Overview of the Potency of Moxifloxacin Ophthalmic Solution 0.5% (VIGAMOX®)

• Published in: Survey of ophthalmology 2005-11, Vol.50 (6), p.S7-S15
• Main Authors: Schlech, Barry A., Alfonso, Eduardo
• Format: Article
• Language: English
• Subjects: Animals; antibiotic; Aza Compounds - administration & dosage; Aza Compounds - pharmacokinetics; Aza Compounds - pharmacology; Bacteria - drug effects; breakpoints; Drug Resistance, Bacterial; Eye Infections, Bacterial - drug therapy; Eye Infections, Bacterial - metabolism; fluoroquinolone in vitro; Fluoroquinolones; Humans; in vivo; MIC; Microbial Sensitivity Tests; moxifloxacin; MPC; Ophthalmic Solutions - administration & dosage; Ophthalmic Solutions - pharmacokinetics; Ophthalmic Solutions - pharmacology; pharmacodynamics; pharmacokinetic; potency; Quinolines - administration & dosage; Quinolines - pharmacokinetics; Quinolines - pharmacology; therapeutic index; VIGAMOX
• ISSN: 0039-6257; 1879-3304
• DOI: 10.1016/j.survophthal.2005.05.002

Antibiotics have been the mainstay of therapy for infectious diseases since their origins in the 1940s. As microorganisms changed and resistance developed, more advanced antibiotics were ultimately needed to provide adequate coverage and spectrum. By selecting optimal antibiotics and dosing regimens, clinicians can avoid treatment failures and adverse events and can help prevent the emergence of further antibiotic resistance. The fourth-generation ophthalmic fluoroquinolones include moxifloxacin (VIGAMOX®, Alcon Laboratories, Inc., Fort Worth, TX) and gatifloxacin (Zymar, Allergan, Irvine, CA), and they are now approved for the treatment of bacterial conjunctivitis. This review highlights four scientific methods that compare and rank antibiotic potencies and predict their clinical efficacy and their propensity to develop resistance: 1) in vitro assay for minimum inhibitory concentrations, 2) in vivo models for pharmacokinetic and pharamacodynamic properties, 3) therapeutic index or inhibitory quotient, and 4) in vitro assay for mutant prevention concentration. The fourth-generation ophthalmic fluoroquinolones perform well in these assays. Both antibiotics have better in vitro activity against gram-positive bacteria than ciprofloxacin or ofloxacin. Moxifloxacin penetrates better into ocular tissues than gatifloxacin and older fluoroquinolones; in vitro activity of moxifloxacin and gatifloxacin against gram-negative bacteria is similar to that of older fluoroquinolones. Moxifloxacin also has better mutant prevention characteristics than other fluoroquinolones. These findings support the use of the newer fluoroquinolones for the prevention and treatment of serious ophthalmic infections (e.g., keratitis, endophthalmitis) caused by susceptible bacteria.