged use. Hemodynamics researches after one-time administration of drug showed what карвелэнд reduces before - and an afterload. At patients with dysfunction of a left ventricle or a circulatory unefficiency карвелэнд favorably influences hemodynamic indicators, raises fraction of emission and reduces the sizes of a left ventricle. At administration of drug the ratio of lipoproteins of high density to lipoproteins of low density remains normal, concentration of electrolytes in serum do not change.

Pharmacokinetics. After intake карвелэнд it is quickly soaked up. The maximum concentration in serum is reached approximately in 1 hour. Absolute bioavailability of a karvelend at the person makes about 25%. Meal does not influence bioavailability. At an abnormal liver function bioavailability increases for 80% thanks to reduction of effect of the first passing through a liver. At long therapy cumulation of a karvelend is not observed. The elimination half-life of a karvelend makes 6-10 hours, plasma clearance about 590 ml/min. Removal happens, mainly, to bile. A small part of a dose is removed through kidneys in the form of various metabolites.

Indications to use:

- essential hypertensia (as mono - or a combination therapy)
- stable and unstable stenocardia, bezbolevy ischemia of a myocardium;
- slight, moderate and heavy chronic heart failure of ischemic or cardiomyopathic genesis, in combination with digitalis drugs, diuretics and APF inhibitors or without them.

Route of administration and doses:

карвелэнд it is necessary to swallow of tablets, washing down with enough liquid. To connect administration of drug with meal it is not obligatory, however, the patient with a circulatory unefficiency preferably to appoint him during food (for delay of speed of absorption and decrease in risk of emergence of orthostatic reactions).

Essential hypertensia. The recommended initial dose makes 12,5 mg in the first 2 days once a day, then on 25 mg once a day. If necessary it is possible to increase a dose bucketed no more than two weeks, reaching the highest recommended dose of 50 mg once a day (or divided into two receptions).

Stenocardia. The recommended initial dose makes 12,5 mg two times a day. If necessary afterwards it is possible to increase a dose bucketed not less than two weeks, bringing to the highest daily dose equal 100 mg divided into two receptions. For patients of advanced age the highest daily dose makes 50 mg divided into 2 receptions.

Chronic cordial. The dose is selected individually, under careful observation of the doctor. The recommended initial dose makes 3,125 mg two times a day within two weeks. At good tolerance the dose is increased by bucketed not less than two weeks, to 6,25 mg two times a day, then to 12,5 mg 2 times a day, then to 25 mg two times a day. The dose should be increased to maximum which is well transferred by the patient.

For all patients with heavy chronic heart failure and for patients with easy and moderate degree of chronic heart failure with body weight less than 85 kg the recommended maximum dose - 25 mg 2 times a day.

At patients with slight and moderate chronic heart failure and with the body weight more than 85 kg recommended maximum dose makes 50 mg two times a day.

Before each increase in a dose the doctor has to examine the patient for identification of possible increase of symptoms of heart failure or a vazodilatation. At tranzitorny increase of symptoms of heart failure or a delay of liquid it is necessary to increase a dose of diuretics though sometimes it is necessary to reduce a dose of a karvelend or temporarily to cancel it.

If treatment karvelendy is interrupted more than for 1 week, then its appointment is resumed in a smaller dose, and then increased according to the stated above recommendations. If treatment karvelendy is interrupted more, than for 2 weeks, then it it is necessary to renew in a dose 3,125 mg two times a day, then select a dose according to the stated above recommendations.

Treatment karvelendy is usually carried out is long. As well as other b-blockers, it cannot be cancelled sharply, especially at patients coronary heart disease. Drug should be cancelled gradually (within 1-2 weeks), reducing its dose half each 3 days.

Features of use:

At purpose of a karvelend to patients with a renal failure reversible deterioration in function of kidneys was noted. The dose of drug is regulated depending on a functional condition of kidneys.

As карвелэнд can cause bradycardia, at reduction of heart rate to the level of 55 beats per minute drug should be cancelled.

At the patients with chronic heart failure receiving foxglove drugs, diuretics and/or APF inhibitor карвелэнд it is necessary to apply with care as also it, and drugs of a foxglove slow down cordial conductivity. At co-administration of a karvelend, as well as other beta-blockers, with antagonists of calcium like verapamil or diltiazem, and also an antiaritmikama of the I class it is necessary to control an ECG and arterial pressure carefully.

To patients with chronic obtsruktivny diseases of lungs and the bronkhospastichesky component which is not receiving peroral or inhalation antiasthmatic drugs карвелэнд appoint if possible advantages of its use exceed potential risk. At the beginning of reception and at increase in a dose of a karvelend of these patients it is necessary to observe carefully, reducing a drug dose at emergence of initial signs of a bronchospasm.

