Composition, form of production and packaging
Tablets covered with a film membrane of orange color, oblong, with oblique margins; on a break - yellowish-white color.
1 tab.
Lomefloxacin (in the form of hydrochloride) 400 mg
Excipients: microcrystalline cellulose, talc, magnesium stearate, silicon dioxide colloid, sodium croscarmellose, hydroxypropylmethylcellulose, titanium dioxide, dichloromethane (methylene chloride), isopropyl alcohol, Sunset Yellow Lake dye.
5 pieces. - blisters (1) - cardboard boxes.
1000 pcs. - plastic cans.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Lomefloxacin is a synthetic antimicrobial agent of the fluoroquinolone group of a broad spectrum of bactericidal action. Inhibits the activity of bacterial DNA-gyrase, forming a complex with its tetramer (subunit of A2B2 gyrase) and disrupts transcription and replication of DNA, leads to the death of a 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.
In vitro with a minimum inhibitory concentration (MIC) of 2 Ојg / ml 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 resistant to: Streptococcus spp. Groups A, B, D and G, Streptococcus pneumoniae, Pscudomonas cepacia, Ureparasma urealyticum, Mycoplasma hominis and anaerobic bacteria.
It acts on both extracellular and intracellularly located Mycobacterium tuberculosis, shortens 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 Ојg / ml).
PHARMACOKINETICS
After ingestion, lomefloxacin is almost completely absorbed from the digestive tract (absorption - 93-98%, food intake reduces it by 12%). After taking 400 mg C maxin blood plasma is achieved after 1-2 hours and is 3-5.2 mg / l. Eating a meal reduces C max by 18%.
The equilibrium concentration in plasma is determined after 48 hours. The connection with plasma proteins is 9-11%. 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.
T 1/2 - 8-9 hours; the average renal clearance is 143-147 ml / min.
In elderly patients, plasma clearance is reduced by 25%. When the SC decreases to 10-40 ml / min T 1/2 increases. By the kidneys, 70-80% is excreted by 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 surgery;
- exacerbation of chronic bronchitis caused by Haemophilus influenzae or Moraxella catarrhalis;
- pulmonary tuberculosis (as part of complex therapy): extensive caseous-necrotic tissue damage, pronounced nonspecific component of inflammation, drug resistance of mycobacterium to rifampicin, or poor tolerance of rifampicin.
DOSING MODE
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 to 6 hours before the procedure; transurethral surgery - 400 mg once 2 to 6 hours before surgery.
Tuberculosis: 400 mg / day, for 14 - 28 days or more.
At CC less than 30 ml / min and the patient on hemodialysis initial dose - 400 mg / day, followed by a decrease to 200 mg / day.
SIDE EFFECT
From the digestive system: nausea, vomiting, dry mouth, gastralgia, abdominal pain, diarrhea or constipation, flatulence, pseudomembranous colitis, dysphagia, discoloration of the tongue, anorexia or bulimia, taste distortion, dysbiosis, increased activity of "liver" transaminases.
From the nervous system: fatigue, malaise, asthenia, headache, dizziness, insomnia, hallucinations, convulsions, hyperkinesia, tremor, paresthesia, nervousness, anxiety, depression, agitation.
From the genitourinary system: glomerulonephritis, dysuria, polyuria, anuria, albuminuria, urethral hemorrhages, 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, pain in the back and chest.
On the part of the hemostasis system and hemopoiesis: bleeding from the organs of the gastrointestinal tract, thrombocytopenia, purpura, fibrinolysis, nosebleeds, lymphadenopathy.
On the part of the respiratory system: dyspnea, bronchospasm, cough, hypersecretion of phlegm, influenza-like symptoms.
From the senses: visual impairment, pain and noise in the ears, pain in the eyes.
From the cardiovascular system: lowering blood pressure, tachycardia, bradycardia, extrasystole, arrhythmias, progression of heart failure, angina pectoris, pulmonary embolism, myocardiopathy, phlebitis.
Allergic reactions: pruritus, hives, photosensitivity, malignant exudative erythema (Stevens-Johnson syndrome).
Influence on the fetus: the experiment described fetotoxic action (arthropathy).
Other: candidiasis, increased sweating, chills, thirst, superinfection.
CONTRAINDICATIONS
- hypersensitivity (including to other fluoroquinolones);
- pregnancy, lactation period;
- age to 18 years (the period of formation and growth of the skeleton);
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
With caution: cerebral atherosclerosis, epilepsy and other CNS diseases with epileptic syndrome, prolongation of the QT interval, hypokalemia, simultaneous administration of antiarrhythmic drugs of the IA class (quinidine, procainamide) and III class (amiodarone, sotalol).
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
At CC less than 30 ml / min and the patient on hemodialysis initial dose - 400 mg / day, followed by a decrease to 200 mg / day.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
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 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, hyperemia, swelling, blistering, rash, itching, dermatitis) or hypersensitivity, neurotoxicity (excitation, convulsions, tremor, photophobia, confusion, toxic psychosis, hallucinations) therapy should be stopped.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (possible only after assessing the patient's individual reaction).
OVERDOSE
Treatment: induction of vomiting or gastric lavage, adequate hydration, symptomatic therapy. Hemo- and peritoneal dialysis with an overdose are ineffective.
DRUG INTERACTION
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 is used in conjunction with isoniazid, pyrazinamide, streptomycin and ethambutol (not recommended combination with rifampicin - antagonism).
Does not affect the pharmacokinetics of isoniazid. Does not interact with theophylline, caffeine.
Drugs that block tubular secretion, slow down excretion. There is no cross-resistance with penicillins, cephalosporins, aminoglycosides, co-trimoxazole, metronidazole.
Increases the activity of indirect anticoagulants and increases the toxicity of non-steroidal anti-inflammatory drugs.
Vitamins with mineral supplements should be used 2 hours before or 2 hours after taking Lomefloxacin.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
Store at a temperature of no higher than 25 В° C in a dry, protected from light place. Keep out of the reach of children. Shelf life - 3 years.
