Ng E W, Samiy N, Ruoff K L, Cousins F V, Hooper D C, von Gunten S, D'Amico D J, Baker A S
Massachusetts Eye and Ear Infirmary, and the Department of Ophthalmology, Harvard Medical School 02114-3096, USA.
Am J Ophthalmol. 1998 Aug;126(2):278-87. doi: 10.1016/s0002-9394(98)00157-3.
To investigate the ocular pharmacokinetics and efficacy of oral trovafloxacin, a novel fluoroquinolone antibiotic, in Staphylococcus epidermidis endophthalmitis.
Albino rabbits (n = 20) were infected with an intravitreal inoculum of S epidermidis (1.0 x 10(8) colony-forming units [CFU/0.1 ml) and 24 hours later received a single oral dose of trovafloxacin (250 mg/kg). Serum and intraocular samples from infected and control (noninfected) eyes were obtained up to 24 hours after antibiotic administration for measurement of trovafloxacin levels. A second group of rabbits (n = 72) was infected intraocularly and randomized 24 hours later to oral trovafloxacin (250 mg/kg twice a day) for 6 days or no treatment (control). Treatment efficacy was assessed by vitreous culture, clinical examination, and histopathology.
Following a single dose of trovafloxacin, maximal vitreous levels were achieved at 8 hours in infected eyes, with a penetration ratio of 36%. Vitreous levels were greater than 15 times the minimum inhibitory concentration of the strain employed. In animals with established endophthalmitis, treated eyes were sterilized after 5 days (P = .0495) compared with control eyes, which autosterilized at 14 days. Clinical and histologic examination revealed significant amelioration of anterior segment inflammation in treated eyes, although severe destruction of posterior segment structures occurred in both groups after 6 days of therapy.
These data support trovafloxacin as a potential oral agent for treatment or prophylaxis of S epidermidis endophthalmitis, although retinal alterations that occur over the period required for vitreous sterilization suggest that it will not replace intravitreal therapy in established endophthalmitis.
研究新型氟喹诺酮类抗生素口服曲伐沙星在表皮葡萄球菌性眼内炎中的眼内药代动力学及疗效。
20只白化兔眼玻璃体内接种表皮葡萄球菌（1.0×10⁸菌落形成单位[CFU/0.1ml]），24小时后给予单次口服曲伐沙星（250mg/kg）。给药后24小时内，采集感染眼及对照（未感染）眼的血清和眼内样本，测定曲伐沙星水平。第二组72只兔眼内感染，24小时后随机分为口服曲伐沙星（250mg/kg，每日两次）治疗6天组或不治疗（对照组）。通过玻璃体培养、临床检查和组织病理学评估治疗效果。
单次给予曲伐沙星后，感染眼在8小时达到最高玻璃体浓度，穿透率为36%。玻璃体浓度大于所用菌株最低抑菌浓度的15倍。在已发生眼内炎的动物中，治疗组眼在5天后除菌（P = 0.0495），而对照眼在14天后自行除菌。临床和组织学检查显示，治疗组眼前节炎症明显改善，尽管治疗6天后两组后节结构均发生严重破坏。
这些数据支持曲伐沙星作为治疗或预防表皮葡萄球菌性眼内炎的潜在口服药物，尽管在玻璃体除菌所需时间内出现的视网膜改变表明，在已发生的眼内炎中它不能替代玻璃体内注射治疗。
