R E V I E W Review of moxiﬂoxacin hydrochloride ophthalmic solution in the treatment of bacterial eye infections Darlene Miller Abrams Ocular Microbiology Laboratory, Bascom Palmer Eye Institute, Anne Bates Leach Eye Hospital, Miller School of Medicine- University of Miami, FL, USA Correspondence: Darlene Miller Research Assistant Professor, Scientiﬁc Director, Abrams Ocular Microbiology Laboratory, Bascom Palmer Eye Institute, Anne Bates Leach Eye Hospital, Miller School of Medicine-University of Miami, 900 NW 17th Street, Miami, Florida 33136, USA Tel +1 305 326 6034 Fax +1 305 547 3661 Email dmiller@med.miami.edu negative ocular pathogens. concentrations Introduction Abstract: Moxifloxacin hydrochloride ophthalmic solution 0.5% (Vigamox®) is the ocular formulation/adaptation of moxifloxacin. Moxifloxacin is a broad spectrum 8-methoxyﬂuoroquinolone which terminates bacterial growth by binding to DNA gyrase (topoisomerase II) and topoisomerase IV, essential bacterial enzymes involved in the replication, translation, repair and recombination of deoxyribonucleic acid. Afﬁnity for both enzymes improves potency and reduces the probability of selecting resistant bacterial subpopulations. Vigamox is a bactericidal, concentration dependent, anti-infective. It is preservative free, and well tolerated with minimal ocular side effects. It provides increased penetration into ocular tissues and ﬂuids with improved activity against Streptococci and Staphylococci species and moderate to excellent activity against clinically relevant, gram- Keywords: moxifloxacin, vigamox, pharmacodynamic indices, minimal inhibitory Moxiﬂoxacin hydrochloride ophthalmic solution 0.5% is the ocular formulation/adap- tation of moxiﬂoxacin, an 8-methoxyﬂuoroquinolone, broad spectrum, anti-infective. It was introduced in 2003 as Vigamox® (Alcon Laboratories, Inc, Fort Worth, TX, USA) for the treatment of susceptible microorganisms recovered from patients with bacterial conjunctivitis. It is used more frequently off label for treatment of keratitis and as a prophylaxis agent in cataract and refractive surgeries (Vigamox 2004; Alfonso and Crider 2005; Schlech and Alfonso 2005). It is an isotonic, preservative free, solution with a near neutral pH of 6.8. The formula of Vigamox includes 5 mg/mL (0.5%) of moxiﬂoxacin, boric acid, and puri- ﬁed water. Lack of the preservative BAK (benzalkonium chloride) makes it unique among current topical antibiotics licensed for use. Vigamox is currently available in more than 40 countries. Moxiﬂoxacin hydrochloride ophthalmic solution 0.5%, under the trade name Vegamox®, was introduced into Japan in 2006, with approval for the treatment of bacterial conjunctivitis, keratitis and surgical prophylaxis. Chemistry Figure 1 shows the basic molecule and Figure 2 the moxiﬂoxacin molecule. Table 1 shows the impact of core modiﬁcations. Moxiﬂoxacin Moxiﬂoxacin is a broad spectrum, 8-methoxy ﬂuoroquinolone with improved activ- ity against Streptococci and Staphylococci and moderate to excellent activity against clinically relevant, gram negative ocular pathogens (Smith et al 2001; Keating and Scott 2004). Clinical Ophthalmology 2008:2(1) 77–91 © 2008 Dove Medical Press Limited. All rights reserved 77