Lomefloxacin
Lomefloxacin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Lomefloxacine
ATX code: J01MA07
Active ingredient: lomefloxacin (lomefloxacin)
Producer: Pharmasintez JSC (Russia), Valenta Pharmaceuticals JSC (Russia)
Description and photo updated: 22.11.2018
Lomefloxacin is a fluoroquinolone, an antimicrobial agent.
Release form and composition
Dosage form - film-coated tablets: spherical, capsule-shaped, almost white or white, with a line on one side; the cross-section shows a white or almost white core (5 or 10 pieces in a blister strip, in a cardboard box 1, 2, 3, 5 or 10 packages).
Composition of one tablet:
- active substance: lomefloxacin (in the form of hydrochloride) - 400 mg;
- auxiliary components: povidone (medium molecular weight polyvinylpyrrolidone, kollidon 25), crospovidone, magnesium stearate, sodium carboxymethyl starch (primogel), potato starch, lactose monohydrate, sodium lauryl sulfate, colloidal silicon dioxide (aerosil grade A-300);
- shell: ready-made water-soluble film shell, consisting of copovidone (copolyvidone), polyethylene glycol 6000 (macrogol 6000), titanium dioxide, hydroxypropyl methylcellulose (hypromellose), polydextrose, glyceryl caprylocaprate.
Pharmacological properties
Pharmacodynamics
Lomefloxacin is a broad-spectrum antimicrobial bactericidal agent belonging to the fluoroquinolone group. The mechanism of its action is explained by the ability to act on DNA gyrase - a bacterial enzyme that provides supercoiling, forms a complex with its tetramer (subunit of gyrase A2B2), disrupts the replication and transcription of deoxyribonucleic acid (DNA), resulting in the death of the microbial cell.
Beta-lactamases produced by pathogens do not affect the activity of lomefloxacin.
The drug is effective against the following microorganisms:
- gram-negative aerobes: Haemophilus influenzae, Enterobacter cloacae, Proteus mirabilis, Klebsiella pneumoniae, Escherichia coli, Moraxella catarrhalis, Citrobacter diversus, Pseudomonas aeruginosa (only for urinary tract infections);
- gram-positive aerobes: Staphylococcus saprophyticus;
- others: Chlamydia trachomatis.
With a minimum inhibitory concentration of 2 μg / ml, lomefloxacin is also active against the following microorganisms, however, clinical efficacy has not been studied in strictly controlled studies:
- gram-negative aerobes: Klebsiella ozaenae, Klebsiella oxytoca, Enterobacter agglomerans, Citrobacter freundii, Aeromonas hydrophila, Serratia liquefaciens, Hafnia alvei, Enterobacter aerogenes, Providencia alcalifaciens, Morganella morganii, Serratia vulinusus, Proteinacea vulgarese,
- gram-positive aerobes: Staphylococcus epidermidis and Staphylococcus aureus (including methicillin-resistant strains);
- others: Legionella pneumophila.
Anaerobic bacteria, Ureaplasma urealyticum, Pseudomonas cepacia, Mycoplasma hominis, Streptococcus pneumoniae, Streptococcus spp. Are resistant to the drug. groups A, B, D and G.
The drug has an effect on the bacteria Mycobacterium tuberculosis, located both outside and inside the cell. Reduces the time of their excretion from the body, promotes faster resorption of infiltrates.
Lomefloxacin acts on most microorganisms at low concentrations: to suppress the growth of 90% of strains, a concentration of no more than 1 μg / ml is usually required.
Resistance to the action of lomefloxacin is rare.
Pharmacokinetics
After oral administration, lomefloxacin is almost completely absorbed (95–98%). The simultaneous consumption of food slows down absorption by about 12%.
The maximum concentration reaches within 0.8-1.5 hours. The maximum concentrations are: 0.8 μg / ml - after taking 100 mg; 1.4 μg / ml - after taking 200 mg; 3-5.2 mcg / ml - after taking 400 mg. When eating, the maximum concentration decreases by 18%, and the time to reach it increases to 2 hours.
Stationary plasma concentration is determined after 48 hours.
Lomefloxacin is characterized by a low degree of binding to plasma proteins - 10%.
It penetrates well into tissues and organs: joints, bones, ENT organs, respiratory tract, abdominal organs, soft tissues, genitals, pelvic organs. In them, the concentration of the substance is 2–7 times higher than in plasma.
