Universal reference book for medicines
Name of the preparation: HIXOZID (HIXOZID)

Active substance: isoniazid, non appropriate

Type: Anti-TB drug

Manufacturer: MIR-PHARM (Russia) packed Obninsk chemical-pharmaceutical company (Russia) produced by FARMENT FIRM (Russia)
Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intrapleural administration and inhalation
1 fl.

hydroxymethylquinoxaline dioxide 100 mg

isoniazid 250 mg

350 mg - a bottle of dark glass (1) - packs of cardboard.

350 mg - a bottle of dark glass (10) - packs of cardboard.

350 mg - a bottle of dark glass (200) - carton boxes.

350 mg - a bottle of dark glass (500) - carton boxes.

350 mg - a bottle of dark glass (1000) - carton boxes.

350 mg - a bottle of dark glass (200) - cardboard boxes.

350 mg - a bottle of dark glass (500) - boxes of cardboard.

350 mg - a bottle of dark glass (1000) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Hicksozid is a combination of two drugs: the antibacterial agent hydroxymethylquinoxaline dioxide and the anti-tuberculosis drug isoniazid.

Hydroxymethylquinoxaline dioxide is an antibacterial bactericide of a wide spectrum of action.
It is active against Proteus vulgaris, Pseudomonas aeruginosa, Klebsiella pneumoniae, Escherichia coli, Shigella dysenteriae, Shigella flexneri, Shigella boydii, Shigella sonnei, Salmonella spp., Staphylococcus spp., Streptococcus spp., Pathogenic anaerobes (Clostridium perfringens). It acts on strains of bacteria resistant to other antimicrobial medicines, including antibiotics.
Possible development of drug resistance of bacteria.

Isoniazid - antituberculous;
acts bacteriostatically. Is a prodrug - mycobacterial catalase perecendase metabolizes isoniazid to the active metabolite, which, when bound to the enoyl (acyl-transferring protein) reductase of fatty acid II synthase; violates the conversion of delta 2-unsaturated fatty acids into mycolic acid. The latter is a branched chain fatty acid, which, when combined with arabinogalactan (polysaccharide), participates in the formation of the components of the cell wall of Mycobacterium tuberculosis. Isoniazid is also an inhibitor of mycobacterial catalase peroxidase, which reduces the protection of the microorganism against reactive oxygen species and hydrogen peroxide.
Isoniazid is also active against a small number of strains of Mycobacterium kansasii (for infections caused by this pathogen, it is necessary to determine the sensitivity to isoniazid before starting treatment).

The anti-tuberculosis activity of the combination of hydroxymethylquinoxaline dinoxide + isoniazid exceeds the activity of isoniazid by an average of 5 times, both for sensitive and resistant to anti-tuberculosis drugs, mycobacterium tuberculosis.

PHARMACOKINETICS

Suction

Isoniazid does not affect the bioavailability of hydroxymethylquinoxaline dioxide.
Hydroxymethylquinoxaline dioxide when combined with isoniazid increases the bioavailability of the latter: in the presence of hydroxymethylquinoxaline dioxide, the content in the blood of isoniazid decreases due to its faster penetration into the tissue.
Distribution

Well distributed throughout the body, penetrating all tissues and fluids, including cerebrospinal, pleural, ascites;
high concentrations are created in the lung tissue, kidneys, liver, muscles, saliva and sputum. Penetrates through the placental barrier and into breast milk.
Metabolism

Isoniazid is metabolized in the liver by acetylation with the formation of inactive products.
The liver is acetylated with N-acetyltransferase to form N-acetylisoiniazide, which is then converted to isonicotinic acid and monoacetylhydrazine, which has a hepatotoxic effect by forming a cytochrome P450 system upon N-hydroxylation of the active intermediate metabolite. The rate of acetylation is genetically determined; in people with slow acetylation, there is little N-acetyltransferase. Is the inducer of the isoenzyme CYP2E1. Excretion
Isoniazid is excreted mainly by the kidneys: within 75 hours, 75-95% of the drug is excreted, mainly in the form of inactive metabolites - N-acetylisosodium and isonicotinic acid.
In fast acetylators, the content of N-acetylisiniazide is 93%, while in slow acetylsinides it is not more than 63%. Small amounts are output through the intestine. The drug is removed from the blood during hemodialysis; 5 h hemodialysis allows you to remove from the blood to 73% of the drug. T 1/2 for fast acetylators - 0.5-1.6 h; for slow - 2-5 hours.
INDICATIONS

Treatment of drug-sensitive and drug-resistant forms of pulmonary tuberculosis and pleura as part of complex therapy:

- fibro-cavernous tuberculosis;

- bronchial tuberculosis;

bronchial fistula;

- tuberculosis empyema.

DOSING MODE

Intrapleural, inhalation.
The contents of the vial before injection are dissolved in water for injection (10 ml). Inhalations are carried out using an inhaler.
Intrapleural ( patients with empyema pleural cavity ): patients with a body weight of up to 40 kg - 2 ml, 40-50 kg - 8 ml, with a mass of 60 kg and more - 10 ml.The drug is administered 1 time / day, after eating.

