Ofloxacin Ophthalmic

OFLOXACIN OPHTHALMIC- ofloxacin solution
Apotex Corp.

ofloxacin-bottleofloxacin-carton

DESCRIPTION

Ofloxacin ophthalmic solution 0.3% is a sterile ophthalmic solution. It is a fluorinated carboxyquinolone anti-infective for topical ophthalmic use.

Chemical Name:

(±)-9-Fluoro-2, 3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H -pyrido[1,2,3-de ]-1,4 benzoxazine-6-carboxylic acid.

ofloxacin-01
(click image for full-size original)

Contains: Active: Ofloxacin 0.3% (3 mg/mL).

Preservative: benzalkonium chloride (0.005%). Inactives: Hydrochloric acid, sodium chloride and water for injection. Sodium hydroxide may be added to adjust the pH.

Ofloxacin ophthalmic solution 0.3% is unbuffered and formulated with a pH of 6.4 (range — 6.0 to 6.8). It has an osmolality of 300 mOsm/kg. Ofloxacin is a fluorinated 4-quinolone which differs from other fluorinated 4-quinolones in that there is a six member (pyridobenzoxazine) ring from positions 1 to 8 of the basic ring structure.

CLINICAL PHARMACOLOGY

Pharmacokinetics:

Serum, urine and tear concentrations of ofloxacin were measured in 30 healthy women at various time points during a ten-day course of treatment with ofloxacin ophthalmic solution. The mean serum ofloxacin concentration ranged from 0.4 ng/mL to 1.9 ng/mL. Maximum ofloxacin concentration increased from 1.1 ng/mL on day one to 1.9 ng/mL on day 11 after QID dosing for 10 1/2 days. Maximum serum ofloxacin concentrations after ten days of topical ophthalmic dosing were more than 1000 times lower than those reported after standard oral doses of ofloxacin.

Tear ofloxacin concentrations ranged from 5.7 to 31 μg/g during the 40 minute period following the last dose on day 11. Mean tear concentration measured four hours after topical ophthalmic dosing was 9.2 μg/g.

Corneal tissue concentrations of 4.4 μg/mL were observed four hours after beginning topical ocular application of two drops of ofloxacin ophthalmic solution every 30 minutes. Ofloxacin was excreted in the urine primarily unmodified.

Microbiology:

Ofloxacin has in vitro activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Ofloxacin is bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Ofloxacin is thought to exert a bactericidal effect on susceptible bacterial cells by inhibiting DNA gyrase, an essential bacterial enzyme which is a critical catalyst in the duplication, transcription, and repair of bacterial DNA.

Cross-resistance has been observed between ofloxacin and other fluoroquinolones. There is generally no cross-resistance between ofloxacin and other classes of antibacterial agents such as beta-lactams or aminoglycosides.

Ofloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival and/or corneal ulcer infections as described in the INDICATIONS AND USAGE section.

*Efficacy for this organism was studied in fewer than 10 infections

AEROBES, GRAM-POSITIVE: AEROBES, GRAM-NEGATIVE:
Staphylococcus aureus Enterobacter cloacae
Staphylococcus epidermidis Haemophilus influenzae
Streptococcus pneumoniae Proteus mirabilis
ANAEROBIC SPECIES: Pseudomonas aeruginosa
Propionibacterium acnes Serratia marcescens*

The safety and effectiveness of ofloxacin ophthalmic solution in treating ophthalmologic infections due to the following organisms have not been established in adequate and well-controlled clinical trials.ofloxacin ophthalmic solution has been shown to be active in vitro against most strains of these organisms but the clinical significance in ophthalmologic infections is unknown.

AEROBES, GRAM-POSITIVE:
Enterococcus faecalis Staphylococcus hominus
Listeria monocytogenes Staphylococcus simulans
Staphylococcus capitis Streptococcus pyogenes
AEROBES, GRAM-NEGATIVE:
Acinetobacter calcoaceticus var. anitratus Klebsiella pneumoniae
Acinetobacter calcoaceticus var. lwoffii Moraxella (Branhamella) catarrhalis
Citrobacter diversus Moraxella lacunata
Citrobacter freundii Morganella morganii
Enterobacter aerogenes Neisseria gonorrhoeae
Enterobacter agglomerans Pseudomonas acidovorans
Escherichia coli Pseudomonas fluorescens
Haemophilus parainfluenzae Shigella sonnei
Klebsiella oxytoca
OTHER:
Chlamydia trachomatis

Clinical Studies:

Conjunctivitis:

In a randomized, double-masked, multicenter clinical trial, ofloxacin ophthalmic solution was superior to its vehicle after 2 days of treatment in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trial demonstrated a clinical improvement rate of 86% (54/63) for the ofloxacin treated group versus 72% (48/67) for the placebo treated group after 2 days of therapy. Microbiological outcomes for the same clinical trial demonstrated an eradication rate for causative pathogens of 65% (41/63) for the ofloxacin treated group versus 25% (17/67) for the vehicle treated group after 2 days of therapy. Please note that microbiologic eradication does not always correlate with clinical outcome in anti-infective trials.

Corneal Ulcers:

In a randomized, double-masked, multi-center clinical trial of 140 subjects with positive cultures, subjects treated with ofloxacin ophthalmic solution had an overall clinical success rate (complete re-epithelialization and no progression of the infiltrate for two consecutive visits) of 82% (61/74) compared to 80% (53/66) for the fortified antibiotic group, consisting of 1.5% tobramycin and 10% cefazolin solutions. The median time to clinical success was 11 days for the ofloxacin treated group and 10 days for the fortified treatment group.

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