Cyclomycin® Plus (Cyclomicin® plyus)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceCycloserine + PyridoxineCycloserine + Pyridoxine
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    capsules inwards 
    VALENTA PHARM, PAO     Russia
    • Dosage form: & nbspcapsules.
    Composition:

    Composition per one capsule

    One capsule contains: active substances: cycloserine (in terms of 100% substance) - 250 mg; pyridoxine hydrochloride (in terms of 100% substance) - 10 mg;

    Excipients: calcium hydrophosphate dihydrate - 112.4 mg, silicon dioxide colloid (aerosil) - 3.8 mg, magnesium stearate - 3.8 mg;

    hard gelatin capsules - 96.0 mg: titanium dioxide E 171 - 1.0% or 1.3333%, dye sunset yellow E 110 -1.0% or 0.4418%, gelatin up to 100.0%.

    Description:

    Capsules number 0 orange. The contents of capsules are white or white powder with a yellowish tinge color, prone to clumping.

    Pharmacotherapeutic group:Antibiotic.
    ATX: & nbsp

    J.04.A.B.01   Cycloserine

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

    Pharmacodynamics:

    Combined drug.

    Cycloserine, a broad-spectrum antibiotic, disrupts the synthesis of the cell wall, acting as a competitive antagonist of D-alanine, suppresses the enzymes responsible for the synthesis of the cell wall. Active against gram-negative microorganisms in a concentration of 10-100 mg / l (Rickettsia spp., Treponema spp.). The minimum inhibitory concentration (MIC) in relation 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 it develops in 20-60% of cases).

    Pyridoxine, which is part of the drug, reduces the severity of adverse reactions of cycloserine from the side of the central nervous system (CNS).

    Pharmacokinetics:

    Cycloserine is rapidly absorbed from the gastrointestinal tract (GIT). Absorption after oral administration is 70-90%. Virtually does not bind to plasma proteins. Time to reach the maximum concentration (TCmax) - 3-4 hours After taking 250 mg every 12 hours, the maximum concentration (Cmax) - 25-30 μg / ml. It penetrates well into body fluids and tissues. Penetrates into lymphoid tissue, lung tissue, pleural and ascites fluid, phlegm, bile, breast milk. In the abdominal and pleural cavities contains 50-100% of the concentration of the drug in the blood serum. Passes the placental barrier and the blood-brain barrier (concentration in the cerebrospinal fluid corresponds to the concentration in the plasma, determined in the amniotic fluid and fetal blood). About 35% of the administered dose is metabolized.It is allocated mainly by the kidneys in an unchanged form by glomerular filtration (50% - found in urine for 12 hours, 65-70% within 24-72 hours), small amounts are excreted by the intestine. The half-life of cycloserine (T1/2) with a normal kidney function of about 10 hours. In chronic kidney failure after 2-3 days, cumulation phenomena may occur.

    Pyridoxine is rapidly absorbed throughout the small intestine, more is absorbed in the jejunum. Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate with plasma proteins binds to 90%. Well penetrates into all tissues, accumulates mainly in the liver, less - in the muscles and the central nervous system. Penetrates through the placenta, is secreted with breast milk. It is excreted by the kidneys. The half-life of pyridoxine (T1/2) -15-20 days.

    Indications:

    As a part of the combination therapy after an unsuccessful adequate treatment with basic drugs in case of sensitivity of microorganisms to cycloserine. Active pulmonary tuberculosis, extrapulmonary tuberculosis (including kidney damage), chronic forms of tuberculosis.

    The combination of tuberculosis with acute infections of the urinary tract caused by sensitive strains of gram-positive and gram-negative bacteria, in particular Klebsiella spp., Enterobacter spp., Escherichia coli with ineffectiveness of essential medicines.

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

    Contraindications:

    Hypersensitivity to the components of the drug, organic diseases of the central nervous system, epilepsy, depression, expressed state of excitation, psychosis, chronic renal failure (creatinine clearance less than 50 ml / min), acute and chronic heart failure, alcoholism, drug addiction, pregnancy, lactation period, 3 years.

    Carefully:

    • impaired renal function (risk of cumulation of the drug);
    • childhood.

    Pregnancy and lactation:

    Contraindicated in pregnancy.

    Penetrates into breast milk, if necessary, use the drug at the time of treatment should stop breastfeeding.

    Dosing and Administration:

    Inside, immediately before meals (with irritation of the mucous membrane of the gastrointestinal tract - after eating).

    Adults are prescribed 12.5 mg / kg body weight or 500-750 mg / day (cycloserine) in 2-3 doses (the initial dose of cycloserine is 250 mg every 12 hours during the first week, then, if necessary, taking into account the tolerability dose is carefully increased up to 250 mg every 6-8 hours under the control of the level of cycloserine in the blood). The highest single dose of cycloserine for adults is 250 mg; the maximum daily dose is 1 g. Patients over 60 years of age, and also with a body weight of less than 50 kg are prescribed 250 mg (cycloserine) 2 times a day.