At the persons having a heavy allergy or taking a desensitization course карвелэнд can raise an allergochuvstvitelnost.

Printsmetal's stenocardia. Non-selective beta adrenoblockers can provoke emergence of pains in patients with Printsmetal's stenocardia. These patients do not have experience of purpose of a karvelend. Though its alpha and adrenoceptor blocking properties can prevent similar symptomatology, it is necessary to appoint карвелэнд in such cases with care.

Advanced age. Apply with care.

Diabetes mellitus. With care drug appoint to patients a diabetes mellitus as it can mask or weaken hypoglycemia symptoms (especially tachycardia). At patients with heart failure and a diabetes mellitus use of a karvelend can be followed by a decompensation of carbohydrate metabolism.

Psoriasis. The patient with anamnestic instructions on emergence or an exacerbation of psoriasis at use of beta adrenoblockers, Dilatrend it is possible to appoint only after the careful analysis of possible advantage and risk.

General anesthesia and large surgical interventions. Care is required from patients to whom surgical intervention under the general anesthesia, because of a possibility of summation of negative effects of a karvelend and anesthetics is carried out.

Pheochromocytoma. Patients need to appoint a pheochromocytoma prior to use of any beta adrenoblocker alpha adrenoblocker. Though карвелэнд has both beta, and alpha and adrenoceptor blocking properties, there is no experience of its use for such patients therefore with care patients should appoint it with suspicion to a pheochromocytoma.

Contact lenses. The persons using contact lenses have to remember a possibility of reduction of amount of the lacrimal liquid.

Withdrawal. Treatment karvelendy cannot be interrupted sharply, especially at patients with coronary heart disease. Cancellation of a karvelend has to be gradual (within 2 weeks).

Pregnancy and period of a lactation. Beta adrenoblockers reduce perfusion of a placenta that can lead to pre-natal death of a fruit and premature births. Besides, the fruit and the newborn can have undesirable phenomena (in particular, a hypoglycemia and bradycardia, complications from heart and lungs).

Karvelend it is possible to appoint during pregnancy only if possible advantages of its use exceed potential risk for the woman and a fruit.

Karvelend and his metabolites are allocated with breast milk therefore in need of purpose of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Interaction with alcohol. During treatment the ethanol use is excluded.

Side effects:

Central nervous system: dizziness, headaches and weakness, an adynamy (including, increased fatigue) especially in an initiation of treatment, is rare – a depression, sleep disorders, paresthesias.

Cardiovascular system: bradycardia, orthostatic hypotonia, postural hypotension, the expressed decrease in the ABP, hypostases (including, the generalized, peripheral, depending on situation bodies, crotch hypostases, hypostases of the lower extremities, a hypervolemia, a liquid delay), it is rare - faints (in an initiation of treatment), syncopal states (including presinkopalny), an atrioventricular block and heart failure during increase in a dose, disturbance of peripheric circulation (a cold snap of extremities, an aggravation of a syndrome of the "alternating" lameness and Reynaud's syndrome.

Respiratory organs: a bronchospasm and an asthma at predisposed patients, it is rare - a nose congestion.

GIT: dispeptic frustration (including nausea, abdominal pains, diarrhea, vomiting) it is rare – locks, change of activity of hepatic transaminases.

System of a hemopoiesis: seldom - thrombocytopenia. Separate cases of a leukopenia.

Exchange disturbances veshchestv:uvelicheny body weights hypercholesterolemia; patients with already available diabetes mellitus have a hyperglycemia or a hypoglycemia, a decompensation of carbohydrate metabolism.

Integuments: skin reactions (allergic rash, dermatitis, small tortoiseshell and itch).

Urinary system: seldom - a renal failure and a renal failure at patients with a diffusion vasculitis and/or a renal failure, a dysuria.

Organs of sight: vision disorder, reduction of a slezootdeleniye.

Others: extremity pains, dryness in a mouth, impotence.

Interaction with other medicines:

Digoxin. At a concomitant use of a karvelend and digoxin of concentration of digoxin increase approximately by 15%. At the beginning of therapy karvelendy, at selection of its dose or drug withdrawal regular control of concentration of digoxin in a blood plasma is recommended.

insulin or peroral glucose-lowering drugs. Drugs with a beta adrenobloki-ruyushchimi properties can strengthen antihyperglycemic effect of insulin or peroral antihyperglycemic means. Hypoglycemia symptoms, especially tachycardia, can mask or weaken. Regular control of glucose of blood is recommended to the patients receiving insulin or peroral glucose-lowering drugs.

