Astrox - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Ethylmethylhydroxypyridine succinate belongs to the class of 3-hydroxypyridines and has antioxidant, antihypoxic, membrane-protective, nootropic, anticonvulsant, anxiolytic effect, increases the body's resistance to stress. Ethyl methylhydroxypyridine succinate increases the resistance of the organism to the effect of the main damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebral circulation disorder, intoxication with alcohol and antipsychotic drugs (neuroleptics)). Ethyl methylhydroxypyridine succinate 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. Has hypolipidemic action, reduces the level of total cholesterol and low density lipoproteins. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of ethylmethylhydroxypyridine succinate is due to its antihypoxic, antioxidant and membrane-protective action. It inhibits the processes of lipid peroxidation, increases the activity of superoxide dismutase, increases the ratio of lipid proteins, reduces the viscosity of the membrane, and 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, helps preserve the structurally functional organization of biomembranes, neurotransmitter transport and improve synaptic transmission. Ethyl methylhydroxypyridine succinate increases the content of dopamine in the brain.It causes an increase in the compensatory activity of aerobic glycolysis and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle under conditions of hypoxia, with an increase in the content of ATP, creatine phosphate and activation of the energy-synthesizing functions of the mitochondria, stabilization of cell membranes. Ethyl methylhydroxypyridine succinate normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and improves electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic zone, reduces the consequences of reperfusion syndrome in acute coronary insufficiency. Increases antianginal activity nitropreparations. Ethyl methylhydroxypyridine succinate promotes the preservation of retinal ganglion cells and optic nerve fibers in the course of progressive neuropathy, the causes of which are chronic ischemia and hypoxia. It improves the functional activity of the retina and optic nerve, increasing visual acuity.

Pharmacokinetics:

With a single and course use of ASTROXA, the maximum concentration in the blood plasma is reached after 0.58 hours. When administered at a dose of 400-500 mg Cmah in the blood plasma - 3,5-4 mkg / ml. Quickly distributed in organs and tissues. Retention time (MRT) - 0,7-1,3 hours. At the same time, ASTROX is rapidly excreted from the blood plasma and after 4 hours it is practically not detected in it. Pharmacokinetic profiles do not differ significantly in single or continuous administration. Metabolized in the liver by glucuronation. Five metabolites were identified: the liver formed the first metabolite - phosphate 3-hydroxypyridine - which in the blood under the influence of alkaline phosphatase breaks down into phosphoric acid and 3-hydroxypyridine; The 2nd metabolite is formed in large quantities and is found in the urine on the 1-2 day of drug administration, is pharmacologically active; The 3rd metabolite is also excreted in large quantities with urine; The 4th and 5th metabolites are glucuronconjugates. It is excreted in the urine, both in unchanged form, and in the form of glucuronconjugates.

Indications:

As part of complex therapy:

- acute disturbance of cerebral circulation,

- craniocerebral injury, the consequences of craniocerebral trauma,

- discirculatory encephalopathy (including atherosclerotic origin),

- syndrome of vegetative (neurocirculatory) dystonia,

- intellectual-mnestichesky infringements of a various genesis (including infringements of memory at persons of advanced age),

- anxiety disorders in neurotic and neurosis-like states,

- acute myocardial infarction (from the first day),

- primary open-angle glaucoma of different stages',

- the withdrawal of withdrawal symptoms with alcoholism with a predominance in the clinical picture of neurosis-like and vegetative-vascular disorders,

- acute intoxication with antipsychotic drugs.

Contraindications:Hypersensitivity to ethylmethylhydroxypyridine succinate and accessory substance of the preparation, acute violations of the liver and kidneys, children's age, pregnancy, breastfeeding - due to insufficient study of the effect of the drug in these categories of patients.

Carefully:Allergic diseases in the anamnesis.

Pregnancy and lactation:In experimental studies, there was no teratogenic, mutagenic, embryotoxic effect. Adequate and strictly controlled clinical studies of the safety and efficacy of the use of ethylmethylhydroxypyridine succinate during pregnancy and during breastfeeding have not been carried out,so the use of the drug in these periods is contraindicated.

Dosing and Administration:ASTROX is used intramuscularly or intravenously (either jet or drip). The maximum daily dose should not exceed 800-1200 mg (depending on the indications).