Inhalation: patients with a body weight of 30-40 kg - 5 ml, 40-50 kg - 8 ml, 60 kg and more - 10 ml.
The drug is administered daily, 1 time / day, after eating.
The duration of the course of treatment is 16-21 days.

Additionally, with both methods of administration, isoniazid is administered (inside or at / in a daily dose of 10 mg / kg), pyridoxine (vitamin B 6 ) 30 mg 2 times / day after meals.
The purpose of other anti-TB drugs depends on the nature of the tuberculosis process and the nature of drug resistance.
SIDE EFFECT

From the nervous system: headache, dizziness, hyperthermia, insomnia.

From the digestive system: nausea, gastralgia.

Allergic reactions: skin rash, itching, hyperthermia, arthralgia.

Local reactions: irritation at the injection site.

CONTRAINDICATIONS

- diseases of the central nervous system (including epilepsy, propensity to convulsive seizures - the risk of more frequent seizures);

- acute heart failure;

- Insufficiency of adrenal function;

- Pregnancy;

- lactation period;

- children under 18;

- Hypersensitivity to hydroxymethylquinoxaline dioxide and isoniazid.

With caution: hepatic failure, drug-induced hepatitis.

PREGNANCY AND LACTATION

The drug is contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

At a risk of peripheral neuritis (chronic renal failure), 10-25 mg / day of pyridoxine is recommended.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution: hepatic failure, drug-induced hepatitis.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under the age of 18 years.

APPLICATION IN ELDERLY PATIENTS

At a risk of peripheral neuritis (patients over 65 years), the appointment of 10-25 mg / day of pyridoxine is recommended.

SPECIAL INSTRUCTIONS

To slow the development of microbial resistance is prescribed together with other antituberculous drugs.

In connection with the different metabolic rate before the use of isoniazid, it is expedient to determine the rate of its inactivation (by the dynamics of the content in the blood and urine).
In fast acetylators, isoniazid is used in higher doses.
With the risk of peripheral neuritis (patients over 65 years of age, concomitant diabetes, pregnancy, chronic renal failure, alcoholism, hypovitaminosis B6 due to malnutrition, concomitant anticonvulsant therapy), it is recommended that 10-25 mg / day of pyridoxine be administered.

During the treatment, cheese (especially Swiss or Cheshire), fish (especially tuna, sardine) should be avoided, since with the simultaneous use of them with isoniazid may cause reactions (skin hyperemia, itching, sensation of heat or cold, palpitation, increased sweating, chills, headache, dizziness) associated with the suppression of monoamine oxidase and diaminoxidase activity and leading to a disruption of the metabolism of tyramine and histamine contained in fish and cheese.

It should be borne in mind that isoniazid can cause hyperglycemia with secondary glucosuria;
tests with copper reduction can be false positive; the drug does not affect the enzymatic glucose tests.
OVERDOSE

Cases of overdose are not described.

DRUG INTERACTION

The main types of interaction are given for isoniazid.

Pharmacodynamic: with the combination of isoniazid with pyrazinamide, rifampicin, ethambutol and aminoglycosides, antimicrobial activity against MBT increases.

Cycloserine and disulfiram increase the adverse central effects of isoniazid.

Caution should be combined with potentially neuro-, hepato- and nephrotoxic drugs because of the risk of side effects.

Combination with pyridoxine reduces the risk of peripheral neuritis.

Pharmacokinetic: when combined with paracetamol, hepatotoxicity and nephrotoxicity increase;
isoniazid induces a cytochrome P450 system, which increases the metabolism of paracetamol to toxic products.
Ethanol increases the hepatotoxicity of isoniazid and speeds up its metabolism.

Reduces the metabolism of theophylline, which can lead to an increase in its concentration in the blood.

Reduces metabolic transformations and increases the concentration in the blood of alfentanil.

Cycloserine and disulfiram increase the adverse central effects of isoniazid.

Increases hepatotoxicity of rifampicin.

Enhances the action of coumarin and indanedione derivatives, benzodiazepines, carbamazepine, theophylline, as it reduces their metabolism due to the activation of cytochrome P450 isoenzymes.

SCS accelerates metabolism in the liver and reduces active concentrations in the blood.

Suppresses the metabolism of phenytoin, which leads to an increase in its concentration in the blood and increased toxic effect (correction of the dosing regimen of phenytoin may be necessary, especially in patients with slow acetylation of isoniazid);
should be considered when administered as an anticonvulsant with an overdose of isoniazid.
Antacid preparations (especially alminium-containing) slow down absorption and reduce the concentration of isoniazid in the blood (antacids should be taken no earlier than 1 hour after taking isoniazid).

When used simultaneously with enflurane, isoniazid can increase the formation of an inorganic fluoride metabolite, which has a nephrotoxic effect.

When taken together with rifampicin reduces the concentration of ketoconazole in the blood.

Increases the concentration of valproic acid in the blood (monitoring of valproic acid concentration is required, correction of the dosing regimen may be required).

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The preparation should be stored in a place protected from light and inaccessible to children, at a temperature not exceeding 8 ° С.

Shelf life - 3 years.
Do not use after the expiration date indicated on the package.
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