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Bacterial conjunctivitis is a common infectious disease of the eye, characterized by conjunctival hyperemia, eyelid edema, and purulent discharge. Although the prevalence and incidence are not well reported, bacterial conjunctivitis represents one of the most frequent causes of patient visits to both primary care physicians and ophthalmologists. Most cases of nongonococcal and nonchlamydial bacterial conjunctivitis are self-limiting and may resolve without intervention. There is a place for treatment, however, which allows for a shorter time to clinical and microbiological resolution which may decrease the mild morbidity, decrease health care costs of visits and potential complications, return patients back to school or the work force, and limit the potential spread of this communicable infection. Gatifloxacin ophthalmic solution is a broad spectrum 8-methoxyfluroroquinolone bactericidal antibiotic, with good activity against Staphylococcus aureus, Streptococcus species, and Gram-negative pathogens. It also has a relatively good resistance profile, making it a more than adequate choice in the treatment of bacterial conjunctivitis when therapy is warranted.

The aim of this study was to determine the efficacy of 0.3% gatifloxacin ophthalmic solution in preventing bacterial endophthalmitis in rabbits.Eighty-four (84) albino phakic rabbits were injected unilaterally with 2 x 10(4) colony forming units of Enterococcus faecalis into the anterior chamber. The eyes received 0.3% ofloxacin ophthalmic ointment or 0.3% gatifloxacin ophthalmic solution with different regimens in three separate experiments: (1) 1 or 3 drops of gatifloxacin every 2 h or a single application of ofloxacin for 1 day; (2) 3 drops/day of gatifloxacin application started at 0, 6, and 24 h postinoculation, or 1 drop at 0 h, and 3 times daily gatifloxacin for the following 3 days; and (3) 1 or 3 drops of gatifloxacin application started at 0 h and no further application for the following 3 days. The control eyes received no treatment in the three experiments. The effectiveness of these different regimens was assessed by slit-lamp biomicroscopy and bacterial colony counts. The ocular penetration of the drugs was determined in a separate experiment, using 36 normal albino rabbits.The concentration-time curves for gatifloxacin and ofloxacin appeared parallel, with mean peak concentrations of 1161 and 219 ng/mL, respectively, at 1 h postinstillation. In Experiment 1, gatifloxacin significantly reduced the inflammation and the number of living bacteria in the aqueous humor, compared with controls, whereas ofloxacin ointment did not. A single application of ofloxacin ointment was not better than 1 drop of gatifloxacin. The results of Experiment 2 showed that the effectiveness of gatifloxacin decreased as the interval between the inoculation and the onset of treatment increased. In Experiment 3, only 3 drops of gatifloxacin on day 1 kept the inflammation significantly lower than that in the control for 4 days.Immediate postoperative prophylaxis would likely be effective in reducing the risk of enterococcal endophthalmitis by topical gatifloxacin.

Infectious keratitis can be a medical emergency that can lead to a profound loss of vision if not treated promptly and appropriately. Although a shift in the etiology and predisposing factors has been reported within the past few years, bacteria still predominate as the causative organisms of infectious keratitis in temperate climates. The clinical outcome is greatly influenced by the rate of epithelial and stromal healing, which is affected by multiple factors, including the overall health of the patient, status of the ocular surface and selection of the topical ophthalmic preparations used during treatment. Fourth-generation fluoroquinolones, including gatifloxacin, have been widely adopted for an ‘off-label’ treatment of bacterial keratitis because of their broad-spectrum potency and effective penetration, as well as their minimal effects on corneal wound healing.

Pediatric bacterial conjunctivitis is a common, highly contagious infection that requires prompt and effective therapy. In the treatment of bacterial conjunctivitis, gatifloxacin ophthalmic solution 0.3% (Allergan, Inc.) is associated with high clinical cure rates and a low rate of mostly mild adverse effects. In vitro, gatifloxacin ophthalmic solution 0.3% demonstrates bactericidal activity against a broad spectrum of ocular pathogens associated with bacterial conjunctivitis, including many that are resistant to other antibiotics. Gatifloxacin was designed to be less likely than earlier generations of antibiotics to promote antibiotic resistance and is associated with high susceptibility rates. These properties make gatifloxacin an appropriate choice for conditions that require safe and effective treatment in this age of increasing antibiotic resistance.

