Levofloxacin 0.5% Ophthalmic Solution: A Review of its Use in the Treatment of External Ocular Infections and in Intraocular Surgery

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Abstract

Levofloxacin 0.5% ophthalmic solution (Cravit®, Quixin®, Oftaquix®) has well established efficacy and tolerability in the treatment of external ocular infections. Levofloxacin 0.5% ophthalmic solution was generally more effective than ofloxacin 0.3% ophthalmic solution in the treatment of external ocular infections, and noninferiority was seen between levofloxacin 0.5% ophthalmic solution and both moxifloxacin 0.5% and tosufloxacin 0.3% ophthalmic solutions in the treatment of bacterial conjunctivitis. Although levofloxacin 0.5% ophthalmic solution administered in the hour prior to surgery did not reduce the incidence of endophthalmitis in patients undergoing intraocular surgery, additional data are needed to examine an optimal preoperative regimen of this antibacterial; preoperative levofloxacin 0.5% ophthalmic solution plus an iodine eyewash reduced positive culture rates in patients undergoing intraocular surgery. Levofloxacin 0.5% ophthalmic solution was well tolerated in the treatment of external ocular infections. Thus, levofloxacin 0.5% ophthalmic solution remains an important option in the treatment of bacterial conjunctivitis and other external ocular infections, as well as for perioperative use.

Pharmacological Properties

Levofloxacin had in vitro activity against a broad spectrum of Gram-positive and -negative bacteria, according to the results of Japanese studies using ocular isolates. The results of the US Ocular TRUST study demonstrate that susceptibility to levofloxacin was seen in 100% of Streptococcus pneumoniae and Haemophilus influenzae ocular isolates, and 81.1% of meticillin (methicillin)-susceptible Staphylococcus aureus ocular isolates. An identical susceptibility pattern was seen for moxifloxacin and gatifloxacin; the susceptibility of S.pneumoniae to ciprofloxacin was 89.9%. Longitudinal analysis of US Ocular TRUST data demonstrated that the susceptibility of S. pneumoniae to levofloxacin remained stable over an 8-year period. High-level resistance of ocular isolates to levofloxacin generally required a double mutation.

Pharmacological Properties

Following administration of levofloxacin 0.5% ophthalmic solution to healthy volunteers or patients undergoing ocular surgery, mean levofloxacin concentrations in the tears, conjunctiva and cornea consistently exceeded the minimum concentration required to inhibit 90% of isolates (MIC90) for clinically relevant pathogens. Levofloxacin concentrations in the aqueous humour varied according to the administration regimen and were higher than the MIC90 values of some, but not all, clinically relevant pathogens.

Clinical Efficacy

Levofloxacin 0.5% ophthalmic solution was effective in the treatment of bacterial conjunctivitis. Microbial eradication and clinical cure rates were significantly higher with levofloxacin 0.5% ophthalmic solution than with placebo in a US study. In another US study, levofloxacin 0.5% ophthalmic solution was significantly more effective than ofloxacin 0.3% ophthalmic solution in terms of microbial eradication rates. In terms of clinical efficacy, noninferiority was seen between levofloxacin 0.5% ophthalmic solution and both moxifloxacin 0.5% and tosufloxacin 0.3% ophthalmic solutions in two Japanese studies. In a Polish study, the clinical cure rate did not significantly differ between 5-day regimens in which levofloxacin 0.5% ophthalmic solution was instilled three times daily or 2- then 4-hourly; the noncompliance rate was significantly lower with the three-times-daily regimen than with the 2- then 4-hourly regimen. Subgroup analyses also demonstrated the efficacy of levofloxacin 0.5% ophthalmic solution in the treatment of bacterial conjunctivitis in paediatric patients.

Clinical Efficacy

The clinical efficacy rate was significantly higher with levofloxacin 0.5% ophthalmic solution than with ofloxacin 0.3% ophthalmic solution in patients with various external ocular infections, according to the results of a Japanese study. A large, multicentre, postmarketing surveillance study conducted in Japan also showed the efficacy of levofloxacin 0.5% ophthalmic solution in the treatment of external ocular infections; the overall clinical efficacy rate was 96%.

Clinical Efficacy

The ESCRS study demonstrated that in patients undergoing intraocular surgery, the incidence of total or proven infective endophthalmitis was significantly higher in patients not receiving intracameral cefuroxime than in patients receiving intracameral cefuroxime, whereas there was no significant difference between patients not receiving levofloxacin 0.5% ophthalmic solution and those receiving levofloxacin 0.5% ophthalmic solution. Two surrogate endpoint studies in patients undergoing intraocular surgery demonstrated that in terms of positive culture rates, a 3-day regimen of levofloxacin 0.5% ophthalmic solution was generally more effective than a 1-hour or 1-day regimen, and that levofloxacin 0.5% ophthalmic solution plus povidone iodine was more effective than povidone iodine alone.

Tolerability

Levofloxacin 0.5% ophthalmic solution was well tolerated in the treatment of external ocular infections (including in paediatric patients), with the majority of treatment-related adverse events being of mild to moderate severity. Forty-six treatment-related adverse events were reported in 42 of the 6686 patients (0.63%) with external ocular infections who received levofloxacin 0.5% ophthalmic solution in a postmarketing surveillance study. The most commonly reported treatment-related adverse events, none of which were serious, included blepharitis, eye irritation, punctate keratitis, keratitis and ocular pruritus. The tolerability profile of levofloxacin 0.5% ophthalmic solution was generally similar to that of ofloxacin 0.3%, moxifloxacin 0.5% and tosufloxacin 0.3% ophthalmic solutions, although palpebral conjunctival injection improved to a significantly greater extent with levofloxacin than with ofloxacin, and burning/stinging resolved in significantly more levofloxacin than ofloxacin recipients.

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