...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Survey of Ophthalmology >Ocular and systemic pharmacokinetics of latanoprost in humans.
【24h】

Ocular and systemic pharmacokinetics of latanoprost in humans.

机译：拉坦前列素在人的眼和全身药代动力学。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The ocular pharmacokinetics of latanoprost (13,14-dihydro-17-phenyl-18, 19,20-trinor-PGF(2alpha)-isopropyl ester; Xalatan [Pharmacia-Upjohn, Peapack, NJ]) was studied in patients undergoing cataract surgery using radio-immunoassay, and the systemic pharmacokinetics of latanoprost was studied in healthy human volunteers with 3H-latanoprost as well as radioimmunoassay. After topical application, latanoprost was rapidly hydrolysed in the cornea and blood. The maximum concentration of the active drug, latanoprost acid, was detected in the aqueous humor 1-2 hours after topical administration of the clinical dose and amounted to 15-30 ng/ml. The half-life of latanoprost acid in the aqueous humor was 2-3 hours. In the systemic circulation the peak concentration of latanoprost acid appeared 5 minutes after topical application and reached a level of 53 pg/ml with an elimination half-life of 17 minutes. In patients that had been on the drug continuously for more than 1 year, 5 out of 10 had plasma levels of latanoprost acid below the limit of detection (<30 pg/ml). The mean plasma clearance was 0.40 +/- 0.04 l/h. kg, and the volume of distribution was 0.16 +/- 0.02 l/kg after intravenous administration. The corresponding figures after ocular administration were 0.88 l/h. kg, and 0.36 l/kg. The majority of the radioactivity was recovered in urine (88%) and the rest was found in feces. In the eye the main metabolism of latanoprost was the ester hydrolysis. The only prominent chromatographic peak in plasma corresponded to latanoprost acid. In urine no latanoprost or latanoprost acid was detected. Before excretion latanoprost acid was beta oxidized to 1,2-dinor and 1,2,3,4-tetranor latanoprost acid. These metabolites accounted for approximately 66% of the radioactivity in urine. In conclusion, latanoprost is rapidly hydrolyzed in the eye and blood to latanoprost acid. Minimal further metabolism occurs in the eye, but latanoprost acid undergoes beta oxidation and other metabolism outside the eye. After topical application the peak concentration in aqueous humor was approximately 10(-7) M, whereas that in plasma was about 10(-10) M or less.
机译：在接受白内障手术的患者中研究了拉坦前列素（13,14-二氢-17-苯基-18，19,20-trinor-PGF（2α）-异丙酯; Xalatan [Pharmacia-Upjohn，Peapack，NJ]）的眼药代动力学使用放射免疫测定，并在健康的3H-拉坦前列素志愿者中对拉坦前列素的全身药代动力学以及放射免疫测定进行了研究。局部应用后，拉坦前列素在角膜和血液中迅速水解。局部给药临床剂量后1-2小时，在房水中检测到活性药物拉坦前列素酸的最大浓度，为15-30 ng / ml。拉坦前列素酸在房水中的半衰期为2-3小时。在全身循环中，拉坦前列素酸的峰值浓度在局部应用后5分钟出现，达到53 pg / ml的水平，消除半衰期为17分钟。在连续服药超过一​​年的患者中，十分之五的血浆血浆拉坦前列酸水平低于检出限（<30 pg / ml）。平均血浆清除率为0.40 +/- 0.04 l / h。静脉给药后，分布体积为0.16 +/- 0.02 l / kg。眼部给药后的相应数字为0.88 l / h。千克和0.36升/千克。大部分放射性是在尿液中回收的（88％），其余的是在粪便中发现的。在眼中，拉坦前列素的主要代谢是酯水解。血浆中唯一突出的色谱峰对应于拉坦前列酸。尿液中未检测到拉坦前列素或拉坦前列酸。在排泄前，将拉坦前列素β氧化为1,2-二价和1,2,3,4-丁诺拉坦前列酸。这些代谢物约占尿液放射性的66％。总之，拉坦前列素在眼和血液中迅速水解为拉坦前列酸。眼睛中的进一步新陈代谢最少，但拉坦前列酸在眼睛外会经历β氧化和其他新陈代谢。局部应用后，房水中的峰值浓度约为10（-7）M，而血浆中的峰值浓度约为10（-10）M或更小。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号