Bito L Z, Miranda O C, Tendler M R, Resul B
Department of Ophthalmology, College of Physicians and Surgeons, Columbia University, New York, NY 10032.
Exp Eye Res. 1990 Apr;50(4):419-28. doi: 10.1016/0014-4835(90)90143-i.
It has been shown that prostaglandin A2 (PGA2) is a more potent ocular hypotensive agent in cats than other PG free acids. We report here that significant IOP reduction can be achieved in normotensive cat eyes with the use of even lower doses of PGA2-1-isopropyl ester (PGA2-IE) than with PGA2, PGF2 alpha-1-isopropyl ester (PGF2 alpha-IE), or any other known ocular hypotensive agent. Furthermore, single applications of 0.5 microgram of PGA2-IE maintain significant IOP reductions for at least 24 hr. This hypotensive effect is enhanced during the first 3-5 days of daily treatment. Significant IOP reductions were maintained for several months as long as PGA2-IE was applied daily or at least once every 48 hr. None of the cats manifested signs of discomfort in response to treatment with doses ranging from 0.10 to 1.25 micrograms of PGA2-IE. Moreover, the extent of anterior chamber flare was less than that typically observed after the topical application of hypotensive doses of PGE2, PGD2, PGF2 alpha, or the esters or tromethamine salt of PGF2 alpha. Although it is possible that the human eye would respond differently to PGs of the A type, the results of these studies suggests that PGA2-IE or other esters of derived PGs of the A type, and probably the B type, may offer significant therapeutic advantages over the PGF2 alpha tromethamine salt and PGF2 alpha-IE, which have been shown to exert significant hypotensive effects on normal and glaucomatous human eyes.
已表明,前列腺素A2(PGA2)在猫中是比其他前列腺素游离酸更有效的降眼压剂。我们在此报告,使用比PGA2、前列腺素F2α-1-异丙酯(PGF2α-IE)或任何其他已知降眼压剂更低剂量的PGA2-1-异丙酯(PGA2-IE),可使正常眼压的猫眼眼压显著降低。此外,单次应用0.5微克PGA2-IE可使眼压显著降低至少24小时。在每日治疗的前3至5天,这种降眼压作用会增强。只要每天或至少每48小时应用一次PGA2-IE,眼压就能显著降低并维持数月。在用0.10至1.25微克PGA2-IE治疗的猫中,没有一只表现出不适迹象。此外,前房闪辉程度低于局部应用降压剂量的前列腺素E2、前列腺素D2、前列腺素F2α或前列腺素F2α的酯或 tromethamine盐后通常观察到的程度。虽然人眼对A类前列腺素的反应可能不同,但这些研究结果表明,PGA2-IE或其他A类衍生前列腺素的酯,可能还有B类,可能比已证明对正常和青光眼人眼有显著降眼压作用的前列腺素F2α tromethamine盐和PGF2α-IE具有显著的治疗优势。