Description
Latin name
Mexicor
Release form
Solution for iv and intramuscular administration transparent, colorless or slightly colored.
Packaging
2 ml – ampoules of dark glass (5) – blister strip packaging (2) – packs of cardboard.
Pharmacological action
Antioxidant drug that prevents lipid peroxidation of cell membranes. It has angioprotective, enhancing the compensatory activation of aerobic glycolysis and reducing the degree of inhibition of oxidative processes in the Krebs cycle.
The energy-synthesizing effect of the drug is associated with increased delivery and consumption of succinate by the cells, the realization of the phenomenon of the rapid oxidation of succinic acid by succinate dehydrogenase, as well as the activation of the mitochondrial respiratory chain.
When dissociating the drug Mexicor in a cell into succinate and a 3-hydroxypyridine derivative (base), the base exhibits a powerful antioxidant effect that stabilizes cell membranes and restores the functional activity of cells. Reduces the viscosity of the cell membrane, increases its fluidity and has a modulating effect on membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), It effectively restores myocardial contractility with reversible cardiac dysfunction, which represents a significant reserve for increasing the contractility of the heart in patients with coronary artery disease complicated by heart failure.
In patients with stable angina, stress increases exercise tolerance and antianginal activity of nitrates, improves blood rheological properties. The addition of Mexicor to standard IHD therapy improves the clinical condition of patients, increasing exercise tolerance and improving the quality of life.
Mexico stabilizes the membrane structures of the vascular wall, inhibits platelet aggregation, normalizes microcirculatory disorders in the early stages of atherogenesis, has a lipid-lowering effect, and reduces total cholesterol and LDL.
Mexico has a neuroprotective effect on the functional activity and metabolism of the ischemic brain, increases the stability of the blood circulation of the brain under hypoperfusion, and prevents a decrease in brain blood flow during the reperfusion period after ischemia.
The drug helps to adapt to the damaging effects of ischemia, inhibiting depletion of carbohydrate reserves, blocking the post-ischemic decline in glucose and oxygen utilization by the brain and inhibiting the progressive accumulation of lactate. At the same time, indicators of autoregulatory reactions of cerebral vessels improve.
Mexico has nootropic properties, prevents and reduces learning and memory disorders that occur in acute and chronic vascular diseases of the brain, with mild and moderate cognitive impairment of various origins, it has an antioxidant effect, increases concentration and performance.
The inclusion of Mexico in the complex therapy of patients with acute cerebrovascular accident reduces the severity of the clinical manifestations of stroke and improves the course of the rehabilitation period.
Mexico has a selective, not accompanied by sedation and muscle relaxation, anxiolytic effect, eliminates anxiety, fear, tension, anxiety, improves adaptation and emotional status.
Pharmacokinetics
Absorption
After oral administration, the active substance of the drug Mexico is rapidly and completely absorbed from the digestive tract. The time to reach Cmax in blood plasma is 0.46-0.50 h.
Distribution
Quickly distributed in organs and tissues. The average distribution time of the drug in the body is 4.9-5.2 hours.
Metabolism
Metabolized in the liver by glucuronidation. 5 metabolites have been identified: 3-hydroxypyridine phosphate – is formed in the liver and, with the participation of alkaline phosphatase, breaks down to phosphoric acid and 3-hydroxypyridine, the 2nd metabolite is pharmacologically active, is formed in large quantities and is found in urine 1-2 days after taking the drug 3 -th – is excreted in large quantities by the kidneys of the 4th and 5th – glucuron conjugates.
Excretion of
T1 / 2 – 4.7-5.0 hours. On average, within 12 hours with urine, 0.3% of the unchanged drug and 50% of the administered dose are excreted in the form of a glucuronoconjugate. The most intensely active substance and its glucuronoconjugates are excreted in the first 4 hours after taking the drug.
Renal excretion rates of unchanged drug and metabolites have significant individual variability.
Indications
as part of the complex treatment of acute myocardial infarction (from the first day)
as part of the complex therapy of ischemic stroke
discirculatory encephalopathy (including atherosclerotic origin)
mild and moderate cognitive impairment.
