Meksikor

General characteristics. Structure:

Active agent: 50 mg of ethylmethylhydroxypyridine of succinate.

Excipients: succinic acid - 5,0 mg, dinatrium эдетат - 0,1 mg, water for injections - to 1,0 ml.

Pharmacological properties:

Pharmacodynamics. Meksikor improves a functional condition of an ischemic myocardium at a myocardial infarction, improves sokratitelny function of heart, and also reduces displays of systolic and diastolic dysfunction of a left ventricle. Its antioxidant activity, ability to slow down free radical processes (which expressed intensification is observed at ischemia and a necrosis of a myocardium, especially in the period of reperfusion) is the cornerstone of effect of drug and reduces the damaging action of free radicals on cardiomyocytes. In the conditions of critical decrease in a coronary blood-groove Meksikor promotes preservation of the structurally functional organization of membranes of cardiomyocytes, stimulates activity of membrane enzymes - phosphodiesterases, adenylatecyclases, acetylcholinesterases. Drug supports the activation of aerobic glycolysis developing at acute ischemia and promotes in the conditions of a hypoxia to recovery of mitochondrial oxidation-reduction processes, increases synthesis of ATP and creatine phosphate. The specified mechanisms provide integrity of morphological structures and physiological functions of an ischemic myocardium.

Meksikor improves the clinical course of a myocardial infarction, increases efficiency of the carried-out therapy, accelerates recovery of functional activity of a myocardium of a left ventricle, reduces the frequency of arhythmic complications and disturbances of endocardiac conductivity. Drug normalizes metabolic processes in an ischemic myocardium, reduces a necrosis zone, recovers and/or improves electric activity and contractility of a myocardium, and also increases a coronary blood stream in an ischemia zone, increases anti-anginal activity of nitrodrugs, improves rheological properties of blood, reduces effects of a reperfusion syndrome at acute coronary insufficiency.

Meksikor has neuroprotective effect, 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.

Meksikor improves and stabilizes brain metabolism and blood supply of a brain, improves rheological properties of blood and microcirculation. Drug maintains functional activity of a brain, both during ischemia, and in the post-ischemic period. Meksikor possesses the selection, not followed sedation and muscle relaxation, anxiolytic action, eliminates alarm, fear, tension, concern.

Meksikor has nootropic properties, warns and reduces the disturbances of training and memory arising at vascular diseases of a brain (an ischemic stroke, distsirkulyatorny encephalopathy) at easy and moderate cognitive disturbances, renders anti-hypoxemic effect, increases concentration of attention and working capacity.

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

Pharmacokinetics. At intravenous administration drug quickly (within 0,5 - 1,5 hours) passes from a circulatory bed into bodies and fabrics in this connection, its concentration in not changed look quickly decreases. At intramuscular introduction in therapeutic doses the maximum concentration of drug in a blood plasma is reached in 30-40 min. and makes 2,5-3 mkg/ml, at the same time its metabolites are defined in a blood plasma for 7-9 hours.

Removal of drug from an organism happens to urine in a glyukuronokonjyugirovanny form, and also in insignificant quantities in not changed look. 

Indications to use:

- complex therapy: an acute myocardial infarction (since the first days), an ischemic stroke;

- distsirkulyatorny encephalopathy (including atherosclerotic genesis);

- easy and moderate cognitive disorders of various genesis.

Route of administration and doses:

At treatment of an acute myocardial infarction enter intravenously or intramusculary within 14 days, against the background of the traditional therapy of a myocardial infarction including nitrates, beta adrenoblockers, inhibitors of an angiotensin-converting enzyme (APF), trombolitika, anticoagulating and antiagregantny means, and also symptomatic means according to indications.

In the first 5 days, for achievement of the maximum effect, it is desirable to administer the drug intravenously, in the next 9 days Meksikor can be entered intramusculary.

