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

    1 tablet contains:

    active substance: ofloxacin 100 mg or 200 mg;

    Excipients: corn starch 37.4 mg, lactose 50.0 mg, magnesium stearate 5.0 mg, talcum powder 10.0 mg, silicon dioxide colloid 2.5 mg, sodium carboxymethyl starch 10.0 mg;

    film sheath: hypromellose 4.9 mg, titanium dioxide 2.45 mg, propylene glycol 0.98 mg.

    Description:

    Round biconvex tablets covered with a film coat of white or almost white color.

    Pharmacotherapeutic group:Antimicrobial agent-fluoroquinolone
    ATX: & nbsp

    S.01.A.E.01   Ofloxacin

    J.01.M.A.01   Ofloxacin

    Pharmacodynamics:

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

    The antimicrobial spectrum includes Gram-positive aerobes: Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (methicillin-sensitive), Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes.

    Gram-negative aerobes: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerobes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri , Providencia stuartii, Pseudomonas aeruginosa (quickly develop resistance), Serratia marcescens.

    Anaerobes: Clostridium perfringens.

    Other: Chlamydia trachomatis, Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophlia, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum. In most cases, they are insensitive: Nocardia asteroides, anaerobic bacteria (incl. Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile), Enterococcus spp., most Streptococcus spp., does not apply to Treponema pallidum.

    Pharmacokinetics:

    Absorption after oral administration is rapid and complete (95%). Bioavailability is over 96%, plasma protein binding is 25%, the time to reach maximum oral intake is 1-2 hours, the maximum concentration after taking 100, 300 and 600 mg is 1 mg / l, 3.4 mg / l and 6.9 mg / L, respectively, and depends on the dose: after a single dose of 200 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; well penetrates the blood-encephalic barrier, the placental barrier, is secreted with the mother's milk. It penetrates into the cerebrospinal fluid (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 microorganisms sensitive to ofloxacin: respiratory tract (bronchitis, pneumonia), LOP-organ (sinusitis, pharyngitis, otitis media, laryngitis,tracheitis); skin, soft tissues; bones, joints; organs of the abdominal cavity and bile ducts, kidneys (pyelonephritis); uncomplicated infections of the lower parts of the urinary tract (cystitis, urethritis); genitals and pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis, colpitis, orchitis, epididymitis); gonorrhea; chlamydia. Prevention of infections in patients with impaired immune status (including neutropenia).

    Contraindications:

    Hypersensitivity to ofloxacin, the components of the drug and other fluoroquinolones, a deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), a reduction in convulsive threshold (including after traumatic brain injury, stroke or inflammatory processes in the central nervous system); age to 18 years, pregnancy, the period of breastfeeding, the defeat of tendons with the previous treatment with fluoroquinolones, lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

    Carefully:Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), chronic renal failure, hepatic insufficiency,organic diseases of the central nervous system, predisposition to convulsive reactions, myasthenia gravis, hepatic porphyria, glucose-6-phosphate dehydrogenase deficiency, diabetes mellitus, congenital interval elongation syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), psychoses and other mental disorders in the anamnesis; simultaneous reception of drugs that extend the interval Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including antihistamines. astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, drugs that lower blood pressure.
    Pregnancy and lactation:Contraindicated.
    Dosing and Administration:

    Inside. The dose is selected individually depending on the location, the severity of the infection, the sensitivity of microorganisms, as well as the general condition of the patient and the function of the liver and kidneys. Adults - 200-800 mg / day, the course of treatment - 7-10 days, the frequency of application - 2 times a day.A dose of up to 400 mg / day can be given in one session, preferably in the morning. With gonorrhea - 400 mg once.

    In patients with impaired renal function (in the case of creatinine clearance 50-20 ml / min) 100-200 mg / day. When creatinine clearance is less than 20 ml / min - 100 mg every 24 hours; with hemodialysis and peritoneal dialysis - 100 mg every 24 hours.

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

    Tablets are taken whole, washed down with water, before or during meals. The duration 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 body temperature. In the treatment of uncomplicated and complicated infections of the lower urinary tract treatment course - 7 and 10 days respectively, with prostatitis - up to 6 weeks, with infections of the pelvic organs - 10-14 days, with infections of the respiratory system and skin - 10 days.

    Side effects:

    From the digestive system: gastralgia, decreased appetite, nausea, vomiting, diarrhea, constipation, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous colitis, dryness of oral mucosa, pharyngitis.

    From the nervous systemheadache, dizziness, impaired coordination of movements, tremor, convulsions, numbness and paresthesia of the extremities, intense dreams, nightmarish dreams, psychotic reactions, anxiety, state of arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure, insomnia, nervousness.

    From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendosinovitis, tendon rupture, pain in the extremities.

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

    From the side of the cardiovascular system: tachycardia, increase or decrease in blood pressure.

    Allergic reactions: skin rash, itching, urticaria, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm, multiforme exudative erythema (including Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell's syndrome), photosensitivity, vasculitis, anaphylactic shock, itching of the external genitalia in women.

    From the skin: pinpoint hemorrhages (petechiae), bullous hemorrhagic dermatitis, papular rash with cortex, indicative of vascular lesions (vasculitis).

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

    From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininaemia, increased urea, dysuria, urinary retention.

    Other: intestinal dysbacteriosis, superinfection, hypoglycemia (in patients with diabetes mellitus), vaginitis, chest pain, fatigue, asthenia, general weakness, vaginal discharge, epistaxis, thirst, weight loss.
    Overdose:

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

    Treatment - gastric lavage, symptomatic therapy. Hemodialysis and peritoneal dialysis are not effective.

    Interaction:

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

    Increases the concentration of glibenclamide in blood plasma.

    Increases serum concentration of cyclosporine.

    Cimetidine, furosemide, methotrexate and drugs that block tubular secretion, decrease the loss of ofloxacin and, thus, increase the risk of toxic effects.

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

    In the case of the appointment with hypoglycemic agents, both hypo- and hyperglycemia are possible, and therefore it is necessary to monitor the concentration of glucose in the blood plasma.

    When administered with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium hydrogen carbonate), the risk of crystalluria and nephrotoxic effects increases.

    With concurrent administration with glucocorticosteroids, the risk of rupture of the tendon increases, especially in elderly patients.

    At appointment with indirect anticoagulants it is necessary to carry out the control of coagulating system of blood.

    Foods, antacid preparations and multivitamin preparations that contain salts of aluminum, calcium, magnesium, zinc and iron form insoluble chelate complexes with ofloxacin and, thus,its absorption. Therefore, the time interval between taking these drugs and ofloxacin should be at least 2 hours.

    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 be exposed to sunlight, ultraviolet rays (mercury quartz lamps, solarium) during treatment.

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

    For the prevention of hyperconcentration of urine and subsequent crystalluria during the treatment period, it is necessary to pay attention to adequate hydration of the body.

    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 vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, can not be consumed ethanol.
    Form release / dosage:

    Tablets, film-coated, 100 mg and 200 mg.

    Packaging:
    10 tablets in a contour mesh PVC / aluminum package (blister). 1 or 2 blisters in a cardboard box with instructions for medical use.
    Storage conditions:

    Store in a dry, 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 expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000271
    Date of registration:17.02.2011
    Expiration Date:17.02.2016
    The owner of the registration certificate:Protek Biosystems Pvt. Ltd.Protek Biosystems Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspProtekh Biosystems Pvt.LtdProtekh Biosystems Pvt.LtdRussia
    Information update date: & nbsp18.06.2017
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