Encephabol® (Encephabol®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePyrithinolPyrithinol
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  • Encephabol®
    suspension inwards 
    Merck KGaA     Germany
  • Encephabol®
    pills inwards 
    Merck KGaA     Germany
    • Dosage form: & nbspSuspension for oral administration.
    Composition:

    5 ml of suspension (1 teaspoon) contain:

    Active component - Pyrithinol 80.5 mg;

    Excipients - Sodium saccharinate dihydrate 1.1 mg, propyl parahydroxybenzoate -1.75 mg, methyl parahydroxybenzoate 3.25 mg, citric acid monohydrate 5,0 mg, potassium sorbate 6.75 mg, aromatic contragram 2.65 mg, povidone - 50.0 mg, silicon dioxide colloid - 50.0 mg, hyethellosis - 36.805 mg, glycerol 85% - 250.0 mg, sorbitol solution 70% - 750.0 mg, purified water - 4 062.195 mg.

    * Corresponds to the content of pyrithinol dihydrochloride monohydrate 100 mg

    Description:Viscous suspension from milky white to slightly brownish color with a fragrant smell.
    Pharmacotherapeutic group:Nootropic agent.
    ATX: & nbsp

    N.06.B.X.02   Pyrithinol

    Pharmacodynamics:

    Pyrithinol increases pathologically reduced metabolism in the brain by increasing the uptake and utilization of glucose, increases the metabolism of nucleic acids and the release of acetylcholine in the synapses of nerve cells, improves cholinergic transmission between cells of the nervous tissue. Helps stabilize the structure of the cell membrane of nerve cells and their function by inhibiting the enzymes of lysosomes, thus preventing the formation of free radicals.

    Piritinol improves the rheological properties of blood, increases the plasticity of erythrocytes by increasing the ATP content in their membrane, which leads to a decrease in blood viscosity and an improvement in blood flow. Pyrithinol, improving blood circulation in ischemic areas of the brain, increases their supply of oxygen; increases the exchange of glucose. As a result, memory parameters are improved and disturbed metabolic processes in the nervous tissue are restored, which contributes to the full functioning of its cells.

    Pharmacokinetics:

    Pyrithinol is rapidly absorbed when taken orally. Bioavailability averages 85 % (76 - 93%). The maximum concentration in plasma is reached in 30 - 60 minutes after ingestion of 100 mg of pyrithinol dihydrochloride monohydrate. Half-life is about 2.5 hours.

    Pyrithinol metabolizes rapidly. 20 - 40% of the substance reversibly binds to plasma proteins. As the main metabolites, the following substances were identified: 2-methyl-3-hydroxy-4-hydroxymethyl-5-methylmercaptomethylpyridine and 2-methyl-3-hydroxy-4-hydroxymethyl-5-methylsulphinylmethylpyridine. Conjugated metabolites are excreted mainly through the kidneys.The total urinary excretion within 24 hours is 72.4 - 74.2%. The greatest part of the dose received is excreted within the first 4 hours after administration. Only 5% of the dose is excreted with feces.

    At repeated oral appointment cumulation is not observed. Toxic concentrations do not develop even with impaired renal function.

    Penetrates through the blood-brain barrier, metabolites accumulate mainly in the gray matter of the brain.

    Pyrithinol penetrates the placental barrier. The conducted studies did not reveal teratogenic or embryotoxic activity.

    Indications:

    Symptomatic treatment of chronic disorders of brain function in the presence of the following main symptoms:

    - memory impairment, concentration of attention and thinking;

    - decreased motivation;

    - fast fatiguability;

    - other symptoms in cerebrovascular diseases or disorders.

    In pediatrics: disorders of neuropsychiatric development.

    Contraindications:

    - hypersensitivity to pyrithinol and excipients;

    - chronic rheumatoid arthritis in combination with the following concomitant diseases: severe renal or hepatic impairment;severe blood diseases; autoimmune diseases: systemic lupus erythematosus, myasthenia gravis, pemphigus (acute or in anamnesis).

    Since the preparation contains sorbitol, its use is not recommended for patients with rare hereditary diseases associated with intolerance to fructose.

    Since the drug contains parahydroxybenzoate, in rare cases, allergic reactions are possible in predisposing patients, which may manifest with a delay.

    Carefully:

    Caution should be given to patients with severe renal or hepatic insufficiency, severe blood diseases, rheumatoid arthritis, hypersensitivity to D-penicillamine, autoimmune diseases: systemic lupus erythematosus, myasthenia gravis, and pemphigus (acute or in history).

    Pregnancy and lactation:

    Data for a limited number of pregnant women using this drug indicate that there are no undesirable effects of pyrithinol on pregnancy or fetus / newborn health. There are no other relevant epidemiological data at present.Studies in animals have not detected any direct or indirect adverse effect of pyrithinol on pregnancy, embryonic development, childbirth or postnatal development.

    Pyrithinol penetrates the placental barrier and its insignificant amounts (max 0.4%) are excreted into breast milk. There is no threat to the child.

    The drug should be used only if the expected benefit to the mother exceeds the possible risk to the fetus and the baby.

