Meksikor

General characteristics. Structure:

Active agent of ethylmethylhydroxypyridine of succinate in terms of 100% substance - 100 mg;

excipients: potato starch - 54,5 mg, povidone (polyvinylpirrolidone low-molecular medical 12600±2700) - 4,0 mg, lactose (sugar milk) - 40,0 mg, magnesium stearate - 0,5 mg, cellulose microcrystallic - 1,0 mg; capsules firm gelatinous No. 2 (gelatin - 59,3189 mg, titanium E171 dioxide - 1,22 mg, dye a sunset yellow E110 - 0,0036 mg, dye quinolinic yellow E104 - 0,4575 mg).

Pharmacological properties:

Pharmacodynamics. Meksikor reduces displays of an oxidizing stress, slowing down free radical peroxide oxidation of lipids and increasing activity of antioxidant system of enzymes. Meksikor improves cellular power exchange, activating the power synthesizing functions of mitochondrions, strengthening compensatory activation of aerobic glycolysis and reducing extent of oppression of oxidizing processes in a tricarbonic acid cycle. The power synthesizing effect of drug is connected with increase in delivery and consumption by succinate cells, implementation of a phenomenon of bystry oxidation of succinic acid a succinatedehydrogenase, and also with activation of a mitochondrial respiratory chain. At drug dissociation Meksikor in a cell on succinate and derivative 3 oxypyridines (basis), the basis shows the antioxidant influence stabilizing cellular membranes and recovering functional activity of cells. Reduces viscosity of a cellular membrane, increases its flowability and exerts the modulating impact on membrane-bound enzymes (calcium independent phosphodiesterase, adenylatecyclase, ацетилхол to an inesteraz), ion channels and receptor complexes that promotes preservation of structurally functional integrity of biomembranes, improves transport of neurotransmitters and synoptic transfer. Improves metabolism and blood supply of a brain, microcirculation and rheological properties of blood, reduces aggregation of thrombocytes. Improves a functional condition of an ischemic myocardium, sokratitelny function of heart, and also reduces displays of systolic and diastolic dysfunction of a left ventricle. In the conditions of coronary insufficiency increases collateral blood supply of an ischemic myocardium and activates the power synthesizing processes in an ischemia zone that promotes preservation of integrity of cardiomyocytes and maintenance of their functional activity. Effectively recovers contractility of a myocardium at reversible cardiac dysfunction that represents an essential reserve of increase in sokratitelny ability of heart at patients with the coronary heart disease complicated by heart failure.

At patients with a stable angina of exertion increases tolerance to an exercise stress and антианг inalny activity of nitrodrugs, improves rheological properties of blood. Drug addition Meksikor to standard therapy of coronary heart disease improves a clinical condition of patients, increasing tolerance to exercise stresses and improving quality of life.

Meksikor stabilizes membrane structures of a vascular wall, inhibits aggregation of thrombocytes, normalizes disturbances of microcirculation at early stages of an atherogenesis, possesses hypolipidemic action, reduces the content of the general cholesterol and the poured-proteids of low density (PPLD).

Meksikor has neuroprotective effect on functional activity and metabolism of an ischemic brain, increases stability of blood circulation of a brain in the conditions of hypoperfusion, prevents decrease in a blood-groove of a brain in the reperfusion period after ischemia. Drug promotes adaptation to the damaging action of ischemia, braking exhaustion of carbohydrate stocks, blocking post-ischemic falling of utilization of glucose and oxygen a brain and interfering with progressive accumulation of a lactate. At the same time indicators of autoregulyatorny reactions of cerebral vessels improve.

Meksikor has nootropic properties, warns and reduces the disturbances of training and memory arising at acute and chronic vascular diseases of a brain at easy and moderate cognitive disturbances of various genesis, renders antioxidant effect, increases concentration of attention and working capacity.

Drug inclusion Meksikor in complex therapy of patients with an acute disorder of cerebral circulation reduces expressiveness of clinical displays of a stroke and improves a current of the rehabilitation period.

Meksikor possesses the selection, not followed sedation and muscle relaxation, anxiolytic action, eliminates alarm, fear, tension, concern, increases adaptation and the emotional status.

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract. It is quickly distributed in bodies and fabrics. Time of achievement of the maximum concentration (Tmax) in a blood plasma makes 0,46-0,50 hours. The average time of distribution of drug in an organism makes 4,9 - 5,2 hours. It is metabolized in a liver by a ppokuronirovaniye. 5 metabolites are identified: 3 oxypyridines phosphate - are formed in a liver and with the participation of an alkaline phosphatase breaks up to phosphoric acid and 3 oxypyridine; the 2nd metabolite - pharmacological active, is formed in large numbers and it is found in urine for 1-2 days after administration of drug; the 3rd - is brought in large numbers by kidneys; the 4th and 5th - glyukuronkonjyugata. An elimination half-life - 4,7-5 hour. On average in 12 hours kidneys remove 0,3% of not changed drug and 50% in the form of a glyukuronokonjyugat of the entered dose. It is most intensively removed within the first 4 hours after administration of drug. Removal indicators kidneys of not changed drug and metabolites have considerable individual variability.

Indications to use:

- coronary heart disease (as a part of complex therapy);

- complex therapy of an ischemic stroke;

- distsirkulyatorny encephalopathy;

- easy and moderate cognitive frustration.

Route of administration and doses:

Inside. Begin treatment with a dose of 100 mg (1 capsule) 3 times a day, gradually increasing a dose depending on the clinical course of a disease and portability of the carried-out therapy. The maximum daily dose should not exceed 800 mg, one-time 200 mg. It is desirable to distribute a daily dose of drug on several receptions during the day. Course therapy with drug is finished gradually, reducing daily a drug dose by 100 mg (1 capsule).

Therapy course duration at patients with coronary heart disease and disturbances of blood circulation head brain not less than 1,5-2 months. Repeated courses (according to the recommendation of the doctor), it is desirable to carry out in the veseena - the autumn periods.

At complex therapy of distsirkulyatorny encephalopathy, easy and moderate cognitive frustration, drug is appointed without restriction of a course of treatment on duration, in a dose of 100 mg 3-4 times a day.

Features of use:

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Usually drug is transferred well. Emergence of allergic reactions, dispeptic frustration, nausea and dryness in a mouth, diarrheas which quickly disappear independently or at drug withdrawal is in rare instances possible. At prolonged use manifestation of a meteorism, a sleep disorder (drowsiness or disturbance of backfilling) is possible.

Interaction with other medicines:

- strengthens action of antiepileptic means (carbamazepine), protivoparkinsonichesky means (levodopa) and benzodiazepine anxiolytics;

- increases anti-anginal activity of nitrodrugs and hypotensive APF inhibitors and beta adrenoblockers;

- reduces toxic effects of ethanol.

Contraindications:

Hypersensitivity to drug, acute disorders of function of a liver and kidneys, age up to 18 years (efficiency and safety are not established), pregnancy, the breastfeeding period.

Overdose:

Due to the drug hypotoxicity the overdose is improbable. At accidental overdose emergence of symptoms of a sleep disorder - drowsiness, sleeplessness is possible. Symptomatic treatment.

Storage conditions:

To store 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:

Capsules on 100 mg. On 10 capsules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. On 2 planimetric packagings (JSC Moskhimfarmpreparaty of N. A. Semashko") or on 2, 3 or 6 planimetric packagings (CJSC Miraksbiofarm) together with the application instruction place in a pack from a cardboard.