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头孢吡肟(BMY - 28142)在有色兔眼玻璃体内注射后的毒性和药代动力学

Toxicity and pharmacokinetics of cefepime (BMY-28142) following intravitreal injection in pigmented rabbit eyes.

作者信息

Jay W M, Shockley R K

机构信息

Department of Ophthalmology, University of Arkansas for Medical Sciences, Little Rock.

出版信息

J Ocul Pharmacol. 1988 Winter;4(4):345-9. doi: 10.1089/jop.1988.4.345.

Abstract

We delineated the dose- and time-dependent retinal toxicity of cefepime (BMY-28142), a new third generation cephalosporin, using electroretinography in pigmented rabbit eyes. Toxicity was evaluated following intravitreal doses ranging from 0.5 to 20mg/0.1ml (N = 18). Electroretinographic patterns at one and two weeks indicated a toxic response to 20 mg of cefepime. B-waves were normal at one and two weeks for rabbits receiving doses of 0.5 to 10mg. Pharmacokinetic analysis after single intravitreal injection of 1 mg of cefepime (N = 3 rabbits/dose) disclosed the following vitreous fluid levels (ug/ml): 645 at Oh, 431 at 8h, 235 at 24h and 23 at 72h. Peak aqueous humor levels (56 ug/ml) were observed at 8h after injection. At 72h, ug/ml was detected in the aqueous fluid.

摘要

我们使用视网膜电图对色素沉着兔眼进行研究,描绘了新型第三代头孢菌素头孢吡肟(BMY-28142)的剂量和时间依赖性视网膜毒性。玻璃体内注射剂量范围为0.5至20mg/0.1ml(N = 18)后评估毒性。一周和两周时的视网膜电图模式表明对20mg头孢吡肟有毒性反应。接受0.5至10mg剂量的兔子在一周和两周时B波正常。单次玻璃体内注射1mg头孢吡肟(每剂量3只兔子)后的药代动力学分析显示玻璃体液水平如下(μg/ml):0小时时为645,8小时时为431,24小时时为235,72小时时为23。注射后8小时观察到房水峰值水平(56μg/ml)。72小时时,在房水中检测到μg/ml。

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