Expiration date: 10/2025

Active substance: Ethylmethylhydroxypyridine succinate (emoxipine)

Structure and Composition:

Solution for intravenous or intramuscular administration in ampoules of 2 or 5 ml

1ml contains emoxypine 50mg

Tablets, film-coated. 1 tablet contains emoxypine 0.125 g

Excipients:

core - kaolin, sodium carboxymethyl MCC povidone talc, calcium stearate

shell - Hypromellose Titanium dioxide Macrogol Talc

Description pharmaceutical form:

The solution for intravenous and intramuscular injection: a colorless or slightly yellow transparent liquid.

Tablets: round, bi-convex shape, film-coated, white to white with Valium a color shade, on a break - from white to white with gray or yellowish or Valium a color shade.

Pharmacokinetics:

The on / determined by m administration drug plasma for 4 hours after administration. Tmax Cmax is 0.45-0.50 hours at doses of 400-500 mg -. 3.5-4.0 g / ml. Mexiprim moves quickly from the bloodstream to organs and tissues and is rapidly eliminated from the body. The retention time of the drug (MRT) is 0.7-1.3 hours Mexiprim excreted in the urine, mostly -. glyukuronokonyugirovannoy in form and in small quantities - unchanged.

Mexiprim rapidly absorbed from the gastrointestinal tract with a period of 0.08-0.1 hours poluabsorbtsii. Tmax in the blood plasma of 0,46-0,5 hours. Mexiprim size Cmax in plasma is in the range from 50 to 100 ng / ml. T1 / 2 Mexiprim  and mean residence time of the drug in the body are respectively 4,7-5 h and 4.9-5.2 h. Mexiprim in humans is metabolized rapidly to form its glyukuronokonyugirovannogo product. On average, 12 hours is excreted in the urine of 0.3% of the drug - unchanged and 50% - in the form glyukuronokonyugata (of the administered dose). The most intensive Mexiprim and glyukuronokonyugat excreted within the first 4 hours after ingestion. Indicators excretion in the urine Mexiprim and its conjugated metabolites have considerable individual variability.

Description of the pharmacological actions:

Mexiprim is an inhibitor of free-radical processes, membrane protectors, have anti, stressprotektivnym, neuroprotective, anticonvulsant and anxiolytic effects. The drug increases the body's resistance to the effects of various damaging factors (shock, hypoxia and ischemia, cerebrovascular accident, alcohol intoxication and antipsychotic drugs (neuroleptics).

The mechanism of action Mexiprim due to its antioxidant and membrane action. It inhibits lipid peroxidation, increases the activity of superoksidoksidazy, increases the ratio of lipid-protein, reduces the viscosity of the membrane increases its fluidity. Modulates the activity of membrane-bound enzymes (kaltsiynezavisimaya phosphodiesterase, adenylate cyclase, acetylcholinesterase) receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, helps to preserve the structural and functional organization of biological membranes, transport of neurotransmitters and improve synaptic transmission. Mexiprim increases in the brain dopamine mozge. It is a compensatory increase in the activation of aerobic glycolysis and decreased inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with increasing the content of ATP and creatine phosphate, activation energosinteziruyuschih functions of mitochondria, stabilizing cell membranes.

The drug improves metabolism and blood flow to the brain, improves microcirculation and blood rheology, reduces platelet aggregation. It stabilizes the membrane structure of blood cells (erythrocytes and platelets) for hemolysis. It has hypolipidemic effect, reduces total cholesterol and LDL.

Testimony:

Common for both formulations:

• vasoneurosis
  
• anxiety disorders in neurotic and neurosis-like states
  
• relief of abstinence syndrome in alcoholism with a predominance of neurosis and vegetative-vascular disorders
  

The solution for intravenous and intramuscular injection (optional):

• acute cerebrovascular accident
  
• encephalopathy
  
• mild cognitive disorders of atherosclerotic origin.
  

Tablets (optional):

• mild cognitive disorders of various origins (when psychoorganic syndrome and asthenic disorders caused by acute and chronic disorders of cerebral circulation, brain injury, neuroinfections and intoxication, and senile atrophic processes)
  
• memory disorders and intellectual impairment in the elderly
  
• exposure to extreme (stress) factors.
  

Contraindications:

• Increased individual sensitivity to the drug
  
• acute disorders of the liver and kidney function
  
• childhood
  
• pregnancy
  
• breast-feeding.
  

Side effect:

Perhaps the appearance of individual adverse reactions: nausea and dryness of the mouth, drowsiness, allergic reactions.

Drug Interactions:

Compatible with psychotropic drugs. Enhances the action of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa), reduces the toxic effects of ethanol.

Dosage and administration:

V / m, in / in (bolus or infusion). Doses picked individually. When infusion method of administering the drug should be diluted in physiological sodium chloride solution. Started treatment with doses of 50-100 mg, 1-3 times a day, gradually increasing the dose to produce a therapeutic effect. Chip Mexiprim injected slowly over 5-7 minutes, drip - at a rate of 40-60 drops per minute. The maximum daily dose will not exceed 800 mg.

In acute cerebral circulatory disorders (in combination therapy): in the first 2-4 days - / drip 200-300 mg 1 time a day, and then - in / m to 100 mg 3 times a day. Duration of treatment - 10-14 days.

In vascular encephalopathy in decompensation phase: in / bolus or infusion at a dose of 100 mg 2-3 times a day for 14 days. Then introducing drug / m to 100 mg / day for the next 2 weeks. For foreign exchange prevention vascular encephalopathy introducing drug / m at a dose of 100 mg 2 times a day for 10-14 days.

For mild cognitive impairment in elderly patients and in anxiety disorders: drug use / m at a daily dose of 100-300 mg for 14-30 days.

When alcohol withdrawal syndrome: V / m at a dose of 100-200 mg 2-3 times a day or in / drop 1-2 times per day for 5-7 days.

In acute intoxication antipsychotics: in / in a dose of 50-300 mg / day for 7-14 days.

Inside. Applied therapeutic dose and duration of treatment is determined by the sensitivity of patients to the drug. Started treatment with a dose of 0.25-0.5 g average daily dose of 0.25-0.5 g, max - 0.8 The daily dose of drug partitioned into 2-3 doses throughout the day.

For the treatment of patients with anxiety disorders, vegetative-vascular dysfunction and cognitive impairment Mexiprim used within 2-6 weeks.

When coping with alcohol withdrawal syndrome Mexiprim used within 5-7 days.

Course therapy Mexiprim end gradually decreasing for 2-3 days dose.

Overdose:

The symptoms: sleep disturbance (insomnia, in some cases - drowsiness).

Treatment: as a rule, does not require - the symptoms disappear on their own within a day. In severe cases, insomnia is recommended to take 10 mg of nitrazepam, oxazepam, diazepam 10 mg or 5 mg.

Special instructions:

The extent of the restrictions determined by the individual tolerability. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.