Class: Eye, Nose and Ear
Dosage Form: Eye Drops
Description: Broad spectrum bactericidal fluoroquinolone antibiotic
Stock: Out of Stock
Each 1 ml contains:
Disodium edetate…………………….0.1 mg
Dodium hydroxide………………….1 N q.s.
Water for injection to………………….1 ml
Benzalkonium chloride………….0.02 mg
Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor effective against gram positive and gram negative bacteria. The acute toxicity of Lomefloxacin following systemical and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA related processes like initiation, elongation, and termination phases of replication, transcription, DNA repair, recombination, transposition, supercoiling and relaxation of DNA.
The target molecule for quinolones is the A subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole tetramer A2B2 leads to impaired enzyme functions, resulting in a rapid killing of bacteria. Plasmid mediated transfer of resistance has not been observed so far. The frequency of development of resistance through spontaneous mutations is less than 10-8 to 10-9, thus in the same range as other quinolones.
Cross-resistance has only been reported with other quinolones, but not with any other group antibiotics. No clinical studies are available about the efficacy in cases of infections with chalmydia.
The antimicrobial spectrum includes gram-positive and gram-negative bacteria, as reported from various in-vitro studies.
A meta-analysis based on phase II and phase III clinic studies revealed the following sensitive organisms:
a) Sensitive Germs: (MIC90 < 4 mcg/ml)
- Gram-positive: Staphylococcus epidermidis, S. aureus, Bacillus, Corynebacterium
- Gram-negative: Branhamella catarrhalis, Neisseria sp., Acinetobacter ssp., Alcaligenes faecalis,-Enterobacter spp., Flavobacterium spp., Haemophilus influenzae, Klebsiella, Moraxella, Proteus, Pseudomonas aeruginosa, Pseudomonas spp., Serratia spp.
- Anaerobics: Propionibacterium acnes
b) Intermediate sensitive germs: (MIC90 = 4-16 mcg/ml)
- Gram-positive: Streptococcus pneumoniae, Streptococcus spp., Micrococcus, Enterococcus faecalis
c) Resistant germs: (MIC90 > 16 mcg/ml)
- Clostridium difficile, Mycobacterium, fungi
Bacterial infections, including conjunctivitis, blepharitis, and blepharo-conjunctivitis which are due to Lomefloxacin susceptible germs.
Hypersensitivity to the active ingredient, excipients, or to quinolones.
In animal studies, arthrotoxicity in juvenile rats was reported at high (300 mg/kg) but not at low (<100 mg/kg) dosages. Topical application, even with complete absorption, leads to a total dosage of only about 2 mg/day. The maximum daily dose per kg is therefore in the range of about 20-50 mcg/kg which is several orders of magnitude below the arthrotoxic threshold. No adverse effects were noted in children included in clinical studies, although these data are limited.
In order to avoid reduction of efficacy, no ophthalmic preparations containing heavy metals, such as zinc, should be used during 15 minutes preceding and following application of Okacin.
Bacteriostatic ophthalmic antibiotics should not be used concomitantly with Okacin eye drops. Other interactions have not been described to date.
Slight and transient burning immediately after instillation of the eye drops has been reported in 4.7% of users. Although phototoxicity has not been reported after ophalmic use, photosensitization is possible. Since the following allergic reactions have been reported after systemic use of Lomefloxacin, they can not be excluded after topical ophthalmic use: allergic reactions, asthma, dyspnoea, urticaria, eryhtmea, pruritus, and hypersensitization.
Dosage and Administration:
Adults and children (above 1 year of age): Insert 2-3 times daily 1 drop into the lower cojunctival sac. At the beginning of the treatment applications should be more frequent, apply 5 drops witing 20 minutes or 1 drop every hour during 6-10 hours. Duration of the treatment is 7 to 9 days.
There is particularly no risk of adverse effects due to accidental oral ingestion, since a bottle of 5 ml eye drop solution contains only 15 mg Lomefloxacin. This corresponds to 3.75% of the recommended oral daily dose for adults of 400 mg Lomefloxacin. In case of systemic ingestion irrigation of the stomach may be appropriate in young children to decrease further absorption.
Pregnancy and Lactation:
After high systemic doses of Lomefloxacin (50-100 mg/kg), variation of caudal vertebrae have been observed in rabbit foetus. Furthermore, animal studies revealed that after systemic use of 20 mg/kg, Lomefloxacin passes the placenta barrier and is excreted into the maternal milk. Clincal studies on the use of Lomefloxacin eye drops during human pregnancy or lactation are not available. Therefore, the drug should only be used when the benefit outweighs the potential risk for the fetus or the infant. Pregnancy category C.
Long term treatment with antibiotics may enhance development of secondary fungal infections or may support growth of non-susceptible bacteria.
Some isolated cases of phototoxicity have been reported after systemic but not after topical ophthalmic use of Lomefloxacin. Nevertheless, during treatment with Okacin intensive exposure to sunlight or UV-radiation should be avoided.
Contact lenses should not be worn during administration of most ophthalmic solutions.
Store at room temperature, below 25°C.