Terizidone + Pyridoxine-Mac - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 68.4 mg, lactose 30.9 mg, silicon dioxide colloid 2,4 mg, carboxymethyl starch sodium 7.2 mg, magnesium stearate 0.6 mg;

composition of the shell:

hypromellose 2.52 mg, talcum purified 0.52 mg, titanium dioxide 0.26 mg, macro code 400 0.3 mg.

gelatin capsule composition:

dye azorubin cap - 0.0537%, body - 0,0,537%, coloring sunset sunset yellow cap - 1,2900 %, body 1.2900%, titanium dioxide lid - 1.4998%, body - 1.4998%, the color of the brilliant blue 0.7583%, propyl-parahydroxybenzoate 0.20 %, Methyl p-hydroxybenzoate 0.80%, sodium lauryl sulfate 0.08 %, gelatin up to 100%.

Description:

Hard gelatin capsules in the size "0" with the case and the lid of orange color. Contents of capsules: a mixture of fine granules and powder from white to yellowish or yellowish-beige color and a tablet coated with a coat from white to yellowish or yellowish-beige. On the fracture - the mass of the tablet from white to yellowish ooze or yellowish-beige color.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.K.03 Terizidone

A.11.H.A.02 Pyridoxine (vitamin B6)

Pharmacodynamics:

Terizidone

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 that causes infections of the urinary tract, including strains of bacteria that become resistant to other antibiotics.The minimum inhibitory concentration of terizidone for sensitive strains is 4-250 mg / l, c. including for Mycobacterium tuberculosis is 10-40 mg / l, for staphylococci - 8-32 mg / l, for gram-negative bacteria, having a clinical value of 50-250 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.

Pyridoxine

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 antineurotoxic effect. The use of pyridoxine reduces the side effects of the central nervous system.

Pharmacokinetics:

Terizidone

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 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 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. Pyridoxine

Absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolized in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate), Pyridoxalphosphate 90% bound to plasma proteins. 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. The half-life (T1/2) is 15-20 days. It is excreted by the kidneys (with iv in the introduction - with bile 2%), as well as during hemodialysis.

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

Contraindications:

- hypersensitivity to terizidone, cycloserine and pyridoxine;

- 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:

Dosage and administration:

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 weighing less than 50 kg - 1 capsule 3 times a day.

The 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.

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), which are listed above,in this case, it is necessary to stop the drug immediately and consult a doctor. Treatment is symptomatic, Activated carbon. To prevent neurotoxic action, it is possible to administer yeridoxine, anticonvulsant and sedative drugs.

Interaction:

Terizidone

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

Phenytoin: may increase the concentration of phenytoin;

Do not use together with cycloserine, since terizidone is its derivative.

Special instructions:

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 illness. During treatment is not allowed alcohol consumption.

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 taking terizidone should refrain from potentially hazardous activities,associated with the need for concentration and increased speed of psychomotor reactions.

Form release / dosage:Capsules, 250 mg + 10 mg.

Packaging:

4 capsules in an aluminum foil strip.

1 strip with instructions but appliedThey put it in a cardboard box.

10 capsules in an aluminum foil strip.

5 or 10 strips together with the application put in a pack of cardboard. When packaged in a Russian company (Dobrolek LLC, FGBNU RNTS NN Blokhin) 10 strips of K) capsules are placed in a pack of cardboard along 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.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006027/09

Date of registration:23.07.2009 / 30.06.2015

Expiration Date:Unlimited

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 + Pyridoxine-Mack (Terizidone + Pyridoxine-Mak)