Mexicor, 50 mg/ml 5 ml 20 pcs.

Antioxidant drug.

Mexicor reduces manifestations of oxidative stress by inhibiting free-radical lipid peroxidation and increasing the activity of antioxidant enzyme system. Mexicor improves cellular energy exchange by activating the energy-synthesizing functions of mitochondria, increasing compensatory activation of aerobic glycolysis and reducing the degree of inhibition of oxidative processes in the Krebs cycle.

The energosynthetic effect of the drug is associated with increased delivery and consumption by cells of succinate, with the realization of the phenomenon of rapid oxidation of succinate acid by succinate dehydrogenase, as well as with the activation of the mitochondrial respiratory chain.

When Mexicor dissociates in the cell into succinate and a 3-oxypyridine derivative (base), the base exhibits a powerful antioxidant effect, stabilizing cell membranes and restoring functional activity of cells. It reduces cell membrane viscosity, increases its fluidity and modulates membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), ion channels and receptor complexes, which helps to maintain the structural and functional integrity of biomembranes, improves neurotransport and synaptic transmission.

The drug improves cerebral metabolism and blood supply of the brain, improves microcirculation and rheological properties of the blood and reduces platelet aggregation.

It improves functional state of ischemic myocardium, cardiac contractile function, and decreases manifestations of systolic and diastolic dysfunction of the left ventricle.

In conditions of coronary insufficiency it increases collateral blood supply of ischemic myocardium and activates energy-synthesizing processes in ischemic area, helping to preserve the integrity of cardiomyocytes and maintain their functional activity. Effectively restores myocardial contractility in reversible cardiac dysfunction, which is a significant reserve for increasing the contractility of the heart in patients with CHD complicated by heart failure.

In patients with stable angina pectoris the drug increases exercise tolerance and antianginal activity of nitrates, improves blood rheological properties. Addition of Mexicor to standard therapy of coronary artery disease improves clinical condition of patients increasing exercise tolerance and quality of life.

Mexicor stabilizes membrane structures of the vascular wall, inhibits platelet aggregation, normalizes microcirculatory disorders at early stages of atherogenesis, has hypolipidemic effect, reduces total cholesterol and LDL.

Mexicolor promotes neuroprotective action on the functional activity and metabolism of the ischemic brain, increases resistance of cerebral blood circulation in hypoperfusion, prevents decrease of cerebral blood flow in reperfusion period after ischemia.

The drug promotes adaptation to the damaging effects of ischemia by inhibiting the depletion of carbohydrate reserves, blocking the post-ischemic fall in glucose and oxygen utilization by the brain and preventing the progressive accumulation of lactate. At the same time the indicators of autoregulatory reactions of cerebral vessels are improved.

Mexicor has nootropic properties, prevents and reduces impairment of learning and memory processes in acute and chronic cerebral vascular diseases, in mild and moderate cognitive disorders of various genesis, has antioxidant effect, increases concentration and performance.

Inclusion of Mexicor in treatment of patients with acute stroke reduces clinical manifestations of stroke and improves rehabilitation period.

Mexicor has a selective, not accompanied by sedation and muscle relaxation, anxiolytic action, eliminates anxiety, fear, tension, restlessness, increases adaptation and emotional status.

Pharmacokinetics

Intake

After oral administration, the active substance of the drug Mexicor is quickly and completely absorbed from the gastrointestinal tract. Time of reaching Cmax in plasma is 0.46-0.50 h.

Distribution

The drug is rapidly distributed in the organs and tissues. Average time of distribution of the drug in the body is 4.9-5.2 h.

Metabolism

Metabolized in the liver by glucuronidation. Five metabolites were identified: 3-oxypyridine phosphate – is formed in liver and with the help of alkaline phosphatase is divided into phosphoric acid and 3-oxypyridine; the 2nd metabolite – pharmacologically active, is formed in large amounts and is found in urine 1-2 days after taking the preparation; the 3rd one is excreted in large amounts by kidneys; the 4th and the 5th are glucuronconjugates.

The T1/2 is 4.7-5.0 h. On average, 0.3% of unchanged drug and 50% of the administered dose is excreted as glucuronoconjugate in 12 hours with urine. The active substance and its glucuronoconjugates are excreted most intensively in the first 4 hours after drug administration.

The renal excretion rates of unchanged drug and metabolites have significant individual variability.

Indications

Active ingredient

How to take, the dosage

In the treatment of acute myocardial infarction, Mexicor® is administered by IV or IV/m over 14 days with traditional therapy including nitrates, beta-adrenoblocators, ACE inhibitors, thrombolytics, anticoagulants and antiaggregants, as well as symptomatic agents as indicated.

In the first 5 days for maximum effect the drug should preferably be administered by IV, in the next 9 days the drug can be administered by IV.

In/v infusion of the drug is carried out by drop infusion, slowly (in order to avoid side effects), on physiological solution or 5% solution of dextrose (glucose) in the volume of 100-150 ml for 30-90 minutes. If necessary, slow trickle administration of the drug for at least 5 minutes is possible.

The drug is administered (intravenously or intramuscularly) 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg/kg of body weight; the single dose is 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose – 250 mg.

In acute disturbances of cerebral circulation (ischemic stroke) Mexicor® is used as part of complex therapy in the first 2-4 days by IV drip 200-300 mg 2-3 times/day, then intravenously 100 mg 3 times/day. Treatment duration is 10-14 days. The drug is further administered orally as capsules, 100 mg 2 times a day for 14 days and 100 mg 3 times a day for the next 7 days. The frequency and duration of repeated courses of therapy are determined by the physician.

In patients with dyscirculatory encephalopathy in decompensation phase, Mexicor® should be given by IV fluids or by drop infusion at a dose of 100 mg 2-3 times daily for 14 days. Then the drug is administered v/m 100 mg/day for the next 2 weeks. Later the drug is prescribed in the form of capsules 100 mg 2-4 times per day; the frequency and duration of therapy shall be determined by the physician.

For the course of prophylaxis of discirculatory encephalopathy Mexicor® is administered in a dosage of 100 mg 2 times per day for 10-14 days.

For the treatment of mild and moderate cognitive impairment, Mexicor® is administered in/m at a dose of 100-300 mg/day for 14 days. If necessary, the drug is used later in capsulated form at 100 mg 2-4 times per day (as recommended by the physician) without limiting the course of treatment by duration.

Interaction

Special Instructions

Contraindications

Side effects

Intravenous administration, especially by injection, may cause:

Digestive system disorders: dryness and a metallic taste in the mouth.

Respiratory system disorders: throat farting, feeling of discomfort in the chest and shortness of breath.

Others: feeling of “flowing” heat throughout the body.

In general, these effects are time-consuming and transient.

The following side effects can occur with prolonged administration:

Digestive system: nausea, flatulence.

CNS side effects: sleep disorders (drowsiness or impaired falling asleep).

Overdose

Symptoms: sleep disturbance (insomnia), in some cases somnolence; when administered intravenously, rarely a slight and transient (up to 1.5-2 hours) increase in BP.

Treatment: the development of symptoms of overdose usually does not require the use of curing agents; the above symptoms of sleep disturbances disappear on their own within 24 hours. In particularly severe cases, the use of one of the hypnotic and anxiolytic drugs for oral administration (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg) is recommended. Antihypertensive agents are used in cases of excessive BP elevation.

Similarities