L-optic eye drops 0.5%, 5 ml

• Treatment of superficial bacterial eye infections caused by sensitive microorganisms in adults and children over 1 year old;

• prevention of complications after surgical and laser eye surgeries.

When using the drug, official national guidelines for the appropriate use of antibacterial drugs, as well as the sensitivity of pathogenic microorganisms in a particular country, should be taken into account.

Apply topically to the affected eye.

Instill 1-2 drops into the affected eye (s) every 2 hours up to 8 times / day during wakefulness during the first 2 days, then 4 times / day from the 3rd to the 5th days. The duration of the course of treatment is determined by the severity of the condition, clinical manifestations and bacteriological characteristics. The average duration of the course of therapy is 5 days. When using several drugs, the interval between their instillations should be at least 15 minutes.

Eye drops in the form of a clear solution from pale yellow to light yellow with a greenish tinge.

1 ml

levofloxacin (in the form of hemihydrate) 5 mg

Excipients: sodium chloride - 8.75 mg, benzalkonium chloride - 0.05 mg, hydrochloric acid solution 10% or sodium hydroxide solution 1M - up to pH 6.5 ± 0.05, purified water - up to 1 ml.

• Children under 1 year old;

• hypersensitivity to drug components;

• hypersensitivity to levofloxacin and other quinolones.

pharmachologic effect

Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones. The active substance contains levofloxacin - the levorotatory isomer of ofloxacin.

Levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and stitching of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall and membranes of microbial cells.

Levofloxacin is active against most strains of microorganisms in vitro and in vivo.

Sensitive microorganisms (minimum inhibitory concentration (MIC) <2 mg / ml, zone of inhibition> 17 mm):

• aerobic gram-positive microorganisms: Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium jeikeium, Enterococcus spp. (including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (coagulase negative methicillin susceptible / moderately susceptible strains), Staphylococcus aureus (methicillin susceptible strains), Staphylococcus epidermidis (methicillin susceptible strains), Staphylococcus spp. (leukotoxin-containing); Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumonia (penicillin-sensitive / moderately sensitive / resistant strains), Streptococcus pyogenes, Streptococcus spp. viridian groups (penicillin-sensitive / resistant strains);

• aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp. (Enterobacter aerogenes, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenza (ampicillin-susceptible / resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (strains producing and non-producing ?-lactamase), Morganella morganii, Neisseria gonorrhoeae (producing and non-producing strains. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (incl.Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (hospital-acquired Pseudomonas aeruginosa infections may require combination treatment), 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 spp. (including Legionella pneumophila), Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (MIC = 4 mg / l; zone of inhibition 16-14 mm):

• aerobic gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains);

• aerobic gram-negative microorganisms: Campylobacter jejuni, Campylobacter coli;

• anaerobic microorganisms: Prevotella spp., Porphyromonas spp.

Resistant microorganisms (MIC> 8 mg / L; zone of inhibition <13 mm):

• aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains);

• aerobic gram-negative microorganisms: Alcaligenes xylosoxidans;

• anaerobic microorganisms: Bacteroides thetaiotaomicron;

• other microorganisms: Mycobacterium avium.

Levofloxacin resistance develops as a result of a stepwise process of mutations in genes encoding both type II topoisomerases: DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as the mechanism of influence on the penetration barriers of the microbial cell (a mechanism characteristic of Pseudomonas aeruginosa) and the efflux mechanism (active removal of the antimicrobial agent from the microbial cell), can also reduce the sensitivity of microorganisms to levofloxacin.

Due to the peculiarities of the mechanism of action of levofloxacin, there is usually no cross-resistance between levofloxacin and other antimicrobial agents.

Pharmacokinetics

After instillation into the eye, levofloxacin is well preserved in the tear film. In studies on healthy volunteers, it was shown that the average concentrations of levofloxacin in the tear film, measured 4 and 6 hours after topical application, were 17 ?g / ml and 6.6 ?g / ml, respectively. In five out of six volunteers, levofloxacin concentrations were 2 ?g / ml and higher 4 hours after instillation. In four out of six volunteers, this concentration remained 6 hours after instillation.

The average concentration of levofloxacin when using eye drops in aqueous humor is statistically significantly higher than the average concentration of ofloxacin (p = 0.0008). In fact, it is approximately twice as high as the average concentration of ofloxacin (1139.9 ± 717.1 ng / ml and 621.7 ± 368.7 ng / ml, respectively).

