Kansamin - instructions for use, doses, side effects, contraindications

For a dosage of 125 mg: purified water - 14-15 mg, sodium lauryl sulfate - 0.24 mg, methyl parahydroxybenzoate - 0.8 mg, propyl parahydroxybenzoate - 0.2 mg, dye brilliant blue - 0.1500 mg; titanium dioxide - 1,1252 mg, gelatin - up to 100 mg.

For a dosage of 250 mg: purified water - 14-15 mg, sodium lauryl sulfate - 0.24 mg, methyl parahydroxybenzoate - 0.8 mg.propyl parahydroxybenzoate 0.2 mg, a brilliant blue dye 0.8864 mg; dye azorubin - 0.5363 mg; dye quinoline yellow - 0.0600 mg; titanium dioxide - 1.6129 mg, gelatin - up to 100 mg.

For a dosage of 500 mg: lid: purified water - 14-15 mg, sodium lauryl sulfate - 0.24 mg, methyl parahydroxybenzoate - 0.8 mg, propyl parahydroxybenzoate 0.2 mg, dye quinoline yellow 0.100 mg; titanium dioxide - 1.1627 mg, gelatin - up to 100 mg. housing: purified water - 14-15 mg, sodium lauryl sulfate - 0.24 mg, methyl parahydroxybenzoate - 0.8 mg. propyl parahydroxybenzoate 0.2 mg, titanium dioxide 2.05 mg, gelatin up to 100 mg.

Description:

For a dosage of 125 mg: hard gelatin capsules of blue color No. "2";

For a dosage of 250 mg: hard gelatin capsules of dark brown color No. "1";

For a dosage of 500 mg: hard gelatin capsules № "00", body white, cover yellow.

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

Pharmacotherapeutic group:Antibiotic

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.01 Cycloserine

Pharmacodynamics:

Cycloserin is a broad-spectrum bactericidal antibiotic that disrupts the synthesis of the cell wall. Acting as a competitive antagonist of D-alanine, it suppresses the enzymes responsible for the synthesis of the bacterial cell wall. It is active against gram-negative microorganisms (Escherichia coli, Enterobacter spp) and Mycobacterium tuberculosis. Drug resistance appears slowly (after 6 months of treatment it develops in 20-60% of cases).

Pharmacokinetics:

Well absorbed from the gastrointestinal tract. Absorption after oral administration is 70-90%. Virtually does not bind to plasma proteins.

Time to reach the maximum concentration - 3-4 hours Proportionally accepted dose of 0.25, 0.5 and 1 g maximum concentration (C_max) is 6, 24 and 30 μg / ml, respectively. After taking 250 mg every 12 hours C_max is 25-30 μg / ml.

It penetrates well into body fluids and tissues, including cerebrospinal fluid, breast milk, bile, sputum, lymphatic tissue, lungs, ascites and synovial fluid, pleural effusion, passes through the placenta. Partially (35%) is metabolized in the liver. The half-life (T_1/2) with normal kidney function is about 10 hours. It is excreted by the kidneys by glomerular filtration in unchanged form: 50% after 12 hours, 65-70% within 24-72 hours, small amounts - by the intestine. With chronic renal failure, after 2-3 days, cumulation phenomena may occur.

Indications:

Treatment of the active form of pulmonary tuberculosis and extrapulmonary form of tuberculosis (including renal tuberculosis) under the condition of sensitivity to cycloserine Mycobacterium tuberculosis and with ineffectiveness of essential medicines (rifampicin, isoniazid, streptomycin, ethambutol), only in combination with other anti-tuberculosis drugs.

Acute urinary tract infections caused by sensitive strains of Escherichia coli, Enterobacter spp. Use Kansamin for the treatment of these infections should be only after other means for treatment have been exhausted, and provided that the sensitivity of microorganisms to cycloserine is determined.

Contraindications:

Hypersensitivity to cycloserine or any other component of the drug, organic diseases of the central nervous system, epilepsy, epileptic seizures (including in the anamnesis), mental disorders (anxiety, psychosis, depression, including in the history), renal failure (creatinine clearance less than 25 ml / min), alcoholism, pregnancy, lactation, children under 3 years of age and body weight less than 25 kg.

It is not recommended to take patients with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome, since the preparation contains lactose.

Carefully:

Children's age (from 3 to 18 years), chronic renal failure (creatinine clearance more than 25 ml / min).

Pregnancy and lactation:

The drug is contraindicated for use in pregnancy and lactation.

Dosing and Administration:

Inside, immediately before meals (with irritation of the mucous membrane of the gastrointestinal tract - after eating). The usual dose is from 500 mg to 1 g per day for several doses under the control of the concentration of the drug in the blood.

The initial dose for adults is often 250 mg twice daily with a 12-hour interval during the first two weeks. The daily dose should not exceed 1 g.

