Lomefloxacin

A broad-spectrum antimicrobial bactericidal agent from the group of fluoroquinolones . It acts on the bacterial enzyme DNA gyrase , which provides supercoiling , forms a complex with its tetramer (subunits of A2B2 gyrase ) and disrupts transcription and replication of DNA , leading to the death of a microbial cell . Beta-lactamases produced by pathogens do not affect the activity of lomefloxacin . 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 ; With a minimum inhibitory concentration of 2 μg / ml, it is active against the following microorganisms (however, the clinical efficacy of 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 , Serganiculiensiferienslienifensi , califeniella inflariensiformes other microorganisms: Legionella pneumophila . Resistant to the drug: A, B, D and G groups of streptococcus , Streptococcus pneumoniae , Pseudomonas cepacia , Ureaplasma urealyticum , Mycoplasma hominis and anaerobic bacteria. It acts on both extra- and intracellularly located Mycobacterium tuberculosis , reduces the time of their release from the body, provides faster absorption of infiltrates . Most microorganisms act in low concentrations (the concentration required to inhibit the growth of 90% of the strains , usually not more than 1 μg / ml). Resistance is rare.

Absorption - 95-98%; ingestion reduces absorption by 12%. TCmax - 0.8-1.5 hours. Cmax after oral administration of 100 mg is 0.8 μg / ml, 200 mg - 1.4 μg / ml, 400 mg - 3-5.2 μg / ml. Eating reduces Cmax by 18% and increases TCmax to 2 hours. Css in plasma is determined after 48 hours. Communication with plasma proteins - 10%. It penetrates well into organs and tissues, where the concentration of lomefloxacin is 2-7 times higher than in plasma. An insignificant part of the drug undergoes metabolism with the formation of metabolites . T _1/2 - 8-9 hours; average renal clearance - 145 ml / min. In elderly patients, plasma clearance is reduced by 25%. When creatinine clearance (CC) is reduced to 10-40 ml / min / 1.73 m², T _1/2 increases. Kidneys by tubular secretion excrete 70-80% (mainly unchanged, 9% - in the form of glucuronides , 0.5% - in the form of other metabolites); through the intestines - 20-30%.

Uncomplicated urinary tract infections caused by Escherichia coli , Klebsiella pneumoniae , Proteus mirabilis (gram-negative, spore-forming, optionally anaerobic bacteria) or Staphylococcus saprophyticus (coagulase-negative staphylococcus , a common pathogen of urinary tract infections). 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 lesions, a pronounced non-specific component of inflammation , drug resistance of mycobacteria to rifampicin, or poor tolerance of rifampicin.

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

Caution

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

Inside (regardless of food intake, washed down with 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 gland - 400 mg once 1-6 hours before the procedure; transurethral surgery - 400 mg once 2-6 hours before surgery. Tuberculosis: 400 mg / day, for 14-28 days or more. With CC less than 30 ml / min and for patients on hemodialysis, the initial dose is 400 mg / day, followed by a decrease to 200 mg / day.

• 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 perversion, dysbiosis , increased activity of “liver” transaminases .
• From the nervous system: fatigue, malaise, asthenia , headache , dizziness , fainting, insomnia , hallucinations , convulsions , hyperkinesis , tremors , paresthesias , 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, perineal pain, vaginal candidiasis ; in men - orchitis , epididymitis .
• From the side of metabolism: hypoglycemia , gout .
• From the musculoskeletal system: arthralgia , vasculitis , spasms of the calf muscles , back and chest pains.
• Hematopoietic organs and hemostasis: bleeding from the organs of the gastrointestinal tract , thrombocytopenia , purpura , increased fibrinolysis , epistaxis, lymphadenopathy .
• From the respiratory system: dyspnea , bronchospasm , cough , hypersecretion of sputum , flu-like symptoms.
• From the sensory organs: impaired vision, pain and tinnitus, pain in the eyes .
• From the cardiovascular system: lowering blood pressure , tachycardia , bradycardia , extrasystole , arrhythmias , progression of heart failure and angina pectoris , pulmonary embolism , myocardiopathy , phlebitis .
• Allergic reactions: pruritus, urticaria , photosensitivity , malignant exudative erythema (Stevens-Johnson syndrome) .
• Effect on the fetus: the experiment described the fetotoxic effect (arthropathy) .
• Other: candidiasis , increased sweating, chills , thirst , superinfection .

Overdose

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

With cirrhosis of the liver , a dosage regimen correction is not required (subject to normal renal function). During the treatment period, prolonged exposure to sunlight and the use of artificial UV radiation should be avoided (evening use reduces the risk of a reaction to UV radiation). At the first signs of photosensitivity (increased skin sensitivity, burns , hyperemia , edema, blisters, rashes, itching, dermatitis ) or hypersensitivity, manifestations of neurotoxicity (agitation, convulsions, tremors , photophobia , confusion, toxic psychoses , hallucinations), therapy should be stopped. 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.

Does not affect the pharmacokinetics of isoniazid . Does not interact with theophylline , caffeine . Increases the activity of oral anticoagulants and increases the toxicity of NSAIDs . Antacids and Sucralfate should not be taken for 4 hours before and 2 hours after taking lomefloxacin (forms chelating compounds with them, which reduces its bioavailability ). In the treatment of patients with tuberculosis, lomefloxacin is used together with isoniazid, pyrazinamide , streptomycin and ethambutol (a combination with rifampicin is not recommended - anatagonism). Medicines 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 use of lomefloxacin.