Inductors or inhibitors of hepatic metabolism. Rifampicin reduces plasma concentration of a karvelend approximately by 70%.

The drugs reducing the maintenance of catecholamines. The patients accepting at the same time drugs with beta and adrenoceptor blocking properties and the drugs reducing the maintenance of catecholamines (for example, Reserpinum and inhibitors of a monoaminooxidase), have to be under careful observation in connection with risk of development of arterial hypotension and/or the expressed bradycardia.

Cyclosporine. At purpose of a karvelend it was noted to the patients who transferred renal transplantation at whom chronic vascular graft rejection developed it is moderate is new increase in average minimum concentration of cyclosporine. To maintain concentration of cyclosporine in the therapeutic range, approximately at 30% of patients the dose of cyclosporine had to be reduced (on average by 20%), dose adjustment was not necessary for other patients. Due to the expressed individual fluctuations of a required daily dose of cyclosporine careful monitoring of concentration of cyclosporine after the beginning of therapy karvelendy and, if necessary, the corresponding correction of a daily dose of cyclosporine is recommended.

Clonidine. Co-administration of a clonidine with drugs with the beta blocking properties can exponentiate antigipertenzivny and an urezhayushchy cordial rhythm effects. If is planned to stop a combination therapy drug with beta and adrenoceptor blocking properties and a clonidine, the first should cancel beta adrenoblocker, and in several days it is possible to cancel a clonidine, gradually reducing its dose.

Blockers of "slow" calcium channels (verapamil, diltiazem) and other antiarrhytmic means (propranolol, Amiodaronum). At co-administration of a karvelend and diltiazem separate cases of disturbances of atrioventricular conductivity were noted (seldom - with disturbances of indicators of a hemodynamics). As well as in a case with other drugs with beta and adrenoceptor blocking properties, purpose of a karvelend together with blockers of "slow" calcium channels (verapamil or diltiazem) is recommended to be carried out under control of an ECG and arterial pressure.

As well as with beta and adrenoceptor blocking activity, карвелэнд action of other at the same time accepted anti-hypertensive means or drugs which render hypotensive effect as side effect can strengthen other drugs.

Special attention should be paid when carrying out the general anesthesia on a possibility of synergistic negative inotropic action of a karvelend and some anesthetics.

Contraindications:

- hypersensitivity to a karvelend or any component of drug,
acute heart failure,
- the dekompensirovanny heart failure (the IV class NYHA) demanding intravenous administration of drugs
- atrioventricular block of II and III degrees,
- heavy bradycardia less than 50 blows/min.,
- sick sinus syndrome (including sinotrialny blockade),
- the expressed arterial hypotonia (systolic arterial pressure less than 85 mm of mercury.),
- cardiogenic shock,
- chronic diseases of lungs with a bronkhospastichesky component, bronchial asthma,
- clinically expressed damage of a liver,
- pregnancy,
- lactation,
- age up to 18 years.

Overdose:

Symptoms: the expressed decrease in the ABP, bradycardia, heart failure, cardiogenic shock, a cardiac standstill; breath disturbances, a bronchospasm, vomiting, confusion of consciousness and generalized spasms are possible.

Treatment: in addition to actions of the general character, it is necessary to carry out monitoring and correction of zhiznennovazhny indicators, if necessary - in intensive care unit. It is possible to use the following events:

a) to lay the patient on a back

b) at the expressed bradycardia - atropine on 0,5-2 mg intravenously;

c) for maintenance of cardiovascular activity - a glucagon on 1-10 mg intravenously struyno, then on 2-5 mg an hour in the form of long infusion;

d) sympathomimetics (Dobutaminum, изопреналин, орципреналин or adrenaline) in various doses, depending on body weight and a therapeutic effectiveness. In need of administration of drugs with positive inotropic action, appoint phosphodiesterase inhibitors. If in a clinical picture of overdose arterial hypotension dominates, enter noradrenaline; it is appointed in the conditions of continuous monitoring of indicators of blood circulation.

At bradycardia, resistant to treatment, use of an artificial pacemaker is shown.

At a bronchospasm enter beta-adrenergic agonists in the form of an aerosol (at inefficiency - intravenously) or Aminophyllinum intravenously. At spasms intravenously slowly enter diazepam or clonazepam. As at heavy overdose with symptomatology of shock lengthening of an elimination half-life of a karvelend and removal of drug from depot is possible, it is necessary to continue a maintenance therapy rather long time. Duration of the supporting / disintoxication therapy depends on weight of overdose, it should be continued before stabilization of a condition of the patient.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 30 tablets in banks polymeric. On 10 tablets in planimetric cell upakovke.1 bank, 1 or 3 blister strip packagings in a pack.