The claim that benzalkonium chloride (BAK) synergistically enhances the antibiotic efficacy of gatifloxacin ophthalmic solution 0.3% (preserved with 0.005% BAK [50 microg/mL), Zymar; Allergan Inc., Irvine, Calif, USA) has been the subject of several studies. The purpose of this prospective clinical study was to test the hypothesis that BAK would be significantly diluted shortly after topical ocular administration and would thereafter have little or no effect on the enhancement of the antibiotic efficacy of commercial gatifloxacin on the ocular surface. This hypothesis was tested by investigators who measured the concentration of tear film BAK at successive time points after topical administration of commercial gatifloxacin. After subjects (N=10) received 5 separate instillations of a single 35-microL drop of gatifloxacin 0.3% ophthalmic solution in each eye, tear samples were collected at 30 sec, 1 min, 3 min, 5 min, and 20 min, with the use of graduated 5-microL glass microcapillaries. A validated high-performance liquid chromatography method was used to measure the concentration of BAK in each tear sample. The results showed rapid BAK dilution to 6.4 microg/mL, 3.2 microg/mL, 1.4 microg/mL, below the detection limit, and below the detection limit at 30 sec, 1 min, 3 min, 5 min, and 20 min after instillation of a single 35-microL drop of gatifloxacin. Because such rapid dilution reduces the concentration of BAK to near zero in minutes and does not allow the time (1 h) required for effective bacterial kill power, BAK is not expected to have a clinically significant effect on enhancement of the antimicrobial efficacy of gatifloxacin on the human ocular surface.

To evaluate the effect of gatifloxacin ophthalmic solution 0.3% (Zymar, Allergan, Inc., Irvine, CA, USA) on corneal endothelial cell density and morphology and to measure gatifloxacin penetration into aqueous humor.This was a single-center, open-label clinical study. Ten patients undergoing standard cataract surgery and 20 nonsurgical subjects instilled gatifloxacin 0.3% four times per day for 2 days, then every 10 min for 1 hr on the third day (the surgery day for the cataract patients). Corneal endothelial cells were counted using noncontact specular microscopy. Anterior chamber fluid was withdrawn from the surgical patients, and the gatifloxacin concentration was quantified by high-pressure liquid chromatography.Baseline endothelial cell counts (mean +/- SD) were 2400 +/- 442 in the surgical group and 2520 +/- 212 in the nonsurgical group. The mean differences from baseline 1 hr after the last dose of gatifloxacin 0.3% were -51 +/- 213 (p = 0.23) in the surgical group and -7 +/- 150 (p = 0.42) in the nonsurgical group. In the nonsurgical group, the mean difference from baseline 3 weeks after the last dose was 18 +/- 147 (p = 0.71). The mean concentration (+/- SD) of gatifloxacin in aqueous humor was 1.26 +/- 0.55 microg/ml.A preoperative, prophylactic course of gatifloxacin 0.3% ophthalmic solution did not significantly affect endothelial cell density or morphology, while meaningful drug concentration was achieved in the aqueous humor.

Gatifloxacin is a fourth generation fluroquinolone antibiotic that has been prescribed for systemic use. However, the drug which was developed by Kyorin (Japan) was linked to toxic reactions and death and was banned in the United States and Canada for use as an oral dosage form. It continues to be used as a topical application for ophthalmic conditions as the systemic toxicity seen when taking the drug orally has not been observed with ophthalmic use. The available data indicate that ocular use of gatifloxacin is safe, and effective against a broad spectrum of bacteria, including intracellular bacteria and anaerobes.