Ethyl methyl mercaptopyridine malate - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antihypoxants and antioxidants

Included in the formulation

Ethoxydol®

pills inwards

MEDIMPEX, CJSC Russia

АТХ:

N.07.X.X Other drugs for the treatment of diseases of the nervous system

Pharmacodynamics:

Ethylmethylhydroxypyridine malate is an inhibitor of free-radical processes, has a membrane-protective, antihypoxic, nootropic, anticonvulsant, anxiolytic effect, increases the body's resistance to stress.

It has anti-ischemic properties, improves blood flow in the ischemia zone, limits the area of ischemic damage, reveals lipid-lowering effect, reduces the content of total cholesterol and low-density lipoproteins in serum.

The drug increases the resistance of the body to the effects of various damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebral circulation disorders, intoxication with alcohol and antipsychotic drugs - neuroleptics).

The drug improves cerebral metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis.

The mechanism of action of the drug is due to its antioxidant, antihypoxic and membrane-protective action. It inhibits lipid peroxidation, increases the activity of superoxidease, increases the ratio of lipid-protein, reduces the viscosity of the membrane, increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structural and functional organization of biomembranes, neurotransmitter transport and the improvement of synaptic transmission.

Pharmacokinetics:

When administered intramuscularly, the drug is determined in the blood plasma for 4 hours after administration. The maximum concentration is observed through0,25 hand when the dose of 100 mg of the preparation is 0.3-1.06 μg / ml. Quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. The retention time of the drug is 1.84-2.38 hours. Half-lifeis 1.15-1.75 hours.It is excreted from the body by the kidneys, mainly in the form of glucuronides and in small amounts in unchanged form.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract at an average rate of 0.569 ± 0.086 hours. In healthy volunteers, it was found that with oral administration of tablets at a dose of 100 mg, the maximum concentrationin blood plasma is achieved through 0.28 ± 0.08 hours and is 487.0 ± 72.4 ng / ml, followed by rapid elimination of the drug, with a half-life of 1.46 ± 0.13 hours.

Quickly distributed to organs and tissues of the body. It is determined in the blood plasma for 7-10 hours. The drug is extensively metabolized in the liver to form phosphate-3-hydroxypyridine, glucuronoconjugated products.

Indications:

Intramuscular and intravenous: acute disorders of cerebral circulation; encephalopathy; syndrome of vegetative dystonia; light cognitive disorders of atherosclerotic origin; anxiety disorders in neurotic and neurosis-like states; relief of withdrawal syndrome with alcoholism with prevalence of neurosis-like and vegetative-vascular disorders; acute intoxication with antipsychotic drugs.

Inside: ischemic heart disease (as part of complex therapy); complex therapy of ischemic stroke; encephalopathy; mild to moderate cognitive impairment.

ICD-10

IX.I20-I25.I20 Angina pectoris [angina pectoris]

IX.I20-I25.I25 Chronic ischemic heart disease

IX.I20-I25.I24.8 Other forms of acute coronary heart disease

IX.I60-I69.I63 Cerebral infarction

IX.I60-I69.I61 Intracerebral haemorrhage

XIX.T36-T50.T43 Poisoning with psychotropic drugs, not elsewhere classified

V.F40-F48.F48.0 Neurasthenia

VI.G90-G99.G93.4 Encephalopathy, unspecified

V.F00-F09.F07 Personality and behavioral disorders due to illness, damage or dysfunction of the brain

IX.I60-I69.I69 Effects of cerebrovascular disease

IX.I60-I69.I67.2 Cerebral atherosclerosis

Contraindications:

For intravenous and intramuscular administration: pregnancy; lactation period; age to 18 years; hypersensitivity to the drug or its components.

For chewing tablets: lactose intolerance, lactase deficiency, glucose-galactose malabsorption; acute hepatic and / or renal insufficiency; pregnancy, lactation; age to 18 years (efficacy and safety not established).

Carefully:Allergic diseases and reactions in the anamnesis.

