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H. Sakamoto, A. Ueno, T. Nakamura, T. Ishibashi; Aqueous and Vitreous Penetration of Levofloxacin after Topical and/or Oral Administration in Humans . Invest. Ophthalmol. Vis. Sci. 2003;44(13):3449.
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Purpose: To investigate aqueous and vitreous penetration of levofloxacin (LVFX), an optical S-(-) isomer of ofloxacin, LVFX was administered topically and/or orally to the patients undergoing initial vitrectomy. Methods: Thirty-seven patients undergoing initial vitrectomy with phacoemulsification and aspiration (PEA) were enrolled. Before vitrectomy, LVFX was administered orally and/or topically to the patients. The patients were divided randomly into three groups; Group 1: topical application of LVFX (three times on preoperative day and seven times on operative day), Group 2: oral administration of LVFX (200 mg twice on preoperative day and 200 mg once 3 hours before operation), Group 3: topical and oral administration of LVFX. The aqueous humors were collected before PEA. After PEA, vitrectomy was performed without irrigation. The concentrations of LVFX in aqueous humors and vitreous humors were measured. Results: LVFX concentrations in the aqueous humors in Groups 1, 2 and 3 were 0.774 ± 0.572 µg/ml, 1.420 ± 0.502 µg/ml, and 1.866 ± 0.443 µg/ml, respectively. LVFX concentrations in the vitreous humors in Groups 1, 2 and 3 were 0.202 ± 0.448µg/ml, 1.494 ± 0.485 µg/ml, and 1.349 ± 0.545 µg/ml, respectively. Conclusions: Topical application showed relatively poor penetration of LVFX into the vitreous body. On the other hand, LVFX concentrations in the vitreous bodies after oral administration at a dose of 400 mg a day were sufficient for prophylaxis of ocular infections; the aqueous and vitreous concentrations of LVFX after oral administration were higher than MIC90s of major ocular pathogens.
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