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

Antimicrobial agent of the group of fluoroquinolones. Has a bactericidal effect. Inhibits the activity of DNA-gyrase, an enzyme involved in the transcription and replication of bacterial DNA.

Highly active against aerobic gram-negative bacteria: Escherichia coli, Salmonella spp., Citrobacter diversus, Enterobacter cloacae, Haemophilus influenzae, Klebsiella pneumoniae, Proteus vulgaris, Morganella morganii, Legionella pneumophila, Neisseria gonorrhoeae, Neisseria meningitidis, Moraxella catarrhalis.

Lomefloxacin is moderately sensitive Proteus mirabilis, Proteus stuartii, Providencia rettgeri, Pseudomonas aeruginosa, Serratia liquefaciens, Serratia agglomerans, Haemophilus parainfluenzae, Providencia alcalifaciens, Aeromonas hydrophila, Hafnia alvei, Mycobacterium tuberculosis, Chlamydia trachomatis, as well as some Gram-positive aerobic bacteria (Staphylococcus aureus, Staphylococcus epidermidis).

Lomefloxacin is stable Streptococcus spp., Pseudomonas cepacia, Ureaplasma urealyticum, Mycoplasma hominis and anaerobic bacteria.

Lomefloxacin has anti-tuberculosis activity, acting both on the outside and intracellularly located Mycobacterium tuberculosis.

Pharmacokinetics:

After oral administration, it is almost completely absorbed from the gastrointestinal tract, the absorption is 95-98%. Binding to plasma proteins - 10%. Widely distributed in the body. Concentrations in tissues and body fluids are usually 2-7 times higher than in plasma, especially in the tissues of the prostate and urine.

The half-life of lomefloxacin is 7-9 hours. About 70-80% is excreted unchanged in urine within 24 hours. In patients with impaired renal function, the elimination half-life increases significantly.

Indications:

Pills: urinary tract infection (including prevention of infection before and after transurethral surgery): cystitis, pyelonephritis, urethritis; Gastrointestinal tract (dysentery, typhoid fever, salmonellosis, cholera) and bile ducts, respiratory infections (including exacerbation of chronic bronchitis), purulent skin and soft tissue infections, infected wounds, burns, gonorrhea, chlamydia (including chlamydial conjunctivitis and blepharoconjunctivitis ), prostatitis, osteomyelitis. Tuberculosis of the lung (as part of complex therapy) - osteo-progressive forms, multiple drug resistance of mycobacteria, poor tolerance of rifampicin.

Eye drops: bacterial infections of the anterior part of the eye: conjunctivitis, blepharitis, blepharoconjunctivitis, including chlamydial etiology.

ICD-10

I.A00-A09.A00 Cholera

I.A15-A19.A15 Tuberculosis of respiratory organs, confirmed bacteriologically and histologically

I.A15-A19.A15.8 Tuberculosis of other respiratory organs, confirmed bacteriologically and histologically

I.A50-A64.A54 Gonococcal infection

I.A50-A64.A56.1 Chlamydial infections of the pelvic organs and other urogenital organs

VII.H00-H06.H01.0 Blepharitis

VII.H10-H13.H10.2 Other acute conjunctivitis

VII.H10-H13.H10.4 Chronic conjunctivitis

VII.H10-H13.H10.5 Blepharoconjunctivitis

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J40-J47.J42 Chronic bronchitis, unspecified

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N30-N39.N30 Cystitis

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:

Hypersensitivity, pregnancy, breast-feeding, age to 18 years (the period of formation and growth of the skeleton).

Carefully:

Cerebral atherosclerosis, epilepsy and other CNS diseases with convulsive 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:

For all fluoroquinolones: adequate and well-controlled studies in humans have not been conducted. Since the use of fluoroquinolones in studies on immature animals has led to the development of arthropathy, the use of drugs in this group is not recommended during pregnancy. For Lomefloxacin: Reproduction studies in rats receiving oral doses 34 times higher than the recommended dose for humans did not report any harm to the fetus. An increase in embryonic loss in monkeys was observed with doses 6-12 times higher than the recommended doses for humans (calculated as mg / kg). No teratogenic effects were observed in rats or monkeys using doses 16 times the recommended doses for humans. Studies in rabbits: maternal toxicity and associated fetal toxicity,a decrease in the weight of the placenta and changes in the coccygeal spine occurred when doses were used that were 2 times higher than those recommended for humans (when calculating mg / m²). There is no information on the penetration into breast milk. If the appointment of alternative antibacterial drugs is not possible and the use of fluoroquinolones is necessary, breast-feeding is not recommended.

The category of FDA recommendations is C.

Dosing and Administration:

Uncomplicated urinary tract infections - 400 mg per day for 3-5 days; uncomplicated acute cystitis in women - 400 mg per day for 3-7 days; Complicated urinary tract infections - 400 mg per day for 10-14 days; prevention of infectious and inflammatory diseases of the urinary tract in transurethral operations - 400 mg once 2 to 6 hours before the operation.

Infections of the digestive tract (shigellosis, typhoid, salmonellosis, cholera) - 400 mg per day for 5 days.

Purulent infections of the skin and soft tissues, infected wounds, burns, osteomyelitis - 400 mg per day for 5-14 days; chronic osteomyelitis - 400-800 mg per day for 3-8 weeks.

Tuberculosis of the lungs (as part of complex therapy), tuberculosis - 200 mg twice a day, for 14-28 days or more.