    In children, the initial dose of cycloserine is 10-20 mg / kg of body weight per day, the maximum daily dose is 750 mg.

    Side effects:

    In treatment, side effects can occur, mainly due to the effect of cycloserine on the nervous system. These phenomena usually occur when the dose is reduced or the drug is withdrawn.

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

    From the side of the digestive system, nausea, heartburn, diarrhea, increased activity of "hepatic" aminotransferases in the serum.

    From the cardiovascular system and hematopoiesis system: sideroblastic and megaloblastic anemia, when applied at a dose of 1 g / day, exacerbation of chronic heart failure.

    Other: deficiency of cyanocobalamin and folic acid, allergic reactions (skin rash, itching, fever, coughing).

    If any of the side effects listed in the manual are aggravated or any other side effects not indicated in the instructions are noted, the doctor should be informed immediately.

    Overdose:

    Overdosage is observed at a plasma cycloserine concentration of 25-30 mg / ml (high doses, impaired renal clearance). Acute poisoning can occur when ingested more than 1 g per day. Symptoms of chronic intoxication occur with long-term administration of cycloserine in a dose of more than 500 mg per day.

    Symptoms: headache, dizziness, increased irritability, paresthesia, dysarthria, paresis, convulsions, psychosis, confusion or loss of consciousness (coma).

    Treatment: symptomaticActivated carbon, anticonvulsant and sedatives). Effective hemodialysis. For the prevention of neurotoxic effects are introduced pyridoxine at the rate of 200-300 mg / day. All activities are conducted against the background of drug withdrawal.

    Interaction:

    Cycloserin increases the rate of excretion of pyridoxine by the kidneys. Reduces resistance to isoniazid, streptomycin and paraaminosalicylic acid (PASK). Isoniazid increases the toxic effect of the drug on the central nervous system (increases the incidence of dizziness, drowsiness, it may be necessary to adjust the dose of both drugs).

    Ethionamide enhances the neurotoxic effect of cycloserine (simultaneous administration of ethionamide increases the risk of side effects from the CNS, especially convulsive syndrome).

    Pyridoxine reduces the intensity of adverse reactions of cycloserine on the part of the nervous system. Strengthens the action of diuretics, weakens the activity of levodopa. Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine.

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

    Special instructions:

    With monotherapy, the rapid development of mycobacterial resistance to cycloserine is possible, so the drug should be used only in combination with other anti-tuberculosis drugs in the absence of the effect of treatment with first-line drugs, such as streptomycin, isoniazid, rifampicin, ethambutol. Before the treatment, it is necessary to isolate the culture of microorganisms, to determine the sensitivity of the strain to cycloserine and other anti-tuberculosis drugs. During the period of treatment, alcohol is not allowed.

    To identify signs of toxic effects of the drug on the central nervous system, careful monitoring of patients receiving cycloserine in a dose exceeding 500 mg / day. The drug should be administered under the control of the level of cycloserine in the blood (the concentration of cycloserine should not exceed 30 mg / ml, at a higher concentration, toxicity is likely). During the treatment period, hematologic parameters, kidney and liver function should also be monitored. In patients with impaired renal function, a weekly urine test should be monitored.

    For the prevention of neurotoxic effects (including seizures, agitation, tremor) during the period of treatment, it is possible to prescribe anticonvulsant and sedative drugs, benzodiazepine drugs (diazepam) and nootropic drugs (piracetam). To prevent or reduce the toxic effects of cycloserine, glutamic acid can also be given 0.5 g 3-4 times per day (before meals), and daily IM injection of sodium ATP (1 ml of 1% solution).

    To reduce adverse reactions, you should limit the mental tension of patients and exclude possible factors of overheating (exposure to the sun with uncovered head, hot shower).

    It should be borne in mind that the presence of pyridoxine in the preparation may cause distortion of the results in the determination of urobilinogen with Ehrlich's reagent.

    In case of development of allergic dermatitis or symptoms of central nervous system (CNS) damage (convulsions, psychosis, drowsiness, confusion, hyperreflexia, headache, dizziness, tremor, peripheral paresis, dysarthria) treatment with the drug should be canceled. During the treatment period, the electroencephalogram (EEG) should be monitored.In some cases, the use of cycloserine and other anti-tuberculosis drugs can lead to the development of deficiency of cyanocobalamin and folic acid, megaloblastic anemia.

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

    Given the possible side effects, when taking the drug should be careful during work drivers of vehicles and people whose profession requires increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Capsules 250 mg + 10 mg.

    Packaging:

    For 10 capsules in a contour mesh package made of PVC or PVC / PVDC film and aluminum foil printed lacquer.

    5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard for consumer containers.

    Storage conditions:

    In 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 expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000611
    Date of registration:21.09.2011
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.10.2015
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