Composition, form of production and packaging
Capsules 1 caps.
terizidone 250 mg
pyridoxine hydrochloride 10 mg
10 pieces. - Packings without cell contour (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Terizidone is a broad-spectrum antibiotic, is a derivative of D-cycloserine. Terizidone competitively blocks enzymes that incorporate alanine into alanyl-alanine dipeptide, the main component of the mycobacterium wall. Does not have cross-resistance with other anti-TB drugs. Terizidone has antibacterial activity against mycobacteria tuberculosis and bacteria that cause urinary tract infections, including strains of bacteria that become resistant to other antibiotics. The minimum inhibitory concentration of terisidone for sensitive strains is 4-250 mg / l, including 10-40 mg / l for mycobacteria of tuberculosis, 8-32 mg / l for staphylococci, and 50-250 for gram-negative bacteria mg / l.
The following bacteria are sensitive to terizidone:
Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, and Staphylococcus aureus. Staphylococcus epidermidis. To this preparation are also sensitive Enterococcus faecalis, Escherichia coli, Citrobacter, Enterobacter, Morganella morganii Klebsiella pneumoniae, Pseudomonas aeruginosa.
Pyridoxine acts as a coenzyme, participating in biochemical reactions, including the metabolism of amino acids and glycogen, in the synthesis of nucleic acids, hemoglobin, sphingomyelin and other sphingolipids, in the synthesis of the mediator serotonin, dopamine, norephedrine and gammaaminobutyric acid. Pyridoxine has an antineurotoxic effect. The use of pyridoxine reduces the side effects of the central nervous system.
After oral administration of 250 mg of terizidone C max is about 6.5 Ојg / ml, the peak concentration of the drug in the blood plasma is achieved in 2-4 hours.Terizidone is absorbed from the gastrointestinal tract quickly and almost completely - by 70-90%. Food intake does not affect the rate of absorption. Widely distributed in tissues and body fluids, for example in the lungs, bile, penetrates into ascitic, pleural and synovial fluid, lymph, and saliva. Very well penetrates into the cerebrospinal fluid (concentration in the cerebrospinal fluid reaches 80-100% concentration in the blood serum), a higher concentration level is noted in patients with inflammation of the meninges. When administered in doses of 250 mg of terizidone, high concentrations of the drug are found in the blood and urine, which allows it to be used to treat infections of the urinary tract, incl. chronic forms.
Kidney excretion occurs slowly and evenly, T 1/2 - 24 hours. Delayed excretion of the drug by the kidneys leads to the fact that the concentration level of terizidone in the urine persists for 12 hours, 60-70% of the drug is excreted unchanged by glomerular filtration. A small amount is excreted with feces. The value of the elimination constant is -0.0262 h- 1 . A small amount of terizidone is metabolized, which causes a low / weak toxic effect on the kidneys.
With renal failure, the elimination half-life is extended to 72 hours.
Absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate binds to plasma proteins by 90%. It penetrates well into all tissues; accumulates mainly in the liver, less in the muscles and central nervous system. Penetrates through the placenta, is secreted with breast milk. T 1/2 is 15-20 days. It is excreted by the kidneys (with iv in the introduction - with bile 2%), as well as during hemodialysis.
- tuberculosis (various forms and localizations) in the complex treatment of drug-resistant forms of tuberculosis.
Inside, on an empty stomach on 1 capsule 3-4 times a day, every 6-8 hours or as directed by a doctor. For patients with a body weight of more than 50 kg - 1 capsule 4 times a day. For patients with a body weight of less than 50 kg - 1 capsule 3 times a day. The duration of treatment is 3-4 months.
From the side of the central nervous system: rarely - headache, dizziness, increased excitability, tremor, insomnia, a feeling of intoxication; very rarely - convulsions (including epileptic), dysarthria, mental disorders, such as mania or depression.
From the gastrointestinal tract: abdominal pain, flatulence and diarrhea.
Very rarely: allergic reactions, skin rash.
- hypersensitivity to terizidone, cycloserine and pyridoxine;
- renal failure (CC less than 50 ml / min);
- epilepsy, epileptic seizures (including anamnesis);
- organic diseases of the central nervous system;
- disorders of the psyche (anxiety, psychosis, depression, including in the anamnesis);
- Chronic heart failure;
- Children under 12 years old.
PREGNANCY AND LACTATION
Pregnant women terizidone can be prescribed if the expected benefit to the mother exceeds the risk to the fetus.
Terizidone is excreted in breast milk, during breastfeeding it is necessary to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in renal failure (creatinine clearance less than 50 ml / min).
APPLICATION FOR CHILDREN
Contraindicated up to 12 years.
It is recommended to take together with glutamic acid in a dose of 500 mg 3 times a day. Terizidone should be used cautiously and under medical supervision in patients with epilepsy, with mental illnesses. During the treatment, alcohol is not allowed.
It is necessary to carefully monitor, at the first signs of neurotoxicosis, to control the concentration of the drug in the blood and to perform the appropriate dose adjustment.
Effect of the drug on the ability to drive a vehicle or work with moving mechanisms:
When receiving terizidona should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.
Data on drug overdose are absent.
In case of an overdose, there may be an increased manifestation of all side effects (with the exception of allergic reactions) listed above, in which case it is necessary to stop taking the drug and consult a doctor immediately. Treatment is symptomatic, activated charcoal. For the prevention of neurotoxic action, it is possible to administer pyridoxine, anticonvulsant and sedative drugs.
Ethionamide and isoniazid increase the risk of adverse reactions from the nervous system.
Terizidone may increase the level of phenytoin concentration.
Do not use together with cycloserine, since terizidone is its derivative.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
In a dry, the dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 2 years.