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Pharmacokinetics of intravenously administered tigecycline in eye compartments: an experimental study

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Abstract

Purpose

The purpose of this study was to evaluate the ocular distribution of intravenously administered tigecycline in a rabbit uveitis model.

Methods

Tigecycline, which has a broad spectrum of activity against many gram-positive, gram-negative, and anaerobic organisms, was given intravenously to rabbits at 7 mg/kg of body weight starting 24 h after induction of uveitis by intravitreal endotoxin injection. Tigecycline concentrations were determined by high performance liquid chromatography-mass spectrometry (LC-MS/MS) assay in the aqueous humor, vitreous humor, and plasma 1, 3, 6, and 24 h after administration of a single dose.

Results

The maximum concentrations were found within 1 h after the end of the intravenously given tigecycline, and were 1,308.60 ± 301.76 ng/mL in plasma, 181.40 ± 51.32 ng/mL in vitreous humor and 145.00 ± 55.29 ng/mL in aqueous humor of the inflamed eye. After 24 h, no drug was detectable in the aqueous and vitreous of the normal eyes, whereas small amounts of drug were detectable in inflamed eyes and in plasma.

Conclusions

Tigecycline did not reach therapeutically significant levels in the aqueous and the vitreous humor of rabbit eyes. The findings suggest a limited role for intravenously administered tigecycline in the treatment of bacterial endophthalmitis.

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Acknowledgments

This work was supported by grants from Konya Training and Research Hospital (KTRH-28), Konya, Turkey.

Author disclosure statement

The authors have no financial or proprietary interest in any material or method mentioned. The authors report no conflicts of interest. The authors alone are responsible for the content and writing of article.

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Authors and Affiliations

  1. Department of Ophthalmology, Konya Training and Research Hospital, Konya, 42090, Turkey

    Muammer Ozcimen, Yasar Sakarya, Sertan Goktas, Rabia Sakarya, Ismail Alpfidan & Erkan Erdogan

  2. Department of Infectious Diseases and Clinical Microbiology, Konya State Hospital, Konya, 42060, Turkey

    Serap Ozcimen

  3. Feritpasa Mah, Malazgirt sok, Kardelen Apt. No: 14 Selcuklu, Konya, Turkey

    Muammer Ozcimen

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  1. Muammer Ozcimen
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  2. Yasar Sakarya
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Correspondence to Muammer Ozcimen.

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Ozcimen, M., Sakarya, Y., Ozcimen, S. et al. Pharmacokinetics of intravenously administered tigecycline in eye compartments: an experimental study. Graefes Arch Clin Exp Ophthalmol 252, 1993–1997 (2014). https://doi.org/10.1007/s00417-014-2784-2

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  • DOI: https://doi.org/10.1007/s00417-014-2784-2

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