Therion

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

This element completely blocks the action of the enzyme that transforms alanine into the component alanyl-alanine dipeptide, which is the main component 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 cause urinary tract infections and tuberculosis, and also has a significant effect on strains that are resistant to other known antibiotics. The MIC level of the drug for susceptible strains is 4-130 mg/ml. [ 2 ]

Indications Therion

It is used for pulmonary or extrapulmonary tuberculosis, includingtuberculosis affecting the kidneys and urogenital system (in case of resistance of tuberculosis mycobacteria to standard anti-tuberculosis drugs and the lack of effect from the use of other anti-tuberculosis regimens).

Release form

The medicinal substance is released in capsules - 50 or 100 pieces inside a bag, which is placed in a container.

Pharmacodynamics

Strains of Candida albicans, Klebsiella pneumoniae, Pasteurella multocida, Staphylococcus aureus with Escherichia coli, Shigella, Staphylococcus epidermidis and Pseudomonas aeruginosa show sensitivity to therisidone. In addition, strains of Bacillus subtilis, Koch's bacillus, Salmonella enterica, various streptococcal strains (including pyogenic streptococcus) and rickettsia, which cause endemic typhus, paratyphoid fever and typhus. [ 3 ]

Pharmacokinetics

Suction.

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

Distribution processes.

It is distributed within many tissues and body fluids, including bile, lymph with synovium, sperm, cerebrospinal fluid, lungs, pleural and ascitic fluids. CSF passes inside at 80-100% of plasma levels (in inflammations affecting the meningeal membranes).

Metabolic processes and excretion.

Excretion through the urinary tract occurs in stages, at a low rate, so even after 24 hours from the moment of oral administration, plasma levels remain in the middle of the Cmax values.

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

Dosing and administration

The medication is taken 1 capsule of 0.25 g 3 times a day or 1 capsule of 0.3 g 2 times a day. Do not take more than 15-20 mg/kg of the medication per day.

People over 60 years of age and weighing less than 60 kg are required to take 0.25 g of the medication twice a day.

• Application for children

There is no information regarding safety or medicinal efficacy when using the drug in pediatrics, so it is not used in children.

Use Therion during pregnancy

Therion is used during pregnancy only in situations where the potential benefit to the woman is greater than the potential for adverse effects on the fetus.

The level of the drug in breast milk is close to its plasma levels, which is why breastfeeding is discontinued during therapy.

Contraindications

Among the contraindications:

• severe intolerance associated with terizidone or other components of the drug;
• renal failure;
• psychoses;
• epilepsy;
• alcoholism.

Side effects Therion

Main side effects:

• problems associated with the functioning of the nervous system: drowsiness, confusion with subsequent memory loss, convulsions, dysarthria and tremor. In addition, mood swings, aggressiveness, headaches, increased irritability, dizziness, hyperreflexia, psychosis (may be accompanied by suicidal attempts), paresis of a peripheral nature, comatose state and seizures of a clonic type (major or minor);
• signs of allergy: itching or epidermal rash;
• other disorders: megaloblastic anemia, heartburn, increased liver aminotransferase levels, nausea and diarrhea (especially in people with liver disease).

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

Mainly toxic reactions are observed from the central nervous system: confusion, paresthesia, headaches, severe irritability, dysarthria, dizziness and psychosis. When too large doses are administered, seizures, peripheral paresis and comatose states may develop. Ethyl alcohol increases the likelihood of epileptic seizures.

Symptomatic and supportive measures are taken. The introduction of activated carbon more effectively reduces the absorption of Terion compared to gastric lavage. If 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 may result in life-threatening toxic effects.

Interactions with other drugs

Combination with ethionamide enhances the neurotoxic effect of Terion.

The drug should not be combined with alcoholic beverages, especially when administering large doses of the drug, because alcohol increases the likelihood of developing epileptic seizures.

People who use the drug 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 dose size.

Storage conditions

Therion should be kept in a place closed to small children. Temperature level – no more than 25°C.

Shelf life

Therion can be used within a 24-month period from the date of manufacture of the medicinal product.

Analogues

The analogues of the drug are the substances Teriz and Terizidone.