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Khalid F. Tabbara, MD; Soliman A. Al-Kharashi, MD; Samir M. Al-Mansouri, MD; Othman M. Al-Omar, MD; Hendrik Cooper; Ahmed M. Abu El-Asrar, MD; George Foulds, PhD

Arch Ophthalmol. 1998;116:1625-1628.

Objective  To assess azithromycin levels in human serum, aqueous humor, tear fluid, and conjunctival tissue specimens after administration of a single 1-g oral dose of azithromycin.

Methods  Sixty patients undergoing cataract surgery were included in this analysis. Serum, aqueous, and tear specimens were collected 3, 6, and 12 hours and 1, 2, 3, and 4 days after azithromycin administration. Conjunctival tissue biopsy specimens were collected 1, 2, 3, 4, 6, 8, 10, 12, and 14 days after azithromycin administration. All specimens were subjected to analysis by high-performance liquid chromatography–mass spectrometry.

Results  Azithromycin concentration ranges during the specified sampling times were as follows: serum, 21 to 974 ng/mL; tear, 82 to 2892 ng/mL; aqueous, 10 to 69 ng/mL; and conjunctival, 0.7 to 32 µg/g. Levels above the 90% minimal inhibitory concentration (MIC₉₀) for Chlamydia trachomatis were detected after 4 days in all tear samples and after 14 days in all conjunctival tissue specimens following oral azithromycin administration.

Conclusion  We demonstrated prolonged high levels of azithromycin in drug-targeted ocular tissue. Prolonged high concentrations of azithromycin in conjunctival tissue make this drug suitable for treatment of conjunctivitis caused by chlamydiae and other susceptible organisms.

From the Department of Ophthalmology, College of Medicine, King Saud University (Drs Tabbara, Al-Kharashi, Al-Mansouri, Al-Omar, and Abu El-Asrar and Mr Cooper), and The Eye Center (The Eye Foundation for Research in Ophthalmology) (Dr Tabbara), Riyadh, Saudi Arabia; and the Drug Metabolism Department, Pfizer Central Research, Groton, Conn (Dr Foulds). The authors do not have any commercial or proprietary interest in any of the drugs or equipment mentioned in this study.

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