Therion

Therion is an anti-tuberculosis medication containing the active ingredient terizidone.

This element completely blocks the action of the enzyme that transforms alanine into the alanyl-alanine dipeptide component, which is the main constituent of the microbial membrane of mycobacteria. Does not create cross-resistance with other anti-tuberculosis drugs. [1]

The drug has a wide range of strong antimicrobial effects; it has a significant effect on strains that lead to infection of the urinary system and the development of tuberculosis, and also noticeably affects strains resistant to other known antibiotics. The MIC level of the drug for susceptible strains is 4-130 mg / ml. [2]

Indications Therion

Used for tuberculosis pulmonary or extrapulmonary type, including tuberculosis infecting the kidney and the urogenital system (in the case of tuberculous mycobacteria resistance relative to a standard anti-TB drugs and no effect of the use of other schemes TB).

Release form

The release of the drug substance is made in capsules - 50 or 100 pieces inside a sachet, which is placed in a container.

Pharmacodynamics

Strains of Candida albicans, Klebsiella pneumonia, Pasteurella multicide, Staphylococcus aureus with Escherichia coli, Shigella, Staphylococcus epidermidis and Pseudomonas aeruginosa show susceptibility to terizidone. In addition, strains of hay bacillus, Koch's bacillus, salmonella enteric, various streptococcal strains (among them pyogenic streptococcus) and rickettsia, which lead to the appearance of endemic typhus, paratyphoid and typhoid fever. [3]

Pharmacokinetics

Suction.

When administered orally on an empty stomach, terizidone is absorbed at high speed and fully (70-90%), reaching the Cmax after 2-4 hours.

Distribution processes.

It is distributed inside many tissues and body fluids - among them bile, lymph with synovium, semen, cerebrospinal fluid, lungs, pleural and ascites fluids. Inside the CSF passes 80-100% of the plasma parameters (with inflammation affecting the meningeal membranes).

Metabolic processes and excretion.

Excretion through the urinary ducts is carried out in stages, at a low speed, therefore, even after 24 hours from the moment of oral administration, plasma indicators remain in the middle of the Cmax values.

Prolonged urinary tract excretion maintains therapeutically effective urinary parameters for 12 hours; 60-70% excreted in the urine unchanged - with the help of CF; a small part is excreted with feces, and some more undergo metabolic processes.

Dosing and administration

The medication is consumed in 1 capsule 0.25 g 3 times a day or 1 capsule 0.3 g 2 times a day. You can not use more than 15-20 mg / kg of the drug per day.

Persons over the age of 60 with a weight of less than 60 kg are required to take 0.25 g of the medication 2 times a day.

• Application for children

There is no information regarding safety, as well as medicinal efficacy when using drugs in pediatrics, therefore it is not used in children.

Use Therion during pregnancy

Therion is used during pregnancy only in situations where the likely benefits for the woman are more expected than the possibility of developing negative consequences for the fetus.

The level of the drug inside breast milk is close to its plasma levels, which is why breastfeeding is stopped for the period of therapy.

Contraindications

Among the contraindications:

• severe intolerance associated with terizidone or other elements of the drug;
• failure of the kidneys;
• psychosis;
• epilepsy;
• alcoholism.

Side effects Therion

The main side symptoms:

• problems associated with the work of the NA: drowsiness, confusion with subsequent loss of memory, convulsions, dysarthria and tremors. In addition, mood changes, aggressiveness, headaches, increased irritability, dizziness, hyperreflexia, psychosis (may be accompanied by suicidal attempts), peripheral paresis, coma and seizures of the clonic type (large or small);
• signs of allergies: itching or epidermal rash;
• other disorders: anemia of the megaloblastic type, heartburn, an increase in hepatic aminotransferase rates, nausea and diarrhea (especially in persons with hepatic diseases).

There is information about the development of exacerbation of CHF in individuals who use 1000-1500 mg of the drug per day.

Overdose

Acute overdose is noted in the case of taking more than 1000 mg of the drug. Chronic poisoning is determined by the size of the dosage and can develop with daily use of more than 0.5 g of drugs.

Basically, toxic reactions are noted from the central nervous system: confusion, paresthesia, headaches, severe irritability, dysarthria, dizziness and psychosis. With the introduction of too large portions, the development of seizures, peripheral paresis, as well as a coma may be noted. Ethyl alcohol increases the likelihood of developing epileptic seizures.

Symptomatic and supportive measures are taken. The introduction of activated carbon more effectively reduces the absorption of Therion in comparison with gastric lavage. When neurotoxic signs appear, 0.2-0.3 g of pyridoxine should be used per day.

Hemodialysis allows the drug to be excreted from the blood, but can lead to life-threatening toxicity.

Interactions with other drugs

The combination with ethionamide enhances the neurotoxic effect of Therion.

You can not combine the medicine with alcoholic beverages, especially with the introduction of large portions of drugs, because alcohol increases the likelihood of developing epileptic seizures.

Persons who use the medication together with isoniazid should be under medical supervision, because such a combination can potentiate the toxic effect on the central nervous system and require a change in the serving size.

Storage conditions

Therion must be kept in a place closed from the penetration of small children. Temperature level - no more than 25 ° С.

Shelf life

Therion can be used within a 24-month term from the date of manufacture of the drug.

Analogs

The analogs of the drug are the substances Theriz and Therizidone.