LOFOKS (Pills)
Active material: Lomefloxacin
When ATH: J01MA07
CCF: Fluoroquinolone antibacterial drug
ICD-10 codes (testimony): A00, A01, A02, A03, A15, A54, A56.0, A56.1, A56.4, A74.0, J04, J15, J20, J37, J42, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M86, N10, N11, N30, N34, N41, T30, T79.3, Z29.2
When CSF: 06.17.02.01
Manufacturer: Synthesis of (Russia)
Pharmaceutical form, composition and packaging
Pills, coated white or nearly white, oval biconvex.
| 1 tab. | |
| lomefloxacin (the hydrochloride) | 400 mg |
Excipients: microcrystalline cellulose, polyvinylpyrrolidone (povidone), lactose, potato starch, collidone CL-M (krospovydon), talc, magnesium stearate, stearic acid, hydroxypropylmethylcellulose (gipromelloza), hydroxypropyl, polyethylene oxide-4000, Titanium dioxide, propylene glycol.
5 PC. – packings Valium planimetric (1) – packs cardboard.
5 PC. – packings Valium planimetric (2) – packs cardboard.
Pharmacological action
Antibacterial drug broad-spectrum fluoroquinolones from the Group, diphthorquinolone. It has bactericidal activity, the mechanism of which is associated with the effect on the DNA gyrase of bacteria, providing supercoiling. Lomefloxacin forms a complex with its tetramer (subunit of gyrase A2B2) and disrupts DNA transcription and replication, which leads to the death of a microbial cell. Β-lactamases produced by pathogens do not affect the activity of lomefloxacin.
Preparation highly active against gram-negative aerobic microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter different, Klebsiella pneumoniae, Enterobacter cloacae, Proteus vulgaris, Salmonella spp., Shigella spp., Moraxella catarrhalis, Morganella morganii, Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Pseudomonas aeruginosa (Some strains of).
C drug moderately sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Serratia dissolving, Serratia wilting, Pseudomonas aeruginosa (most strains), Mycobacterium tuberculosis, Chlamydia trachomatis, Hafnia avenue, Citrobacter freundii, Aeromonas hydrophila, Proteus is wonderful, Proteus stuartii, Rettgeri Providence, Alcalifaciens Providence, Klebsiella oxytoca, Klebsiella ozaenae, Enterobacter aerogenes, Enterobacter agglomerans.
Acts as outside, and intracellularly located mycobacteria: Mycobacterium tuberculosis, reduces the time of their excretion from the body, provides faster resorption of infiltrates.
Acts on most microorganisms in low concentrations (concentration, necessary to suppress growth 90% strains, is usually no more 1 ug / ml). Resistance is rare.
C drug resistant: Streptococcus spp., Pseudomonas cepacia, Ureaplasma urealyticum, Treponema pale, Mycoplasma hominis and anaerobic bacteria.
Pharmacokinetics
Absorption
After oral administration, lomefloxacin is almost completely absorbed from the gastrointestinal tract., absorption is 95-98%. Food intake reduces absorption by 12%. Tmax – 0.8-1.5 no. Cmax after oral dose 100 mg of 0.8 ug / ml, 200 mg – 1.4 ug / ml, 400 mg – 3-5.2 ug / ml. Eating decreases Cmax on 18% and increases Tmax to 2 no.
Distribution
The equilibrium state is achieved after 48 no. Plasma protein binding – 10%. Well into the organs and tissues (Airways, ENT organs, soft tissue, bones, joints, abdominal organs, pelvic, genitals), where it reaches a concentration 2-7 times higher, than in plasma.
Metabolism and excretion
A small part of the drug is metabolized to form metabolites. T1/2 – 8-9 no; the average kidney klirens – 145 ml / min. It is excreted mainly by the kidneys by tubular secretion up to 70-80% (mainly unchanged, 9% – in the form of glucuronides, 0.5% – as other metabolites); through the intestine – 20-30%.
Pharmacokinetics in special clinical situations
In elderly patients, plasma clearance decreases by 25%.
In case of impaired renal function and creatinine clearance 10-40 ml / min / 1.73m2 T1/2 increases.
Testimony
Infectious-inflammatory diseases, caused by microorganisms sensitive to lomefloxacin:
- Urinary tract infections (incl. cystitis, pyelonephritis, uretrit, prostatitis);
- Infections of the digestive tract (incl. dysentery, typhoid fever, salmonellosis, cholera) and biliary tract;
- Respiratory infections (incl. exacerbation of chronic bronchitis);
-fatigue infections of the skin and soft tissues (incl. infected wounds, burns);
- Osteomyelitis;
- Gonorrhea;
- Chlamydia (incl. chlamydial conjunctivitis and Blepharoconjunctivitis).
Prevention of infectious complications before and after transurethral surgery.
Pulmonary tuberculosis (in the complex therapy):
- acutely progressive forms;
- multidrug resistance of mycobacteria;
- poor tolerance of rifampicin.
Dosage regimen
The drug is taken orally, regardless of the meal, drinking plenty of fluids; the multiplicity of reception – 1 time / day. The dose and duration of treatment depends on the severity of the disease and the sensitivity of the pathogen..
At uncomplicated urinary tract infections The recommended dose is 400 mg / day for 3-5 days; at complicated infections of the urinary tract – 400 mg / day for 10-14 days.
To prevention of infectious and inflammatory diseases of the urinary tract during transurethral operations the drug is prescribed in a dose 400 mg dose of 2-6 hours before the operation.
At acute gonorrhoea the recommended dose – 600 mg dose; at chronic gonorrhea – 600 mg / day for 5 days (against the background of specific immunotherapy).