    Dosing and Administration:

    Adults: 2 teaspoons of suspension 3 times a day (600 mg of pyrithinol dihydrochloride monohydrate per day).

    Newborns: from 3 days after birth, 1 ml of suspension per day for a month, the dose is taken in the morning. Starting from 2 months after birth, this dose is increased by 1 ml every week, until the daily dose reaches 5 ml (1 teaspoon).

    Children from 1 year: 1½ teaspoons of suspension 1 to 3 times a day (50 to 300 mg of pyrithinol and hydrochloride monohydrate per day, depending on the indications).

    Children from 7 years old: - 2 teaspoons of the suspension 1-3 times a day (50 to 600 mg of pyrithinol dihydrochloride monohydrate per day, depending on the indications).Take the drug should be during or after a meal. In cases of sleep disorders, the last daily dose should not be taken in the evening or at night.

    The duration of treatment depends on the clinical picture of the disease. Typically, therapeutic success is achieved after 3-4 weeks of treatment. The optimal effect usually occurs in 6-12 weeks. Duration of treatment should be at least 8 weeks, and if necessary, it can be continued. In newborns with a high risk of developing perinatal pathology of the central nervous system, the average duration of treatment is an average of 6 months.

    After three months, you should check for evidence of further treatment.

    Side effects:

    The frequency of side effects of the drug is assessed as follows: Very frequent:> 1/10 Frequent:> 1/100, <1/10 Infrequent:> 1/1000, <1/100 Rare:> 1/10 000, <1/1000 Very rare: <1 / 10,000

    Disturbances from the blood and lymphatic system (*)

    Infrequently: Eosinophilia, thrombocytopenia;

    Very rarely: leukopenia, agranulocytosis;

    Disorders from the gastrointestinal tract

    Often: Nausea, vomiting, stomatitis, diarrhea;

    General disorders and disorders at the site of administration

    Infrequent: Headache, dizziness, taste disorders *, a feeling of cold, fatigue;

    Disturbances from the liver and bile ducts

    Infrequently: Liver failure *;

    Very rarely: Hepatitis *, cholestasis *, cholestatic hepatitis *, jaundice;

    Immune system disorders (*)

    Often: Hypersensitivity reactions of varying severity mainly in the form of rashes on the skin or mucous membranes, itching, fever;

    Rarely: Autoimmune insulin syndrome;

    Disorders from the metabolism and nutrition

    Infrequently: Decreased appetite;

    Disturbances from musculoskeletal and connective tissue

    Very rarely: myalgia, arthralgia, myasthenia gravis, polymyositis *;

    Disturbances from the nervous system

    Often: Sleep disturbances;

    Infrequent: Increased excitability;

    Very rarely: Paresthesia *;

    Disorders from the kidneys and urinary tract

    Often: Proteinuria;

    Very rarely: Nephrotic syndrome, hematuria *;

    Disturbances from the respiratory system, chest and mediastinal organs

    Very rarely: dyspnea;

    Disturbances from the skin and subcutaneous tissues

    Often: Rash *, itching;

    Very rarely: Flat lichen *, urticaria *, bullous pemphigoid skin reaction *, alopecia *, onycholysis *;

    Laboratory and instrumental data (*)

    Infrequently: Increased transaminase activity, the appearance of antinuclear antibodies;

    Very rare: The appearance of LE cells, the appearance of anti-insulin antibodies.

    * If these side effects occur, treatment should be immediately discontinued and symptomatic therapy should be prescribed if necessary.

    Overdose:

    In case of an overdose, the severity of side effects increases. It is necessary to consult a doctor. The first help consists in washing the stomach, taking activated charcoal.

    Interaction:

    Pyrithinol can potentiate the adverse reactions of penicillamine, preparations of gold, sulfasalazine, levamisole.

    Special instructions:

    Presumably, patients with rheumatoid arthritis experience increased sensitivity to the compounds (including pyrithinol), which has a thiol group (SH-group), which is associated with the underlying disease. In this regard, patients with rheumatoid arthritis may have more frequent adverse reactions, characteristic of anti-rheumatic drugs, including leukopenia,agranulocytosis, eosinophilia, thrombocytopenia, liver dysfunction, increased transaminase activity, cholestasis, rash, itching, alopecia, lichen, bullous pemphigoid skin reaction, the appearance of antinuclear antibodies, the appearance of LE cells, the appearance of anti-insulin antibodies, paresthesia.

    Patients with rheumatoid arthritis are recommended to undergo regular medical examinations and laboratory tests.

    Patients with known hypersensitivity to D-penicillamine may experience similar side effects due to chemical similarity to pyrithinol (thiol groups).

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

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, due to the possibility of unwanted reactions in some patients, such as dizziness and fatigue.

    Form release / dosage:

    Suspension for oral administration.

    Packaging:

    To 200 ml in a bottle of dark glass with an aluminum screw cap with the control of the first opening.The bottle is placed in a cardboard box along with the instructions for use.

    Storage conditions:

    Store at a temperature of 20 - 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013412 / 01
    Date of registration:22.01.2008
    The owner of the registration certificate:Merck KGaAMerck KGaA Germany
    Manufacturer: & nbsp
    Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.
    Information update date: & nbsp16.10.2015
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