Isoniazid + Rifampicin - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Other synthetic antibacterial agents

Included in the formulation

Iso-Eremfat

pills inwards

Rimzer Artsynaimitel, AG Germany

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

АТХ:

J.04.A.M.02 Isoniazid in combination with rifampicin

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.

Rifampicin

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

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.

Rifampicin

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

Metabolism in the liver. Penetrates through blood-brain and placental barriers, excreted in breast milk.

The half-life is 2.5-5 hours. Elimination with feces and kidneys.

Indications:

It is used to treat the initial stage of tuberculosis of any localization.

ICD-10

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:

Liver failure, age under 12 years and weight less than 45 kg, I trimester of pregnancy, lactation period, individual intolerance.

Carefully:

II-III trimester of pregnancy, chronic alcoholism, chronic renal failure, liver disease.

Pregnancy and lactation:

Recommendations for FDA - Category C. It is used with caution in II-III trimester of pregnancy.

Dosing and Administration:

Use in children

Contraindicated up to 12 years of age.

Inside, 10-15 mg per day in terms of isoniazid.

Adults

Inside, 1 tablet once a day. At a body weight below 50 kg - on 450 mg (in recalculation on isoniazid), over 50 kg - 600 mg once a day.

The highest daily dose: 600 mg (isoniazid).

The highest single dose: 600 mg (isoniazid).

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.

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.

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.

Rifampicin reduces the effects of anticoagulants, hormonal contraceptives, antiarrhythmics, ketoconazole, cyclosporine, phenytoin, 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

Isoniazid + Rifampicin (Isoniazidum + Rifampicinum)