Children (over 3 years old and weighing more than 25 kg). The usual dose is from 10 mg / kg of body weight per day for several doses, after which it varies depending on the concentration of the drug in the blood and the therapeutic effect. The daily dose should not exceed 750 mg.

The elderly. Patients over 60 years of age, as well as with a body weight of less than 50 kg, are prescribed 250 mg twice daily.

The course of treatment with cycloserine in infections of the urinary tract is 7-10 days, with tuberculosis - 6 months or more.

Side effects:

From the central nervous system: convulsions, drowsiness, headache, tremor, dysarthria, dizziness, confusion and impaired orientation, accompanied by loss of memory; psychosis (incl.with suicidal attempts); irritability, aggressiveness, peripheral paresis, hyperreflexia, paresthesia, large and small seizures of clonic convulsions, coma.

From the cardiovascular system and hemopoiesis: exacerbation of chronic heart failure (at doses of 1000-1500 mg / day), sideroblastic and megaloblastic anemia.

From the digestive system: nausea, heartburn, diarrhea especially in elderly patients with pre-existing liver disease.

Allergic reactions: skin rash, itching.

Laboratory indicators: increased activity of "hepatic" aminotransferases.

Other: deficiency of cyanocobalamin and folic acid.

Overdose:

Symptoms: headache, dizziness, confusion, increased irritability, paresthesia, psychosis, dysarthria, paresis, convulsions, coma.

Treatment: symptomatic, Activated carbon, antiepileptic drugs. For the prevention of neurotoxic effects are introduced pyridoxine in a dose of 200-300 mg / day, anticonvulsant and sedative drugs.

Interaction:

Ethanol increases the risk of epileptic seizures, especially in individuals with alcoholism.

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

Isoniazid increases the incidence of dizziness, drowsiness.

Cycloserin increases the rate of excretion of pyridoxine by the kidneys (may cause the development of anemia and peripheral neuritis, additional use of pyridoxine is required).

Special instructions:

Treatment with cycloserine should be canceled or the dose should be reduced if the patient develops allergic dermatitis or symptoms of the central nervous system, such as convulsions, psychosis, drowsiness, confusion, hyperreflexia, headache, tremor, dizziness, peripheral paresis or dysarthria.

The risk of seizures increases in patients with alcoholism.

When taking the drug should be monitored hematological indicators, kidney function, the concentration of the drug in the blood and the state of liver function.

Before the start of therapy with cycloserine, it is necessary to isolate cultures of microorganisms and determine the sensitivity of strains to this preparation.In the case of tuberculosis infection, it is necessary to determine the sensitivity of the mycobacterial strain to other antituberculosis drugs.

In the treatment of patients with reduced renal function receiving cycloserine in a dose of more than 500 mg per day, in which the signs and symptoms of an overdose are suspected, the concentration of the drug in the blood should be monitored at least once a week. The dose of cycloserine should be adjusted so that the concentration of the drug in the blood is below 30 mg / l.

Anticonvulsants and sedatives can be effective in preventing the symptoms of central nervous system damage, such as seizures, arousal or tremor.

Patients who receive more than 500 mg of cycloserine per day should be under the direct supervision of a doctor because of the possible development of such symptoms. It is possible to prevent or reduce the toxic effect of cycloserine by prescribing glutamic acid 500 mg 3-4 times daily (before meals) during the treatment period, and daily iv administration of sodium ATP (1 ml of 1% solution), pyridoxine 200-300 mg / day.

In some cases, the use of cycloserine and other anti-TB drugs can cause the development of vitamin B12 and / or folate deficiency, megaloblastic and sideroblastic anemia. In case of anemia during treatment, it is necessary to conduct an appropriate examination and treatment of the patient. It is necessary to limit mental tension of patients and to exclude possible factors of an overheat (stay on the sun with the uncovered head, hot douche).

In connection with the rapid development of resistance with monotherapy with cycloserine, it is recommended that it be combined with other anti-tuberculosis drugs.

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

During the treatment with cycloserine, care must be taken when driving vehicles and mechanisms.

Form release / dosage:

Capsules of 125 mg, 250 mg and 500 mg.

Packaging:

Primary packaging of medicinal product. 10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. For 30, 50 or 100 capsules in a can of polymer with a lid pulled with the control of the first opening. Free space is filled with cotton wool.On cans are labeled with paper label or from polymer materials, self-adhesive.

Secondary packaging of medicinal product.

By 1, 2, 3, 5, 6 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard for consumer containers. For 1 can, along with instructions for use, are placed in a pack of cardboard for consumer containers.

Storage conditions:

In the original packaging of the manufacturer 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:LP-002116

Date of registration:02.07.2013 / 16.02.2016

Expiration Date:02.07.2018

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp30.11.2017

Illustrated instructions

Instructions

Kansamin (Kansamin)