Besifloxacin: Efficacy and Safety in Treatment and Prevention of Ocular Bacterial Infections

Abstract

This comprehensive review summarizes the mechanism of action, pharmacokinetics, efficacy, and safety of besifloxacin ophthalmic suspension, 0.6% and examines its role in the treatment of ocular surface bacterial infections. Besifloxacin possesses balanced activity against bacterial topoisomerase II (also called DNA gyrase) and topoisomerase IV. It has shown a low potential to select for bacterial resistance in vitro and demonstrated strong in vitro activity against many Gram-positive, Gram-negative, and anaerobic organisms, including methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis (MRSA and MRSE, respectively). Ocular pharmacokinetic studies have shown that besifloxacin achieves high, sustained concentrations in the tear fluid and conjunctiva following topical administration, with negligible systemic exposure. Large randomized, controlled clinical trials have established the efficacy and safety of besifloxacin administered three times daily for 5 days for treatment of acute bacterial conjunctivitis in both adults and children, with high rates of clinical resolution (up to more than 70% by day 5) and bacterial eradication (more than 90% by day 5), and a low incidence of adverse events. Additionally, besifloxacin applied twice daily for 3 days demonstrated greater efficacy than vehicle in treating bacterial conjunctivitis. Case reports, a large retrospective chart review, and animal studies have provided supporting evidence for the efficacy of besifloxacin in the management of acute bacterial keratitis. There is some evidence to suggest that besifloxacin may provide an advantage over other current-generation fluoroquinolones in antimicrobial prophylaxis for ocular surgery. Besifloxacin is an appropriate option for treatment of bacterial conjunctivitis, and its use in the treatment of bacterial keratitis and lid disorders, as well as for surgical prophylaxis, appears promising and warrants further evaluation.

Antibiotic Resistance Rates by Geographic Region Among Ocular Pathogens Collected During the ARMOR Surveillance Study

“…Compared with other fluoroquinolones, besifloxacin has more balanced targeting of DNA gyrase and topoisomerase IV; this, in turn, results in the need for multistep mutations and reduces the possibility of spontaneous resistance [ 23 – 25 ]. Furthermore, besifloxacin may have a lower incidence of resistance development due to its use being limited to topical ophthalmic infections only, although cross-resistance from other fluoroquinolones is possible [ 26 ].…”

Phytochemicals as modulators of M1-M2 macrophages in inflammation

“…Cis- palmitoleate (C16:1 n-7), a monounsaturated fatty acid, confers an anti-inflammatory M2-like polarization to macrophages by promoting anti-inflammatory gene expression ( Mrc1 , Tgfb1 , Il10 , and Mgl2 ) and oxidative metabolism, characteristic of M2 macrophages. It also has been shown to prevent palmitate-induced IκBα degradation, RelA nuclear translocation, NO production, and cytokine secretion [ 120 ], Besifloxacin is a novel fluoroquinolone initially developed by Bausch & Lomb for the topical treatment of ophthalmic infections [ 121 ]. It significantly inhibits LPS-stimulated cytokine production including GM-CSF, IL-1β, IL-8, IP-10, MCP-1 and MIP-1.…”

Besifloxacin: A Critical Review of Its Characteristics, Properties, and Analytical Methods

“…[19] Mechanism of action and resistance Regarding the mechanism of action, as well as other fluoroquinolones, besifloxacin binds to bacterial enzymes DNA gyrase and topoisomerase IV, which are essential for DNA replication in bacteria. [11,28,29] Thus, inhibition of these enzymes interferes with transcription, replication, and separation of bacterial chromosomal DNA during cell division. [20] Fluoroquinolones have bactericidal action.…”