Intravenous administration of drug is made by drop infusion, slowly (in order to avoid side effects) for 0,9% solution of sodium of chloride or 5% solution of a dextrose (glucose) of 100 - 150 ml within 30-90 min. If necessary perhaps slow jet administration of drug, lasting not less than 5 minutes.

Administration of drug (intravenous or intramuscular) is carried out by 3 times a day, every 8 hours. The daily therapeutic dose makes 6-9 mg/kg of body weight a day, a single dose - 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, one-time - 250 mg.

At acute disorders of cerebral circulation (an ischemic stroke) Meksikor apply in complex therapy in the first 2-4 days intravenously kapelno 200-300 mg 2-3 times a day, then intramusculary on 100 mg 3 times a day. Duration of treatment makes 10-14 days. Further drug is appointed in capsules on 100 mg 2 times a day within 14 days and on 100 mg 3 times a day during the next 7 days. Frequency and duration of repeated courses of therapy is defined by the doctor.

At distsirkulyatorny encephalopathy in a phase of a decompensation of Meksikorsleduyet to appoint intravenously struyno or kapelno in a dose of 100 mg 2-3 times a day for 14 days. Then the drug is administered intramusculary on 100 mg a day for the next 2 weeks. Further drug is appointed in capsules on 100 mg 2-4 times a day (according to the recommendation of the doctor), the frequency and duration of courses of therapy are determined by the doctor.

For course prevention of dispirkulyatorny encephalopathy the drug is administered intramusculary in a dose of 100 mg by 2 times a day for 10-14 days.

For treatment of easy and moderate cognitive frustration of Meksikornaznachayut intramusculary in a dose of 100-300 mg a day within 14 days. In need of further drug is used in the encapsulated form on 100 mg 2-4 times a day (according to the recommendation of the doctor) without restriction of a course of treatment on duration.

Features of use:

At an acute myocardial infarction, acute (an ischemic stroke) and chronic (distsirkulyatorny encephalopathy) disturbances of cerebral circulation after completion of parenteral administration of drug, for maintenance of the reached therapeutic effect, Meksikor in a dosage form is recommended to continue drug use: capsules on 100 mg 3 times a day. Duration of therapy is defined by the doctor.

Side effects:

At intravenous administration, especially jet, emergence of dryness in a mouth and "metal" smack, feeling of "the spreading heat" in all body, irritation in a throat and a sensation of discomfort in a thorax, feeling of shortage of air is possible. As a rule, the specified phenomena are caused by the high speed of administration of drug and have tranzitorny character.

Against the background of long administration of drug emergence of the following side effects is possible: from digestive tract - nausea, a meteorism; from the central nervous system - a sleep disorder (drowsiness or disturbance of backfilling).

Interaction with other medicines:

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

- exponentiates effect of the nitrocontaining drugs.

Contraindications:

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

Overdose:

Symptoms: sleep disorder (sleeplessness), in certain cases drowsiness; at intravenous administration in rare instances insignificant and short-term (till 1,5-2 o'clock) increase in arterial pressure.

Treatment: development of symptoms of overdose, as a rule, does not demand use of the stopping means, the specified symptoms of a sleep disorder disappear independently within a day. In especially hard cases use of one of somnolent and anxiolytic means for intake (nitrazepam of 10 mg, oxazepam of 10 mg or diazepam of 5 mg) is recommended. At excessive increase in arterial pressure apply antihypertensives under control of arterial pressure.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 50 mg/ml. On 2 ml or 5 ml in ampoules from light-protective glass with a color ring of a break or a color point of a break. On 5 ampoules place in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or without foil (in the pallet). 

2 blister strip packagings with ampoules on 2 ml (Federal State Unitary Enterprise GOSZMP, Federal State Budgetary Institution RKNPK Ministry of Health and Social Development Rossii-EPMBP and JSC Biomed of I. I. Mechnikov) or 1, 2 or 4 blister strip packagings with ampoules on 5 ml (JSC Biomed of I. I. Mechnikov) together with the application instruction place in a pack from a cardboard. Apply the label on each ampoule self-adhesive.