Lomefloxacin - instructions for use, dose, side effects, contraindications

Core: lactose monohydrate - 104.0 mg, potato starch - 48.0 mg, povidone (polyvinylpyrrolidone medium molecular weight, callidone 25) - 12.5 mg, sodium carboxymethyl starch (primogel) 5.0 mg, crospovidone 10.0 mg, talcum powder - 10.0 mg, sodium lauryl sulfate 3.0 mg, magnesium stearate 6.0 mg, silicon dioxide colloid (aerosil grade A-300) 11.0 mg

Film sheath: ready water-soluble film shell - 10.0 mg

(Sheath composition: hydroxypropylmethylcellulose (hypromellose) 25.0%, copovidone (copolyvidone) 22.5%, polyethylene glycol 6000 (macrogol 6000) -9.5%, glyceryl caprylcaprate 3.0%, polydextrose 15.0% , titanium dioxide -25.0%).

Description:

Tablets covered with a film shell, spherical capsular shaped, with a risk on one side, white or almost white.

On the cross section, the nucleus is white or almost white in 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. It is active against 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, other microorganisms: Chlamydia trachomatis.

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

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.

TO lomefloxacin are stable: Streptococcus spp. groups A, B,D and G, Streptococcus pneumoniae, Pseudomonas cepacia, Ureaplasma urealyticum, Mycoplasma hominis and anaerobic bacteria.

Acts both on the outside,and on 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 (TCmax) - 0.8-1.5 hours. The maximum concentration (Cmah) after ingestion 100 mg is 0.8 μg / ml, 200 mg - 1.4 μg / ml, 400 mg - 3-5.2 μg / ml. Eating reduces Cmby 18% and increases TSmah to 2 hours.

Stationary concentration (Css) in plasma is determined after 48 h. Connection with plasma proteins -10%. It penetrates well into organs and tissues (respiratory tract, ENT organs, soft tissues, bones, joints, abdominal organs, pelvis, genitals), 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 (T1 / 2) 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 the clearance of creatinine to 10-40 ml / min / 1.73 m2 T1 / 2 increases.

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

Indications:

Infectious-inflammatory diseases caused by susceptible to lomefloxacin microorganisms: 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. Urogenital chlamydiosis. Exacerbation of chronic bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis. Tuberculosis of the lungs (as part of complex therapy): extensive caseous necrotic tissue damage, a pronounced nonspecific component of inflammation, drug resistance of mycobacteria to rifampicin, or poor tolerance of rifampicin.

Contraindications:

Hypersensitivity to lomefloxacin and other fluoroquinolones, other components of the drug, pregnancy, period, lactation, age to 18 years (period of formation and growth of the skeleton), lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Cerebral atherosclerosis, epilepsy and other diseases of the central nervous system with epileptic syndrome, electrolyte imbalance (eg, hypokalemia, hypomagnesemia), simultaneous administration of antiarrhythmic drugs of IA class (quinidine, procainamide) and III class (amiodarone, sotalol), lengthening interval syndrome Q-T, other diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia), renal failure, elderly age, tendon damage with previous treatment with fluoroquinolones.

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 hours before the procedure;

transurethral surgery - 400 mg once 2 to 6 hours before surgery;

Urogenital chlamydia: 400 mg / day for 14-28 days.

Tuberculosis of the lungs (as part of complex therapy): 400 mg / day for 14-28 days or more.

In patients with moderate or severe impairment of renal function (with clearance of creatinine less than 30 ml / min and patients on hemodialysis) the initial dose - 400 mg / day, followed by a decrease to 200 mg / day.

Side effects:

Co side of the digestive system: nausea, vomiting, dryness of the oral mucosa, gastralgia, abdominal pain,diarrhea or constipation, flatulence, pseudomembranous colitis, dysphagia, discoloration of the tongue, decreased appetite or bulimia; perversion of taste, dysbacteriosis, increased activity of hepatic transaminases.

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

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 musculoskeletal system: arthralgia, vasculitis, calf muscle cramps, back and chest pain.

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, nasal bleeding, lymphadenopathy.

From the respiratory system: dyspnea, bronchospasm, cough, hypersecretion of sputum, flu-like symptoms.

From the sense organs: impaired vision, pain and noise in the ears, pain in the eyes.

Co cardiovascular system: lowering of arterial pressure, tachycardia, bradycardia, extrasystole, arrhythmias, progression of heart failure, angina, pulmonary embolism, myocardiopathy, phlebitis.

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

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

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

Overdose:Information about overdose is very limited. Symptomatic therapy is performed. Hemo- and peritoneal dialysis with an overdose are ineffective.

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 (NSAIDs).

Do not take antacids 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 together with isoniazid, pyrazinamide, ethambutol and other anti-tuberculosis drugs (not recommended combination with rifampicin - antagonism).

Drugs that block tubular secretion, slow the excretion of lomefloxacin. Joint application with antiarrhythmic drugs, I A class (quinidine, procainamide) and III class (amiodarone, sotalol) may cause lengthening of the interval Q-T. 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 treatment, prolonged exposure to sunlight and the use of artificial, ultraviolet light should be avoided (evening reception reduces the risk of reaction to ultraviolet radiation).At the first sign of photosensitization (increased skin sensitivity, burn, redness, swelling, blisters, rashes, itching, dermatitis) or hypersensitivity, neurotoxicity (excitation, convulsions, tremors, photophobia, confusion, toxic psychosis, hallucinations) therapy should be discontinued.

During the treatment period, care must be taken when dealing with potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when operating vehicles and mechanisms.

Form release / dosage:The tablets covered with a film cover, on 400 mg.

Packaging:

For 5 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3, 5 or 10 contour packs, together with the instruction for use, is placed in a pack of cardboard. The packets are placed in a group package.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002263

Date of registration:19.03.2012 / 18.02.2016

Expiration Date:Unlimited

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp02.04.2018

Illustrated instructions

Instructions

Lomefloxacin (Lomefloxacine)