MEKSIKOR (Solution for in / and the / m)
Active material: эtilmetilgidroksipiridina succinate
When ATH: C01EB
CCF: Antioxidant drugs
ICD-10 codes (testimony): F07, G93.4, i20, I20.0, I21, I61, I63, I67.2, I69
When CSF: 01.12.11.04
Manufacturer: ÈkoFarmInvest LLC (Russia)
Pharmaceutical form, composition and packaging
Solution for in / and the / m clear, colourless or slightly yellowish.
1 ml | 1 amp. | |
эtilmetilgidroksipiridina succinate | 50 mg | 100 mg |
Excipients: succinic acid, Trilon b, water d / and.
2 ml – vials of dark glass (5) – packings Valium planimetric (1) – packs cardboard.
2 ml – vials of dark glass (5) – packings Valium planimetric (2) – packs cardboard.
Pharmacological action
Antioxidant drugs, possessing an anti-ischemic, is an antianginal, antihypoxic, angioprotektornym, gipoholesterinemičeskim, anxiolytic and nootropic effect, regulates metabolic processes miocarde and vascular wall.
Meksikor® reduces oxidative stress, braking free radical lipid peroxidation and increasing the activity of the antioxidant system of enzymes. Meksikor® improves cellular energy exchange, activating the ènergosinteziruûŝie function of mitochondria, increasing compensatory activation of aerobic Glycolysis and reducing the degree of oppression oxidizing processes in the cycle of Krebsa.
Ènergosinteziruûŝee effect of the drug is linked to the increase in the delivery and consumption of cells succinate, implementation of rapid phenomenon of oxidation of succinic acid sukcinatdegidrogenazoj, as well as the activation of the mitochondrial respiratory chain. When dissociation Meksikora® in a cage on succinate and derivative of 3-oksipiridina (ground), the Foundation has shown powerful antioxidant effects, stabilizing cell membranes and regenerating the functional activity of cells. Meksikor® decreases viscosity of the cell membrane, increases its turnover and provides modulation effect on the membrane enzymes (calcium-independent fosfodiesterzu, adenylyl Cyclase, azetilholinesterzu), ion channels and receptor complexes, that contributes to the conservation of structural and functional integrity of biomembranes, improves transport of neurotransmitters and sinapticescuu transfer. The drug increases the concentration in the brain of dopamine.
Integrated impact Meksikora® on energy metabolism and increases the body's resistance to stress-syndrome and heavy oxygen-dependent States (shock, gipoksiya, išemiâ), exo- and endogenous intoxication, prevents and reduces violations of learning and memory, occur with aging, acute and chronic violations of cerebral circulation.
Meksikor® improves functional status of išemizirovannogo infarction, reducing manifestation of systolic and diastolic left ventricular dysfunction, as well as electrical instability of the myocardium. In critical conditions reduce coronary blood flow Meksikor® considerably activates ènergosinteziruûŝie processes in the zone reduces the severity of ischemia and oxidative stress, increases blood supply and collateral oxygen-transport ability of red blood cells, improves blood rheology, that helps limit the magnitude of the hearth of necrosis, maintenance of contractile and propulsive heart function. Meksikor® significantly reduces the adverse effects of reperfuzionnogo syndrome, improving clinical efficacy of methods to restore coronary circulation in acute coronary insufficiency. Meksikor® effectively restores the airway diseases in reversible cardiac dysfunction, caused by States “hibernation” (hibernation) and “oglušennosti” infarction, that represents a substantial reserve increase the contractility of the heart in patients with ischemic heart disease.
Meksikor® increases the effectiveness of koronarookklûzionnyh therapy of arrhythmia due to own scale activity and ability to reduce the likelihood of Cardial side effects major complications drugs, preserving or increasing their activity.
Meksikor® improves the clinical course of acute myocardial infarction and unstable angina pectoris, increases the effectiveness of combination therapy (nitrates, antiagregantov, antihypertensive drugs), Accelerates recovery of functional activity of the myocardium of the left ventricle, reduces the frequency of arrhythmic complications and disorders of intracardiac conduction.
