Neurophasole (Neurophazol)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceMorpholinoethylthioethoxybenzimidazoleMorpholinoethylthioethoxybenzimidazole
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  • Neurophasole
    concentrate d / infusion 
    LEKKO, ZAO     Russia
    • Dosage form: & nbsptooncentrate for solution for infusion
    Composition:

    1 ml of the preparation contains:

    active substance: morpholinoethylthioethoxybenzimidazole dihydrochloride 5.0 mg;

    Excipients: sodium chloride, water for injection.

    Description:Transparent, colorless or slightly colored liquid.
    Pharmacotherapeutic group:Neuroprotective agent
    ATX: & nbsp

    N.05.B   Anxiolytics

    Pharmacodynamics:

    Neurophasol possesses neuroprotective properties.

    The mechanism of action of Neurophazole is due to the interaction with sigma1-receptors, through which the phospholipid frame of the receptor structures of the cell surface is restored; normalization of the calcium balance; counteracting glutamate excitotoxicity and increased production of nitric oxide; restoration of the deficit of nerve growth factors.

    Neurophazole improves the survival of neurons and reduces the severity of cytotoxic reactions in the damaging effects of oxidative stress and glutamate, normalizes the level of caspase-3, one of the main enzymes activated by apoptosis.

    The drug has a stimulating effect on the formation of neurotrophic brain factors - NGF (nervegrowth factor, nerve growth factor) and BDNF (brain-derived neurotrophic factor - cerebral neurotrophic factor).

    The drug has a protective effect on cells of the penumbra zone in conditions of local ischemia, reduces the severity of post-insult disorders and accelerates the restoration of neurologic functions. With cerebral ischemia, Neurophazol suppresses NO-synthesis pathway for the formation of nitric oxide in neurons of the brain, prevents an increase in activity NO-syntase. It causes an improvement in energy metabolism, restoring the activity of succinate dehydrogenase in brain ischemia. Promotes increased cerebral blood flow in ischemic conditions, without affecting systemic arterial pressure. The participation of GABA-ergic system in the implementation of cerebrovascular and neuroprotective action of the drug was established.

    Pharmacokinetics:

    The half-life of Neurophazole is 0.82 hours. Rate constant elminationaland from the blood plasma - 2.12 hours-1. The concentration of the drug in the blood plasma increases in proportion to the increase in the dose of Neurophazole. After intravenous administration, it is quickly captured by cells of different organs and tissues. Well penetrates the blood-brain barrier.According to experimental data, it undergoes intensive metabolism in the liver. It is excreted from the body mainly in the form of metabolites. 24 hours after administration, unchanged in the urine, 0.07% is recorded, in feces 0.05% of the administered dose.

    Indications:

    A cerebral infarction (ischemic stroke).

    Contraindications:

    - BVariability, lactation period;

    - individual intolerance to the drug;

    - age to 18 years.

    Dosing and Administration:

    Neurophazole is used as a part of complex therapy in the form of intravenous drip infusions in a dose of 10 mg 2 times a day. The recommended duration of treatment is 10 days.

    Before use, 10 mg of the drug is diluted in 150-200 ml of 0.9% sodium chloride solution, the recommended rate of administration is 40-60 drops / min.

    Side effects:Perhaps the development of headaches, dizziness, general weakness, which are of a short-term nature and are self-sufficient. Allergic reactions are possible. According to the results of clinical studies, a single case of paroxysmal atrial fibrillation was recorded (there was no connection with the drug intake).
    Overdose:

    If the daily dose is exceeded, there may be a sedative effect and increased drowsiness. As an emergency, caffeine sodium benzoate (caffeine) 20% solution in ampoules of 1.0 ml 2-3 times a day subcutaneously.

    Interaction:

    Neurophazole can be used together with acetylsalicylic acid, enalapril, indapamide, atenolol, nifedipine, digoxin, rheopolyglucin dextran.

    Does not affect the narcotic effect of ethanol and the hypnotic effect of thiopental.

    Potentiates the anticonvulsant effect of carbamazepine.

    It causes an increase in the anxiolytic effect of diazepam.

    Form release / dosage:

    Concentrate for solution for infusion, 5 mg / ml.

    Packaging:

    For 2 ml in bottles of dark glass, sealed with rubber stoppers, with aluminum caps with the control of the first opening.

    5 bottles in a planar cell packaging made of a polyvinyl chloride film.

    2 contour mesh packages together with instructions for use in a pack of cardboard.
    Storage conditions:

    In the dark place at a temperature of 0 to 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002102/10
    Date of registration:16.03.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:LEKKO, ZAO LEKKO, ZAO Russia
    Manufacturer: & nbsp
    Representation: & nbspLEKKO ZAO LEKKO ZAO Russia
    Information update date: & nbsp28.06.2018
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