Lomefloxacin (Lomefloxacine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLomefloxacinLomefloxacin
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    • Dosage form: & nbsptfilm-covered laths
    Composition:

    Active substance: Lomefloxacin hydrochloride in terms of Lomefloxacin 0.4 g;

    Excipients: cellulose microcrystalline, potato starch silicon dioxide colloid, copovidone (Kollidon VA-64), calcium stearate, talc.

    Opadrai II (series 85): polyvinyl alcohol, macrogol, titanium dioxide E 171, talc.
    Description:Round, biconvex tablets, covered with a film coat of white color. Type of tablets on a break: from almost white to light yellow color.
    Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone
    ATX: & nbsp

    J.01.M.A   Fluoroquinolones

    J.01.M.A.07   Lomefloxacin

    Pharmacodynamics:

    Antimicrobial bactericide of broad spectrum of action from the group of fluoroquinolones.Affects the bacterial enzyme DNA-gyrase, which provides supercoiling, forms a complex with its tetramer (subunit of gyrase A2B2) and disrupts transcription and replication of DNA, leads to the death of the microbial cell.

    Beta-lactamases, produced by pathogens, do not affect the activity of lomefloxacin.

    Active in relation to:

    - Gram-negative aerobic microorganisms: Citrobacter diversus, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa (only for urinary tract infections);

    - Gram-positive aerobic microorganisms: Staphylococcus saprophyticus.

    With a minimum inhibitory concentration of 2 μg / ml, it is active against the following microorganisms (however, clinical efficacy in infections caused by these microorganisms has not been studied in strictly controlled studies):

    - Gram-positive aerobic microorganisms: Staphylococcus aureus (including methicillin-resistant strains), Staphylococcus epidermidis (including methicillin-resistant strains);

    - Gram-negative aerobic microorganisms: Aeromonas hydrophila, Citrobacter freundii, Enterobacter aerogenes, Enterobacter agglomerans, Haemophilus parainfluenzae, Hafnia alvei, Klebsiella oxytoca, Klebsiella ozaenae, Morganella morganii, Proteus vulgaris, Providencia alcalifaciens, Providencia rettgeri, Serratia liquefaciens, Serratia marcescens;

    - other microorganisms: Legionella pneumophila.

    The drug is stable: A, AT, D and G group of streptococcus, Streptococcus pneumoniae, Pseudomonas cepacia, Ureaplasma urealyticum, Mycoplasma hominis and anaerobic bacteria.

    It acts both on the outside and on the intracellularly located Mycobacterium tuberculosis, reduces the time of their isolation from the body, provides a faster resolution of infiltrates.

    Most microorganisms act at low concentrations (the concentration necessary to control the growth of 90% of strains, usually not more than 1 μg / ml).

    Resistance is rare.

    Pharmacokinetics:

    Absorption - 95-98%; food intake reduces absorption by 12%. Time to reach the maximum concentration in blood plasma is 0.8-1.5 hours. The maximum concentration in the blood plasma after ingestion of 100 mg is 0.8 μg / ml, 200 mg - 1.4 μg / ml, 400 mg - 3- 5.2 μg / ml. The intake of food reduces the maximum concentration in the blood plasma by 18% and increases the time to reach the maximum concentration in the blood plasma to 2 hours. The equilibrium concentration in the blood plasma is determined after 48 hours. The connection with plasma proteins is 10%. It penetrates well into the organs and tissues (respiratory tract, ENT organs, soft tissues, bones, joints, abdominal cavity organs, pelvis, genitalia), where the concentration of lomefloxacin is 2-7 times higher than in plasma.

    A small part of the drug undergoes metabolism with the formation of metabolites. The half-life is 8-9 hours; the average renal clearance is 145 ml / min.In elderly patients, plasma clearance is reduced by 25%. With a decrease in creatinine clearance to 10-40 ml / min / 1.73 m2, the elimination half-life increases.

    The kidneys produce 70-80% of the tubular secretion (mostly unchanged, 9% - in the form of glucuronides, 0.5% - in the form of other metabolites); through the intestine - 20-30%.

    Indications:

    Uncomplicated urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis or Staphylococcus saprophyticus.

    Complicated urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Citrobacter diversus or Enterobacter cloacae.

    Prevention of urinary tract infections with transrectal biopsy of the prostate gland, transurethral operative interventions.

    Exacerbation of chronic bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis.

    Tuberculosis of lungs (as part of complex therapy): extensive caseous necrotic tissue damage, pronounced nonspecific component of inflammation, drug resistance of mycobacteria to rifampicin, or poor tolerance of rifampicin.

    Contraindications:

    Hypersensitivity (including other fluoroquinolones), with creatinine clearance less than 30 ml / min, pregnancy, lactation period, age of 18 years (period of formation and growth of the skeleton).

