Isoniazid + Pyrazinamide + Rifampicin + [Pyridoxine] (Isoniazidum + Pyrazinamidum + Rifampicinum + [Pyridoxinum])

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

Other antibiotics

Included in the formulation
  • Protubwitis
    pills inwards 
    FARMASINTEZ, JSC (Irkutsk)     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    J.04.A.M   Combinations of antituberculous 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.

    Pyrazinamide

    In the body it turns into pyrazinic acid, which is active only in acidic medium (foci of caseous decay). Prevents the synthesis of mycolic acid, the main substrate of mycobacterium tuberculosis membranes.

    Rifampicin

    Semisynthetic antibacterial agent of bactericidal action.Selectively inhibits the DNA-dependent and RNA polymerase of mycobacteria tuberculosis and leprosy.

    Pyridoxine

    Vitamin B6. In the body, phosphorylation is converted to pyridoxal-5-phosphate, which is part of the enzymes involved in the 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 reached after 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.

    T ½ for "fast acetylators" is 1 hour, for "slow acetylators" - 3 hours. Elimination by the kidneys.

    Pyrazinamide

    After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract.The maximum concentration of pyrazinic acid in blood plasma is reached after 2 hours. The connection with plasma proteins is 10-20%.

    Metabolism in the liver.

    T ½ is 8-9 hours. Elimination by the kidneys.

    Rifampicin

    After oral administration, up to 98% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 2-3 hours. The connection with plasma proteins is 84-91%.

    Metabolism in the liver. Penetrates through the hemoencephalic and placental barrier, excreted in breast milk.

    T ½ is 2.5-5 h. Elimination with feces and kidneys.

    Pyridoxine

    After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is achieved after 2 hours. The connection with plasma proteins is 90%.

    Metabolism in the liver. Penetrates through the placenta, found in breast milk.

    T ½ is 15-20 days. Elimination by the kidneys. It is deduced by hemodialysis.

    Indications:

    It is used to treat pulmonary and extrapulmonary forms of tuberculosis and lepra. Used for the purpose of preventive treatment of persons who are in contact with a patient with tuberculosis. It is used for the bending of tuberculin sensitivity.

    ICD-10

    I.A15-A19.A15.8   Tuberculosis of other respiratory organs, confirmed bacteriologically and histologically

    I.A15-A19.A17   Tuberculosis of the nervous system

    I.A15-A19.A18   Tuberculosis of other organs

    Contraindications:

    Peptic ulcer of the stomach and duodenum, cardiovascular failure, epilepsy, propensity to convulsive seizures, diseases of the eyes, violations of the liver and kidneys, age of 12 years, pregnancy and lactation, individual intolerance.

    Carefully:

    Atherosclerosis, psoriasis, bronchial asthma, diseases of the nervous system, eczema in the exacerbation phase, gout, myxedema.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Use in children

    Inside, at 10-15 mg / kg / day in terms of rifampicin, not more than 600 mg / day.

    The grown-ups

    Inside from morning on an empty stomach, according to rifampicin - 10 mg / kg body weight, not more than 0.6 g.

    The highest daily dose: 0.6 g.

    The highest single dose: 0.6 g.

    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.

    Pyrazinamide

    Central and peripheral nervous system: dizziness, headache, depression, increased excitability, sleep disorders, convulsions, hallucinations.

    Hemopoietic system: thrombocytopenia, porphyria, hypercoagulation.

    Digestive system: a sensation of metallic taste in the mouth, vomiting, diarrhea.

    Musculoskeletal system: myalgia, arthralgia, rarely - gouty arthritis.

    Dermatological reactions: acne, photosensitivity.

    urinary system: interstitial nephritis.

    Allergic reactions.

    Rifampicin

    Central and peripheral nervous system: headache, disorientation, hallucinations.

    Respiratory system: bronchospasm.

    Hemopoietic system: eosinophilia.

    Digestive system: nausea, vomiting, decreased appetite, diarrhea, hepatitis, enterocolitis.

    Dermatological reactions: a rash.

    Sense organs: impaired vision.

    Allergic reactions.

    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 developing 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 hyperemia of the skin, itching, headache due to isoniazid suppression of monoamine oxidase and diamino oxidase activity in the blood plasma and metabolic disturbances of histamine and tyramine.

    Rifampicin reduces the effects of anticoagulants, hormonal contraceptives, antiarrhythmics,ketoconazole, cyclosporine, phenythion, chloramphenicol, glucocorticosteroids, enalapril, slow calcium channel blockers, cimetidine.

    Opiates, antacids, ketoconazole, - reduce the bioavailability of rifampicin.

    Special instructions:

    It is recommended to use reliable contraceptive methods during taking the drug.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    Instructions
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