Pregnancy and lactation:

Contraindicated in pregnancy and lactation, as strictly controlled clinical studies of safety of use of the drug during pregnancy and during lactation was not carried out.

Dosing and Administration:

Intramuscularly and intravenously (struino or drip).

With the infusion method of administration, the drug should be diluted in a 0.9% solution of sodium chloride.

Doses are selected individually. Begin therapy with a dose of 50-100 mg 1-3 times a day, gradually increasing to obtain a therapeutic effect.

Intravenously, the drug is injected slowly for 5-7 minutes, drip - at a rate of 40-60 drops per minute. The maximum daily dose should not exceed 800 mg.

In acute disorders of cerebral circulation, it is prescribed in complex therapy for the first 2-4 days intravenously (drip) at a dose of 200-300 mg, then intramuscularly at 100 mg 3 times a day. Duration of treatment is 10-14 days.

With discirculatory encephalopathy in the phase of decompensation - intravenously (jet or drip) at a dose of 100 mg 2-3 times a day for 14 days, then - intramuscularly at 100 mg twice a day for 14 days.

For the course of prophylaxis of discirculatory encephalopathy - intramuscularly at a dose of 100 mg 2 times a day for 10-14 days.

In light cognitive impairment in elderly patients and with anxiety disorders intramuscularly at a dose of 100-300 mg per day for 14-30 days.

With abstinent alcohol syndrome - intramuscularly in a dose of 100-200 mg 2-3 times a day or intravenously drip 1-2 times a day for 5-7 days.

In acute intoxication with antipsychotic drugs - intravenously at a dose of 50-300 mg per day for 7-14 days.

With light cognitive impairment in elderly patients and with anxiety disorders - intramuscularly at a dose of 100-300 mg per day for 14-30 days.

Inside.

Tablets are chewed and washed down with water. For complex therapy of coronary heart disease and ischemic stroke therapy, 100 mg (1 tablet) is prescribed 3 times a day, gradually increasing the dose to obtain a therapeutic effect. The maximum single dose is 200 mg, the daily dose is 800 mg. Course - not less than 2 months, repeated courses - on the recommendation of a doctor. Duration of treatment and the choice of individual dose depends on the severity of the patient's condition and the effectiveness of treatment.

In the complex treatment of pulmonary and moderate cognitive disorders, the drug is prescribed without restriction of the course of treatment for a duration of 100 mg 3-4 times a day.

Side effects:

For parenteral administration. Possible: dryness and metallic taste in the mouth, sensation of "spilling heat" throughout the body, unpleasant odor, sore throat and chest discomfort, a sense of lack of air (usually associated with an excessively high rate of administration and short-term) ; with prolonged use - nausea, flatulence; sleep disturbances (drowsiness or falling asleep).

For tablets. Usually the drug is well tolerated. In rare cases, there may be allergic reactions, dyspeptic disorders, nausea and dry mouth, diarrhea, which quickly disappear on their own or when the drug is withdrawn. With prolonged use, manifestation of flatulence, sleep disturbance (drowsiness or falling asleep) is possible.

Overdose:

For parenteral administration. Symptoms: sleep disorders (insomnia, in some cases, drowsiness); with intravenous administration - an insignificant and short-term (up to 1.5-2 h) increase in blood pressure.

Treatment: as a rule, is not required - the symptoms disappear on their own within 24 hours. In severe cases with insomnia appoint nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.With excessive increase in blood pressure - antihypertensive drugs under the control of blood pressure.

For tablets. Due to the low toxicity of the drug, an overdose is unlikely. In case of an accidental overdose, there may be symptoms of sleep disturbance - drowsiness, insomnia. Treatment is symptomatic.

Interaction:

Strengthens the action of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa).

Reduces the toxic effects of ethyl alcohol.

Increases antianginal activity of nitro drugs and antihypertensive ACE inhibitors and beta-blockers.

Special instructions:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Instructions

Ethyl methylhydroxypyridine malate (Aethylmethylhydroxypyridini malas)