At urogenital chlamydia (including bacterial-chlamydial and gonorrheal-chlamydial infections) the drug is prescribed for 400-600 mg / day, length of treatment – to 28 days.
At chlamydial infection in patients with rheumatism – by 400 mg / day for 20 days.
At chlamydial conjunctivitis – by 400 mg / day, a course of treatment – to 10 days.
At mycoplasma infection – 600 mg / day, a course of treatment – to 10 days.
At purulent infections of soft tissues, infected wounds – 400 mg / day for 5-14 days.
At chronic osteomyelitis – 400-800 mg / day for 3-8 weeks.
At tuberculosis appoint 200 mg 2 times / day for 14-28 days or more.
At acute uncomplicated bronchitis, ʙronxopnevmonii – by 400 mg / day, a course of treatment – to 10 days.
At complicated pneumonia, exacerbation of chronic bronchitis – by 400-800 mg / day, a course of treatment – to 14 days.
At mycoplasma infection – by 400-800 mg / day for 2-3 Sun.
In patients with mild or acute violations of the kidney (CC less than 30 ml / min) and patients on hemodialysis starting dose is 400 mg/day, followed by a decline to 200 mg / day.
Side effect
From the digestive system: nausea, vomiting, dry mouth, gastralgia, stomach ache, diarrhea or constipation, flatulence, pseudomembranous enterocolitis, dysphagia, color change language, decreased appetite or bulimia, dysgeusia, dysbiosis, increase in liver transaminases.
From the central and peripheral nervous system: fatiguability, malaise, asthenia, headache, dizziness, insomnia, hallucinations, convulsions, hyperkinesia, tremor, paresthesia, nervousness, anxiety, depression, excitation.
From the urinary system: glomerulonephritis, dizurija, polyuria, anurija, albuminuria, Urethral bleeding, kristallurija, hematuria, urinary retention, swelling.
On the part of the reproductive system: female – vaginitis, leykoreya, intermenstrual bleeding, pain in the perineum, vaginal candidiasis; males – orchitis, epididymitis.
Metabolism: gipoglikemiâ, gout.
On the part of the musculoskeletal system: arthralgia, vasculitis, leg cramps, back and chest pain.
From the hematopoietic system: bleeding from the digestive tract, thrombocytopenia, purpura, increased fibrinolysis, nose bleed, lymphadenopathy.
The respiratory system: dyspnoea, respiratory tract infections, cough, sputum hypersecretion, flu-like symptoms.
From the senses: blurred vision, pain and tinnitus, sore eyes.
Cardio-vascular system: fainting, decrease in blood pressure, tachycardia, bradycardia, arrythmia, Arrhythmia, progression of heart failure, angina, pulmonary embolism, miokardiopatija, phlebitis.
Allergic reactions: itching, hives, malignant exudative erythema (Stevens-Johnson syndrome), bronchospasm.
Other: candidiasis, increased sweating, chills, thirst, superimposed infection, photosensitivity.
Contraindications
- Pregnancy;
- Lactation (breast-feeding);
- Up to 18 years (period of formation and growth of the skeleton);
- hypersensitivity to the components of the drug and to other fluoroquinolones.
Lomefloxacin should not be used in patients with prolonged QT interval..
FROM caution prescribe a drug for cerebral atherosclerosis, epilepsy and other diseases of the central nervous system with epileptic syndrome.
Pregnancy and lactation
Lofox® contraindicated during pregnancy and lactation (breast-feeding).
IN experimental studies described fetotoxic effects (arthropathy).
Cautions
With cirrhosis of the liver, no correction of the dosage regimen is required (normal renal function).
During the treatment period, prolonged exposure to the sun and exposure to artificial UV radiation should be avoided. (evening reception reduces the risk of reaction to UV radiation).
At the first sign of photosensitivity (increased sensitivity of the skin, burn, redness, edema, blisters, rash, itching, dermatitis) or hypersensitivity, manifestations of neurotoxicity (excitation, convulsions, tremor, photophobia, confusion, toxic psychosis, hallucinations) therapy should be discontinued.
Lomefloxacin should not be given to patients with an extended QT interval., if hypokalemia, with the simultaneous use of class IA antiarrhythmic drugs (quinidine, prokaynamyd) and III (Amiodarone, sotalol).
Effects on ability to drive vehicles and management mechanisms
In the period of treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Overdose
Information about an overdose of the drug Lofox® very limited.
Treatment: if necessary, symptomatic therapy is carried out. Diagnostic- and peritoneal dialysis in case of overdose are ineffective.
Drug Interactions
With the simultaneous use of lomefloxacin does not affect the pharmacokinetics of isoniazid; does not interact with theophylline, caffeine.
With the simultaneous use of lomefloxacin increases the activity of oral anticoagulants and increases the toxicity of NSAIDs.
With simultaneous administration, antacids and sucralfate should not be taken for 4 hour before and 2 hours after administration of lomefloxacin, tk. it chelates with them, which reduces its bioavailability.
In the treatment of tuberculosis, lomefloxacin is used in conjunction with isoniazid, pirazinamidom, streptomycin and ethambutol (combination with rifampicin is not recommended due to antagonism of action).
With the simultaneous use of drugs, block tubular secretion, slow down the excretion of lomefloxacin.
No cross-resistance with penicillins, cephalosporins, aminoglikozidami, co-trimoxazole, metronidazolom.
Vitamins with mineral supplements should be used for 2 hours before or after 2 hours after administration of lomefloxacin.
When combined with class IA antiarrhythmic drugs (quinidine, prokaynamyd) and III (Amiodarone, sotalol) It may prolong the QT interval.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, protected from light, reach of children, at a temperature no higher than 25 ° C. Time life – 2 year.