Gonorrhea - 200-400 mg per day 2 days, 600 mg once; chronic gonorrhea - 600 mg per day for 5 days (against a background of specific immunotherapy).

Chlamydia (including chlamydial conjunctivitis and blepharoconjunctivitis), urogenital chlamydia (including bacterial chlamydia and gonorrhea-chlamydia infection) - 400-600 mg per day, duration of treatment course up to 28 days; chlamydial infection in patients with rheumatism - 400 mg per day for 20 days; Chlamydia conjunctivitis - 400 mg per day, treatment course up to 10 days.

Chronic bronchitis (exacerbation) caused by H. influenzae or M. catarrhalis - 400 mg per day for 14 days.

Bacterial infections of the anterior part of the eye (conjunctivitis, blepharitis, blepharoconjunctivitis, including chlamydial etiology) - adults 1 drop 2-3 times a day in the lower conjunctival sac for 7-9 days. At the beginning of treatment, more frequent administration is necessary: 5 drops for 20 minutes (1 drop at intervals of 5 minutes) or 1 drop per hour for 6-10 hours.

Side effects:

On the part of the digestive system: nausea, vomiting, dry mouth, epigastric pain, flatulence, constipation / diarrhea, dysbiosis, pseudomembranous colitis, dysphagia, bleeding in the gastrointestinal tract, discoloration of the tongue, decrease / increase in appetite, taste distortion,increased activity of hepatic transaminases.

From the nervous system and sensory organs: headache, dizziness, fatigue, malaise, asthenia, insomnia, nervousness, hallucinations, depression, agitation, convulsions, hyperkinesis, tremor, paresthesia, pain and tinnitus, vision impairment, eye pain.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): hypotension, tachycardia, bradycardia, arrythmia, cyanosis, the progression of heart failure and angina pectoris, myocardial infarction, pulmonary embolism, cerebrovascular disorders, cardiomyopathy, phlebitis, thrombocytopenia, purpura, increased fibrinolysis, epistaxis, lymphadenopathy.

On the part of the respiratory system: dyspnea, respiratory infections, bronchospasm, cough, increased sputum secretion, influenza-like symptoms.

From the musculoskeletal system: cramps calf muscles, arthralgia, myalgia, vasculitis, back and chest pain.

From the genitourinary system: glomerulonephritis, dysuria, polyuria, anuria, albuminuria, crystalluria, hematuria, difficulty urinating, painful urination, edema, in women - vaginitis,leukorrhea, intermenstrual bleeding, pain in the perineum, vaginal candidiasis, in men - orchitis, epididymitis.

Allergic reactions: itching, urticaria, photosensitivity, malignant exudative erythema.

Other: flushes to the face, increased sweating, chills, thirst, hypoglycemia, gout, candidiasis, superinfection.

Eye drops: burning sensation in the eyes after instillation; with prolonged use - the development of secondary fungal infection.

Overdose:

There is no specific antidote. 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:

Aluminum, calcium and / or magnesium-containing antacids, iron sulphate, magnesium-containing laxatives, sucralfate - decrease in the absorption of lomefloxacin (take lomefloxacin 2 hours before and 6 hours after taking the medication).

Warfarin - an increase in anticoagulant effect (monitoring international normalized attitude, prothrombin time).

Didanosine - reduced absorption of lomefloxacin (not used simultaneously).

Drugs that block tubular secretion - slowing the withdrawal of lomefloxacin.

Special instructions:

Cross-resistance: microorganisms resistant to a single fluoroquinolone are resistant to other drugs of this class.

Recently there has been a widespread spread of resistance (including cross-over) to fluoroquinolones E. coli; K. pneumoniae, Salmonella spp., N. gonorrhoeae (weak stability); H. influenzae, S. epidermidis, Pseudomonas aeruginosa.

With moderate salmonellosis, antibacterial drugs do not have a positive effect on the clinical course, prolong the period of bacterial release, lead to the emergence of side-effects of medicinal reactions.

When used to prevent bacterial complications in gastrointestinal bleeding in patients with cirrhosis, the incidence of bacterial complications and deaths has been shown to decrease.

Are able to cause arthropathy in the fetus.

Distinctive characteristics

In acute uncomplicated cystitis in women, clinical and microbiological efficacy is comparable to norfloxacin,on the safety profile inferior to norfloxacin (the frequency of any unwanted reactions, including those leading to drug withdrawal, the frequency of photosensitization reactions was significantly higher when using lomefloxacin in comparison with norfloxacin).

With complicated infections of the urinary tract, the effectiveness is comparable with levofloxacin, ciprofloxacin.

In the treatment of uncomplicated urinary tract infections, the efficacy is comparable to norfloxacin.

In terms of effectiveness, it is comparable with ofloxacin in the treatment of bacterial infections.

Avoid UV radiation (evening reception reduces the risk of photosensitization).

There was no difference in the clinical efficacy of lomefloxacin and norfloxacin in topical treatment of acute bacterial conjunctivitis.

The strength of the photosensitizing effect is equal to ciprofloxacin, more dangerous than trovafloxacin.

With chronic bacterial prostatitis, the effectiveness is comparable with ciprofloxacin.

In the Cochrane database, no clinical studies have been found to study the efficacy and safety of the use of lomefloxacin in tuberculosis.

With cirrhosis of the liver - correction of the dosing regimen is not required (under the condition of normal kidney function).

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Instructions

Lomefloxacin (Lomefloxacinum)