Lomefloksatsin

General characteristics. Structure:

Active ingredient: 400,0 mg of a lomefloksatsin.

Excipients: starch corn, cellulose microcrystallic, sodium stearate, colloid silicon dioxide, EDTA sodium, diamond blue glikolit starch, talc, magnesium.

Antimicrobic ftorkhinolonovy means with pronounced bactericidal properties of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. An antimicrobic microbicide of a broad spectrum of activity from group of ftorkhinolon (the second generation). Influences bacterial DNK-girazu enzyme, the providing superspiralling, forms a complex with its tetramer (A2B2 giraza subunit) and breaks a transcription and DNA replication, leads to death of a microbic cell. It is highly active concerning gram-negative aerobic microorganisms. Affects both on out of - and intracellularly located Mycobacterium tuberculosis, reduces terms of their allocation from an organism, provides more bystry rassasyvaniye of infiltrates. Affects the majority of microorganisms in low concentration. Resistance develops seldom.

Pharmacokinetics. Drug is well soaked up. Cmax is reached in 0.8-1.5 h. Communication with proteins of plasma - 10%. Well gets into bodies and fabrics (airways, ENT organs, soft tissues, bones, joints, abdominal organs, a small pelvis, a genitalia) where concentration of a lomefloksatsin is 2-7 times higher, than in plasma. An insignificant part of drug is exposed to metabolism with formation of metabolites. An elimination half-life - 8-9 h; average renal clearance - 145 ml/min. At decrease in KK to 10-40 ml/min. the elimination half-life increases. It is removed by kidneys by canalicular secretion to 70-80%, through intestines – 20-30%.

Indications to use:

Tuberculosis: as a part of complex therapy for patients with allocation of MBT steady against an isoniazid and rifampicin (MLU), sharply progressing forms, including concerning strains of MBT sensitive to antitubercular drugs; and also in the empirical modes of chemotherapy. Infections of urinary tract (including prevention before transurethral surgeries): cystitis, pyelonephritis, urethritis, prostatitis; GIT (dysentery, typhoid, salmonellosis, cholera) and biliary tract; infections of a respiratory organs (including exacerbation of chronic bronchitis); purulent infections of skin and soft tissues, contaminated wounds, burns. Osteomyelitis. Gonorrhea, clamidiosis (including Chlamidia conjunctivitis also blefarokonjyunktivit).

Route of administration and doses:

Inside (regardless of meal, washing down with enough liquid), 1 time a day.

The dose and duration of treatment depends on disease severity and sensitivity of the activator. Tuberculosis - on 200 mg 2 times a day, within 14-28 days and more; the maximum term at treatment lekarstvenno of steady tuberculosis makes 3 months. Acute uncomplicated bronchitis, bronchial pneumonia - 400 mg/days, a course of treatment - up to 10 days; the complicated pneumonia, an exacerbation of chronic bronchitis - 400-800 mg/days, a course of treatment - up to 14 days; a mycoplasmal infection - 400-800 mg/days during 2-3 weeks.

At the moderated or expressed renal failure (at KK less than 30 ml/min. and the patient on a hemodialysis) an initial dose - 400 mg/days, with the subsequent decrease to 200 mg/days. Uncomplicated infections of urinary tract - 400 mg/days within 3-5 days; the complicated infections of urinary tract - 400 mg/days within 10-14 days; acute gonorrhea - 600 mg once; chronic gonorrhea - 600 mg/days within 5 days (against the background of specific immunotherapies). Urogenital clamidiosis (including bacterial and Chlamidia and gonorrheal and Chlamidia infections) - 400-600 mg/days, treatment duration - up to 28 days.

Features of use:

During treatment it is necessary to avoid long impact of a sunlight and use of artificial UF-lighting. At the first signs of a photosensitization or hypersensitivity, manifestations of a neurotoxicity therapy needs to be stopped. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. With care it is necessary to appoint at cerebral atherosclerosis, epilepsy, etc. TsNS diseases with an epileptic syndrome.

Side effects:

Nausea, vomiting, dryness in a mouth, an abdominal pain, diarrhea or locks, a meteorism, a pseudomembranous coloenteritis, a dysphagy, language discoloration, a loss of appetite, a food faddism, dysbacteriosis. Fatigue, indisposition, adynamy, headache, dizziness, unconscious states, sleeplessness, hallucinations, spasms, hyperkinesias, tremor, paresthesias, nervousness, uneasiness, depression, excitement. Glomerulonephritis, dysuria, polyuria, anury, albuminuria, urethral bleedings, crystalluria, hamaturia, ischuria, hypostases; women have a vaginitis, a leukorrhea, intermenstrual bleedings, crotch pains, vaginal candidiasis; men have an orchitis, an epididymite. Hypoglycemia, gout. Arthralgia, vasculitis, spasms of gastrocnemius muscles, dorsodynias and breasts. Thrombocytopenia, purpura, increase in a fibrinolysis, nasal bleeding, limfoadenopatiya. Bronchospasm, cough, phlegm hypersecretion, grippopodobny symptoms. Vision disorder, pain and sonitus, eye pain. Decrease in the ABP, tachycardia, bradycardia, premature ventricular contraction, arrhythmias, progressing of SN and stenocardia, thrombembolia of a pulmonary artery, myocardiopathy, phlebitis. Allergic reactions: skin itch, small tortoiseshell, photosensitization, malignant exudative erythema.

Interaction with other medicines:

Does not influence isoniazid pharmacokinetics. Increases activity of peroral anticoagulants and increases toxicity of NPVP. It is not necessary to accept antiacid HP and сукральфат during 4 h to and 2 h after reception of a lomefloksatsin (forms with them chelate connections that reduces its bioavailability). At treatment of patients with tuberculosis ломефлоксацин use together with an isoniazid, Pyrazinamidum, streptomycin and Ethambutolum (the combination to rifampicin - an anatagonizm is not recommended). The HP blocking canalicular secretion slow down removal. There is no cross stability with penicillin, cephalosporins, aminoglycosides, co-trimoxazole, metronidazole. Vitamins C mineral additives should be applied for 2 h to or in 2 h after use of a lomefloksatsin.

Contraindications:

Hypersensitivity (including to other Ftorkhinolonam); pregnancy, lactation period; age up to 18 years (the period of formation and growth of a skeleton).

Overdose:

Treatment: symptomatic therapy. Haemo - and peritoneal dialysis at overdose are ineffective.

Storage conditions:

List B. In the dry, protected from light place at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 400 mg; the blister packaging on 5 tablets in a cardboard box with the instruction.