LOMEFLOX
Eye Drops
Composition:
Each ml contains Lomefloxacin 3
mg (as hydrochloride 3.31 mg)
Properties:
Lomefloxacin, a difluorioniated
quinolone derivative, is a bacterial gyrase inhibitor, effective
against gram positive and gram negative bacteria. Lomefloxacin
interferes with bacterial DNA related processes like initiation,
elongation and termination phases of replication, transcription,
DNA repair, recombination, transposition, supercoling and
relaxation of DNA, resulting in a rapid killing of sensitive
bacteria.
Cross-resistance has only been
reported with other quinolones, but not with any other group
of antibiotics. No clinical studies are available about the
efficacy in case infections with chlamydia.
Antimicrobial spectrum:
The antimicrobial spectrum includes
the following gram-positive and gram-negative bacteria, as
reported from various in vitro studies:
Sensitive germs (MIC90<4µg/ml):
Gram Positive: Staphylococcus epidermidis,
S. aureus, Bacillus,
Corynebacterium
Gram Negative: Branhamella catarrhalis, Neisseria spp. Alcaligenes faecalis, Enterobacter
spp., Flavobacterium spp., Acinetobacter
spp., Heamophilus influenza, Klebsiella, Proteus, Pseudomonas
aeruginosa, Psedomans spp., Serratia spp.
Anaerobic germs:
Propionibacterium
acnes.
Intermedium sensitives germs (MIC90= 4 -16µg/ml):
Gram- Positive:
Streptococcus pneumoniae, Streptococcus sp., Micrococcus,
Enterococcus faecalis.
Resistant germs (MIC90>16µg/ml):
Clostridium difficile, Mycobacterium, Fungi.
Pharmacokinetics:
In rabbits, topical application
of 50 µl solution
containing 0.3% 14 C- labelled Lomefloxacin revealed
the following results:
Cmax (µg-Eq/g) Tmax(minutes)
Cornea
55.68
15
Conjunctiva
11.39
15
Aqueous humour
7.58
60
In animal studies, tear levels
after two application of 50 µl of 0.3% Lomefloxacin were at
40-200 µg/ml at 2 hours and still 7-27 µg/ml at 6 hours. Even
at 24 hours more than 3 µg/ml were
observed. Although these results cannot directly be transferred
to the human eye since physiology of the cornea and penetration
through the cornea varying considerably between rabbits and
humans, penetration of Lomefloxacin through the human cornea
has been confirmed. In humans, concentration however may not
be high enough for the treatment of endophthalmitis.
Systemic absorption following topical
ophthalmic application of 0.3% Lomefloxacin eye drop is very
low. After application of four times daily 2 drops two weeks,
blood levels were below the detection limit of
0.005 µg/ml.
Indications:
Bacterial infections,
including conjunctivitis, blepharitis and blepharo-conjunctivitis
which are due to Lomefloxacin susceptible germs.
Dosage/Use:
Adults and children (above 1 year
of age): Apply 2-3 times daily 1 drop into the lower conjunctival
sac. At the beginning of the treatment application should
be more frequent, apply 5 drops within 20 minutes or 1 drop
every hour during 6-10 hours. Duration of the treatment: 7
to 9 days.
Contraindications:
Hypersensitivity to
the active ingredient, to excipients, or to quinolones. No adverse effects were noted
in children included in clinical studies, although this data
are limited.
Precautions:
Long term treatment with antibiotic
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 Lomefloxacin intensive exposure to sunlight
or UV-radiation should be avoided.
Pregnancy and lactation:
After high systemic doses of Lomefloxacin
(50-100mg/kg), variations 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 execrated into the maternal milk. Clinical
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 foetus or the infant.
Adverse reactions:
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
ophthalmic use, photosensitization is possible. Since the
following allergic reactions have been reported after systemic
use of Lomefloxacin, they cannot be excluded after topical
ophthalmic use: allergic reactions, asthma, dyspnoea, urticaria,
erythema, pruritus and hypersensitization.
Drug Interactions:
In order to avoid reduction of
efficacy, no ophthalmic preparation containing heavy metals,
such as zinc, should be used during 15 minutes preceding and
following application of Lomeflox.
Bacteriostatic ophthalmic
antibiotics should not be used concomitantly with Lomefloxacin
eye drops. Other interactions have not been described to date.
Over dose:
There is practically no risk of
adverse effect due to accidental oral ingestion, since a bottle
of 5 ml eye drop solution contains only 15 mg Lomefloxacin.
This corresponds to 3.7% 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.
Additional Information:
None of patients wearing
contact lenses: Contact lenses should not be worn during ophthalmic
infection. When two or more ophthalmic preparation
are used concomitantly, an interval
of at least 5 minutes should be observed between the medication,
in order to avoid washing out of the drug.
Lomeflox eye drops may be used up to the
date indicated with “EXP” on the pack. Close the bottle immediately
after use. Store at room temperature (<25o C) and protect from light. Do
not use longer than 1 month after first opening. Keep out
of the reach of children.
Packing:
Dropper bottle of
5 ml.
