Review of third-and fourth-generation fluoroquinolones in ophthalmology: in-vitro and in-vivo efficacy

Abstract

Fourth-generation agents have increased potency against Gram-positive bacteria compared with levofloxacin, while maintaining similar potency against Gram-negative bacteria. Although levofloxacin 1.5% has demonstrated superior ocular penetration relative to gatifloxacin, the limited available data do not suggest this translates into superior clinical activity compared with moxifloxacin, which has significantly greater ocular penetration and better Gram-positive potency than gatifloxacin.

Phenotypic and molecular characterization of quinolone resistance in Mycobacterium abscessus subsp. bolletii recovered from postsurgical infections

“…Fourth-generation quinolones are important drugs used in ophthalmology and are more effective against Gram-positive bacteria compared to the other generations (Scoper, 2008;Stroman et al, 2005). This generation has also been demonstrated to be more active against mycobacteria and less affected by mutations in DNA gyrase .…”

Toxic Anterior Segment Syndrome (TASS) and Prophylaxis Against Postoperative Endophthalmitis

“…It has been suggested that moxifloxacin would be preferable to cefuroxime because of its broader spectrum of action, better MIC levels and lower bacterial resistance. (O´Brien et al, 2007) (Scoper, 2008) (Jensen et al, 2008). Moxifloxacin is available as a self-preserved commercial ophthalmic formulation and requires no special preparation for intracameral therapy.…”

Emerging 8-Methoxyfluoroquinolone Resistance among Methicillin-Susceptible Staphylococcus epidermidis Isolates Recovered from Patients with Endophthalmitis

“…Coagulase-negative staphylococci (CoNS), including the most common species, Staphylococcus epidermidis, are the most frequently isolated organisms from culture-proven endophthalmitis cases (1,4,5). Topical fluoroquinolone agents (ciprofloxacin, ofloxacin, and levofloxacin) have been widely used as the first-line option for both prophylaxis and management of endophthalmitis and other ocular infections (6,7). However, recovery of ocular fluoroquinolone-resistant pathogens emerged soon after the introduction and widespread use of these agents in the 1990s and has significantly increased in the last 2 decades (7,8).…”

“…The 8-methoxyfluoroquinolones, gatifloxacin (Zymar; Allergan) and moxifloxacin (Vigamox; Alcon), are the most frequent and widely used agents in ophthalmology due to their increased potency against Gram-positive pathogens and reduced rates of resistance compared with the older fluoroquinolones (6,7). Despite its withdrawal for systemic use, gatifloxacin is still available for topical ophthalmic use in well-tolerated eye drop formulations of 0.3% and 0.5%.…”

“…Both gatifloxacin and moxifloxacin inactivate simultaneously the topoisomerases II (DNA gyrase) and IV, which are necessary for DNA replication, while older fluoroquinolones, including levofloxacin, preferentially target either topoisomerase II or IV. Dual-acting fluoroquinolones not only demonstrate increased potency but also are thought to minimize selection of resistant strains because of the double point mutations in both DNA gyrase and topoisomerase IV that are necessary for an organism to become resistant to these newer agents (7). Although older fluoroquinolones are associated with higher resistance rates than the newer compounds, evolving resistance to gatifloxacin and moxifloxacin among CoNS isolates from endophthalmitis patients has been documented (9,10).…”