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

Lactose monohydrate 30 mg / 30 mg, talc purified 10 mg / 10 mg, hard gelatin capsules No. 0 blue (for a dosage of 250 mg + 10 mg) and blue / cyan (for a dosage of 300 mg + 10 mg).

The composition of capsules of gelatinous solid blue and blue colors No. 0: Gelatin - 83.2267%, titanium dioxide 1.6970%, water 14.5%, sodium lauryl sulfate 0.15%, bronopol - 0.1%, povidone - 0, 1%, methyl parahydroxybenzoate 0.075%, propyl parahydroxybenzoate 0.025%, dye indigo carmine 0.1263%.

Ingredients per one capsule produced by OJSC Pharmasynthesis, Russia

Active substances:

Terizidone 250 mg 300 mg

Pyridoxine hydrochloride 10 mg of 10 mg Excipients:

Lactose monohydrate 30 mg / 30 mg, talc purified 10 mg / 10 mg, hard gelatin capsules No. 0 blue (for a dosage of 250 mg + 10 mg) and blue / cyan (for a dosage of 300 mg + 10 mg).

Description:

For dosage of 250 mg + 10 mg: gelatin capsules number "0". The capsule case is blue, the capsule cover is blue.

For the dosage of 300 mg +10 mg: gelatin capsules number "0". The capsule case is blue, the capsule cover is blue.

The contents of the capsules are white or white with a yellowish tinge powder.

Pharmacotherapeutic group:anti-tuberculosis drug.

ATX: & nbsp

J.04.A.K.03 Terizidone

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

Pharmacodynamics:

Terizidone is a bacteriostatic antibiotic with a wide spectrum actions. Terizidone active with respect to Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, and Staphylococcus aureus and Staphylococcus epidermidis. To this preparation are also sensitive Enterococcus faecalis, Escherichia coli, Citrobacter spp., Enterobacter spp., Morganella morganii, Klebsiella pneumoniae and Pseudomonas aeruginosa. Cases of development of secondary resistance are rare. There is no cross-resistance between terizidone and other anti-tuberculosis drugs.

Pyridoxine. Entering the body, it is phosphorylated, converted to pyridoxal-5-phosphate and is part of the enzymes that carry out decarboxylation, transamination and racemization of amino acids, as well as the enzymatic conversion of sulfur-containing and hydroxylated amino acids. Participates in the exchange of tryptophan (participation in the reaction of serotonin biosynthesis) and reduces the toxicity of isonicotinic acid hydrazides.

Pharmacokinetics:

Terizidone. After oral administration, the drug is almost completely absorbed from the gastrointestinal tract (70-90%). The maximum concentration in plasma is achieved in 2-3 hours. Food intake does not affect the rate of absorption. The effective minimum concentration for Mycobacterium tuberculosis - 10-40 mg / l, for Staphylococcus spp. - 8-32 mg / l, for gram-negative bacteria of clinical significance, 20-250 mg / l. The half-life (T1 / 2) is 21 hours. Widely distributed in tissues and body fluids, lungs, bile, ascitic fluid, pleural effusion and synovial fluid, lymph and in sputum. Very well penetrates into the cerebrospinal fluid (80-100% of the concentration in the serum), a higher concentration in the cerebrospinal fluid is created by inflammatory changes in the meninges.

In organism terizidone is metabolized slightly.From 60 to 70% of the drug is excreted by the kidneys unchanged; a small amount is excreted through the intestine and a small part in the form of metabolites.

Pyridoxine absorbed quickly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolized in the liver with the formation of pharmacologically active metabolites (pyridoxalphosphate and pyridoxamino phosphate). Pyridoxalphosphate with plasma proteins binds to 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. The half-life is 15-20 days. It is excreted by the kidneys.

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

Contraindications:

- hypersensitivity, including cycloserine;

-organic diseases of the central nervous system, including atherosclerosis of cerebral vessels;

-epilepsy;

-psychic disorders;

-alcoholism;

- pregnancy;

- lactation period;

-baby age to 14 years;

- lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

Carefully:

-elderly age;

- chronic heart failure;

- chronic renal failure;

- ulcer disease of the stomach and duodenum;

-cardiac ischemia.

