Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:J.04.A.C.01 Isoniazid
Pharmacodynamics: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 completely absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is achieved in 1-4 hours. The connection with plasma proteins is from 1 to 10%.
Therapeutic effect develops after the reception. Metabolism in the liver by acetylation to inactive metabolites, penetrates the placental barrier, is excreted in breast milk.
The rate of acetylation of the drug is genetically determined, so the half-life of isoniazid varies.
Half-life for "fast acetylators" is 1 hour, for "slow acetylators" - 3 hours. Elimination by the kidneys.
Indications:It is used for the treatment of all forms of tuberculosis, including tuberculosis meningitis, for children who are in close contact with tuberculosis patients, children older than 3 years with a positive reaction to tuberculin: more than 10 mm; adults with a positive skin reaction: more than 5 mm.
I.A15-A19.A15 Tuberculosis of respiratory organs, confirmed bacteriologically and histologically
I.A15-A19.A17.0 Tuberculous meningitis (G01 *)
I.A15-A19.A18 Tuberculosis of other organs
Contraindications:Epilepsy, propensity to convulsive seizures, violations of the liver and kidneys, individual intolerance, children under 3 years old.
Carefully:Atherosclerosis, psoriasis, bronchial asthma, diseases of the nervous system, eczema in the phase of exacerbation, myxedema.
Pregnancy and lactation:Recommendations for FDA - Category C.Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside after eating to 0,005-0,015 g / kg body weight for 1-3 admission.
Intravenous: 30-60 mg per day (10% solution).
Intramuscularly: in a dose of 2-15 mg / kg per day.
Inhalation: daily, for 1-6 months, 5-10 mg / kg in 1-2 divided doses.
Intracavernous: in the form of a 10% solution of 10-15 mg / kg per day.
The highest daily dose: 60 mg.
The highest single dose: 60 mg.
Side effects:Central and peripheral nervous system: memory disorders, insomnia, mental disorders disorders, euphoria, peripheral neuritis, muscle twitching.
The cardiovascular system: pain in the heart.
Digestive system: drug hepatitis.
Dermatological reactions: itching, skin rash.
Sense organs: optic neuritis - blurred vision or loss of vision.
Reproductive system: gynecomastia, menorrhagia.
Allergic reactions.
Overdose:Metabolic acidosis, neurotoxic effect: dysarthria, lethargy, disorientation, hyperreflexia, convulsions, coma.
Treatment is symptomatic. Effective hemodialysis.
Interaction:Strengthens the action indirect hemocoagulants.
Inhibits the metabolism of benzodiazepines, phenytoin and theophylline.
Simultaneous use with paracetamol and other hepatotoxic substances increases the risk of toxic hepatonecrosis.
Antatsidnye means slow down and reduce the absorption of isoniazid in the intestine, it is recommended to take them with an interval of 1 hour.
With the simultaneous use of certain fish species (tuna, sardinella) and cheeses (Swiss), there may be a hyperemia of the skin, itching, headache due to the isoniazid suppression of monoamine oxidase and diaminoxidase activity in the blood plasma and a violation of the metabolism of histamine and tyramine.
Special instructions:To prevent and reduce the side effects of isoniazid, the intake of vitamins B1 and B6, as well as glutamic acid.