Composition, form of production and packaging
Capsules 1 caps.
terizidone 250 mg
pyridoxine hydrochloride 10 mg
10 pieces. - packings without cell contour (1) - packs cardboard.
10 pieces. - Packings without glue contour (2) - packs cardboard.
10 pieces. - Packings without glue contour (3) - packs cardboard.
10 pieces. - Packings without cell contour (10) - packs cardboard.
Capsules 1 caps.
terizidone 300 mg
pyridoxine hydrochloride 10 mg
10 pieces. - packings without cell contour (1) - packs cardboard.
10 pieces. - Packings without glue contour (2) - packs cardboard.
10 pieces. - Packings without glue contour (3) - packs cardboard.
10 pieces. - Packings without cell contour (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
Terizidone is a bacteriostatic antibiotic with a wide spectrum of action. Terisidone is active against Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, as well as Staphylococcus aureus and Staphylococcus epiderrnidis. 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 enzymes that carry out decarboxylation, transamination and racemization of amino acids, as well as 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 the plasma is achieved in 2-3 hours. Food intake does not affect the rate of absorption. 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. T 1/2 - 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 the body, terizidone is metabolized insignificantly. 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 is absorbed rapidly throughout the small intestine, more is absorbed in the jejunum. Metabolized in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate 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. T 1/2 - 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.
DOSING MODE
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, in terms of terizidone, in 2-3 doses. For adults with a body weight of more than 80 kg - a daily dose of 1200 mg, in terms of terizidone, in two divided doses. 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 EFFECT
Terizidone.
From the nervous system: headache, dizziness, increased excitability, tremor, insomnia and a sense of intoxication. In single cases - 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.
CONTRAINDICATIONS
- organic diseases of the central nervous system, including atherosclerosis of cerebral vessels;
- epilepsy;
- mental disorders;
- Alcoholism;
- Pregnancy;
- lactation period;
- children's age till 14 years;
- lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome;
- hypersensitivity, including cycloserine.
Carefully:
- elderly age;
- Chronic heart failure;
- chronic renal failure;
- Stomach ulcer and duodenal ulcer;
- cardiac ischemia.
PREGNANCY AND LACTATION
Contraindicated during pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: chronic renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With severe liver damage, pyridoxine in high doses can cause deterioration of its function.
APPLICATION FOR CHILDREN
Contraindicated in children under 14 years.
APPLICATION IN ELDERLY PATIENTS
Use with caution in old age.
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 taking terizidone, should be informed of the possibility of developing side effects from the central nervous system and are instructed to immediately inform the attending physician when depression or changes in the behavior of the patient.
With severe liver damage, pyridoxine in high doses can cause deterioration of its function.
When determining urobilinogen with Erlich reagent, pyridoxine can distort 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).
Impact on the ability to drive vehicles and manage mechanisms
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.
OVERDOSE
Symptoms: increased neurotoxicity, including convulsions, dysfunction of the gastrointestinal tract.
Treatment: symptomatic, activated charcoal, anticonvulsant and sedative drugs are used to prevent and treat neurotoxic effects. Hemodialysis is effective.
DRUG 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 zestrogen-containing oral contraceptives weaken the effect of pyridoxine. It is combined with cardiac glycosides (pyridoxine promotes the synthesis of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
In a dry, the dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 2 years.