Dosing and Administration:

Inside, daily, regardless of food intake.

For adults and children (over 14 years): with a body weight of less than 50 kg, 1 capsule is prescribed (with a dosage of 250 mg + 10 mg) 3 times a day.

If necessary, the frequency of intake is reduced, increasing the dose - 1 capsule (300 mg + 10 mg) 2 times a day.

For adults with a body weight of 60 to 80 kg, the daily dose is 900 mg, on terizidone, in two - three receptions. For adults with a body weight of more than 80 kg - a daily dose of 1200 mg, recalculated by terizidone, in two steps. On the prescription of the doctor, a single dose of the drug for patients with a body weight of more than 50 kg can be reduced to 250 mg, in terms of terizidone, with a frequency of reception 4 times a day. When creatinine clearance is less than 30 ml / min, it is recommended to reduce the frequency of administration of the drug and reduce the single dose to 250 mg in terms of terizidone. The duration of the course of treatment is from 3 to 4 months.

Side effects:

From the nervous system: headache, dizziness, increased excitability, tremor, insomnia and a sense of intoxication. In isolated cases - f, convulsions, depression, psychosis.

From the digestive system: abdominal pain, flatulence, diarrhea.

Other. Allergic reactions.

Pyridoxine.

Allergic reactions, hypersecretion of hydrochloric acid, numbness of the limbs, the appearance of a feeling of compression in the limbs - a symptom of "stocking" and "gloves", skin rash, itching of the skin.

Overdose:

Symptoms: increased neurotoxicity, including convulsions, impaired function of the gastrointestinal tract.

Treatment: symptomatic, Activated carbonanticonvulsant and sedative drugs are used to prevent and treat neurotoxic effects. Hemodialysis is effective.

Interaction:

Terizidone. Ethanol increases the risk of seizures.

Ethionamide increases the risk of side effects from the central nervous system, especially convulsive syndrome.

Isoniazid increases the incidence of dizziness, drowsiness. Pyridoxine. Strengthens the action of diuretics; weakens the activity of levodopa. Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine. Combines with cardiac glycosides (pyridoxine promotes an increase in the synthesis of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate.

Special instructions:

Terizidone can cause the development of insufficiency of cyanocobalamin and / or folic acid. In these cases it is necessary to conduct an appropriate examination and treatment of the patient. It is recommended to monitor the blood and urine tests every month, the liver function indicators: the activity of alanine aminotransferase and aspartate aminotransferase, the concentration of bilirubin. 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 convulsions, so during the intake of the drug should avoid the use of alcoholic beverages.

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

With severe liver damage pyridoxine in large doses can cause deterioration of its functions.

When determining urobilinogen using Ehrlich's reagent, it can distort the results.

When treating tuberculosis with isonicotinic acid hydrazide and its derivatives per 1 g of isonicotinic acid hydrazide administered, 0.1 g of pyridoxine should be administered (to prevent dysfunction of the central nervous system).

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

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

Form release / dosage:

Capsules 250 mg + 10 mg and 300 mg + 10 mg.

Packaging:In the production of the drug at the Lok Beta Pharmaceuticals (I) Pvt Ltd, India:
10 capsules per circuit cell packaging made of polyvinylchloride film and foil aluminum printed.

1 or 3 contour mesh packs in a cardboard box with instructions for use.

In the production or packaging, preparation packaging at the enterprise OJSC "Pharmaceuticals" (Russia):

10 capsules per contour cell pack of film and foil aluminum printed.

By 1, 2 or 3 contour mesh Packages together with the use in a pack of cardboard for consumer packaging.

For 30 or 100 capsules are placed in a package from low density polyethylene. On package paste a label of paper label or written or from polymeric materials, self-adhesive. One package together with instructions for use In a polymer jar with a lid of polypropylene or high-pressure polyethylene with the 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 Pa. The cans are labeled with label or written paper or from polymeric materials, self-adhesive.

Storage conditions:

In 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 indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005422/10

Date of registration:10.06.2010

The owner of the registration certificate:ArSiAi Synthesis, ZAOArSiAi Synthesis, ZAO

Manufacturer: & nbsp

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

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp23.09.2015

Illustrated instructions

Instructions

Terizidone plus (Terizidon Plus)