A small part of lomefloxacin is metabolized, as a result of which metabolites are formed.
The average renal clearance is 145 ml / min. The half-life is 8-9 hours.
Excreted: 70–80% by the kidneys by tubular secretion (mainly unchanged, in the form of glucuronides - 9%, in the form of other metabolites - 0.5%), 20–30% through the intestines.
Plasma clearance is reduced by 25% in elderly patients.
With a reduced creatinine clearance (10–40 ml / min / 1.73 m 2), the half-life increases.
Indications for use
According to the instructions, Lomefloxacin is used to treat infectious and inflammatory diseases caused by microorganisms that are sensitive to its action. In particular, the indications for the use of the drug are:
- uncomplicated urinary tract infections caused by Staphylococcus saprophyticus, Klebsiella pneumoniae, Escherichia coli, Proteus mirabilis;
- complicated urinary tract infections caused by Citrobacter diversus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Enterobacter cloacae, Proteus mirabilis;
- exacerbation of chronic bronchitis caused by Moraxella catarrhalis, Haemophilus influenzae;
- urogenital chlamydia;
- pulmonary tuberculosis (as part of complex therapy): a pronounced nonspecific component of inflammation, extensive caseous-necrotic tissue lesions, poor tolerance of rifampicin or drug resistance of mycobacteria to rifampicin.
Also, the drug is used to prevent urinary tract infections in the case of transurethral surgeries and transrectal biopsy of the prostate gland.
Contraindications
- lactose intolerance / lactase deficiency / glucose-galactose malabsorption;
- age up to 18 years (or rather, the period of growth and formation of the skeleton);
- period of pregnancy and lactation;
- hypersensitivity to any component of the drug or other fluoroquinolones.
Lomefloxacin should be used with caution in renal failure, electrolyte imbalance (for example, hypokalemia or hypomagnesemia), epilepsy and other diseases of the central nervous system with epileptic syndrome, cerebral atherosclerosis, prolongation of the QT interval syndrome and other diseases of the cardiovascular system (heart failure, heart failure myocardium); in old age; in the case of the simultaneous use of class IA antiarrhythmic drugs (quinidine, procainamide) or class III (amiodarone, sotalol); with tendon damage during previous treatment with fluoroquinolones.
Instructions for the use of Lomefloxacin: method and dosage
Lomefloxacin is taken orally, regardless of meals: the tablets are swallowed whole and washed down with water in sufficient quantities.
The daily dose should be taken at one time.
Effective doses and duration of the therapeutic course depend on the type of pathogen, its sensitivity and the severity of the disease.
Unless otherwise prescribed by a doctor, the following treatment regimens are usually followed:
- complicated urinary tract infections: 400 mg once a day for 14 days;
- uncomplicated cystitis caused by Proteus mirabilis, Klebsiella pneumoniae, Staphylococcus saprophyticus: 400 mg per day for 10 days;
- uncomplicated cystitis in women caused by Escherichia coli: 400 mg once a day for 3 days;
- exacerbation of chronic bronchitis: 400 mg once a day for 14 days;
- pulmonary tuberculosis (as part of complex therapy): 400 mg once a day for 14-28 days or even more;
- urogenital chlamydia: 400 mg per day in a course, lasting from 14 to 28 days;
- prevention of urinary tract infections: 400 mg once 1–6 hours before transrectal biopsy of the prostate, 400 mg once 2–6 hours before transurethral surgery.
Patients with moderate or severe renal impairment (creatinine clearance <30 ml / min) and patients on hemodialysis are recommended to start treatment with a daily dose of 400, then it is reduced to 200 mg.
