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Conjunctival biopsy—serum ratios were significantly greater than circulating serum values, with serum decrease being paralleled by concurrent and rapid conjunctival uptake. These phenomena suggest that extensive absorption or binding mechanisms exist in ocular tissue, leading to this tissue's accumulation of the drug. The ocular pharmacokinetic profile displayed by azithromycin and its increased serum and conjunctival tissue half-life allow for simplified short-term therapeutic schedules.

In addition, its gastric tolerability and diminished incidence of adverse effects make the compound suitable for the treatment of conjunctivitis caused by susceptible organisms such as Chlamydia trachomatis. This study was performed on patients undergoing cataract surgery with no clinical evidence of inflammation. Patients with trachoma or other infectious conjunctivitis have marked conjunctival inflammation. In such patients, there is higher conjunctival and tear levels of azithromycin.

It is cleared primarily by biliary and fecal routes, with a serum half-life greater than 60 hours. Results of an open crossover study investigating the pharmacokinetic profiles of 3- and 5-day mg oral regimens of azithromycin show that the drug is absorbed and distributed rapidly and evenly after administration of each daily dose, with a polyphasic decline of plasma concentrations showing average half-lives of The observed pharmacokinetic profiles of azithromycin with both regimens conformed with previously established models for the drug.

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Use of azithromycin does not inactivate cytochrome P and does not induce the metabolism of other compounds. Metabolism is predominantly hepatic, with biliary excretion of inactive metabolites. Drug elimination is biphasic, with a terminal half-life of up to 5 days. Azithromycin has been approved for use in pediatric patients, and its pharmacokinetic profile is not significantly altered in elderly patients or in those with mild to moderate renal or hepatic insufficiency.

Tissue concentrations of azithromycin above the MIC 90 for many infective organisms have been correlated in animal models of infection. Short treatment protocols consisting of a single 1-g oral dose have been shown to provide adequate concentrations in urogenital tissues, above the MIC 90 for C trachomatis for 10 days 16 , 17 and in its serovars involved in induction and transmission of trachoma. Furthermore, because the chlamydial life cycle is 48 hours, an azithromycin tissue level of greater than the MIC 90 of Chlamydia 14 days after administration of a single oral dose may help eradicate trachoma in endemic areas and control other susceptible organisms causing conjunctival infections.

Reprints: Khalid F. All Rights Reserved. View Large Download. Table 1. Ann Pharmacother. J Antimicrob Chemother. Clin Infect Dis.

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J Chromatogr. Ocular pharmacokinetics of orally administered azithromycin in rabbits.


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