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类二十烷酸作为一类新型的降眼压药物。3. 前列腺素A2 - 1 - 异丙酯是已报道的对猫眼降压作用最强的药物。

Eicosanoids as a new class of ocular hypotensive agents. 3. Prostaglandin A2-1-isopropyl ester is the most potent reported hypotensive agent on feline eyes.

作者信息

Bito L Z, Miranda O C, Tendler M R, Resul B

机构信息

Department of Ophthalmology, College of Physicians and Surgeons, Columbia University, New York, NY 10032.

出版信息

Exp Eye Res. 1990 Apr;50(4):419-28. doi: 10.1016/0014-4835(90)90143-i.

DOI:10.1016/0014-4835(90)90143-i
PMID:2338124
Abstract

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.

摘要

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。

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1
Eicosanoids as a new class of ocular hypotensive agents. 3. Prostaglandin A2-1-isopropyl ester is the most potent reported hypotensive agent on feline eyes.类二十烷酸作为一类新型的降眼压药物。3. 前列腺素A2 - 1 - 异丙酯是已报道的对猫眼降压作用最强的药物。
Exp Eye Res. 1990 Apr;50(4):419-28. doi: 10.1016/0014-4835(90)90143-i.
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Exp Eye Res. 1987 Jun;44(6):825-37. doi: 10.1016/s0014-4835(87)80045-3.
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Eicosanoids as a new class of ocular hypotensive agents. 2. Comparison of the apparent mechanism of the ocular hypotensive effects of A and F type prostaglandins.类二十烷酸作为一类新型的降眼压药物。2. A型和F型前列腺素降眼压作用的表观机制比较。
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Effect of topical prostaglandin PGA2, PGA2 isopropyl ester, and PGF2 alpha isopropyl ester on intraocular pressure in normotensive and glaucomatous canine eyes.局部应用前列腺素PGA2、PGA2异丙酯和PGF2α异丙酯对正常血压和青光眼犬眼眼压的影响。
J Ocul Pharmacol. 1991 Summer;7(2):107-16. doi: 10.1089/jop.1991.7.107.
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Maintained reduction of intraocular pressure by prostaglandin F2 alpha-1-isopropyl ester applied in multiple doses in ocular hypertensive and glaucoma patients.多次给药应用前列腺素F2α - 1 - 异丙酯对高眼压症和青光眼患者眼压的持续降低作用。
Ophthalmology. 1989 Sep;96(9):1329-36; discussion 1336-7. doi: 10.1016/s0161-6420(89)32717-5.
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The ocular effects of prostaglandins and the therapeutic potential of a new PGF2 alpha analog, PhXA41 (latanoprost), for glaucoma management.前列腺素的眼部效应以及新型前列腺素F2α类似物PhXA41(拉坦前列素)在青光眼治疗方面的潜在应用。
J Lipid Mediat. 1993 Mar-Apr;6(1-3):535-43.
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Long-term maintenance of reduced intraocular pressure by daily or twice daily topical application of prostaglandins to cat or rhesus monkey eyes.通过每日或每日两次局部应用前列腺素于猫或恒河猴眼睛来长期维持降低的眼压。
Invest Ophthalmol Vis Sci. 1983 Mar;24(3):312-9.
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PGF2 alpha/pilocarpine interactions on IOP and accommodation in monkeys.前列腺素F2α/毛果芸香碱对猴眼压及调节功能的相互作用。
Exp Eye Res. 1995 Dec;61(6):677-83. doi: 10.1016/s0014-4835(05)80018-1.
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The ocular pharmacokinetics of eicosanoids and their derivatives. 1. Comparison of ocular eicosanoid penetration and distribution following the topical application of PGF2 alpha, PGF2 alpha-1-methyl ester, and PGF2 alpha-1-isopropyl ester.类二十烷酸及其衍生物的眼药代动力学。1. 局部应用前列腺素F2α、前列腺素F2α-1-甲酯和前列腺素F2α-1-异丙酯后眼内类二十烷酸渗透和分布的比较。
Exp Eye Res. 1987 Feb;44(2):217-26. doi: 10.1016/s0014-4835(87)80006-4.

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