Terizidon-Mac - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 62.8 mg, disodium edetate 3.40 mg, hypromellose 20.40 mg, stearic acid 3.40 mg; gelatin capsule composition: titanium dioxide 1,8958%, a dye diamond blue 0,7583%, dye azorubin 0,1487%, armolop 0,090%, povidone 0,500%, sodium lauryl sulfate 0,200%, gelatin up to 100%.

Description:Hard gelatin capsules in the size "0" with a body and a lid of blue color. Contents of capsules: a mixture of fine granules and powder from white to yellowish or yellowish-beige color.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.K Other antituberculous drugs

Pharmacodynamics:

Terizidone is a broad-spectrum antibiotic, is a derivative of Dcycloserine. 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 causing 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, a also Staphylococcus aureus, Staphylococcus epidermidis. TO this drug sensitive also Enterococcus faecalis, Escherichia coli, Citrobacter, Enterobacter, Morganella morganii Klebsiella pneumoniae, Pseudomonas aeruginosa.

Pharmacokinetics:

After oral administration of 250 mg of terizidone, the maximum concentration (C_max) is about 6.5 μg / 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 level of concentration 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, the half-life (T1/2) - 24 hours. Delayed excretion of the drug by the kidneys leads to the fact that the concentration level of terisidone in the urine persists for 12 hours, 60-70 % 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. Terizidone is metabolized in a small amount, which is the reason for a weak toxic effect on the kidneys.

With renal failure, the elimination half-life is extended to 72 hours.

Indications:

- Tuberculosis (various forms and localizations) in the complex treatment of drug-resistant forms of tuberculosis

Contraindications:

- hypersensitivity to terizidone and cycloserine;

- renal failure (creatinine clearance less than 50 ml / min);

- epilepsy, epileptic seizures (including anamnesis);

- organic diseases of the central nervous system;

- mental disorders (anxiety, psychosis, depression, including in the anamnesis);

- chronic heart failure;

- alcoholism;

- children under 12 years.

Carefully:BVariability.

Pregnancy and lactation:

Pregnant women terizidone can be assigned 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.

Dosing and Administration:

Inside, on an empty stomach 250 mg 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 weighing less than 50 kg - 1 capsule 3 times a day Duration of treatment is 3-4 months.

Side effects:

From 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.

Overdose:

Data on drug overdose are absent.

In case of an overdose, an increased manifestation of all side effects (with the exception of allergic reactions) that are listed above is possible, in this case it is necessary to stop taking the drug and consult a doctor immediately. Treatment is symptomatic, Activated carbon. For the prevention of neurotoxic action, it is possible to administer pyridoxine, anticonvulsant and sedative drugs.

Interaction:

Ethionamide and isoniazid: increase the risk of adverse reactions from the nervous system.

Phenytoin: may increase the concentration of phenytoin;

The use of pyridoxine (Vitamin B6) reduces side effects from the central nervous system. Do not use together with cycloserine, since terizidone is its derivative.

Special instructions:

It is recommended to take together with glutamic acid at a dose of 500 mg 3 times a day and pyridoxine at a dose of 20 mg 2 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 on the ability to drive transp. cf. and fur:

When receiving terizidona should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.

Form release / dosage:

Capsules, 250 mg.

Packaging:

4 capsules in an aluminum foil strip.

1 strip together with instructions for application put in a pack of cardboard.

10 capsules in an aluminum foil strip.

5 or 10 strips together with the application put in a pack of cardboard.When packaged at a Russian enterprise (LLC Dobrolek, FGBICU "RNTS named after NN Blokhin" or CJSC "Rafarma") 10 strips of 10 capsules are placed in a pack of cardboard together with instructions for use.

Storage conditions:

Store in a dry, dark 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.

Terms of leave from pharmacies:On prescription

Registration number:LSR-010226/09

Date of registration:15.12.2009

The owner of the registration certificate:McLeodz Pharmaceuticals Co., Ltd. McLeodz Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

MACLEODS PHARMACEUTICALS, Ltd. India

Representation: & nbspAdvansd Trading, OOOAdvansd Trading, OOO

Information update date: & nbsp23.09.2015

Illustrated instructions

Instructions

Terizidone-Mak (Terizidon-Mak)