Active substanceOfloxacinOfloxacin
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  • Dosage form: & nbspsolution for infusions
    Composition:

    100 ml of the solution contain

    Active substance: ofloxacin 200 mg;

    Excipients: sodium chloride, water for injection.

    Description:

    A clear solution of light yellow color.

    Pharmacotherapeutic group:Antimicrobial agent-fluoroquinolone
    ATX: & nbsp

    S.01.A.E.01   Ofloxacin

    J.01.M.A.01   Ofloxacin

    Pharmacodynamics:

    Antimicrobial agent of a broad spectrum of action of a group of fluoroquinolones. The mechanism of action is due to the inhibition of the bacterial DNA-gyrase enzyme involved in the formation of the spatial structure of the DNA molecule upon its replication: DNA gyrase catalyzes negative supercoilingstrands of DNA. Inhibition of DNA gyrase disrupts the growth and division of the bacterial cell, which leads to its death.

    In vitro and in vivo ofloxacin is active against the following microorganisms:

    Citrobacter spp., Bordetella pertussis, Brucella spp., Enterobacter spp, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris (indole-positive and indole-negative), Propionibacterium acnes, Salmonella spp., Shigella spp., Hafhia alvei, Campylobacter jejuni, Yersinia spp., Aeromonas spp., Vibrio spp., Serratia spp., Staphylococcus spp. (methicillin-sensitive strains.

    Different sensitivity to the drug has:

    Enterococcus faecalis, Streptococcus pyogenes, pneumoniae and viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, 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., Eubacter spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.

    Pharmacokinetics:

    After a single 60-minute intravenous infusion of 200 mg ofloxacin, the mean maximum plasma concentration is 2.7 μg / ml; 12 hours after the administration, the concentration is 0.3 μg / ml. Equilibrium concentrations are achieved after the administration of four doses.

    The mean peak and minimum equilibrium concentrations are achieved after intravenous administration of 200 mg ofloxacin every 12 hours for 7 days and are 2.9 and 0.5 μg / ml, respectively. Ofloxacin widely penetrates into many liquids and tissues of the body, including saliva, bronchial secretions, bile, tear and spinal fluid (14-60%), pus, into the lungs, prostate gland, skin; well penetrates the placental barrier, is secreted with the mother's milk.

    Binding to plasma proteins is 20-25%. The half-life of ofloxacin is 6-7 hours. Ofloxacin is subject to partial (5%) metabolism in the liver. Up to 80% of the ingested drug is excreted by the kidneys unchanged, a small part of the active substance is also excreted through the gastrointestinal tract. With hemodialysis, 10-30% of the drug is removed.

    In patients with impaired renal function (creatinine clearance 50 ml or less), the half-life of ofloxacin increases.

    Indications:

    Respiratory tract infections (bronchitis, pneumonia), LOP-organov (sinusitis, pharyngitis, otitis, laryngitis), skin, soft tissue, bone, joints, infectious and inflammatory diseases of the abdominal cavity and biliary tract, kidney (pyelonephritis), urinary tract infections (cystitis, urethritis), pelvic organs (endometritis , salpingitis, oophoritis, cervicitis, parametritis, prostatitis), sex organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia; septicemia, meningitis; prevention of infections in patients with impaired immune status (including neutropenia).

    Contraindications:

    Hypersensitivity, deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), reduction of convulsive threshold (including after craniocerebral trauma, stroke or inflammatory processes in the central nervous system); age to 18 years (until the growth of the skeleton is completed), pregnancy, lactation.

    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:
    Intravenously drip. 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.

    Intravenous drip introduction begins with a single dose of 200 mg, which is injected slowly for 30-60 minutes. When the patient's condition is improved, they are transferred to oral intake of the drug at the same daily dose.

    Urinary tract infections - 100 mg 1-2 times a day, infections of the kidneys and genitals - from 100 mg twice a day to 200 mg twice a day, respiratory tract infections, as well as LOP-organ, skin and soft tissue infection, bone and joint infections, abdominal infection, septic infections - 200 mg 2 times a day. If necessary, increase the dose to 400 mg twice a day.

    For the prevention of infections in patients with a marked decrease in immunity - 400-600 mg / day.

    If necessary, drip intravenously - 200 mg in a 5% solution of glucose. Use only freshly prepared solutions.

    In patients with impaired renal function (when creatinine clearance is 50-20 ml / min), a single dose should be 50% of the average dose with a multiplicity of 2 times a day, or a full single dose is administered once a day. With CC less than 20 ml / min, the first dose is 200 mg, then 100 mg per day every other day.

    With hemodialysis and peritoneal dialysis - 100 mg every 24 hours. The maximum daily dose for liver failure is 400 mg / day.

    Side effects:

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

    From the nervous system: headache, dizziness, motion uncertainty, tremor, convulsions, numbness and paresthesia of the limbs, intense dreams, nightmarish dreams, psychotic reactions, anxiety, psychomotor agitation, phobias, depression, confusion, hallucinations, increased intracranial pressure.

    From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendosynovitis, tendon rupture.

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

    From the side of the cardiovascular system: tachycardia, lowering blood pressure (with intravenous administration, with a sharp decrease in blood pressure, the introduction is discontinued), vasculitis, collapse.

    Allergic reactions: skin rash, itchy skin, hives, allergic pneumonitis, allergic nephritis, eosinophilia, fever, Quincke's edema, bronchospasm, Stevens-Johnson syndrome and Lyell, multiform exudative erythema, anaphylactic shock.

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

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

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

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

    Local Reactions: pain, redness at the injection site, thrombophlebitis.

    Overdose:

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

    Treatment symptomatic therapy. Hemodialysis and peritoneal dialysis are not effective.

    Interaction:

    Compatible with the following infusion solutions: isotonic sodium chloride solution, Ringer's solution, 5% a solution of fructose, 5% solution of dextrose.

    Do not mix with heparin (risk of precipitation).

    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 carbonic anhydrase, 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, be 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. In case of signs of tendinitis, it is necessary to immediately stop treatment, to make an immobilization of the Achilles tendon and consult an orthopedist.

    During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require increased concentration and speed psychomotor reactions, can not be used ethanol.

    When using the drug, women are not recommended to use hygiene 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 or 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 treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require increased concentration and speed psychomotor reactions, can not be used ethanol.

    Form release / dosage:

    Solution for infusion 2 mg / ml.

    Packaging:For 100 ml in a sterile bottle of polyethylene. For 1 bottle in a polypropylene bag, then in a pack of cardboard along with instructions for use.
    Storage conditions:

    In a place protected from light, the temperature should not exceed 25 ° С. Do not freeze. Keep out of the reach of children.

    Shelf life:3 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002613/07
    Date of registration:07.09.2007 / 11.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Protek Biosystems Pvt. Ltd.Protek Biosystems Pvt. Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp18.06.2017
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