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. 2007 Mar;1(1):3-10.

Clinical development of 1% azithromycin in DuraSite, a topical azalide anti-infective for ocular surface therapy

Mitchell H Friedlaender  1 , Eugene Protzko
Affiliations
Free PMC article

Clinical development of 1% azithromycin in DuraSite, a topical azalide anti-infective for ocular surface therapy

Mitchell H Friedlaender et al. Clin Ophthalmol. 2007 Mar.
Free PMC article

Abstract

Conjunctivitis, or inflammation of the conjunctiva, refers to a diverse group of ocular surface diseases of viral or bacterial origin that primarily affect the conjunctiva. In developed countries, the most common causative bacterial pathogens are Staphylococcus aureus, Haemophilus influenzae, and Streptococcus pneumoniae. Most varieties of conjunctivitis are self-limiting; however, some cases can be extremely contagious or cause serious complications if left unchecked. New ocular antibiotics are needed to keep pace with the increasing incidence of bacterial resistance and provide options that decrease the overall treatment burden and encourage patient compliance. Azithromycin is a well known systemic anti-infective with broad spectrum activity against gram positive-, gram negative-, and atypical bacteria species. Ocular use has been limited because its solubility and stability profiles in aqueous media were not favorable for delivery to the eye. An eyedrop of 1% azithromycin in DuraSite((R)) (AzaSite, InSite Vision, Alameda, CA, USA), a bioadhesive ocular drug delivery system, was recently developed and evaluated in clinical trials. This formulation is well tolerated, delivers a high concentration of azithromycin to the conjunctiva, has a broader eradication profile than aqueous azithromycin, and can be effectively dosed with 7 drops, a 65% reduction in the amount of drops required by the most popular antibiotics currently used for conjunctivitis.

Keywords: anti-infective; azalide; clinical trial; conjunctiva; drug-delivery; ocular surface.

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Figures

Figure 1
Figure 1
Azithromycin, an azalide, is derived from erythromycin but differs chemically in that a methyl substituted nitrogen atom is incorporated into the lactone ring, which improves the stability of azithromycin relative to erythromycin.
Figure 2
Figure 2
Modeled bioavailability of azithromycin from 1% azithromycin in DuraSite.
See this image and copyright information in PMC

References

    1. Abelson M, Protzko EE, Shapiro AM, et al. 2006aA randomized trial assessing microbial eradication and clinical efficacy of 1.0% azithromycin ophthalmic solution vs. tobramycin in adult subjects with bacterial conjunctivitis [abstract] Invest Ophthalmol Vis Sci 47E-Abstract 3589 - PMC - PubMed
    1. Abelson MB, Shapiro AM, Heller W, et al. 2006bEfficacy of azithromycin 1% eye drops vs vehicle as first-line therapy for bacterial conjunctivitis [abstract] Presented at annual meeting of the American Academy of OphthalmologyNovember 10–14, 2006Las Vegas, NVAbstract PO074
    1. Alcon Laboratories . Fort Worth, TX: Alcon Laboratories; 2005. Vigamox (moxifloxacin hydrochloride ophthalmic solution) 0.5% as base [prescribing information]
    1. Allergan Inc . Irvine, CA: Allergan Inc; 2004. Zymar (gatifloxacin ophthalmic solution) 0.3% [prescribing information]
    1. Ambrose PG, Blast D, Doern GV, et al. Fluoroquinolone-resistant Streptococcus pnuemoniae, an emerging but unrecognized public health concern: Is it time to resight the goal posts. Clin Infect Dis. 2004;39:1554–6. - PubMed

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