Pharmacological properties

Pharmacodynamics. renders to glutoksy the immunostimulating, haemo stimulating, toksikomodifitsiruyushchy, hepatoprotective action, suppresses medicament resistance of tumor cells to antibiotics of an anthracycline row, the alkylating means; allows to overcome the medicament resistance of micobacterium tuberculosis to an isoniazid associated with katg genes (catalase peroxidase gene) and inha (gene of phenol-apb-reductase). glutoksy exponentiates effect of doxorubicine on tumor cells, funds of chemotherapy (an isoniazid, rifampicin, a rifabutin, Cycloserinum, a kapreomitsin, a levofloksatsin, cationic antimicrobic peptide of a kataltsidin) for micobacterium tuberculosis.

Immunomodulatory effect of the medicine Glutoksim is caused by the influence on kaltsiyzavisimy alarm ways of macrophages mediated by receptors that leads to increase:

• survival and functional capacity of fabric macrophages;
• an exocytosis of submembrane granules with intracellularly parasitizing Micobacterium tuberculosis forms;
• activity of lizosomalny enzymes;
• formation of active forms of oxygen;
• absorption and death of microorganisms;
• secretion of cytokines: interlekina-1, interleukin-6, tumor necrosis factor, interferon, erythropoietin, interleukin-2; cationic antimicrobial peptides — a defensin, kataletsidin.

Gemostimuliruyushchy effect of the medicine Glutoksim is caused by strengthening of marrowy blood formation mediated by receptors: processes of an erythrogenesis, lymphopoiesis and granulotsitomonotsitopoez. Action on progenitors of various lines of uniform elements of blood is mediated by functioning of MAP- and inositol-kinaznoy systems, leads to increase in stability of hemopoietic cages which are differentiated, restores their sensitivity to action of internal causes of a hematopoiesis.

Toksikomodifitsiruyushchy and hepatoprotective effect of medicine are caused by strengthening of an expression of enzymes of the second phase of a detoxication of xenobiotics mediated by receptors, including glutationreduktaza, glutathione peroxidases, glutathione-S-tranferazy, glyukozo-6-fosfatdegidrognazy, gemoksigenazy-1, increase in intracellular level of the restored glutathione that provides protection of cellular structures against toxic action of radicals.

Glutoksim has direct inhibiting effect on activity of a factor of multiple medicament resistance of tumor cells — protein a P-glycoprotein (Pgp) which defines resistance of tumor cells to action of means of chemotherapy, including anthracycline antibiotics, medicines of the alkylating action.

Glutoksim initiates reaction of transformation of an isoniazid (pro-medicine) in pharmacological active form — isonicotinic acid which has bacteriostatic action on Micobacterium tuberculosis caused by negative transformation of genes of katG (catalase peroxidase gene) and inhA (fenol-APB-reduktazy gene).

processes of an exocytosis of vesicles of macrophages with intracellularly parasitizing microorganisms, including Micobacterium tuberculosis, providing their removal from pharmacological storage and making available to effect of antibacterial medicines, including an isoniazid, rifampicin, rifabutin, Cycloserinum, kapreomitsin, levofloxacin.

Glutoksim strengthens secretion of cationic peptides — defensin and kataletsidin macrophages, stimulates their absorption with Mycobacterium tuberculosis, defining the mediated antibacterial effect of medicine.

Pharmacokinetics. Glutoksim treats group of natural metabolites that determines features of his metabolism by the existing cellular enzymatic systems. After in oil, in/in or p / to an injection the bioavailability exceeds 90%. The linear dependence between a dose and concentration of medicine in blood plasma is noted. The C _max medicine in blood plasma at in in introduction is reached within 2–5 min., at in oil — within 7–10 min. As the natural product of the peptide nature Glutoksim is metabolized in bodies and body tissues with elimination by kidneys.

