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

Excipients: cellulose microcrystalline (37.68 mg / 29.50 mg), disodium edetate (2.04 mg / 4.00 mg), hypromellose (12.24 mg / 5.50 mg), magnesium stearate (0 mg / 6.00 mg), stearic acid (2.04 mg / 0 mg).

Composition of gelatin capsule M 2:

Capsule body: titanium dioxide (2.6250%), bronopol (0,0900 %), sodium lauryl sulfate (0.1000%), water (14D0OO%), gelatin (up to 100 %).

Capsule cap: dye azorubin (0.0583%), titanium dioxide (1.1667%), bronopol (0.0900%), sodium lauryl sulfate (0.1000%), water (14.2000 %), gelatin (up to 100%).

The composition of the gelatin capsule № 0: titanium dioxide (1.7500%), brilliant diamond blue (0.0189%), bronopol (0.0900%), silicon dioxide colloid (1.0000%), sodium lauryl sulfate (0.5000%), water (14, 1000%), gelatin (up to 100 %).

Description:

Capsules with a dosage of 150 mg: Hard gelatin capsules in the size "2" with the case of white color and a lid of pink color. Contents of capsules: a mixture of fine granules and powder from white to yellowish or yellowish-beige color.

Capsules with a dosage of 300 mg: Hard gelatin capsules in size "O" with a body and a lid of light 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. Derivative 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 of 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, a also Staphylococcus aureus, Staphylococcus epidermidis. TO this drug sensitive also Enterococcus faecalis, Escherichia coli, Citrobacter spp., Enterobacter spp., Morganella morganii, Klebsiella pneumoniae, Pseudomonas aeruginosa.

Pharmacokinetics:

After oral administration of 250 mg of terizidone, the maximum concentration (Cmax) is about 6.5 μg / ml, the peak concentration of the drug in the blood plasma is achieved in 2-4 hours Terizidone 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% of the concentration in the blood plasma), a higher concentration is noted in patients with inflammation of the meninges.When administered in a dose of 250 mg of terizidone, high concentrations of the drug are found in the blood and urine, which allows

use it for the treatment of urinary tract infections, incl. chronic forms. Kidney excretion occurs slowly and evenly, the elimination half-life (T1 / 2) - 24 hours Slow kidney excretion of the drug leads to the fact that Terizidone concentration in urine is maintained for 12 hours and 60-70 % Terisidone 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 the drug, including cycloserine.

Organic central nervous system diseases, atherosclerosis, cerebrovascular disease, epilepsy and epileptic seizures (including history).Disorders of the psyche (anxiety, psychosis, depression, including in history). Chronic renal failure.

Chronic heart failure.

Alcoholism.

Pregnancy, lactation.

Children up to 14 years.

Carefully:FROM caution The drug is used to treat elderly patients and patients with impaired liver and kidney function, with heart failure.

Pregnancy and lactation:

Concentrations in human milk approach the concentrations found in blood plasma. When using the drug during the period of breastfeeding, breast-feeding should be stopped.

Dosing and Administration:

Inside, without opening capsules, regardless of food intake.

For adults I have children older than 14 years and body weight less than 60 kg - 300 mg 2 times a day (600 mg per day); with a body weight of 60 - 80 kg - 300 mg 3 times a day (900 mg per day). Adults with a body weight of more than 80 kg - 600 mg 2 aza a day (1200 mg per day).

In case of renal dysfunction (creatinine clearance less than 30 ma / m³) dose and multiplicity reception is recommended to reduce.

The duration of treatment is 3-4 months.

The drug does not have the features of the action at the first reception or upon its cancellation.

Under no circumstances should you prematurely discontinue or temporarily discontinue a course of treatment initiated or take the medication irregularly.

If you miss a dose, you need to take the next dose of the drug at the set time, do not take twice the dose of the drug.

Side effects:

the following gradation is used to estimate the incidence of side effects: very often (> 1/10), often (> 1/100, but <1/10), sometimes (> 1/1000, but <1/100), rarely (> 1/10 000, but <1/1000), very rarely (<1/10 000, including reports of isolated cases).

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.

Other: Very rarely: allergic reactions, skin rash.

Overdose:

Cases of drug overdose are not described.

In case of an overdose, it is possible to increase neurotoxicity (convulsions), impairment of the functions of the gastrointestinal tract Measures to help with overdose

Symptomatic therapy, Activated carbon. For the prevention of neurotoxic action, it is possible to administer pyridoxine, anticonvulsant and sedative drugs. Hemodialysis is effective.

Interaction:

Ethanol increases the risk and incidence of adverse reactions, including the development of seizures.

With simultaneous use with pyridoxine, the risk and frequency of adverse reactions from the central nervous system is reduced.

When used simultaneously with ethionamide, the risk of side effects from the central nervous system increases, especially convulsive syndrome.

With simultaneous application with phenytoin, an increase in the concentration phenytoin in the blood plasma.

When used simultaneously with isoniazid, the incidence of dizziness and drowsiness increases.

With simultaneous application with cycloserine, an overdose of the drug is possible.

Special instructions:

The use of the drug against the background of alcohol intake is associated with an increased incidence of side effects, up to the development of seizures,so during the intake of the drug should be avoided the use of alcoholic beverages.

Terizidone can cause the development of vitamin B deficiency12 and / or folic acid. In these cases it is necessary to conduct an appropriate examination and treatment of the patient. It is recommended to take the drug 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.

When the drug is administered, it is necessary to monitor the blood and urine tests, liver function indicators (blood plasma concentration of alanine aminotransferase, aspartate aminotransferase and bilirubin) on a monthly basis.

It is necessary to monitor the patient's condition: medical personnel monitoring patients in the hospital, as well as members of the family of outpatients who receive terizidone, should be informed of the possibility of developing unwanted reactions from the nervous system and instructed about the need to immediately inform the attending physician when depression or changes in the behavior of the patient occur.

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

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

Form release / dosage:

Capsules 150 mg and 300 mg.

Packaging:

4 capsules in an aluminum foil strip. 1 strip with instructions for use put in a pack of cardboard.

10 capsules per strip of aluminum foil. 5 or 10 strips together with the application put in a pack of cardboard. When packaged at a Russian plant (LLC Dobrolek, FGBNU "RNTS named after NN Blokhin") 10 strips of 10 capsules are placed in a pack of cardboard together with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Special precautions for the destruction of the drug

Special precautions for the destruction of an unused medicinal product or a drug with expired shelf life are not it takes.

Shelf life:

2 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001804

Date of registration:17.08.2012

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)