    Carefully:

    Cerebral atherosclerosis, epilepsy, etc.diseases of the central nervous system with epileptic syndrome, lengthening of the interval QT, hypokalemia, simultaneous reception of antiarrhythmic drugs IA class (quinidine, procainamide) and III class (amiodarone, sotalol).

    Dosing and Administration:

    Inside (regardless of food intake, squeezed a sufficient amount of liquid), 1 time per day.

    The dose and duration of treatment depends on the severity of the disease and the sensitivity of the pathogen.

    Uncomplicated cystitis in women caused by Escherichia coli: 400 mg / day for 3 days.

    Uncomplicated cystitis caused by Klebsiella pneumoniae, Proteus mirabilis or Staphylococcus saprophyticus: 400 mg / day for 10 days.

    Complicated urinary tract infections: 400 mg / day for 14 days.

    Exacerbation of chronic bronchitis: 400 mg / day for 14 days.

    Prevention of urinary tract infections: with transrectal biopsy of the prostate - 400 mg once for 1-6 h before the procedure; transurethral surgery - 400 mg once 2 to 6 hours before surgery.

    Tuberculosis: at 400 mg / day, for 14-28 days or more.

    Side effects:

    From the digestive system: nausea, vomiting, dry mouth, gastralgia, abdominal pain, diarrhea or constipation, flatulence,pseudomembranous enterocolitis, dysphagia, discoloration of the tongue, decreased appetite or bulimia, taste distortion, dysbiosis, increased activity of "liver" transaminases.

    From the nervous system: fatigue, malaise, asthenia, headache, dizziness, fainting, insomnia, hallucinations, convulsions, hyperkinesia, tremor, paresthesia, nervousness, anxiety, depression, agitation.

    From the genitourinary system: glomerulonephritis, dysuria, polyuria, anuria, albuminuria, urethral bleeding, crystalluria, hematuria, urinary retention, edema; in women - vaginitis, leukorrhea, intermenstrual bleeding, pain in the perineum, vaginal candidiasis; in men - orchitis, epididymitis.

    From the side of metabolism: hypoglycemia, gout.

    From the side of the musculoskeletal system: arthralgia, vasculitis, convulsions gastrocnemius muscles, pain in the back and chest.

    On the part of the organs of hematopoiesis and the system of hemostasis: bleeding from the organs of the gastrointestinal tract, thrombocytopenia, purpura, increased fibrinolysis, epistaxis, lymphadenopathy.

    From the respiratory system: dyspnea, bronchospasm, cough, hypersecretion of phlegm, influenza-like symptoms.

    From the sense organs: visual impairment, pain and noise in the ears, pain in the eyes.

    From the side of the cardiovascular system: lowering blood pressure, tachycardia, bradycardia, extrasystole, arrhythmias, progression of heart failure and angina pectoris, pulmonary embolism, myocardiopathy, phlebitis.

    Allergic reactions: itching, hives, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome).

    Influence on the fetus: in the experiment fetotoxic action (arthropathy) is described.

    Other: Candidiasis, increased sweating, chills, thirst, superinfection.

    Overdose:

    Treatment: induction of vomiting or gastric lavage, adequate hydration, symptomatic therapy. Hemo- and peritoneal dialysis with an overdose is ineffective (less than 3% is output).

    Interaction:

    Does not affect the pharmacokinetics of isoniazid.

    Does not interact with theophylline, caffeine.

    Increases the activity of oral anticoagulants and increases the toxicity of non-steroidal anti-inflammatory drugs.

    Do not take antacid medicines and sucralfate for 4 hours before and 2 hours after taking Lomefloxacin (forms with them chelate compounds, which reduces its bioavailability).

    In the treatment of patients with tuberculosis lomefloxacin use in conjunction with isoniazid, pyrazinamide, streptomycin and ethambutol (not recommended combination with rifampicin - antagonism).

    Drugs that block tubular secretion slow down excretion.

    There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, co-trimoxazole, metronidazole.

    Vitamins with mineral supplements should be used 2 hours before or 2 hours after the application of Lomefloxacin.

    Special instructions:

    With cirrhosis of the liver, there is no need for correction of the dosing regimen (with normal kidney function).

    During the treatment period, prolonged exposure to sunlight and the use of artificial UV radiation should be avoided (evening reception reduces the risk of reaction to UV radiation). At the first signs of photosensitivity (increased skin sensitivity, burn, hyperemia, swelling, the appearance of blisters, rashes, itching, dermatitis) or hypersensitivity,manifestations of neurotoxicity (agitation, convulsions, tremor, photophobia, confusion, toxic psychosis, hallucinations) therapy should be discontinued.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets, film-coated, 400 mg.

    Packaging:

    10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil. ,

    1 or 2 contour mesh packages together with the instruction for use are placed in a bundle.

    Storage conditions:

    Keep in dry the dark place at a temperature of no higher than 25 FROM.

    Keep out of the reach of children

    Shelf life:

    2 of the year.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005123/08
    Date of registration:01.07.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Information update date: & nbsp02.04.2018
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