Active substanceProthionamideProthionamide
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet contains:

    active substance: protionamide 250.00 mg;

    Excipients: internal part: microcrystalline cellulose 81.40 mg, copolyvidone 4.30 mg, hypromellose (hydroxypropylmethylcellulose) 4.30 mg, crospovidone 8.60 mg, magnesium stearate 1.40 mg;

    shell: hypromellose (hydroxypropylmethylcellulose) 5.40 mg, titanium dioxide 1.30 mg, yellow-orange S 1.10 mg, macrogol 6000 (polyethylene glycol 6000) 2.40 mg.

    Description:

    Yellow-orange tablets, covered with a film sheath, with a notch on one side.

    Pharmacotherapeutic group:anti-tuberculosis drug
    ATX: & nbsp

    J.04.A.D.01   Prothionamide

    Pharmacodynamics:

    Anti-tuberculosis means of series II, acts bacteriostatically, blocks the synthesis of mycolic acids,which are the most important structural component of the mycobacterium tuberculosis cell wall. Has the properties of a nicotinic acid antagonist. In high concentrations, it breaks the synthesis of the protein of the microbial cell and acts bactericidal.

    Effective against mycobacteria tuberculosis, resistant to drugs of the I series.

    The use in combination with other anti-tuberculosis drugs reduces the likelihood of developing tuberculosis resistance.

    Pharmacokinetics:

    Prothionamide is rapidly absorbed in the gastrointestinal tract, creating a maximum concentration of the drug in the blood plasma 2-3 hours after ingestion. Penetrates into healthy and pathologically altered tissues (tubercular foci and caverns in the lungs, serous and purulent pleural effusion, cerebrospinal fluid with meningitis). In the body it is partially converted into sulfoxide, which has tuberculostatic activity. Partially excreted unchanged (up to 15-20% of the dose) with urine and feces.

    Indications:

    Prothionamide is used to treat all forms of tuberculosis, including, with the resistance of the pathogen to other anti-tuberculosis drugs (I series) or their intolerance.

    Contraindications:

    Prothionamide should not be used with individual hypersensitivity to the components of the drug, during pregnancy and lactation, acute gastritis, peptic ulcer and duodenal ulcer, erosive ulcerative colitis, acute hepatitis, cirrhosis, chronic alcoholism.

    Dosing and Administration:

    Take the drug inside after eating.

    Adults appoint 0.25 g 3 times a day; with good tolerance - 0.5 g 2 times a day.

    In patients older than 60 years and with a body weight of less than 50 kg daily dose should not exceed 0.75 g (more often prescribed to 0.25 g 2 times a day).

    Children appoint at the rate of 10-20 mg / kg body weight per day.

    Side effects:

    Side effects of protionamide are manifested from the gastrointestinal tract, liver, skin, endocrine and nervous system.

    On the part of the gastrointestinal tract, loss of appetite, nausea, vomiting, dryness and metallic taste in the mouth. After the withdrawal of the drug, these phenomena tend to quickly pass.

    Often during the treatment there is a rise in the blood level of transaminases. Rare violations of liver function with signs of hepatitis and jaundice are rare.Hepatotoxicity of the drug depends on the existing violations of liver function, such as liver damage due to alcoholism or after surgery. These side effects are noted especially in combination therapy with isoniazid, rifampicin and pyrazinamide.

    Skin reactions are rare, in some cases described pellagro-like reactions, respectively, with a combination of skin manifestations and disorders from the central nervous system.

    Sometimes there are violations of the endocrine system.

    Along with the development of hypoglycemia (a decrease in blood sugar of less than 50 mg%) in diabetic patients, the development of gynecomastia (an increase in mammary glands in men) is described. Rarely there is a violation of the menstrual cycle and impotence, as well as hypothyroidism (a decrease in thyroid function).

    The protionamide can sometimes cause disorders of the peripheral and central nervous system. In a combination with isoniazid cases of polyneuropathy are described. Taking protionamide can cause dizziness, headaches, impaired concentration, mental disorders. Simultaneous reception of other active anti-tuberculosis drugs, such as isoniazid or cycloserine, can lead to an increase in side effects on the central nervous system. The same effect can have a simultaneous reception of alcohol.

    In some cases, allergic reactions and disorders of the bone marrow are described.

    Interaction:

    With combined therapy of tuberculosis, the additive hepatotoxic effect of individual drugs should be taken into account. This is especially true for the combination of a protionamide with isoniazid, rifampicin and pyrazinamide. Additive effect on the central nervous system is noted with the combined use of isoniazid and cycloserine.

    Simultaneous reception of alcohol leads to an intensifying of the stimulating effect on the central nervous system.

    In certain cases, when taking protionamide, it is necessary to reduce the dose of insulin or oral antidiabetic drugs.

    Due to metabolic competition, there is a slowdown in the destruction of other drugs, such as isoniazid or barbiturates, in the body.

    Special instructions:

    It is necessary to avoid the joint use of protionamide and alcohol because of the danger of the emergence of excitatory states of the central nervous system (associated with the increase in the toxic effect of alcohol).

    In the combined use of protionamide with isoniazid and cycloserine, special attention should be paid to the possibility of mental disorders.

    Since the drug is constantly used in combination with other antituberculous drugs, regular monitoring of serum transaminases, gamma-glutamate transferase and alkaline phosphatase is necessary.

    Diabetics need control of blood sugar levels.

    Skin and especially mucous reactions may be the first signs of pellagruide-like side effects. This should be regarded as a precursor to the necessary withdrawal of the drug.

    Form release / dosage:

    Tablets, film-coated, 250 mg.

    Packaging:

    For 100 tablets in a white container made of polypropylene with a white lid of low density polyethylene with a ring of the first opening, the empty space is filled with foam rubber sealant. A container of 100 tablets together with the instruction for use is placed in a cardboard box.

    For 1000 tablets in a brown PVC container with a protective membrane of low pressure polyethylene and a black screw cap made of bakelite with a PVC liner, the empty space is filled with foam rubber sealant, on top of which is placed the instruction for use.For 10, 20, 30, 40 containers (1000 tablets) are placed in a group package - a cardboard box (for hospitals).

    Storage conditions:

    Store at a temperature not exceeding + 25 ° ะก.

    Protect from moisture and light.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N014968 / 01-2003
    Date of registration:15.05.2009
    The owner of the registration certificate:Rimzer Artsynaimitel, AGRimzer Artsynaimitel, AG Germany
    Manufacturer: & nbsp
    Representation: & nbspSVYCH LLC SVYCH LLC Russia
    Information update date: & nbsp09.09.2015
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