Side effects
- on the part of the hematopoietic and hemostatic system: epistaxis, increased fibrinolysis, thrombocytopenia, purpura, bleeding from the gastrointestinal tract, lymphadenopathy;
- from the musculoskeletal system: back and chest pain, vasculitis, arthralgia, cramps of the calf muscles;
- from the respiratory system: flu-like symptoms, sputum hypersecretion, cough, bronchospasm, dyspnea;
- from the side of metabolism: gout, hypoglycemia;
- from the senses: pain / noise in the ears, blurred vision, pain in the eyes;
- from the genitourinary system: urinary retention, anuria, polyuria, albuminuria, dysuria, glomerulonephritis, hematuria, crystalluria, urethral bleeding, edema; in men - epididymitis, orchitis; in women - pain in the perineum, intermenstrual bleeding, vaginitis, vaginal candidiasis, leukorrhea;
- on the part of the cardiovascular system: phlebitis, bradycardia, pulmonary embolism, lowering blood pressure, arrhythmias, myocardiopathy, extrasystole, tachycardia, angina pectoris, progression of heart failure;
- from the nervous system: asthenia, malaise, fatigue, nervousness, hyperkinesis, dizziness, agitation, tremor, anxiety, hallucinations, paresthesia, insomnia, fainting, headache, depression, convulsions;
- from the digestive system: dryness of the oral mucosa, discoloration of the tongue, diarrhea / constipation, flatulence, gastralgia, nausea, vomiting, decreased appetite or bulimia, abdominal pain, dysbiosis, taste perversion, dysphagia, pseudomembranous colitis, increased activity of hepatic transaminases;
- allergic reactions: photosensitivity, urticaria, pruritus, malignant exudative erythema (Stevens-Johnson syndrome);
- others: chills, increased sweating, thirst, candidiasis, superinfection;
- effect on the fetus: fetotoxic effect (arthropathy).
Overdose
Overdose information is limited. Hemodialysis and peritoneal dialysis are ineffective. Conducting symptomatic therapy is shown.
special instructions
During treatment, patients should avoid prolonged exposure to artificial ultraviolet light and sun exposure. To reduce the risk of developing photosensitization reactions allows taking the drug in the evening. Lomefloxacin should be canceled at the first signs of hypersensitivity to light: blistering, increased skin sensitivity, edema, redness, burns, itching, rash, dermatitis.
Also, the drug is canceled in case of hypersensitivity reactions or manifestations of neurotoxicity (hallucinations, photophobia, agitation, confusion, tremors, convulsions, toxic psychoses).
Influence on the ability to drive vehicles and complex mechanisms
During the entire period of treatment with the drug, care should be taken when driving vehicles and performing other types of work with potentially dangerous consequences.
Application during pregnancy and lactation
Lomefloxacin is prohibited for women during pregnancy and breastfeeding.
Pediatric use
The drug is contraindicated in patients under the age of 18.
With impaired renal function
In renal failure, Lomefloxacin should be used with caution.
For violations of liver function
With cirrhosis of the liver, there is no need to adjust the dose of the drug (subject to normal renal function).
Use in the elderly
In old age, Lomefloxacin should be used with caution.
Drug interactions
Lomefloxacin does not interact with caffeine and theophylline, does not affect the pharmacokinetic characteristics of isoniazid. Enhances the effect of oral anticoagulants. Increases the toxicity of non-steroidal anti-inflammatory drugs.
There is no cross-resistance of the drug with co-trimoxazole, cephalosporins, metronidazole, penicillins, aminoglycosides.
Lomefloxacin forms chelated compounds with antacids and sucralfate, which reduces its bioavailability. Therefore, these funds should not be taken within 4 hours before and 2 hours after taking lomefloxacin.
The elimination of lomefloxacin is slowed down by drugs that block tubular secretion.
With the simultaneous use of class IA antiarrhythmics (for example, quinidine or procainamide) and class III (for example, amiodarone or sotalol), QT interval lengthening is possible.
In patients with tuberculosis, lomefloxacin is used in combination with ethambutol, pyrazinamide, isoniazid and other anti-tuberculosis drugs. It is not recommended to combine with rifampicin, since antagonism is noted.
Vitamins and / or mineral supplements, if needed, should be taken 2 hours before or 2 hours after taking lomefloxacin.
Analogs
Lomefloxacin analogs are Lomacin, Xenaquin, Lofox, Lomflox.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry and dark place out of reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Lomefloxacin
According to reviews, Lomefloxacin is an effective antimicrobial agent. However, the main condition for its effectiveness is the sensitivity of the pathogen, the correct selection of the dose and duration of treatment.
In some negative reviews, side effects are described, but most often they are insignificant and disappear after the end of therapy.
Price for Lomefloxacin in pharmacies
The approximate price for Lomefloxacin is 270 rubles. per pack of 5 tablets.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
