Loxidon plus (Loxidon plus)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTerizidone + PyridoxineTerizidone + Pyridoxine
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    • Dosage form: & nbspcapsules
    Composition:

    Active substance:

    Terizidone 150 mg / 250 mg / 300 mg

    Pyridoxine hydrochloride 10 mg / 10 mg / 10 mg

    Excipients: Lactose 5.0 mg / 15.0 mg / 20.0 mg; silicon dioxide colloid (aerosil) - 4.0 mg / 6.7 mg / 8.0 mg; talc - 5.0 mg / 8.3 mg / 10.0 mg.

    The composition of hard gelatin capsules ("Erawat Pharma Limited", India):

    For a dosage of 150 mg + 10 mg: purified water - 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, titanium dioxide 1.1252 mg 2.05 mg, quinoline yellow 0.0562 mg, gelatin - up to 100 mg.

    For a dosage of 250 mg + 10 mg: purified water - 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, indigo carmine 0.1500 mg, quinoline yellow 0.22625 mg, titanium dioxide, 1,1252 mg - 2,6256 mg, gelatin - up to 100 mg.

    For a dosage of 300 mg + 10 mg: water purified - 14-15 mg, sodium lauryl sulfate 0.24 mg, methyl parahydroxybenzoate 0.8 mg, propyl parahydroxybenzoate 0.2 mg, azorubin dye 0.7501 mg, titanium dioxide 0.3750 mg 2.05 mg, gelatin - up to 100 mg.

    Description:

    For a dosage of 150 mg + 10 mg: hard gelatin capsules number "1". The capsule case is white, the capsule cover is yellow.

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

    For a dosage of 300 mg + 10 mg: Hard gelatin capsules № "00". The capsule body is white, the capsule cover is red.

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

    Pharmacotherapeutic group:Anti-TB drug
    ATX: & nbsp

    J.04.A.K.03   Terizidone

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

    Pharmacodynamics:

    Terizidone

    Terizidone is a broad-spectrum antibiotic, is a derivative of D- cycloserine. Terizidone competitively blocks enzymes that incorporate alanine into alanyl-alanine dipeptide, the main component of the mycobacterium wall. Does not have cross-resistance with other anti-TB drugs. Terizidone has antibacterial activity against mycobacteria tuberculosis and bacteria,causing infections of the urinary tract including strains of bacteria that become resistant to other antibiotics. The minimum inhibitory concentration of terisidone for sensitive strains is 4-250 mg / l, including 10-40 mg / l for mycobacteria of tuberculosis, 8-32 mg / l for staphylococci, and 50-250 for gram-negative bacteria mg / l.

    The following bacteria are sensitive to terizidone: Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium, and Staphylococcus aureus. Staphylococcus epidermidis. To this preparation are also sensitive Enterococcus faecalis, Escherichia coli, Citrobacter, Enterobacter, Morganella morganii, Klebsiella pneumoniae, Pseudomonas aeruginosa.

    Pyridoxine

    Pyridoxine acts as a coenzyme, participating in biochemical reactions, including the metabolism of amino acids and glycogen, in the synthesis of nucleic acids, hemoglobin, sphingomyelin and other sphingolipids, in the synthesis of the mediator serotonin, dopamine, norephedrine and gamma-aminobutyric acid. Pyridoxine has antineurotoxic effect. The use of pyridoxine reduces side effects from the central nervous system (CNS).

    Pharmacokinetics:

    Terizidone

    Terizidone is absorbed from the gastrointestinal tract (GIT) quickly and almost completely - by 70-90%.Food intake does not affect the rate of absorption. After oral administration of 250 mg of terizidone, the maximum concentration in the blood plasma (Cmax) is about 6.5 μg / ml, the time to reach the maximum concentration (TCmax) - 2-4 hours. Widely distributed in tissues and body fluids, for example in the lungs, bile, penetrates into ascitic, pleural and synovial fluid, lymph, and saliva. Very well penetrates into the cerebrospinal fluid (concentration in the cerebrospinal fluid reaches 80-100% concentration in the blood serum), a higher concentration is noted in patients with inflammation of the meninges. When administered with terizidone at a dose of 250 mg, the high concentrations of the drug are found in the blood and urine, which makes it possible to use it for the treatment of urinary tract infections, incl. chronic forms.

    Kidney excretion occurs slowly and evenly, the half-life period (T1/2) - 24 hours Slowed excretion of the drug by the kidneys leads to the fact that the concentration level of terizidone in the urine persists for 12 hours, 60-70% of the drug is excreted unchanged by glomerular filtration. A small amount is excreted by the intestine.The value of the elimination constant is -0.0262 h-1. A small amount of terizidone is metabolized, which causes a low / weak toxic effect on the kidneys. With renal failure, the half-life is extended to 72 hours.

    Pyridoxine

    Absorbed rapidly throughout the small intestine, a larger amount is absorbed in the jejunum. Metabolised in the liver with the formation of pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxalphosphate 90% bound to plasma proteins. 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. T1/2 is 15-20 days. It is excreted by the kidneys, as well as by hemodialysis.

