Active substanceOfloxacinOfloxacin
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Active substance:

    Ofloxacin - 200 mg;

    Excipients:

    lactose (milk sugar); corn starch; giprolase

    (hydroxypropylcellulose); sodium carboxymethyl starch (primogel); magnesium stearate.

    Sheath:

    hypromellose (hydroxypropylmethylcellulose); povidone; Macrogol-6000 (polyethylene glycol-6000); titanium dioxide.

    Description:

    The tablets covered with a film cover, white or white with a yellowish shade of color. The color of the tablet on the break is white or white with a yellowish tinge.

    Pharmacotherapeutic group:antimicrobial agent-fluoroquinolone
    ATX: & nbsp

    S.01.A.E.01   Ofloxacin

    J.01.M.A.01   Ofloxacin

    Pharmacodynamics:

    The broad-spectrum antimicrobial agent from the group of fluoroquinolones acts on the bacterial DNA-gyrase enzyme, which provides super-convolution and thus the stability of bacterial DNA (the destabilization of DNA chains leads to their death). Has a bactericidal effect.

    It is active against microorganisms producing beta-lactamase and fast-growing atypical mycobacteria. Sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitides, Escherichia coli, Citrobacter spp., Klebsiella spp., (including Klebsiella pneumoniae), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indole-positive and indole-negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia eterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chiamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Moraxella tarrhalis, Propionibacterium acnes, Pseudomonas spp., Brucella spp.

    Different sensitivity to the drug has: Enterococcus faecal is, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serratia marcescens. Pseudomonas aeruginosa, Acinetobacter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium pneumoniae, Mycobacterium, tuberculosis, and Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

    In most cases, they are insensitive: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.

    Pharmacokinetics:

    Absorption after oral administration is rapid and complete (95%). Bioavailability is over 96%, the connection with plasma proteins is 25%. Time to reach the maximum concentration (TCmah) for oral administration - 1-2 hours. After a single dose of 200 mg and 400 mg, it is 2.5 μg / ml and 5 μg / ml, respectively. Food can slow absorption, but does not have a significant effect on bioavailability.

    Apparent volume of distribution - 100 liters. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, the secret of the prostate gland, penetrates well through the blood-brain barrier, the placental barrier, is secreted with the mother's milk. Penetrates into cerebrospinal fluid with inflamed and non-inflamed meninges (14-60%).

    Metabolized in the liver (about 5%) with formation NOxygen ofloxacin and dimethylfloxacin. The half-life is 4,5-7 hours (regardless of the dose). It is excreted by the kidneys - 75-90% (unchanged), about 4% - with bile. The extrarenal clearance is less than 20%.

    After a single application in a dose of 200 mg in urine is detected within 20-24 hours. In renal / hepatic insufficiency, excretion can be slowed down. Do not cumulate. With hemodialysis, 10-30% of the drug is removed.

    Indications:

    Infectious-inflammatory diseases caused by sensitive microorganisms: respiratory tract infections (bronchitis, pneumonia),ENT organs (sinusitis, pharyngitis, otitis media, laryngitis); skin, soft tissues; bones, joints; Infectious and inflammatory diseases of the abdominal cavity and bile ducts (with the exception of bacterial enteritis); kidneys (pyelonephritis), urinary tract (cystitis, urethritis), pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis); genital organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia; prevention of infections in patients with impaired immune status (including neutropenia).

    Contraindications:

    Hypersensitivity to ofloxacin and other fluoroquinolones, deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), reduction of convulsive threshold (including after cerebrospinal trauma, stroke or inflammatory processes in the central nervous system); age of 18 years (until the skeleton has been completed), pregnancy, lactation, renal dysfunction (with creatinine clearance less than 50 ml / min).

    Carefully:

    atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), chronic renal failure, organic lesions of the central nervous system.

    Pregnancy and lactation:contraindicated
    Dosing and Administration:

    Inside. Doses are selected individually depending on the localization and severity of the infection, as well as the sensitivity of microorganisms, the general condition of the patient and the function of the liver and kidneys.

    Adults-200-800 mg per day. A dose of up to 400 mg / day can be given in one session, preferably in the morning. A dose of over 400 mg / day should be divided into 2 divided doses with an equal time interval.

    With gonorrhea - 400 mg once.

    The maximum daily dose for liver failure is 400 mg / day.