The average concentration of levofloxacin in blood plasma 1 hour after application is from 0.86 ng / ml on the first day to 2.05 ng / ml. Cmax of levofloxacin in plasma, equal to 2.25 ng / ml, was detected on the 4th day after two days of using the drug every 2 hours up to 8 times / day. Cmax of levofloxacin, reached on the 15th day, is more than 1000 times lower than the concentrations observed after ingestion of standard doses of levofloxacin.

Side effect

Classification of adverse reactions by organs and systems, indicating the frequency of their occurrence: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), incl. individual messages; the frequency is unknown (the frequency cannot be estimated from the available data).

The incidence of adverse reactions during therapy with levofloxacin was about 10%. Mild to moderate adverse reactions were noted predominantly on the part of the organ of vision.

From the side of the immune system: rarely - systemic allergic reactions, incl. skin rash; very rarely - anaphylactic shock.

From the nervous system: infrequently - headache.

From the side of the organ of vision: often - burning in the eye, decreased vision, filamentous mucous discharge in the conjunctival cavity; infrequently - chemosis, conjunctival injection, papillary conjunctivitis, eyelid edema, eyelid erythema, eye discomfort, itchy eye, eye pain, dry eye syndrome, photophobia.

From the respiratory system: infrequently - rhinitis, very rarely - laryngeal edema.

If the patient has side effects indicated in the instructions, or they are aggravated, or any other side effects not indicated in the instructions are noted, it is necessary to inform the doctor about this.

Application during pregnancy and lactation

Pregnancy

There is insufficient data on the use of levofloxacin in pregnant women. The results of preclinical studies do not indicate a direct or indirect adverse effect in terms of toxic effects on reproductive function and intrauterine development. The potential risk of the drug to humans is unknown. Levofloxacin eye drops can be used during pregnancy if the potential benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding period

Levofloxacin passes into breast milk. However, when using levofloxacin in therapeutic doses, an effect on the infant is not expected. Levofloxacin eye drops can be used during breastfeeding if the potential benefit to the mother outweighs any potential risk to the infant.

Fertility

After topical application, levofloxacin did not cause impairment of fertility in rats when exposed to much higher than the maximum human dose.

Application in children

Contraindicated in children under 1 year of age.

special instructions

To avoid contamination of the solution, do not touch the tip of the dropper to the eyelids and tissues around the eye.

L-Optic Rompharm, eye drops 0.5%, cannot be administered subconjunctivally and into the anterior chamber of the eye.

Fluoroquinolones for systemic use can cause allergic reactions, even after a single use. If allergic reactions occur during treatment with levofloxacin, you must immediately stop using the drug.

With long-term treatment with levofloxacin (as well as with other antibiotics), excessive growth of insensitive microorganisms is possible, incl. fungal flora.

If the course of the disease worsens or there is no improvement in the use of the drug, it is necessary to cancel therapy with levofloxacin and switch to therapy with antibacterial drugs of other groups, with an extended ophthalmological examination, including biomicroscopy and a fluorescein test.

There are no data on the efficacy and safety of levofloxacin in the treatment of corneal ulcers. In the course of clinical studies, the formation of corneal precipitates was not observed.

Drops should not be used when wearing soft contact lenses, due to the presence of benzalkonium chloride in the drops, which can be absorbed by contact lenses and have an adverse effect on the eye tissue and cause discoloration of contact lenses.

Contact lenses of any type should not be worn if you have symptoms of bacterial conjunctivitis.

With the simultaneous use of several ophthalmic preparations for topical use, it is necessary to observe a 15-minute interval between instillations.

The prevalence of acquired resistance in plated strains of microorganisms can vary depending on the geographic region and over time. Therefore, country-specific information on levofloxacin resistance is required. For the treatment of severe infections or in case of ineffectiveness of treatment, a microbiological diagnosis should be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin.

Use in pediatrics

If the drug is used in children, it is necessary to consult a doctor before taking the drug.

Influence on the ability to drive vehicles and use mechanisms

The drug does not significantly affect the ability to drive vehicles and mechanisms. Immediately after instillation, temporary blurred vision is possible. It is not recommended to drive vehicles and engage in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, until the clarity of visual perception is restored.

Overdose

The amount of levofloxacin contained in one bottle of eye drops is too small to cause toxic reactions even after accidental ingestion. After topical application of an excess dose of eye drops, the eyes should be rinsed with clean (tap) water at room temperature.

Drug interactions

Because Cmax of levofloxacin in plasma after topical application is 1000 times less than after oral administration, the effects of interaction with other drugs are unlikely.