    Indications:Tuberculosis of various forms and localizations in the complex therapy of drug-resistant forms of tuberculosis.
    Contraindications:

    Hypersensitivity to terizidone or cycloserine, pyridoxine, as well as to any other component of the drug; organic diseases of the central nervous system, cerebral atherosclerosis; epilepsy,epileptic seizures (including in the anamnesis); mental disorders (anxiety, psychosis, depression, including in the anamnesis); severe renal failure (creatinine concentration> 2 mg / dL); alcoholism; children's age till 14 years; pregnancy, lactation; lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

    Carefully:

    Elderly age, ischemic heart disease, impaired liver function, impaired renal function (creatinine clearance less than 30 ml / min), chronic heart failure, peptic ulcer of the stomach and duodenum.

    Pregnancy and lactation:

    The use of the drug during pregnancy is contraindicated.

    The concentrations of terisidone in human milk are close to those in blood plasma. In the case of the drug during lactation it is necessary to stop breastfeeding.

    Dosing and Administration:

    Inside, regardless of food intake (dose indicated by terizidon): adults and children over 14 years of age and body weight less than 60 kg - 300 mg twice a day (600 mg / day); with a body weight of 60-80 kg - 300 mg three times a day (900 mg / day).

    Adults with a body weight of more than 80 kg - 600 mg twice a day (1200 mg / day).

    If the renal function is impaired (creatinine clearance less than 30 ml / min), the dose of the drug and the frequency of administration are reduced: 250 mg once a day daily or 500 mg 3 times a week (for example, Monday, Wednesday, Friday). When the creatinine concentration is more than 2 mg / dl, the drug is contraindicated.

    The duration of treatment is 3-4 months.

    The drug does not have the features of the action at the first reception or upon its cancellation.

    Under no circumstances should you prematurely discontinue or temporarily discontinue a course of treatment initiated or take the medication irregularly.

    If you miss a dose, you need to take the next dose of the drug at the set time, do not take a double dose.

    Side effects:

    To estimate the incidence of undesired reactions, the following grades are used: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1 / 10000, <1/1000), very rarely (<1/10000, including reports of single cases).

    From the central nervous system: rarely - headache, dizziness, increased excitability, tremor, insomnia, a feeling of intoxication; very rarely - convulsions (including epileptic), dysarthria, mental disorders, such as mania or depression.

    From the gastrointestinal tract: rarely - abdominal pain, flatulence and diarrhea. Other: very rarely - allergic reactions, skin rash.

    Due to the presence of pyridoxine (in addition): hypersecretion of hydrochloric acid, numbness and the appearance of a feeling of squeezing in the extremities (simtom "stocking" and "gloves"), reducing lactation.

    Overdose:

    Symptoms: There is no evidence of drug overdose.

    In case of overdose, it is possible to increase neurotoxicity (including epileptiform seizures), impaired function of the gastrointestinal tract.

    Treatment: symptomatic, Activated carbon. For the prevention of neurotoxic action, it is possible to administer pyridoxine, anticonvulsant and sedative drugs. Hemodialysis is effective.

    Interaction:

    Terizidone

    Ethanol increases the risk of adverse reactions, incl. epileptic seizures.

    When used simultaneously with ethionamide, the risk of side effects from the central nervous system increases (especially seizures).

    With simultaneous use with fentoyinom increase in the concentration of phenytoin in the blood plasma.

    Simultaneous use with isoniazid increases the incidence of dizziness,drowsiness.

    With simultaneous application with cycloserine, an overdose of the drug is possible.

    Pyridoxine

    Strengthens the action of diuretics; weaken the pharmacological effects of levodopa. Isoniazid, penicillamine, cycloserine and estrogen-containing oral contraceptives weaken the effect of pyridoxine.

    The drug is combined with cardiac glycosides (pyridoxine promotes increase of contractile proteins in the myocardium), with glutamic acid and potassium and magnesium asparaginate.

    Special instructions:

    The use of the drug against the background of alcohol is associated with an increased incidence of side effects, up to the development of seizures, so during the intake of the drug should avoid alcohol.

    The use of the drug simultaneously with cycloserine is prohibited because of a possible overdose.

    Terizidone can cause a deficiency 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 take together with glutamic acid in a dose of 500 mg 3 times a day.

    When treating the drug should be monitored monthly blood and urine tests, liver function indicators (activity of alanine aminotransferase, aspartate aminotransferase, bilirubin concentration in blood plasma).

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

    With severe liver damage pyridoxine in large doses can cause a deterioration in its function.

    When determining urobilinogen using Ehrlich's reagent pyridoxine can distort results.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Capsules 150 mg + 10 mg, 250 mg + 10 mg, 300 mg + 10 mg.

    Packaging:

    Primary packaging of medicinal product.

    10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

    For 30, 60, 100 or 120 capsules in a polymer jar with a cover pulled with the control of the first opening. Free space is filled with cotton wool. Labels are applied to cans from paper label, or writing, or from polymer materials, self-adhesive.

    Secondary packaging of medicinal product.

    For 1, 2 or 3 contour squares, together with the instructions for use, are placed in a pack of cardboard for consumer tare subgroups chrome or chrome - ersatz. The packets are placed in a shipping container.

    On 1 bank together with the instruction on application place in a pack from a cardboard for consumer tare of subgroups chrome or chrome - ersatz or other similar quality. The packets are placed in a shipping container.

    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-002439
    Date of registration:23.04.2014 / 25.02.2016
    Expiration Date:23.04.2019
    The owner of the registration certificate:FARMSINTEZ, PAO FARMSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp03.04.2018
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