L-Optic Rompharm, eye drops 0.5% 5 ml

The antimicrobial drug L-Optic is a broad-spectrum fluoroquinolone. It has bactericidal properties. Levofloxacin is able to block DNA-gyrease (topoisomeraseII) and topoisomeraseIV of bacterial microflora, disrupting superspiralization and elimination of DNA breaks. It inhibits DNA synthesis, causing profound morphological disruption of cytoplasm, cell wall and bacterial cell membranes.

Levofloxacin stays in the tear film for a long time after instillation.

Active against Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter diversus, Citrobacter freundii, Clostridium perfringens, Chlamydia pneumonia, Enterococcus faecalis, Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter sakazakii, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Legionella pneumophila, Moraxella catarrhalis, Mycoplasma pneumoniae, Morganella morganii, Proteus mirabilis, Pseudomonas aeruginosa, Pseudomonas fluorescens, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia marcescens, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes and Streptococcus agalactiae, Streptococcus spp. viridians group.

Pharmacokinetics

Levofloxacin persists well in the tear film after instillation into the eye. In studies on healthy volunteers, the average concentrations of levofloxacin in the tear film measured 4 and 6 hours after topical administration were 17 µg/ml and 6.6 µg/ml, respectively.

Five of six volunteers had levofloxacin concentrations of 2 μg/mL or higher 4 h after instillation. In four of the six volunteers this concentration was maintained 6 h after instillation. The mean concentration of levofloxacin in aqueous humor eye drops was statistically significantly higher than the mean concentration of ofloxacin (p=0.0008). In fact, it is approximately twice as high as the average ofloxacin concentration (1139.9±717.1 ng/mL and 621.7±368.7 ng/mL, respectively).

The mean plasma concentration of levofloxacin 1 h after administration ranged from 0.86 ng/mL at 1 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 concentrations of levofloxacin achieved on day 15 were more than 1,000 times lower than those observed after oral administration of standard doses of levofloxacin.

Indications

Infections of the anterior eye caused by microorganisms sensitive to levofloxacin.

Active ingredient

Composition

1 ml – levofloxacin (in hemihydrate form) 5 mg.

Auxiliary substances:

Sodium chloride – 8.75 mg,

benzalkonium chloride – 0.05 mg,

Hydrochloric acid 10% solution or sodium hydroxide 1M solution – to pH 6.5±0.05,

purified water – up to 1 ml.

How to take, the dosage

It is administered topically in the affected eye.

In children over 1 year and adult patients 1 or 2 drops are put into the affected eye conjunctivally up to 8 times daily (or every 2 hours) while awake. This continues for the first two days, then (day 3-7) the dosing regimen is switched to 4 times a day. The duration of use of L-optic is up to 7 days.

Interaction

After topical administration the Cmax of levofloxacin in plasma is 1000 times less than that of oral administration, so the effects of interaction with other drugs are unlikely.

Special Instructions

L-Optik Eye Drops 5% are not administered subconjunctivally and avoid direct contact with the anterior eye chamber.

To avoid infection of the solution, the pipette tip should not touch any surface.

Hypersensitivity reactions have been observed with fluoroquinolones, even after a single dose. If allergic reactions occur during treatment with levofloxacin, its use should be stopped immediately.

As with therapy with other antibiotics, long-term use of L-optic may lead to growth of fungi as well as other resistant microorganisms.

In treatment, if there is no improvement in the first 3 or 5 days, the drug should be withdrawn and an alternative therapy should be prescribed.

These eye drops are not indicated for use with soft contact lenses because they contain the preservative benzalkonium chloride, which is absorbed by contact lenses and can have adverse effects on the vision and cause discoloration of contact lenses.

Contact lenses of all types are contraindicated if you have symptoms of bacterial conjunctivitis.

The simultaneous administration of multiple topical ophthalmic drugs requires a 15-minute break between doses.

Influence on driving and operating machinery

If visual acuity decreases while injecting L-Optic drops, driving and operating dangerous machinery are not recommended until visual acuity returns to normal.

Contraindications

The use of the drug in children, adolescents under 18 years of age, and pregnant women should be used with extreme caution.

Side effects

Overdose

The volume of levofloxacin that one bottle of L-Optic drops contains is too small to cause significant toxic reactions even if ingested unintentionally. If the drops are applied topically in excess, the eye should be rinsed immediately with clean, running room temperature water.

Symptoms of overdose: erosive lesions of the gastrointestinal mucosa, nausea, prolongation of the QT interval, dizziness, confusion, seizures are possible if taken orally.

Treatment: symptomatic therapy, dialysis is ineffective.

Pregnancy use

Ongoing animal studies have not shown any specific risks. But since there are no data from clinical studies and because of the risk of fluoroquinolones on cartilage formation the drug can only be prescribed if the expected benefits of therapy for the mother exceed the possible risk to the fetus.

Breastfeeding should be discontinued if it is necessary to prescribe the drug during lactation.

Pediatric use

It is contraindicated in children under 1 year of age.

With caution: children under 18 years of age.

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