    Tablets should be taken whole, washed down with water before and during meals. The duration of the course of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should continue for at least 3 more days after the disappearance of the symptoms of the disease and complete normalization of temperature. In the treatment of salmonellosis treatment course - 7-8 days, with uncomplicated infections of the lower urinary tract treatment course - 3-5 days.

    Side effects:

    From the gastrointestinal tract: gastralegia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

    From the nervous system: decreased reaction rate, headache, dizziness, sleep disturbance, general weakness; in some cases - uncertainty of movements, tremor, muscle cramps, numbness and paresthesia in the limbs, "nightmarish" dreams, psychotic reactions, anxiety, arousal, fear, depression, confusion, visual and auditory hallucinations, impaired coordination, increased intracranial pressure .

    From the musculoskeletal system: tendonitis, myalgia, arthralgia,

    tendosynovitis, tendon rupture.

    From the sense organs: diplopia, violation of color perception, violation of taste, smell, hearing.

    From the cardiovascular system: tachycardia, lowering blood pressure.

    Allergic reactions: skin rash, itching, urticaria, angioedema, allergic nephritis, allergic pneumonitis, eosinophilia, bronchospasm, weakness, anaphylactic shock, multiforme exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Leyella's syndrome), purpura, fever.

    From the skin: spot hemorrhages (petechiae), dermatitis bullous hemorrhagic,papular rash with a cortex, indicating the defeat of blood vessels (vasculitis).

    On the part of the hematopoiesis system: leukopenia, agranulocytosis, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

    From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininemia, increased urea levels.

    Other: dysbacteriosis, superinfection, hypoglycemia (in patients with diabetes mellitus), photosensitivity, vaginitis.

    Overdose:

    Symptoms: dizziness, confusion, inhibition, disorientation, drowsiness, vomiting.

    Treatment: gastric lavage, symptomatic therapy. With hemodialysis, 10-30% of the drug is removed.

    Interaction:

    Food products, antacids containing aluminum, calcium, magnesium or iron salts, reduce the absorption of ofloxacin, forming insoluble complexes (the time interval between administration of these drugs should be at least 2 hours).

    Reduces the clearance of theophylline by 25 % (with simultaneous use should reduce the dose of theophylline).

    Cimetidine, furosemide, methotrexate and drugs that block tubular secretion - increase the concentration of ofloxacin in plasma.

    Increases the concentration of glibenclamide in plasma.

    At simultaneous admission with antagonists of vitamin K, it is necessary to control the blood coagulation system.

    When administered with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines, the risk of neurotoxic effects increases.

    At simultaneous appointment with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

    When administered with drugs that alkalinize urine (inhibitors of craboanhydrase, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

    Special instructions:

    It is not a drug of choice for pneumonia caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

    It is not recommended to use more than 2 months, exposed to sunlight, ultraviolet rays (mercury-quartz lamps, solarium).

    In the event of side effects from the central nervous system, allergic reactions, pseudomembranous colitis, drug withdrawal is necessary.With pseudomembranous colitis, confirmed colonoscopically and / or histologically, oral administration of vancomycin and metronidazole is indicated.

    Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon), especially in elderly patients. When

    the appearance of signs of tendonitis, it is necessary to immediately stop treatment, to make an immobilization of the Achilles tendon and consult an orthopedist.

    When using the drug, women are not recommended to use tampons, due to the increased risk of thrush development.

    Against the backdrop of treatment, myasthenia flow may worsen, and porphyria attacks may be more frequent in predisposed patients.

    Can lead to false-negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation Mycobacterium tuberculosis).

    In patients with impaired liver and kidney function, it is necessary to monitor the concentration of ofloxacin in plasma. In severe renal and hepatic insufficiency, the risk of toxic effects increases (dose adjustment is required).


    Effect on the ability to drive transp. cf. and fur:During the period of treatment 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, one should not use ethanol.
    Form release / dosage:

    Tablets, film-coated, 200 mg.

    Packaging:

    For 10 or 20 tablets in a dark glass jar for drug storage, sealed with a plastic stopper with a sealing element.

    For 10 or 20 tablets in cans of polymeric with screw caps.

    For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    Each can, 1 or 2 contiguous cells packs of 10 tablets, 1 circuit pack of 20 tablets together with the instructions for use are placed in a pack of cardboard.

    Storage conditions:

    List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the date shown on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N000735 / 01
    Date of registration:08.08.2008
    The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspBRYNTSALOV-A, CJSCBRYNTSALOV-A, CJSC
    Information update date: & nbsp08.08.2008
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