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 OCUFLOX® 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 OID dosing for 10 ½ 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 pg/mL were observed four hours after beginning topical ocutar application of two drops of OCUFLOX® 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:

ANAEROBIC SPECIES:

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

The safety and effectiveness of OCUFLOX® in treating ophthalmologic infections due to the following organisms have not been established in adequate and well-controlled clinical trials. OCUFLOX® 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:

AEROBES, GRAM-NEGATIVE:

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