Corvotonum

General characteristics. Structure:

Active agent - Molsidominum of 4 mg.

Excipients: lactoses monohydrate, кросповидон, macrogoal 6000, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Korvaton is anti-anginal drug from group of sidnonimin. Molsidominum as a result of a number of metabolic transformations emits nitrogen oxide (NO) stimulating soluble guanylate cyclase; accumulation of tsGMF causes relaxation of smooth muscle cells of a vascular wall (more veins).

The main mechanism of anti-anginal action of Molsidominum consists in decrease in preload of heart. Molsidominum reduces the venous pressure, end diastolic pressure in ventricles and pulmonary pressure. Reduces the need of a myocardium for oxygen. Expands large coronary arteries, improves collateral circulation at coronary atherosclerosis. At chronic heart failure under the influence of Korvaton dilatation of ventricles decreases. Besides, drug inhibits an early phase of aggregation of thrombocytes, reduces allocation (or synthesis) serotonin, thromboxane and other factors promoting aggregation of thrombocytes.

Korvaton's action begins approximately within the first 20 min. after intake, the maximum effect is reached in 30-60 min., duration of action makes from 4 to 6 h.

Pharmacokinetics.  After intake it is absorbed almost completely from a GIT. Bioavailability makes 60-70%.

Other 30-40% are metabolized in a liver. Molsidominum is metabolized in a liver with formation pharmacological of the active SIN-1 (3-morfolino-sidnonimin) connection of which the unstable substance SIN-1A(N-, morfolino-M-aminosintonitril is formed), the allocating NO with formation pharmacological of inactive SIN-1C. During metabolism also other metabolites are formed.

Minimum effective concentration of Molsidominum in a blood plasma - 3-5 ng/ml. Practically does not contact proteins of plasma.

It is brought by kidneys to 90% (in the form of metabolites) and through intestines (9%); the rest is removed in not changed look. T1/2 makes 0.85-2.35 h.

Does not kumulirut (including at patients with a renal failure). At the expressed liver failure (increase in bromsulfaleinovy test up to 20%-50%) delay of removal and increase in its concentration in a blood plasma is noted.

Indications to use:

— prevention of attacks of stenocardia;

— chronic heart failure (as a part of a combination therapy with cardiac glycosides, diuretics).

Route of administration and doses:

Pill Korvaton has to be taken with enough liquid (about 1/2 glasses) at regular intervals. A pill can be taken both to, and in time or after food.

Corvotonum is appointed on 1 tablet of 1-2 times/days.

If necessary the dose can be increased to 12-16 mg/days (1 tablet of 3-4 times/days).

Features of use:

Corvotonum is not applicable for stopping of attacks of stenocardia!

At patients with high risk of development of hypotensive reaction it is necessary to approach a drug dosage individually.

In an acute phase of a myocardial infarction Korvaton can be used only after blood circulation stabilization.

At a renal failure concentration of Molsidominum in a blood plasma does not change.

Drug can be combined with other anti-anginal means (for example, to add to two - or to ternary treatment - nitrates, blockers of slow calcium channels and blockers of beta adrenoceptors).

At an abnormal liver function, only at the expressed its decrease (increase of bromsulfaleinovy test to 20-50%) concentration of Molsidominum in a blood plasma and an elimination half-life increases that can demand correction of a dose of drug.

For the period of treatment it is necessary to exclude ethanol reception.

Influence on ability to driving of motor transport and to control of mechanisms

During treatment (especially at the beginning) it is necessary to refrain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From TsNS: in an initiation of treatment sometimes - a headache, in rare instances - dizziness.

From a GIT: nausea.

From cardiovascular system: the expressed decrease in the ABP, sometimes up to a collapse.

Others: development of allergic reactions (skin rash, an itch, a bronchospasm), delay of speed of psychomotor reactions is in rare instances possible. Extremely seldom - development of an acute anaphylaxis.

Interaction with other medicines:

At co-administration of Korvaton with peripheral vazodilatator, blockers of slow calcium channels, antihypertensives and ethanol the hypotensive effect amplifies.

At simultaneous use of Korvaton with acetylsalicylic acid antiagregantny activity amplifies.

There is a big risk of development of hypotonia at simultaneous use of inhibitors of phosphodiesterase 5 (FDE 5), such as sildenafit, tadalafit, vardenafit. Combined use of FDE 5 with Molsidominum is contraindicated.

Contraindications:

— shock;

— a vascular collapse or the expressed arterial hypotension (systolic the ABP less than 100 mm Hg);

— decrease in the central venous pressure;

— pregnancy;

— breastfeeding period;

— - sildenafit simultaneous use of inhibitors of phosphodiesterase of type 5 (FDE 5), tadalafit, vardenafit - in connection with high risk of development of arterial hypotension;

— age up to 18 years;

— hypersensitivity to Molsidominum.

With care: the patient with disturbances of cerebral circulation, with the increased intracranial pressure, with tendency to arterial hypotension, elderly patients, after a myocardial infarction, the patient with glaucoma (especially closed-angle).

Overdose:

Symptoms: a severe headache, the expressed lowering of arterial pressure, tachycardia.

Treatment: symptomatic.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, 4 mg of white or almost white color, oblong, biconvex, from two parties the engraving of "MFG" and stylized "h" divided by risky. On 10 pieces in the blister,

3 blisters are placed in cardboard packaging.