Indication

As prophylactic and treatments at the adult secondary immunodeficiency associated with radiation, chemical and infectious factors;

• for restoration of suppressed immune responses and depression of marrowy blood formation;
• for increase in resistance of an organism to various pathological influences — to infectious agents, chemical and/or physical factors (intoxication, radiation, etc.);
• as hepatoprotective cure for a chronic viral hepatitis In and With;
• for potentiation of medical effects of antibacterial therapy of HOBL;
• for prevention of postoperative purulent complications;
• as a part of complex antitubercular therapy of severe common forms of tuberculosis of all localizations;
• with medicinal resistance of Mycobacterium tuberculosis to drugs;
• for prevention of exacerbations of chronic hepatitis at TB patients against the background of antitubercular therapy;
• for treatment of toxic complications of antitubercular therapy;
• as a part of complex therapy of psoriasis, in particular medium-weight and severe forms with presence of an erythrosis, arthropathy;
• as a part of complex therapy of malignant new growths in oncology for prevention and treatment of toxic manifestations khimio- and radiation therapy, namely: promotes decrease haemo - and hepatotoxic action, to effective restoration of functions of marrowy blood formation when performing antineoplastic therapy. For elimination of manifestations of a nonspecific syndrome of a disease (anemia, fatigue, a loss of appetite, the increased painful sensitivity).

Use

Drug glutoksy is administered in/in, in oil, p / to. appoint daily 5–40 mg (to 1 course — 50–300 mg) depending on the nature of a disease.

With the preventive purpose medicament is used in oil daily on 5–10 mg during 2 weeks

as a part of complex therapy of tuberculosis of Glutoksy 60 mg enter 1 time a day the first 10 days daily in oil, the next 20 days of Glutoksy 60 mg enter in oil every other day, 1 injection a day.

a repeated course of treatment in 1–6 months

as a part of complex therapy of psoriasis Glutoksim apply in oil daily in a daily dose of 10 mg within 15 days, then during 5 weeks 2 times a week in a daily dose of 10 mg. Only 25 injections on a course of treatment.

as means of maintenance of chemotherapy in oncology of Glutoksy 60 mg is entered p / to for 1.5-2 h before application of antineoplastic means. Further between courses of chemotherapy of Glutoksy 60 mg enter p / to every other day. At the following course of chemotherapy the scheme of use of medicine repeats.

as means of maintenance of radiation therapy of Glutoksy 60 mg is entered p / to in 0.5-1 h after another session of radiation every other day throughout all course of radiation therapy.

Use of medicine is contraindicated to

Contraindication

Side effects

At certain patients can note slight increase of body temperature (to 37.1-37.5 °c), morbidity in the place of an injection of medicine. at bad subjective shipping of pain glutoksy enter 0.5% of solution of novocaine together with 1–2 ml. in such cases, considering information on safety of use of novocaine, before use of medicine it is necessary to collect carefully the allergological anamnesis, to take skin compatibility tests.

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Special instructions

As solution — the carrier for infusional introduction use 0.9% solution of sodium of chloride or 5% glucose solution.

Use during pregnancy or feeding by a breast. Do not apply.

Children. Do not apply.

Ability to influence speed of response at control of vehicles or work with other mechanisms. An adverse effect it is not established.

Interaction

Glutoksim, at the combined application exponentiates bacteriostatic effect of an isoniazid, rifampicin, a rifabutin, Cycloserinum, a kapreomitsin, levofloksatsin on micobacterium tuberculosis, an anthracycline antibiotic of the doxorubicine alkylating means of an etopozid — on tumor cells.

Glutoksim reduces therapeutic effect of nifedipine and verapamil.

Inhibitors of a cyclooxygenase way of oxidation of arachidonic acid — indometacin, to meloksika — reduce or completely suppress pharmacological effect of the medicine Glutoksim.

Incompatibility. Glutoksim can be entered in one syringe with water-soluble medicines. Drug is compatible to such solvents as 0.9% solution of sodium of chloride or 5% glucose solution.

Overdose

About cases of overdose of medicine it was not reported.

Storage conditions

B the place protected from light at a temperature not above 25 °C.