Active substanceCycloserineCycloserine
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  • Dosage form: & nbspcapsules
    Composition:

    Each capsule contains:

    Active substance: cycloserine (in terms of the active substance) 250 mg. Excipients: magnesium stearate, silicon dioxide colloid, calcium phosphate, talc.

    Capsule shell contains: titanium dioxide, dye Ponso 4R, dye quinoline yellow, gelatin, water.

    Description:

    Hard gelatin capsules of size 1 with a white or almost white body and a red lid.

    The contents of the capsules are white to light yellow powder.

    Pharmacotherapeutic group:Antibiotic.
    ATX: & nbsp

    J.04.A.B   Antibiotics

    J.04.A.B.01   Cycloserine

    Pharmacodynamics:

    Antibiotic of a wide spectrum of action. It acts bacteriostatically or bactericidal, depending on the concentration in the focus of inflammation and the sensitivity of microorganisms.

    It breaks the synthesis of the cell wall, acting as a competitive antagonist of D-alanine. Suppresses the activity of enzymes responsible for the synthesis of the cell wall.

    It is active against gram-negative microorganisms, in a concentration of 10-100 mg / l - Rickettsia spp., Treponema spp. The MIC with respect to Mycobacterium tuberculosis is 3-25 mg / L on liquid and 10-20 mg / L and more - on a dense nutrient medium. Drug resistance appears slowly (after 6 months of treatment develops in 20-60% of cases).

    Pharmacokinetics:

    Absorption after oral administration is 70-90%. Virtually does not bind to plasma proteins.

    TSmax - 3-4 hours; in proportion to the dose of 0.25, 0.5 and 1 g of Cmax is 6, 24 and 30 μg / l, respectively. After taking 250 mg every 12 hours Cmax 25-30 μg / ml.

    It penetrates well into body fluids and tissues, including CSF, breast milk, bile, sputum, lymphatic tissue, lungs, ascites and synovial fluid, pleural effusion, passes through the placenta.In the abdominal and pleural cavities contains 50-100% of the concentration of the drug in the blood serum.

    Metabolized to 35% of the administered dose. T1 / 2 with normal renal function -10 h. It is excreted by glomerular filtration in unchanged form: 50% after 12 hours, 65-70% within 24-72 hours, small amounts - with caloric masses. With chronic renal failure after 2 to 3 days, cumulation phenomena

    Indications:

    Tuberculosis (chronic forms, drug reserve, as part of combination therapy).

    Atypical mycobacterial infections (including those caused by Mycobacterium avium), urinary tract infections.

    Contraindications:

    Hypersensitivity, organic diseases of the central nervous system, epilepsy, epileptic seizures (including in the anamnesis), mental disorders (anxiety, psychosis, depression, including in the anamnesis), CHF, CRF (creatinine clearance less than 50 ml / min) , alcoholism.

    Carefully:

    Childhood.

    Pregnancy and lactation:

    Applicable only in cases of vital necessity.

    Dosing and Administration:

    Inside, immediately before meals (with irritation of the mucous membrane of the gastrointestinal tract after eating), adults - 0.25 g every 12 hours for the first 12 hours, then if necessary taking into account the tolerability dose carefully increased to 250 mg every 6-8 hours under the control of the concentration of the drug in the blood serum.

    The maximum daily dose - 1 in patients older than 60 years and weighing less than 50 kg - 0.25 g of 2 times a day. The daily dose for children is 0.01-0.02 g / kg (not more than 0.75 g / day).

    Side effects:

    From the nervous system: headache, dizziness, insomnia or drowsiness, "nightmarish" dream, anxiety, irritability, memory loss, paresthesia, peripheral neuritis, tremor, euphoria, depression, suicidal tendencies, psychosis, epileptiform convulsions.

    From the cardiovascular system: exacerbation of chronic heart failure in patients taking from 1 to 1.5 g of cycloserine per day.

    From the digestive system: nausea, heartburn, diarrhea.

    Allergic reactions (rash, pruritus), megaloblastic anemia and increased levels of liver transaminases, nausea, heartburn, diarrhea, especially in elderly patients with preexisting liver disease.

    Other: fever, coughing.

    Overdose:

    Overdosing occurs when cycloserine plasma concentrations of 25-30 mg / ml as a result of receiving cycloserine in high doses and / or disorders of renal clearance. Acute poisoning can occur if ingested more than 1 g / day.

    Symptoms of chronic intoxication with long-term admission in a dose of more than 500 mg / day: 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:

    Increases the rate of excretion of pyridoxine by the kidneys (may cause the development of anemia and peripheral neuritis, an increase in the dose of pyridoxine is required).

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

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

    Isoniazid increases the incidence of dizziness, drowsiness.

    Special instructions:

    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 strain to other anti-tuberculosis drugs.

    Treatment with cycloserine should be canceled or the dose should be reduced if the patient develops an allergic dermatitis or symptoms of the central nervous system, namely: headache, dizziness, drowsiness, confusion, tremor, peripheral paresis, dysarthria, convulsions and psychosis. In view of the low therapeutic index of cycloserine, the risk of seizures increases in patients with chronic alcoholism.

    Poisoning is usually observed at drug concentrations in the blood of more than 30 mg / l, which may be the result of an overdose or impaired renal clearance. When taking the drug should monitor hematological indicators, kidney function (the concentration of creatinine and urea nitrogen in the blood), the concentration of the drug in the blood and the function of the liver.

    In the treatment of patients with reduced renal function, taking a daily dose of more than 500 mg and who are suspected to have signs and symptoms of an overdose, the level of the drug in the blood should be monitored at least once a week. The dose needs to be adjusted in such a way as to maintain the level of the drug in the blood below 30 mg / l.To prevent symptoms of central nervous system damage, in particular, seizures, arousal or tremor, it is possible to use anticonvulsants or sedatives. 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 to 4 times daily (before meals) during the treatment period, and daily administration of the sodium salt of ATP (1 ml of a 1% solution), as well as pyridoxine in a dose 200-300 mg / day. For the prevention of adverse neurotoxic effects, psychotropic drugs of benzodiazepine diazepam (5 mg) or phenazepam (1 mg) overnight, as well as piracetam in a dose of 800 mg 2 times a day.

    In some cases, the use of cycloserine can cause the development of vitamin deficiency AT12 and / or folic acid, 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:

    The effect of cycloserine on the ability to drive a car and use mechanisms is not established.

    Form release / dosage:

    Capsules of 250 mg.

    Packaging:

    For 10 capsules in a blister AL / PVC.

    For 1, 5, 10 blisters in a cardboard pack 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.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001790
    Date of registration:31.05.2010
    The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group India
    Information update date: & nbsp09.10.2015
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