For infusion introduction the drug is diluted in a 0.9% solution of sodium chloride. Stream ASTROX injected slowly for 5-7 minutes, drip - at a speed of 40-60 drops per minute.

For treatment acute disorders of cerebral circulation use in the first 10-14 days intravenously drip 200-500 mg 2-4 times a day. Further it is recommended to administer intramuscularly 200-250 mg 2-3 times a day for 14 days.

For treatment of craniocerebral trauma and the consequence of craniocerebral trauma ASTROKS is used for 10-15 days intravenously drip by 200-500 mg 2-4 times a day.

For treatment dyscirculatory encephalopathy in the phase of decompensation ASTROKS are used intravenously struino or drip 200-500 mg 1-2 times a day for 14 days. Then the drug is administered intramuscularly at 100 250 mg per day for the next 2 weeks.

For course of prophylaxis of discirculatory encephalopathy the drug is administered intramuscularly at 200-250 mg twice a day for 10-14 days.

When syndrome of vegetative (neurocirculatory) dystonia, neurotic and neurosis-like states the drug is administered intramuscularly at a dose of 50-400 mg per day for 14 days.

When intellectual-mnestic (cognitive) violations of various genesis (including. memory disorders in the elderly) and with anxiety disorders the drug is used intramuscularly at 100-300 mg per day for 14 to 30 days

For treatment acute myocardial infarction ASTROX is administered intravenously or intramuscularly for 14 days, against a background of standard therapy of myocardial infarction, including nitrates, beta adrenoblockers, angiotensin converting enzyme inhibitors, thrombolytics, anticoagulant and antiplatelet agents, and symptomatic drugs according to indications. In the first 5 days, to achieve maximum effect, the drug is preferably administered intravenously, in the next 9 days ASTROX can be administered intramuscularly. Intravenous administration of the drug is carried out by dropwise infusion, slowly (to avoid side effects) on a 0.9% solution of sodium chloride or 5% solution of dextrose (glucose) in a volume of 100-150 ml for 30-90 minutes. If necessary, a slow jet injection of the drug, which lasts at least 5 minutes, is possible.Administration of the drug (intravenous or intramuscular) is carried out 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg / kg of body weight per day, single dose - 2-3 mg / kg of body weight. The maximum daily dose should not exceed 800 mg, single dose - 250 mg.

When open-angle glaucoma of various stages ASTROX is administered intramuscularly at 100-300 mg per day, 1-3 times per day for 14 days.

When abstinence alcohol syndrome apply 200-500 mg 2-3 times per day intramuscularly or intravenously drip, for 5-7 days.

When acute intoxication with antipsychotic agents the drug is administered intravenously at 200-500 mg per day for 7-14 days.

Side effects:From the gastrointestinal tract: possibly the appearance of nausea, dryness of the oral mucosa, diarrhea.

From the nervous system: drowsiness.

From the immune system: allergic reactions.

Overdose:

Due to low toxicity, an overdose is unlikely and to date no such cases have been reported. In case of an accidental overdose, drowsiness and sedation may occur. 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 a day.With excessive increase in blood pressure - antihypertensive drugs under the control of blood pressure. In severe cases with insomnia - nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.

Interaction:

Enhances the action of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian drugs (levodopa), nitrates. Reduces the toxic effects of ethyl alcohol.

Special instructions:The drug is not prescribed for children under 18 years due to insufficient knowledge of the effect of the drug.

Effect on the ability to drive transp. cf. and fur:

During drug treatment it is necessary to refrain from driving vehicles and practicing other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection, 50 mg / ml.

Packaging:

2 ml per ampoule with a ring or break point from the light-protective glass. 5 ampoules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil. It is allowed to package the preparation in a contour mesh package without foil (pallet).2 contour mesh packages together with instructions for use are placed in a pack of cardboard for consumer packaging.

For 20, 50 or 100 contour squares from polyvinylchloride film and aluminum foil together with 10, 25 or 50 instructions for the use of the preparation, respectively, in a box of cardboard (for inpatient).

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001701

Date of registration:04.05.2012 / 22.06.2017

Expiration Date:Unlimited

Date of cancellation:2017-05-04

The owner of the registration certificate:HOMEKSFARM LLCHOMEKSFARM LLC Russia

Manufacturer: & nbsp

GosMPS, FSUE Russia

Information update date: & nbsp20.10.2017

Illustrated instructions

Instructions

Astrox (Astrox)