Meksikor® stabilizes the membrane structure of the vascular wall, It inhibits platelet aggregation, normalizes microcirculation infringements in the early stages of atherogenesis, provides lipidkorrigiruûŝee effect on the ratio of Pro- and antiaterogennah fractions of blood lipids, lowering cholesterol levels, VLDL, LDL and triglycerides, while raising HDL-Xc.
Use Meksikora® in the treatment of patients with coronary artery disease and hypertension crisis course shortens postkrizovoy stabilization, reduces the chance of recurrence and frequency development gipertoniceski kriza acute coronary insufficiency amid crisis, do effect gipotenziveh funds.
Meksikor® improves and stabilizes the cerebral metabolism and blood circulation of the brain, improves blood rheology and microcirculation. Drug supports the functional activity of the brain, as during ischemia, and in period 2, hampering the development of the phenomenon “No-reflow”, and restoring the autoregulâtornye reaction cerebral vessels. Meksikor® Accelerates recovery of bioelectric activity of brain išemizirovannogo, has a selective, not accompanied by sedation and miorelaksaciei, anxiolytic action, eliminates anxiety, fear, voltage, anxiety, improves adapt and emotional status.
Meksikor® nootropnami properties, prevents and reduces violations of learning processes and memory, occurring with acute and chronic cerebral vascular diseases, Aging, in light and moderate cognitive violations of various Genesis, provides antihypoxia effect, improves concentration and performance.
Add Meksikora® the complex treatment of patients with acute violation of cerebral circulation reduces the severity of clinical manifestations of stroke and improves during rehabilitation period.
Pharmacokinetics
Absorption
When injecting the active substance of the preparation Meksikor® is determined plasma within 4 no. The time to reach Cmax – 0.58 no.
Distribution
Quickly moves from the blood to organs and tissues. High membranotropnaâ activity allows for 72 h maintain a sufficiently high concentrations of the drug in cell membranes.
Metabolism
Biotransformiroetsa intensively in the liver with the formation of 5 glûkuronokon″ûgirovannyh metabolites. The first metabolite (phosphate 3-oksipiridina) It is formed in the liver and influenced by ALP breaks down into phosphoric acid and 3-oksipiridin. Second pharmacologically active metabolite is produced in large quantities and detected in the urine for 1-2 days after injection. The third metabolite is excreted in large quantities in the urine. Fourth and fifth metabolites constitute glûkuronokon″ûgaty.
Deduction
The average holding time drug in plasma – 0.7-1.3 no. Average, for 12 h the urine output 0.3% unchanged drug and 50% of the administered dose – as glûkuronokon″ûgata.
Testimony
- Acute myocardial infarction (from the first hours of the disease);
- Unstable angina;
- CHD, abnormal arterial hypertension krizovogo currents, chronic insufficiency of blood circulation, išemičeskimi ventricular arrhythmias;
- Acute cerebrovascular accident;
- Encephalopathy (incl. atherosclerotic Genesis);
light and moderate cognitive disorders of different Genesis;
— intellectual and memory disorders in patients of elderly and senile age.
Dosage regimen
The drug is administered / m or / (bolus or infusion). The duration of treatment and the choice of individual dose depends on the Nosological disease, the severity of the patient's condition and treatment effectiveness.
In/in the introduction of the drug spend by drip infusions, slowly (to avoid side effects), the physiological solution or 5% dextrose (Glucose) in volume 100-150 ml for 30-90 m. If necessary, slow jet of the drug for a period of not less than 5 m.
The daily therapeutic dose is 3-9 mg / kg body weight, single dose – 1-3 mg / kg body weight. The maximum daily dose should not exceed 800 mg, single – 250 mg.
