Astrox, 50mg/ml 2ml 10pcs

ASTROX belongs to the class of 3-oxypyridines. It has antioxidant, antihypoxic, membrane stabilizing, nootropic, stress-protective, anticonvulsant, anxiolytic effect. It inhibits lipid peroxidation processes, increases antioxidant enzyme system activity, restores disturbed membrane structure and function, has a modeling effect on ion channels, neurotransport, and improves synaptic transmission. The drug increases resistance to the effects of various damaging factors (shock, hypoxia, ischemia, trauma, cerebral circulation disorders, intoxication with alcohol and antipsychotics (neuroleptics) by activating energy-synthesizing functions of mitochondria and improving energy metabolism in the cell. ASTROX has hypolipidemic effect, reduces the content of total cholesterol and low-density lipoproteins. The mechanism of action is based on the ability of ethylmethylhydroxypyridine succinate to increase the compensatory activation of aerobic glycolysis and decrease the degree of inhibition of oxidative processes in the Krebs cycle in hypoxia with increase of ATP and creatine phosphate content and stabilization of cell membranes.

ASTROX is an inhibitor of free-radical processes of lipid peroxidation. It activates superoxidase, influences physicochemical membrane properties, increases the content of polar lipid fractions (phosphotidylserine and phosphotidylinositol etc.) in the membrane.) in membrane, decreases cholesterol/phospholipids ratio, decreases lipid layer viscosity and increases membrane fluidity, activates energy-synthesizing functions of mitochondria and improves energy exchange in a cell and, thus, protects cell apparatus and cell membrane structure. Changes in the functional activity of biological membranes caused by the drug lead to conformational changes in protein macromolecules of synaptic membranes, so that it has a modulating effect on the activity of membrane-bound enzymes, ion channels and receptor complexes, in particular benzodiazepine, GABA, acetylcholine, increasing their ability to bind to ligands, increasing neurotransmitter activity and activation of synaptic processes.

Pharmacokinetics

At a single and course of administration of ASTROX the maximum concentration in blood plasma is reached after 0.58 h. When administered in a dose of 400-500 mg the Cmax in blood plasma is 3.5-4 mcg/ml. It is rapidly distributed in organs and tissues. Retention time of the drug (MRT) is 0.7-1.3 hours. At the same time ASTROX is rapidly eliminated from the blood plasma and is practically undetectable in the blood plasma after 4 hours. Pharmacokinetic profiles do not differ significantly with both single and continuous administration. It is metabolized in the liver by glucuronidation. Five metabolites have been identified: 1st metabolite is formed in the liver – 3-oxypyridan phosphate – which in the blood under the influence of alkaline phosphatase breaks down into phosphoric acid and 3-oxypyridine; 2nd metabolite is formed in large quantities and found in the urine on 1-2 days of drug administration, it is pharmacologically active; 3rd metabolite is also excreted in large quantities with the urine; 4th and 5th metabolites are glucuronconjugates. It is excreted with urine both unchanged and as glucuronconjugates.

Indications

acute cerebral circulatory disorders;

discirculatory encephalopathy;

vegetative dystonia syndrome;

neurotic disorders with anxiety syndrome;

Intellectual and mental disorders of various genesis (including.ч. memory impairment in elderly people);

Correction of withdrawal syndrome in alcoholism with predominance of neurosis-like and vegetovascular disorders in the clinical picture;

acute intoxication with antipsychotic drugs.

Active ingredient

Composition

active substance – ethylmethylhydroxypyridine succinate – 50 mg, excipient – water for injection – up to 1 ml

How to take, the dosage

ASTROX is administered intramuscularly or intravenously (by trickle or drip). Treatment begins with a dose of 50-100 mg 1-3 times a day, gradually increasing the dose until therapeutic effect is obtained. Duration of treatment and choice of individual dose depends on the severity of the patient’s condition and effectiveness of treatment. Maximum daily dose should not exceed 800 mg.

For infusion the drug is diluted in 200 ml of physiological 0.9% sodium chloride solution. ASTROX is administered slowly over 5-7 minutes by jetting, by drip – at a rate of 60 drops per minute.

For treatment of acute impairment of cerebral circulation, ASTROX is administered intravenously by drip 200-300 mg once a day for the first 2-4 days. Later it is recommended to administer intramuscularly 100 mg 3 times a day. The duration of treatment is 10-14 days.

For treatment of dyscirculatory encephalopathy in decompensation phase ASTROX is administered intravenously by trickle or drip infusion of 100 mg 2-3 times daily during 14 days. Then the drug is administered intramuscularly by 100 mg per day for the next 2 weeks. For course prophylaxis of discirculatory encephalopathy the drug is administered intramuscularly by 100 mg 2 times daily during 10-14 days.

In case of alcohol withdrawal syndrome ethylmethylhydroxypyridine succinate is administered by 100-200 mg intramuscularly 2-3 times a day or by intravenous drip 1-2 times a day, for 5-7 days.

In cases of intellectual and cognitive disorders, the drug is prescribed intramuscularly 100-300 mg per day for 14 to 30 days.

In acute intoxication with neuroleptics and narcotic drugs the drug is administered intravenously 50-300 mg per day for 7-14 days.

In cases of neurotic disorders and vegetative dystonia syndrome the drug is given intramuscularly in a dose of 50-400 mg per day for 14 days.

Interaction

When used in combination, ASTROX increases the effect of anticonvulsants (carbamazepine), tranquilizers (phenazepam, diazepam), anti-Parkinsonian drugs (levodopa), nitrates. Reduces the toxic effects of ethyl alcohol.

Special Instructions

In the beginning of treatment with the drug, it is necessary to refrain from potentially dangerous activities that require increased concentration and quick psychomotor reactions (attention of drivers!)

Contraindications

Hypersensitivity, acute liver and renal dysfunction, childhood, pregnancy, breast-feeding – due to the insufficient study of the drug action in this category of patients.

With caution: history of allergic diseases

Side effects

Nausea, dry mouth or a “metallic” taste in the mouth, a feeling of “overflowing heat” in the whole body, possible allergic reactions, unpleasant odor, throat and chest discomfort, shortness of breath (usually associated with excessive speed of administration and short-term); with long-term use – nausea, flatulence; sleep disorders (drowsiness or failure to fall asleep).

Overdose

Due to the low toxicity, overdose is unlikely and no such cases have been reported to date. In case of accidental overdose, drowsiness and sedation may occur. When administered intravenously, slight and transient (up to 1.5-2 hours) increase in BP. Treatment is usually not required – symptoms disappear on their own within 24 hours. If there is an excessive increase in blood pressure, hypotensive drugs under BP control are used. In severe cases of insomnia – nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg.

Similarities