Included in the formulation
АТХ:J.04.A.K Other antituberculous drugs
Pharmacodynamics:The isoniazid molecule in complex with iron, which is a chelate complex of ferrous iron with isoniazid. Isonicotinic acid hydrazide is not able to interact with the active centers of metal-containing enzymes, and the included primary amino group of hydrazide does not allow the complex to interact with N-acetyltransferase. Due to these qualities, in the appointment of isonicotinoylhydrazine, iron does not require dose adjustment depending on the rate of acetylation, as a result of which the toxicity of the drug decreases and the effect is prolonged.
Inhibits the enzymes necessary for the synthesis of mycolic acids, which are the main structural fragments of the cell walls of mycobacterium tuberculosis.
The most intensive synthesis of mycolic acids is carried out in growing cells, so isoniazid has a bactericidal action on them, and bacteriostatic action on mature cells. The high selectivity of the chemotherapeutic effect of isoniazid is due to the fact that there are no mycolic acids in the tissues of the macroorganism, as well as in other microorganisms.
Pharmacokinetics:After oral administration, the empty stomach is slowly absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 5-6 hours. Metabolism in the liver.
The half-life is 7 hours. Elimination by the kidneys.
Indications:It is used for the treatment of pulmonary tuberculosis and other organs with concomitant diseases of the central nervous system, liver and intolerance of other anti-tuberculosis drugs.
I.A15-A19.A15 Tuberculosis of respiratory organs, confirmed bacteriologically and histologically
I.A15-A19.A17 Tuberculosis of the nervous system
I.A15-A19.A18 Tuberculosis of other organs
Contraindications:Coronary heart disease, pulmonary heart failure, thyroid gland disorders, disorders of the blood coagulation system, individual intolerance, children's age.
Carefully:Atherosclerosis, psoriasis, bronchial asthma.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:First day: inside 250 mg in the morning after eating. In the absence of side effects in the following days: 250 mg 2 times a day, morning and evening, 30-40 minutes after eating. The course of treatment is 6-8 months or more.
The highest daily dose: 500 mg.
The highest single dose: 250 mg.
Side effects:Central and peripheral nervous system: headache.
The cardiovascular system: myocarditis, thrombophilia.
Digestive system: dyspeptic phenomena.
Exchange system substances: hemosiderosis of parenchymal organs.
Endocrine system: hypothyroidism of the thyroid gland.
Allergic reactions.
Overdose:Cases of overdose are not described.
Treatment is symptomatic.
Interaction:It is not recommended simultaneous use of the drug with isoniazid.
Special instructions:Monthly monitoring of the electrocardiogram and coagulogram.