Levofloxacin eye drops 5 mg/ml 5 ml with dropper cap No. 1

Directions for use and doses

Levofloxacin eye drops are instilled into the cavity of the conjunctival sac in the amount of 1-2 drops every two hours during the first two days of therapy. Subsequently, the frequency is reduced to four times a day (for 3-7 days). The duration of treatment is a week. If at the same time the doctor prescribed another drug for topical application, then the interval between medications should be 15 minutes. To prevent contamination of the vial and solution, avoid contact of the dropper tip with non-sterile surfaces.

The safety of Levofloxacin in newborns for the treatment of gonococcal conjunctivitis and corneal ulcers has not been studied. In elderly people, no dosage adjustment or frequency of administration of the drug is required.

Side effects of Levofloxacin

Allergic reactions: sometimes – itching and redness of the skin; rarely - general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, constriction of the bronchi and possibly severe suffocation; very rarely - swelling of the skin and mucous membranes (for example, in the face and throat), sudden drop in blood pressure and shock, increased sensitivity to solar and ultraviolet radiation, allergic pneumonitis, vasculitis; in some cases - severe skin rashes with blistering, for example, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by milder skin reactions. The above reactions can develop after the first dose, a few minutes or hours after administration of the drug.

From the digestive system: often - nausea, diarrhea, increased activity of liver enzymes (for example, alanine aminotransferase and aspartate aminotransferase); sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders; rarely - diarrhea mixed with blood, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis.

On the metabolic side: very rarely - a decrease in the concentration of glucose in the blood, which is of particular importance for patients with diabetes (possible signs of hypoglycemia: increased appetite, nervousness, perspiration, trembling). Experience with the use of other quinolones suggests that they can cause exacerbation of porphyria in patients already suffering from this disease. A similar effect cannot be excluded when using the drug levofloxacin.

From the nervous system: sometimes - headache, dizziness and/or stupor, drowsiness, sleep disturbances; rarely - anxiety, paresthesia in the hands, trembling, psychotic reactions such as hallucinations and depression, agitation, convulsions and confusion; very rarely - impaired vision and hearing, impaired taste and smell, decreased tactile sensitivity.

From the cardiovascular system: rarely - increased heartbeat, decreased blood pressure; very rarely - vascular (shock-like) collapse; in some cases - prolongation of the QT interval.

From the musculoskeletal system: rarely - tendon damage (including tendinitis), joint and muscle pain; very rarely - tendon rupture (for example, Achilles tendon); this side effect can be observed within 48 hours after the start of treatment and can be bilateral in nature, muscle weakness, which is of particular importance for patients with bulbar syndrome; in some cases - muscle damage (rhabdomyolysis).

From the urinary system: rarely - increased levels of bilirubin and creatinine in the blood serum; very rarely - deterioration of kidney function up to acute renal failure, interstitial nephritis.

From the hematopoietic organs: sometimes - an increase in the number of eosinophils, a decrease in the number of leukocytes; rarely - neutropenia, thrombocytopenia, which may be accompanied by increased bleeding; very rarely - agranulocytosis and the development of severe infections (persistent or recurrent increase in body temperature, deterioration in health); in some cases - hemolytic anemia; pancytopenia.

Other: sometimes - general weakness; very rarely - fever.

Any antibiotic therapy can cause changes in the microflora that is normally present in humans. For this reason, increased proliferation of bacteria and fungi resistant to the antibiotic used may occur, which in rare cases may require additional treatment.

special instructions

Levofloxacin eye drops can only be used topically. The solution cannot be injected into the anterior chamber of the eye or subconjunctivally.

The solution contains benzalkonium chloride, which is a preservative. In this regard, there is no need to use the drug when wearing hydrophilic contact lenses, because in this case eye irritation may occur. If there are signs of bacterial conjunctivitis, then contact methods of refractive correction should be completely abandoned.

Due to the fact that after instillation of the medicine, a temporary decrease in vision may occur, it is not recommended to engage in potentially hazardous activities during this period, in particular, driving a car.

Due to the fact that systemic fluoroquinolols can lead to serious allergic reactions even after a single dose, Levofloxacin eye drops should be discontinued if signs of allergy and hypersensitivity occur.

If you use the drug for a long time, there is a high probability of resistance developing in microorganisms, as well as the growth of fungal flora. If there is a decrease in the effectiveness of Levofloxacin eye drops or an increase in clinical symptoms, then it is necessary to change the medicine to another antibiotic.

Levofloxacin-Optic

Levofloxacin is the L-isomer of the racemic drug substance ofloxacin. The antibacterial activity of ofloxacin relates mainly to the L-isomer. As an antibacterial drug of the fluoroquinolone class, levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks (deoxyribonucleic acid), suppresses DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes.

Mechanism of resistance development

Resistance to levofloxacin can develop primarily through two main mechanisms, namely: a decrease in the intracellular concentration of the drug or changes in the targets of the drug.

Changes in the targets of the two bacterial enzymes DNA gyrase and topoisomerase IV are the result of mutations in the chromosomal genes encoding DNA gyrase (gyrA and gyrB) and topoisomerase IV (parC and parE; grlA and grlB in Staphylococcus aureus).

Drug resistance due to low intracellular concentration develops as a result of changes in the porin channel system of the outer cell membrane, which leads to a decrease in fluoroquinolone entry into gram-negative bacteria, or from efflux pumps.

Efflux-mediated resistance has been described for pneumococci (PmrA), staphylococci (NorA), anaerobic and gram-negative bacteria.

