Thioureidoimiminomethylpyridinium perchlorate (Thioureidoiminomethylpyridinii perchloras)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Other synthetic antibacterial agents

Included in the formulation
  • Perchloron®
    pills inwards 
    FARMASINTEZ, JSC (Irkutsk)     Russia
    • АТХ:

    J.04.A.K   Other antituberculous drugs

    Pharmacodynamics:

    Anti-tuberculosis drug. The mechanism of action is not established. Active with respect to Mycobacterium tuberculosis and Mycobacterium bovis. Has a pronounced inhibitory effect on the viability of mycobacteria tuberculosis, including those resistant to other antituberculous drugs.

    Thioureidoiminomethylpyridinium perchlorate is a low-toxic substance that does not cause significant structural and functional damage to vital organs and systems, as well as irritating effects on the mucous membranes of the gastrointestinal tract.

    The mechanism of action is not definitively established, the study continues.

    Pharmacokinetics:

    After oral administration, it is rapidly absorbed in the gastrointestinal tract. The time to reach the maximum concentration in the blood (TCmax) is 1.5-3 hours. After a single oral dose of 400 mg, 800 mg, 1200 mg and 1600 mg, the maximum concentration in the blood (Cmax) is 2.61 ± 0.34 μg / ml, 5.07 ± 0.69 μg / ml, 5.42 ± 0.65 μg / ml and 8.17 ± 1.91 μg / ml, respectively.

    The half-life is 12-27 hours. The time to establish a steady-state concentration (Css) of active substance in the blood for prolonged use is 14 days.The concentration of active substance in the blood at the course of taking the drug (1 time per day), measured 15 minutes before the next dose is 23.4 μg per 1 ml of blood plasma.

    The pathways of metabolism of the active substance are not established, the study continues.
    Indications:

    Tuberculosis of the lungs, including multidrug-resistant Mycobacterium tuberculosis (as part of combination therapy).

    ICD-10

    I.A15-A19.A15   Tuberculosis of respiratory organs, confirmed bacteriologically and histologically

    Contraindications:
    • Hypersensitivity to the active substance or to any components of the drug;
    • Violation of the function of the liver and / or kidneys (the possibility of using the drug in this category of patients has not been studied);
    • Pregnancy;
    • The period of breastfeeding;
    • Children's age (up to 18 years).
    Carefully:

    Elderly age.

    Pregnancy and lactation:

    Propenate is contraindicated for use during pregnancy and during breastfeeding.

    Recommendations FDA - category X.

    Dosing and Administration:

    Inside after eating once a day.

    The drug is administered to adults at the rate of 9.5-12.5 mg / kg / day: with a body weight of less than 50 kg, 400-600 mg / day; with a body weight of 50-80 kg - 800-1000 mg / day; with a body weight of more than 80 kg - not more than 1200 mg / day.

    Duration of therapy up to 3 months.

    Side effects:

    From the side nervous system: dizziness, headache, weakness, drowsiness, loss of consciousness, neuropsychiatric reactions (aggression, depression).

    From the side of cardio-vascular system: tachycardia, palpitations, lowering blood pressure.

    From the side digestive system: pain in the epigastric region, increased activity of "hepatic" transaminases, nausea, vomiting.

    Allergic reactions: itching, rash, skin hyperemia, toxic-allergic reactions, angioedema.

    Other: bronchospasm. fever, eosinophilia. feeling of hot.

    Overdose:

    Data on acute overdose in humans are absent.

    Treatment: the specific antidote is unknown. In case of an overdose, general supportive therapy with the control of the basic physiological parameters should be carried out.

    Recommended gastric lavage, the appointment of activated charcoal.

    Interaction:

    Interaction with other drugs has not been adequately studied.

    When used simultaneously with other antituberculous drugs (isoniazid, amikacin, rifabutin, rifampicin) there is an increase in activity against mycobacteria tuberculosis, while the possibility of mutual potentiation of side effects should be taken into account.

    Special instructions:

    When developing allergic reactions it is recommended to cancel the drug. To stop fever, do not use metamizole sodium (analgin). In case of development of other aforementioned adverse reactions, the possibility of reducing the dose to 400 mg / day or drug withdrawal should be considered.

    Instructions
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