When treating Acute myocardial infarction Meksikor® misleading in/in or/m during 14 day amid traditional therapy, includes trombolitiki, nitrates, beta-blockers, ACE inhibitors, anticoagulants and antiplatelet agents, as well as symptomatic means according to. First 5 days to achieve the maximum effect of the drug it is advisable to install/, subsequent 9 Nights – the drug can be entered in/m. Injecting drug (w / w or w / o) exercise 3 times / day, every 8 no. After the completion of injecting the drug to maintain the achieved effect it is recommended to continue to apply Meksikora® orally in the form of capsules 0.1 g 3 times / day for 2 Months. The daily therapeutic dose is 6-9 mg / kg body weight, single dose – 2-3 mg / kg body weight. The maximum daily dose should not exceed 800 mg, single – 250 mg.
In the integrated therapy unstable angina Meksikor® apply the first 5 days of hospitalization in/drip in the dose 3-6 mg / kg body weight / day, further – orally in capsule form on 100 mg 3-4 times / day for 2-3 Months.
In the treatment of complicated hypertensive crises for kardial′nomu version, as well as the uncomplicated hypertonic crisises are at high risk for complications and repeated crises, Meksikor® used in the first 3-5 SUT since hospitalization/in drip or/m (for out-patient patient-administered) dose 3-6 mg / kg body weight / day, further – orally in capsule form on 100 mg 3-4 times / day for 3 Months.
At acute stroke Meksikor® used in the treatment of the first 2-4 days in/drip in the 200-300 mg 2-3 times / day, then/m 100 mg 3 times / day. The duration of treatment is 10-14 d. Acute and chronic violations of cerebral circulation following completion of injecting the drug to maintain the achieved effect it is recommended to continue to apply Meksikora® orally in the form of capsules 100 mg 3 times / day for 2 Months.
At dyscirculatory encephalopathy in the phase of decompensation Meksikor® should be used in/in struino or drip in the dose 100 mg 2-3 times / day for 14 days. Then the drug is injected in/m 100 mg/day for the next 2 weeks.
To course of prevention dyscirculatory encephalopathy Meksikor® injected i / m in a dose of 100 mg 2 times / day for 10-14 days.
At vegetative-vascular dysfunction Meksikor® apply/m 100 mg 3 times / day for 10-14 days.
At neurotic and neurotic disorders with manifestations of anxiety Meksikor® apply/m 100 mg 4 times / day for 10-14 days.
At light and moderate cognitive disorders, vascular dementia Meksikor® apply the/m in a dose of 100-300 mg / day for 14 days.
Side effect
From the digestive system: may cause dryness and metallic taste in the mouth.
The respiratory system: sore throat, chest discomfort and lack of air.
Other: feeling “razlivaûŝegosâ” heat throughout the body, sense of smell; allergic reactions.
Appear when excessively high speed injection side effects, usually, disappear when slowing or cessation of drug administration.
Contraindications
- Acute liver dysfunction;
- Acute renal dysfunction;
- Childhood and adolescence up 18 years;
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug.
Pregnancy and lactation
We do not recommend the use of drugs in pregnancy and lactation because of insufficient knowledge of the drug during these periods.
Cautions
The caution should appoint Meksikor® patients with a history of allergological history.
Use in Pediatrics
Efficacy and safety of Meksikora assignment® children and adolescents under the age of 18 years not set.
Effects on ability to drive vehicles and management mechanisms
At the beginning of treatment is advisable to refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Overdose
With regard to the low toxicity of the drug overdose unlikely. In case of accidental overdose, you may experience drowsiness and sedative action.
Drug Interactions
Meksikor® reinforces the effect protivosudorozhnykh funds (Carbamazepine), antiparkinsonian (levodopa) and benzodiazepine anxiolytics.
Meksikor® improves antianginalnuu activity of nitrates and antihypertensive activity antigipertenziveh funds.
Combined use of Meksikora® with nibentanom, propranolol and verapamil reduces the risk of developing aritmogennyh effects last.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, the dark place at a temperature from 0° to 25° c. Shelf life - 2 year.