Included in the formulation
АТХ:J.04.A.C.51 Isoniazid in combination with other drugs
Pharmacodynamics:Combined anti-tuberculosis drug.
Isoniazid
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.
Pyridoxine
Vitamin B6. In the body, phosphorylation is converted to pyridoxal-5-phosphate, which is part of the enzymes involved in decarboxylation, transamination and racemization of amino acids. Prevents the development of peripheral polyneuropathy, which develops due to the impact of anti-tuberculosis drugs.
Pharmacokinetics:Isoniazid
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.
Pyridoxine
After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 90%.
Metabolism in the liver. Penetrates through the placenta, found in breast milk.
The half-life is 15-20 days. Elimination by the kidneys. It is deduced by hemodialysis.
Indications:It is used to treat tuberculosis of any location, including for the prevention. It is used in combination therapy.
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
XXI.Z20-Z29.Z29.8 Other specified preventive measures
Contraindications:Epilepsy, propensity to convulsive seizures, diseases of the eyes, violations of the liver and kidneys, age up to 3 years, individual intolerance.
Carefully:Peptic ulcer of stomach and duodenum, cardiovascular failure, renal failure, pregnancy and lactation, age over 35 years.
Pregnancy and lactation:Recommendations for FDA - Category C. It is used in pregnancy and lactation in a dose of not more than 10 mg / kg (in terms of isoniazid) in those cases where the expected effect of treatment exceeds the risk for the fetus and newborn.
Dosing and Administration:For treatment: inside after meals, 600-900 mg per day for 1-3 hours.
For prophylaxis: inside after meals, 5-10 mg / kg per day for 2 doses for 2 months.
The highest daily dose: 600 mg.
The highest single dose: 600 mg.
Side effects:Isoniazid
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: medicinal hepatitis.
Dermatological reactions: itching, skin rash.
Sense organs: optic neuritis - blurred vision or loss of vision.
Reproductive system: gynecomastia, menorrhagia.
Allergic reactions.
Pyridoxine
Central and peripheral nervous system: a feeling of constriction and compression of the distal parts of the limbs - a symptom of "gloves" and "stocking."
Digestive system: heartburn.
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 types of fish (tuna, sardinella) and cheeses (Swiss), there may be a hyperemia of the skin, itching,headache due to isoniazid suppression of monoamine oxidase and diaminoxidase activity in blood plasma and metabolic disorders of histamine and tyramine.
Pyridoxine weakens the effects of levodopa and reduces the neurotoxic effects of isoniazid.
Special instructions:In the treatment it is not recommended to drive vehicles and work with moving mechanisms.