Plasmid-mediated quinolone resistance (defined by the qnr gene) has been detected against Klebsiella pneumoniae and Escherichia coli.

The development of cross-resistance between fluoroquinolones is possible.

Single mutations may not lead to clinical resistance, but multiple mutations cause clinical resistance to all drugs in the fluoroquinolone class. Alterable outer membrane porins and efflux systems can have broad substrate specificity, affecting multiple classes of antibacterial agents and leading to multiple resistance.

Efficiency has been established in vitro and confirmed in clinical studies against gram-positive aerobes - Enterococcus faecalis, Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus saprophyticus, Streptococcus pneumoniae (including multi-resistant strains - MDRSP), Streptococcus pyogenes ; gram-negative aerobes - Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus paraintluenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens and other microorganisms - Chlamydia pneumoniae, Mycoplasma pneumoniae.

For most (≥90%) strains of the following microorganisms, minimal inhibitory concentrations of levofloxacin (2 μg/ml or less) have been established in vitro, however, the effectiveness and safety of the clinical use of levofloxacin in the treatment of infections caused by these pathogens has not been established in adequate and well-controlled studies : gram-positive aerobes - Staphylococcus haemolyticus, Streptococcus (group C/F), Streptococcus (group G), Streptococcus agalactiae, Streptococcus milleri, Streptococcus viridans; gram-negative aerobes - Acinetobacter lwoffii, Acinetobacter baumannii, Bordetella pertussis, Citrobacter (diversus) koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter sakazakii, Klebsiella oxytoca, Morganella morganii, Pantoea (Enterobacter) agglomerans, Proteus vulgaris, Providencia rettgeri, Providencia s tuartii, Pseudomonas fluorescens ; gram-positive anaerobes - Clostridium perfringens.

Sensitive microorganisms: aerobic gram-positive microorganisms - Corynebacterium diphtheriae, Enterococcus spp., including Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive/leukotoxin-containing/moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive/moderately sensitive/resistant strains), Streptococcus pyogenes, Streptococcus spp. viridans group (penicillin-sensitive/resistant strains); aerobic gram-negative microorganisms - Acinetobacter spp., including Acinetobacter baumannii, Acinetobacillus actinomycetecomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp., including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus in fluenzae (ampicillin -sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp., including Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella Catarrhalis. Cypery beta-lactamaz strains), Morganella Morganii, Neisseria Gonorrhoeae (producing and non-income-propeling straw penicillinase) , Neisseria meningitidis, Pasteurella spp., including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida, Proteus vulgaris, Providencia spp., including Providencia rettgeri, Providencia stuartii, Pseudomonas spp., including Pseudomonas aeruginosa, Serratia spp., including Serratia marcescens, Salmonella spp.; anaerobic microorganisms - Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veilonella spp.; other microorganisms - Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (MIC more than 4 mg/l): aerobic gram-positive microorganisms - Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains); aerobic gram-negative microorganisms - Burkhoideria cepacia, Campylobacter jejuni, Campylobacter coli; anaerobic microorganisms - Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Resistant microorganisms (MIC more than 8 mg/ml): aerobic gram-positive microorganisms - Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains); aerobic gram-negative microorganisms - Alcaligenes xylosoxidane; other microorganisms - Mycobacterium avium.

Minimum inhibitory concentrations of levofloxacin for certain microorganisms

The in vitro activity of levofloxacin is approximately 2 times higher than that of ofloxacin against representatives of Enterobacteriaceae, Pseudomonas aeruginosa and gram-positive microorganisms.

In the case of using levofloxacin in the treatment of chlamydial diseases of the organs of vision, concomitant therapy is required.

The degree of sensitivity of microorganisms to levofloxacin may have significant geographical differences.
The maximum concentration of levofloxacin achieved using 0.5% eye drops is more than 100 times the minimum inhibitory concentration (MIC) of levofloxacin for sensitive microorganisms.

Drug interactions

There are reports of a pronounced decrease in the threshold of convulsive readiness with the simultaneous use of quinolones and substances that can, in turn, reduce the cerebral threshold of convulsive readiness. This also applies equally to the simultaneous use of quinolones and theophylline.

The effect of Levofloxacin is significantly weakened when used simultaneously with sucralfate. The same thing happens with the simultaneous use of magnesium or aluminum containing antacids, as well as iron salts. Levofloxacin should be taken at least 2 hours before or 2 hours after taking these medications. No interaction was detected with calcium carbonate.

When using vitamin K antagonists simultaneously, monitoring of the blood coagulation system is necessary.

The elimination (renal clearance) of levofloxacin is slightly slowed down by the action of cimetidine and probenecid. It should be noted that this interaction has virtually no clinical significance. However, with the simultaneous use of drugs such as probenecid and cimetidine, which block a certain excretion pathway (tubular secretion), treatment with levofloxacin should be carried out with caution. This applies primarily to patients with limited renal function.

Levofloxacin slightly increases the half-life of cyclosporine.

Taking glucocorticosteroids increases the risk of tendon rupture.

Overdose

Symptoms of an overdose of Levofloxacin appear at the level of the central nervous system (confusion, dizziness, disturbances of consciousness and seizures of the epileptic type). In addition, gastrointestinal disorders (for example, nausea) and erosive lesions of the mucous membranes, prolongation of the QT interval may occur.

Treatment should be symptomatic. Levofloxacin is not eliminated by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). There is no specific antidote.