Contraindications
acute liver dysfunction
acute renal dysfunction
children and adolescents under 18 years of age (efficacy and safety not established)
pregnancy
lactation (breast-feeding)
hypersensitivity to the drug.
Use during pregnancy and lactation
The use of the drug during pregnancy and lactation is contraindicated.
Composition
1 ml1 amp.
ethylmethylhydroxypyridine succinate 50 mg100 mg
Excipients: succinic acid – 5 mg, disodium edetate – 0.1 mg, water d / i – up to 1 ml.
Dosage and administration of
In the treatment of acute myocardial infarction, Mexicor ® is administered intravenously or intravenously for 14 days with traditional therapy including nitrates, beta-blockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, and also symptomatic indications.
In the first 5 days, to achieve the maximum effect, it is desirable to administer the drug in / in the next 9 days – the drug can be administered in / m.
In / in the introduction of the drug is carried out by drip infusion, slowly (to avoid side effects), in saline or 5% solution of dextrose (glucose) in a volume of 100-150 ml for 30-90 minutes If necessary, slow jet injection of a drug lasting at least 5 minutes is possible.
Administration of the drug (in / in or in / m) is carried out 3 times / day, every 8 hours. The daily therapeutic dose is 6-9 mg / kg body weight, a single dose is 2-3 mg / kg body weight. The maximum daily dose should not exceed 800 mg, a single – 250 mg.
In case of acute cerebrovascular accident (ischemic stroke), Mexicor ® is used as a part of complex therapy in the first 2-4 days iv in a drop of 200-300 mg 2-3 times / day, then in / m 100 mg 3 times / day . The duration of treatment is 10-14 days. Subsequently, the drug is administered orally in the form of capsules of 100 mg 2 times / day for 14 days and 100 mg 3 times / day for the next 7 days. The frequency and duration of repeated courses of therapy is determined by the doctor.
In case of discirculatory encephalopathy in the decompensation phase, Mexicor ® should be used iv in a drop or drop dose of 100 mg 2-3 times / day for 14 days. Then the drug is administered in / m at 100 mg / day for the next 2 weeks. In the future, the drug is prescribed in the form of capsules of 100 mg 2-4 times / day, the frequency and duration of the course of therapy is determined by the doctor.
For the course of prophylaxis of dyscirculatory encephalopathy, Mexicor ® is administered IM in a dose of 100 mg 2 times / day for 10-14 days.
For the treatment of mild and moderate cognitive impairment, Mexico ® is prescribed IM at a dose of 100-300 mg / day for 14 days. If necessary, in the future, the drug is used in capsule form, 100 mg 2-4 times / day (as recommended by a doctor) without limiting the course of treatment for the duration.
Side effects of
When given in the on / in, especially the jet, it is possible:
From the digestive system: dry and metallic taste in the mouth.
From the respiratory system: sore throat, discomfort in the chest and lack of air.
Others: a sensation of heat spreading throughout the body.
As a rule, these phenomena are due to the high speed of drug administration and are transient in nature.
Against the background of prolonged administration of the drug, the following side effects may occur:
From the digestive system: nausea, flatulence.
From the side of the central nervous system: sleep disturbances (drowsiness or falling asleep).
Drug interaction
Mexicore ® enhances the action of anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa) and benzodiazepine anxiolytics.
Mexicore ® potentiates the effect of nitrates.
Overdose
Symptoms: sleep disturbance (insomnia), in some cases drowsiness with / in the introduction in rare cases slight and short-term (up to 1.5-2 h) increase in blood pressure.
Treatment: the development of symptoms of overdose, as a rule, does not require the use of relief agents, these symptoms of sleep disorders disappear on their own within a day. In particularly severe cases, it is recommended to use one of the sleeping pills and anxiolytic medicines for oral administration (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg). With excessive increase in blood pressure, antihypertensive agents are used.
Storage conditions
In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Expiration
3 years.
Do not use after the expiry date stated on the package.
De Active ingredient
Ethylmethylhydroxypyridine succinate
drugstore terms
Dosage form
Dosage form
injection and infusion
