Tear Concentrations of Azithromycin following Topical Administration of a Single Dose of Azithromycin 0.5%, 1.0%, and 1.5% Eyedrops (T1225) in Healthy Volunteers

Abstract

Once daily instillation of T1225 1.0% and 1.5% was shown to reach an AUIC markedly above the required threshold for an antibacterial activity against Gram-positive bacteria (25-35). These results suggest that a BID instillation is more likely to ensure antimicrobial activity against Gram-negative bacteria (threshold >100).

Ocular Pharmacokinetics of Besifloxacin Following Topical Administration to Rabbits, Monkeys, and Humans

“…The besifl oxacin levels in tears measured in this study were generally higher than the levels reported following a single topical ocular instillation of ciprofl oxacin (0.3%), 24 ofl oxacin (0.3%), 24 norfl oxacin (0.3%), 24 levofl oxacin (0.5%), 12 or azithromycin (1%) 13 (Fig. 9).…”

“…Data for ciprofl oxacin, ofl oxacin, and norfl oxacin are from Akkan and colleagues 24 ; data for levofl oxacin are from Raizman and colleagues 12 ; data for azithromycin are from Chiambaretta and colleagues. 13 …”

“…Separate subgroups of subjects (n = 8/collection time) were sampled at each of eight predetermined collection times over the measurement of drug levels at multiple intervals after dosing, and subsequent comparison of the resulting PK parameters, such as peak concentration (C max ) and/or area under the concentration-time curve (AUC), with the concentrations required for inhibition of bacterial growth (eg, MIC 90 ). This approach has been used to assess the ocular PK/PD properties of moxifl oxacin, 7 gatifl oxacin, 7 levofl oxacin, 12 and azithromycin 13 in humans, as well as ofl oxacin, gentamicin, and tobramycin in rabbits. 14 Besifl oxacin (Fig.…”

Efficacy and safety of azithromycin 1.5% eye drops in paediatric population with purulent bacterial conjunctivitis

“…This could explain why even bacteria resistant to plasma concentrations of azithromycin are susceptible to azithromycin eye drop treatment (which has an antibiotic concentration several times the minimum inhibitory concentration for bacteria usually defined as resistant)27. The pharmacokinetic properties of azithromycin justify the short treatment duration of only one drop twice-daily for 3 days for a rapid antibacterial action29. The present study has confirmed that this treatment regimen, already established in adults, is also effective in the paediatric population, including children younger than 24 months old.…”

Antimicrobial Agents in Ophthalmology

“…The drug is currently available as eyedrops at a concentration of 1.5 % as Azyter ® (Laboratoires Theá, Clermont-Ferrand, France) and 1.0 % concentration as Azasite (Inspire Pharmaceuticals Inc, NC, USA). The tear concentration of topical azithromycin was studied following topical administration of a single dose of azithromycin 1.0 and 1.5 % in healthy volunteers [ 32 ]. This study was a prospective, randomized double-masked study.…”