体外体内药物动力学和药效学nepafenac, amfenac ketorolac, bromfenac。

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沃尔特斯T, Raizman M,欧内斯特·P,盖顿J,莱曼R

体外体内药物动力学和药效学nepafenac, amfenac ketorolac, bromfenac。

J白内障折射Surg. 9月2007;33 (9):1539 - 45。

PubMed ID

17720067 (在PubMed

]

文摘

目的:评价房水浓度和环氧合酶(COX)抑制活动nepafenac, amfenac, ketorolac, bromfenac后局部眼Nevanac管理局(nepafenac 0.1%), Acular LS (ketorolac 0.4%),或Xibrom (bromfenac 0.09%)。设置:五私人眼科实践在美国。方法:要求白内障摘除术的患者被随机1 3治疗组:Nevanac, Acular LS或Xibrom。患者服用1滴测试药物的30岁,60岁,120年,180年,或者240分钟前白内障手术。穿刺术的时候,房水样本收集和分析药物浓度。此外,COX-1(稳态)和cox - 2(诱导)抑制nepafenac活动,amfenac, ketorolac, bromfenac决定通过体外测量前列腺素E(2)(铂族元素(2))的抑制作用。结果:七十五名患者参加了实验。的药物前体nepafenac最短时间达到峰值浓度和最大的峰值房水浓度(C (max))。nepafenac的C (max)显著高于其他药物(P < . 05),包括高浓度ketorolac (0.4%)。曲线下的面积(AUC) nepafenac明显高(P < . 05)比amfenac的AUC, ketorolac,和bromfenac。 The combined AUCs of nepafenac and amfenac were the highest of all drugs tested (P<.05). Ketorolac showed the most potent COX-1 inhibition, whereas amfenac was the most potent COX-2 inhibitor. The PGE(2) aqueous humor levels of each study medication were highly variable; as a result, meaningful interpretation of the data was not possible. CONCLUSION: Nepafenac showed significantly greater ocular bioavailability and amfenac demonstrated greater potency at COX-2 inhibition than ketorolac or bromfenac.

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药物

Nepafenac