Terizidone - instructions for use, dose, side effects, contraindications

gelatin - 83.2267%, titanium dioxide - 1.667%, water - 14.5%, sodium lauryl sulfate - 0.15 %, Bronopol - 0.1%, povidone - 0.1 %, methyl parahydroxybenzoate 0.075 %. propyl parahydroxybenzoate 0.025%, quinoline yellow dye -0.1563%.

Description:

Hard gelatin capsules № "О", the case and a cover of a capsule of yellow color; The contents of the capsule are white or white with a yellowish tinge powder.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.K Other antituberculous drugs

Pharmacodynamics:

Terizidone is a bacteriostatic broad-spectrum antibiotic. After oral administration, it is hydrolyzed to Dcycloserine. The mechanism of action is associated with inhibition of the synthesis of the components of the cell wall. Terizidone active with respect to Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, and Staphylococcus aureus and Staphylococcus epidermidis.

The drug is also sensitive: Enterococcus faecalis, Escherichia coli, Citrobacter spp., Enterobacter spp., Morganella morganii, Klebsiella pneumoniae and Pseudomonas aeruginosa.

Development of secondary resistance is rare. Cross-resistance with other anti-TB drugs is not observed.

Pharmacokinetics:

Absorption from the gastrointestinal tract - 70-90% (eating does not affect the rate of absorption). The maximum concentration in the blood plasma (Stach) is about 6.5 μg / ml. The time to reach the maximum concentration (TCmax) is 2-3 hours. The effective minimum concentration for Mycobacterium tuberculosis is 10-40 mg / l, for Staphylococcus spp. - 8-32 mg / l, for gram-negative bacteria (of clinical significance) - 20-250 mg / l.

It is well distributed in tissues and body fluids (lungs, bile, ascites fluid, pleural effusion, synovial fluid, lymph, sputum). It penetrates the hemato-encephalic barrier (the concentration in the cerebrospinal fluid reaches 80-100% of that in the blood serum).Higher concentrations in the cerebrospinal fluid are created by inflammatory changes in the meninges.

Metabolized slightly. The half-life (T1 / 2) -21h. It is excreted by the kidneys (in unchanged form - 60-70%), intestines (a small amount in unchanged form and in the form of metabolites).

Indications:Tuberculosis of various forms and localizations in the complex therapy of resistant forms of the disease.

Contraindications:

Hypersensitivity to terizidon (including cycloserine), other components of the drug, organic diseases of the central nervous system (including atherosclerosis of the brain vessels), epilepsy, mental disorders, alcoholism, pregnancy, the period of breastfeeding, children's age ( up to 14 years), lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:Elderly age, chronic heart failure, chronic renal failure.

Pregnancy and lactation:The drug is contraindicated for use during pregnancy and during breastfeeding.

Dosing and Administration:

The drug is taken orally, regardless of food intake.

For adults and children over 14 years of age, the daily dose is 750-1000 mg.

For patients with a body weight of up to 60 kg, the drug is prescribed 250 mg three times a day, for patients with a body weight of more than 60 kg, 250 mg four times a day. When creatinine clearance is less than 30 ml / min, the drug is recommended to be administered 250 mg daily or 500 mg 3 times a week. As terizidone is withdrawn during hemodialysis, it should be taken at the end of the procedure.

The course of treatment is 3-4 months or more.

Side effects:

Undesirable reactions classified by organs and systems are listed below in descending frequency of detection: very often (> 1/10), often (> 1/100, <1/10), sometimes (> 1/1000, <1/100 ), rarely (> 1/10000, <1/1000), very rarely (<1/10000), including individual cases.

From the nervous system: rarely - headache, dizziness, increased excitability, tremor, insomnia, a feeling of intoxication; very rarely - convulsions, depression, psychosis.

From the digestive system: rarely or very rarely - abdominal pain, flatulence, diarrhea.

Other: very rarely - allergic reactions.

Overdose:

Symptoms: increased neurotoxicity (including convulsions), a violation of the function of the gastrointestinal tract.

Treatment: symptomatic, reception of activated charcoal, anticonvulsant, sedatives. Hemodialysis is effective.

Interaction:

Ethanol increases the risk of seizures.

When used simultaneously with ethionamide, protionamide, the risk of side effects from the central nervous system increases (especially seizures).

Simultaneous use with isoniazid increases the incidence of dizziness, drowsiness.

Special instructions:

Terizidone can cause deficiency of cyanocobalamin and / or folic acid, it is necessary to conduct appropriate examination and treatment.

It should be monitored monthly blood and urine indicators, liver function (alanine aminotransferase, aspartate aminotransferase, bilirubin).

It is necessary to avoid the use of ethanol, t. simultaneous administration with terizidone increases the incidence of side effects (up to the development of seizures).

In connection with the possibility of developing adverse reactions from the nervous system (depression, behavior change), it is necessary to monitor the patient's mental status.

To reduce the risk of side effects from the central nervous system, simultaneous intake of vitamin B6 is recommended.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Capsules of 250 mg.

Packaging:

Primary packaging of medicinal product. 10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. For 30 or 100 capsules are placed in a bag of low density polyethylene. A sticker is applied to the package from paper label or written or from polymer materials, self-adhesive.

Secondary packaging of medicinal product. For 1, 2, 3 contour squares, together with instructions for use, are placed in a pack of cardboard for consumer containers. The packets are placed in a group package.

One package together with the instruction for use is placed in a polymer can with a lid of polypropylene or high-pressure polyethylene with a control of the first opening or a can of polyethylene terephthalate for medicines with a screw cap or with the control of the first opening.Labels are applied to cans from paper label or writing paper, or from polymer materials, self-adhesive. Banks are placed in a group package.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002264

Date of registration:04.10.2013

The owner of the registration certificate:FARMSINTEZ, PAO FARMSINTEZ, PAO Russia

Manufacturer: & nbsp

LOK-BETA PHARMACEUTICALS (I), Pvt. Ltd. India

Representation: & nbspFARMSINTEZ, PAO FARMSINTEZ, PAO Russia

Information update date: & nbsp22.09.2015

Illustrated instructions

Instructions

Terizidone (Terizidon)