眼和系统性药物动力学latanoprost的人类。

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Sjoquist B, Stjernschantz J

眼和系统性药物动力学latanoprost的人类。

Surv角膜切削。2002年8月,47增刊1:S6-12。

PubMed ID

12204697 (在PubMed

]

文摘

14-dihydro-17-phenyl-18 latanoprost眼部药物动力学(13日,19日,20-trinor-PGFα(2)异丙酯;Xalatan [Pharmacia-Upjohn Peapack,新泽西]),研究了使用radio-immunoassay接受白内障手术的患者,和latanoprost系统性药物动力学的研究在健康志愿者3 h-latanoprost以及放射免疫检定法。局部应用后,latanoprost迅速水解角膜和血液。活性药物的最大浓度,latanoprost酸,房水中发现局部管理的临床剂量和1 - 2小时后达到15 - 30 ng / ml。房水中的半衰期latanoprost酸2 - 3小时。在体循环latanoprost酸的浓度峰值出现局部应用和5分钟后达到了一个水平的53个pg / ml消除半衰期为17分钟。在药物的病人,连续超过1年,5个10的等离子体latanoprost酸水平低于检测极限(< 30 pg / ml)。等离子体间隙是0.40 + / - 0.04 l / h。公斤,体积的分布为0.16 + / - 0.02 l /公斤后静脉管理。相应的数据后眼部政府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.

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药物

Latanoprost