Ofloxacin

OFLOXACIN — ofloxacin solution/ drops
American Regent, Inc.

Sterile

Rx Only

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.

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Contains: Active: ofloxacin 0.3% (3 mg/mL).
Preservative: benzalkonium chloride (0.005%).Inactives: sodium chloride and Water for Injection. May also contain hydrochloric acid and/or sodium hydroxide to adjust pH.

Ofloxacin ophthalmic solution 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.

AEROBES, GRAM-POSITIVE: AEROBES, GRAM-NEGATIVE:
Staphylococcus aureus Enterobacter cloacae
Staphylococcus epidermidis Haemophilus influenzae
Streptococcus pneumoniae Proteus mirabilis
Pseudomonas aeruginosa
ANAEROBIC SPECIES: Serratia marcescens*
Propionibacterium acnes
*Efficacy for this organism was studied in fewer than 10 infections

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)
Citrobacter diversus catarrhalis
Citrobacter freundii Moraxella lacunata
Enterobacter aerogenes Morganella morganii
Enterobacter agglomerans Neisseria gonorrhoeae
Escherichia coli Pseudomonas acidovorans
Haemophilus parainfluenzae Pseudomonas fluorescens
Klebsiella oxytoca Shigella sonnei
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 trial of 140 subjects with positive cultures, ofloxacin ophthalmic solution treated subjects 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.

INDICATIONS AND USAGE

Ofloxacin ophthalmic solution is indicated for the treatment of infections caused by susceptible strains of the following bacteria in the conditions listed below:

CONJUNCTIVITIS:
Gram-positive bacteria: Gram-negative bacteria:
Staphylococcus aureus Enterobacter cloacae
Staphylococcus epidermidis Haemophilus influenzae
Streptococcus pneumoniae Proteus mirabilis
Pseudomonas aeruginosa
CORNEAL ULCERS:
Gram-positive bacteria: Gram-negative bacteria:
Staphylococcus aureus Pseudomonas aeruginosa
Staphylococcus epidermidis Serratia marcescens*
Streptococcus pneumoniae
Anaerobic species:
Propionibacterium acnes
*Efficacy for this organism was studied in fewer than 10 infections.
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