Clinical and pharmacological group: & nbsp

Quinolones / fluoroquinolones

Included in the formulation
  • Combiflox
    pills inwards 
  • АТХ:

    J.01.R.A.09   Ofloxacin and ornidazole

    Pharmacodynamics:

    Ornidazole. The 5-nitroimidazole derivative. Many anaerobic bacteria and microaerophilic intracavitary parasites have a high negative redox potential. When exposed to microorganisms the enzyme systems of these pathogens reduce the nitro group of ornidazole (the nitro group of the molecule of ornidazole is an electron acceptor). Refurbished ornidazole is built into the respiratory chain of protozoa and anaerobes, preventing the action of flavoproteins - carriers of electrons. As a result, respiratory processes are violated, which leads to cell death. In addition, in some species of anaerobes and protozoa in the reduction of the nitro group ornidazole promotes the formation of free radicals that damage DNA.

    The drug is active against Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica, as well as some anaerobic bacteria (Bacteroides spp., Clostridium spp., Fusobacterium, Helicobacter pylori, anaerobic cocci).

    Ofloxacin. A synthetic antibacterial preparation of a broad spectrum of action from the group of fluoroquinolones. Suppresses bacterial DNA-gyrase and / or topoisomerase IV.

    Ofloxacin inhibits DNA-gyrase (topoisomerase type II of gram-negative microorganisms) and topoisomerase of Gram-positive bacteria.As a result, it disrupts supercoiling and cross-linking of DNA gaps, suppresses DNA synthesis, ninterrupts the processes of replication, transcription and DNA repair, causes deep morphological changes in the cytoplasm, cell wall and membranes of sensitive microorganisms.

    Active with respect to Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus pneumoniae, Streptococcus pyogenes, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerogenes, 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, Serratia marcescens, Clostridium perfringens, Chlamydia trachomatis, Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Nocardia asteroides, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile, Enterococcus spp., Streptococcus spp., does not apply to Treponema pallidum.

    Pharmacokinetics:

    Rapidly absorbed from the gastrointestinal tract, binding to plasma proteins by 15% in ornidazole, 25% for ofloxacin.

    Ornidazole penetrates the blood-brain barrier, half-life period is 13 hours, is excreted by the kidneys (60-70%) and gastrointestinal tract (20-25%), of which 5% in an unmodified form.

    Ofloxacin is metabolized in the liver, elimination half-life is 12-14 h, is excreted by the kidneys and gastrointestinal tract. Cumulates.

    Indications:

    Mixed bacterial infections and infectious-inflammatory processes organs of the abdominal cavity and bile ducts,kidneys (pyelonephritis), lower urinary tract (cystitis, urethritis), genital organs and pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis, colpitis, orchitis, epididymitis) caused by sensitive microorganisms.

    XIV.N10-N16.N10   Acute tubulointerstitial nephritis

    XIV.N10-N16.N11   Chronic tubulointerstitial nephritis

    XIV.N30-N39.N30   Cystitis

    XIV.N30-N39.N34   Urethritis and urethral syndrome

    XIV.N40-N51.N41   Inflammatory diseases of the prostate

    XIV.N40-N51.N45   Orchitis and epididymitis

    XIV.N70-N77.N70   Salpingitis and oophoritis

    XIV.N70-N77.N71   Inflammatory diseases of the uterus, except the cervix

    XIV.N70-N77.N72   Inflammatory disease of the cervix

    XIV.N70-N77.N73.0   Acute parametritis and pelvic cellulite

    Contraindications:

    • Epilepsy (including in the anamnesis).
    • The defeat of the tendons with the previous treatment with fluoroquinolones.
    • Pregnancy.
    • Hypersensitivity.
    • Decreased convulsive threshold (including after traumatic brain injury, stroke or inflammatory processes in the central nervous system).
    • Age to 18 years.
    • Breastfeeding period.

    Carefully:

    Atherosclerosis of cerebral vessels, cerebral circulation disorders (in anamnesis).

    Diseases of the liver.

    Predisposition to convulsive reactions.

    Hepatic porphyria.

    Diabetes.

    Syndrome of congenital lengthening of the interval Q-T.

    Psychoses and other mental disorders in the anamnesis.

    Electrolyte imbalance.

    Alcoholism.

    Chronic renal failure.

    Organic diseases of the central nervous system (including multiple sclerosis).

    Myasthenia gravis.

    Deficiency of glucose-6-phosphate dehydrogenase.

    Diseases of the heart.

    Simultaneous reception of drugs that extend the interval Q-T, funds for general anesthesia from the barbiturate group, drugs that reduce blood pressure.

    The age is over 65.

    Pregnancy and lactation:

    The FDA category is not defined. The drug is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Orally 1 hour before meals or 2 hours after meals. 1 tablet contains ofloxacin 200 mg, ornidazole 500 mg. 2 times a day, the course of treatment is 7-10 days.

