BESIFLOXACIN THE FOURTH GENERATION FLUOROQUINOLONE: A REVIEW

Abstract

Besifloxacin is fourth generation ophthalmic fluoroquinolone of synthetic origin, it was approved by the United States Food and Drug Administration (USFDA) in May 2009 for the treatment of bacterial conjunctivitis. It is only fluoroquinolone that has not been studied for systemic use; it was sold first in United States of America (USA) under the trade name of Besivance^® ophthalmic suspension 0.6% formulated with Duracite^®technology. This review article provides an overview of the pharmacology, efficacy and tolerability of besifloxacin suspension in the treatment of bacterial conjunctivitis, along with their different analytical techniques.Besifloxacin is a broad spectrum antibiotic active against ocular bacterial pathogen Streptococcus pneumonia, Staphylococcus aureus, Staphylococcus epidermidis, Haemophilus influenza, Moraxella catarrhalis and Corynebacterium spp.Conjunctival concentration of besifloxacin was reported and found to be C_max- 62.79µg/ml, AUC_0-t -5569min.µg/ml, MIC₉₀ <0.06-4µg/ml after single dose of besifloxacin ophthalmic suspension 0.6% in rabbit. In two randomised, double masked vehicle- control trial study reported the besifloxacin ophthalmic suspension was well tolerated and efficacious than vehicles.Besifloxacin was found to be well tolerated in clinical trial however common adverse effects were blurred vision (2.1%), bacterial conjunctivitis (1.8%), eye pain (1.5%) and non-specific bacterial conjunctivitis. Besifloxacin 0.6% ophthalmic suspension was reported to the well tolerated and efficacious in the treatment of bacterial conjunctivitis.There were several methods of analysis like UV, HPLC and microbiological for the quantification of besifloxacin.

Keywords: Besifloxacin, Moxifloxacin, Gatifloxacin, Bacterial conjunctivitis, HPLC Pharmacokinetic