Ziai N, Dolan J W, Kacere R D, Brubaker R F
Department of Ophthalmology, Mayo Clinic, Rochester, Minn.
Arch Ophthalmol. 1993 Oct;111(10):1351-8. doi: 10.1001/archopht.1993.01090100059027.
To study the effects of a topically applied prostaglandin F2 alpha analogue, PhXA41 (Latanoprost; 13,14-dihydro-17-phenyl-18,19,20-trinor-prostaglandin F2 alpha-isopropyl ester), on aqueous dynamics in the human eye.
A randomized, double-masked study was carried out on 20 normal and 20 ocular hypertensive humans. One eye of each subject was treated with 0.006% PhXA41, while the contralateral eye received placebo twice daily for 5 days.
Compared with placebo, PhXA41 reduced intraocular pressure in both groups by approximately 20%.
Tonographic facility of outflow was increased 24% in the normal group and 30% in the ocular hypertensive group; no changes were observed in the rates of aqueous humor flow in either group. The changes in tonographic facility were insufficient to fully explain the ocular hypotensive effect of the drug, suggesting that PhXA41 enhances outflow via the uveoscleral pathway. The suitability of fluorophotometry as a measure of flow was confirmed by three methods of comparing blood-aqueous barrier permeability: polarization of cameral fluorescence, intensity of backscattered light from the anterior chamber (flare), and cameral fluorescence after oral administration of fluorescein sodium. All of these measured parameters were normal, suggesting that this compound has no clinically significant effects on the blood-aqueous barrier or on the accuracy of fluorophotometry. PhXA41 was well tolerated in both groups. Only four of 40 subjects reported a transient foreign-body sensation, and only one of 40 subjects was observed to have greater than moderate conjunctival hyperemia. Most subjects had no symptoms and no measurable hyperemia.
These results suggest that PhXA41 is a potentially useful ocular hypotensive agent that enhances the egress of aqueous humor via both major outflow pathways. The relative lack of ocular side effects in this study further suggests that this agent has promise for the treatment of chronic glaucoma.
研究局部应用前列腺素F2α类似物PhXA41（拉坦前列素；13,14 - 二氢 - 17 - 苯基 - 18,19,20 - 三降 - 前列腺素F2α异丙酯）对人眼房水动力学的影响。
对20名正常人和20名高眼压患者进行了一项随机、双盲研究。每位受试者的一只眼睛用0.006%的PhXA41治疗，而对侧眼睛每天两次接受安慰剂治疗，持续5天。
与安慰剂相比，PhXA41使两组的眼压均降低了约20%。
正常组的眼压描记流出系数增加了24%，高眼压组增加了30%；两组的房水流量率均未观察到变化。眼压描记系数的变化不足以完全解释该药物的降眼压作用，这表明PhXA41通过葡萄膜巩膜途径增强房水流出。通过比较血 - 房水屏障通透性的三种方法证实了荧光光度法作为流量测量方法的适用性：前房荧光偏振、前房后向散射光强度（闪光）以及口服荧光素钠后的前房荧光。所有这些测量参数均正常，表明该化合物对血 - 房水屏障或荧光光度法的准确性没有临床显著影响。两组对PhXA41的耐受性都很好。40名受试者中只有4人报告有短暂的异物感，40名受试者中只有1人被观察到有大于中度的结膜充血。大多数受试者没有症状，也没有可测量的充血。
这些结果表明，PhXA41是一种潜在有用的降眼压药物，可通过两条主要流出途径增强房水流出。本研究中相对缺乏眼部副作用进一步表明该药物有望用于治疗慢性青光眼。