    With kidney diseases: creatinine clearance of 20-50 ml per minute - 200 mg (calculation of ofloxacin) per day, creatinine clearance less than 20 ml per minute - hemodialysis or peritoneal dialysis - 200 mg (calculation of ofloxacin) 1 time in 2 days.

    In liver diseases: the maximum daily dose contains 400 mg ofloxacin.

    Side effects:

    From the gastrointestinal tract: gastralgia, nausea, diarrhea, flatulence, increased activity of "liver" transaminases,cholestatic jaundice, pseudomembranous colitis, colitis (including hemorrhagic), decreased appetite, vomiting, constipation, abdominal pain, hyperbilirubinemia, dryness of the oral mucosa, hepatitis.

    From the cardiovascular system: tachycardia, collapse, ventricular arrhythmia, including arrhythmia, ventricular tachysystolic type "pirouette", increase or decrease in blood pressure, lengthening of the interval QT.

    From the side of the nervous system: headache, insomnia, nervousness, tremor, convulsions, numbness and paresthesia of the limbs, intense dreams, anxiety, arousal, depression, hallucinations, increased intracranial pressure, insomnia, nervousness, epileptic seizures, extrapyramidal disorders, sensory or sensory peripheral neuropathy, impaired coordination of movement, violation of color perception, taste disorders, impaired sense of smell, hearing and balance, dizziness, lack of confidence in movements, nightmares ", dreams, phobias, confusion, drowsiness, psychotic reactions with suicidal tendencies, temporary loss of consciousness, diplopia, perversion of taste sensations,

    From the musculoskeletal system: tendonitis, arthralgia, tendosinovitis, pain in the extremities, rhabdomyolysis, myalgia, tendon rupture, muscle stiffness, muscle weakness.

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

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

    On the part of the skin: pinpoint hemorrhages (petechiae), papular rash with a cortex, indicating a vascular lesion (vasculitis), bullous hemorrhagic dermatitis.

    From the side of the urinary system: acute interstitial nephritis, hypercreatininaemia, dysuria, acute renal failure, impaired renal function, increased urea concentration, urinary retention,

    Other: intestinal dysbacteriosis, hypoglycemia (in patients with diabetes mellitus), chest pain, asthenia, photosensitivity, nosebleeds, thirst, pharyngitis, dry cough, superinfection, vaginitis, fatigue, general weakness, vaginal discharge, weight loss, rhinitis, acute porphyria (in patients with porphyria).

    Overdose:

    • Dizziness.
    • Inhibition.
    • Drowsiness.
    • Epileptiform cramps.
    • Peripheral neuritis.
    • Confusion of consciousness.
    • Disorientation.
    • Vomiting.
    • Depression.

    Treatment is symptomatic (diazepam with cramps), gastric lavage.

    Interaction:

    Ornidazole:

    Simultaneous reception of anticoagulants coumarinovogo number can lead to increased bleeding.

    The drug is compatible with ethanol.

    Vecuronium bromide is the prolongation of myorelaxing action.

    Ofloxacin:

    The drug reduces the clearance of theophylline by 25%, increases the concentration of glibenclamide in plasma, increases the serum concentration of cyclosporine.

    Simultaneous reception with glucocorticosteroids increases the risk of rupture of the tendon, especially in elderly patients.

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

    When taken concomitantly with drugs that lengthen the interval QT (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, some antihistamines, including astemizole, terfenadine, ebastine) is the extension of the interval QT.

    Food products, antacids containing ions of 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).

    Drugs that alkalinize urine (inhibitors of carbonic anhydrase, citrates, sodium hydrogen carbonate) - the risk of crystalluria and nephrotoxic effects.

    Preparations that block calcium secretion (cimetidine, furosemide, methotrexate) - increased concentration of ofloxacin in the blood.

    Special instructions:

    At the time of taking the drug women should not use tampons - the risk of thrush.

    Can lead to a false-negative test result for tuberculosis.

    It is not compatible with the means that inhibit peristalsis.

    It is not recommended to be exposed to sunlight, ultraviolet rays (mercury quartz lamps, solarium).

    To prevent the hyperconcentration of urine and subsequent crystalluria during treatment, it is recommended to conduct adequate hydration.

    In the event of side effects from the central nervous system, allergic reactions, pseudomembranous colitis, the development of peripheral neuropathy symptoms, it is necessary to cancel the drug.

    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 immediately to stop treatment, to immobilize the Achilles tendon and consult an orthopedist. During the period of treatment can not be consumed ethanol.

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

    With simultaneous application with drugs that extend the interval QT (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, some antihistamines, including astemizole, terfenadine, ebastine), systematic ECG monitoring is necessary.

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

    When using the drug, both on the background of taking and 2-3 weeks after discontinuation of treatment, it is possible to develop diarrhea caused by Clostridium difficile (pseudomembranous colitis). In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole.

    Impact on the ability to drive vehicles and manage mechanisms

    Be careful.

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