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酮咯酸对兔铜绿假单胞菌眼部感染的影响。

Effect of ketorolac on Pseudomonas aeruginosa ocular infection in rabbits.

作者信息

Fraser-Smith E B, Matthews T R

机构信息

Syntex Research, Department of Antimicrobial Research, Palo Alto, California.

出版信息

J Ocul Pharmacol. 1988 Summer;4(2):101-9. doi: 10.1089/jop.1988.4.101.

DOI:10.1089/jop.1988.4.101
PMID:3262701
Abstract

Corticosteroids can exacerbate bacterial ocular infections, even in the presence of antibiotics. Ketorolac tromethamine is a new non-steroidal compound being considered as an anti-inflammatory ophthalmic drug. In this study, rabbits ocularly infected with Pseudomonas aeruginosa were treated topically with 0.4 percent tobramycin sulfate 4 times daily for 7 days to control infection. At the same times, either 0.5 percent ketorolac, 0.1 percent dexamethasone or vehicle was also given topically. Animals were scored for severity of both conjunctivitis (maximum severity rates score of 10) and corneal opacity (maximum of 4) using the Draize scale. Severity of the infection was determined by counting the number of punctate lesions which developed on the cornea. Nine days after treatment ended, the number of these lesions was the same for ketorolac as for the vehicle (respectively, 16.7 +/- 3 and 13.8 +/- 3, mean +/- SE, n = 24), indicating no exacerbation of the infection, whereas with dexamethasone these parameters increased (30.2 +/- 4, n = 24). During treatment, ketorolac reduced conjunctivitis (1.8 +/- 0.2, n = 120) when compared with the vehicle (2.9 +/- 0.2, n = 120), whereas dexamethasone did not (3.8 +/- 0.2, n V 120); neither ketorolac nor dexamethasone reduced corneal opacity (respectively, 2.3 +/- 0.05 and 2.6 +/- 0.1, n = 24) compared with vehicle (2.2 +/- 0.05, n = 24). After treatment, both conjunctivitis and corneal opacity became more severe only in dexamethasone treated eyes (respectively, 4.4 +/- 0.2, n = 120 and 3.0 +/- 0.02, n = 24). Thus, ketorolac appears to be an anti-inflammatory agent that does not worsen bacterial ocular infection.

摘要

皮质类固醇可加重细菌性眼部感染,即使在使用抗生素的情况下也是如此。酮咯酸氨丁三醇是一种新型非甾体化合物,正被考虑用作抗炎眼科药物。在本研究中,对眼部感染铜绿假单胞菌的家兔每天局部给予0.4%硫酸妥布霉素4次,持续7天以控制感染。同时,局部给予0.5%酮咯酸、0.1%地塞米松或赋形剂。使用Draize评分系统对动物的结膜炎严重程度(最高严重程度评分为10分)和角膜混浊程度(最高为4分)进行评分。通过计算角膜上出现的点状病变数量来确定感染的严重程度。治疗结束9天后,酮咯酸组和赋形剂组的这些病变数量相同(分别为16.7±3和13.8±3,平均值±标准误,n = 24),表明感染未加重,而地塞米松组这些参数增加(30.2±4,n = 24)。在治疗期间,与赋形剂相比(2.9±0.2,n = 120),酮咯酸减轻了结膜炎(1.8±0.2,n = 120),而地塞米松则没有(3.8±0.2,n = 120);与赋形剂相比(2.2±0.05,n = 24),酮咯酸和地塞米松均未减轻角膜混浊(分别为2.3±0.05和2.6±0.1,n = 24)。治疗后,仅地塞米松治疗的眼睛结膜炎和角膜混浊变得更严重(分别为4.4±0.2,n = 120和3.0±0.02,n = 24)。因此,酮咯酸似乎是一种不会加重细菌性眼部感染的抗炎药物。

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2
Aqueous, oil, and ointment formulations of ketorolac: efficacy against prostaglandin E2-induced ocular inflammation and safety: a technical note.酮咯酸的水性、油性和软膏制剂:对前列腺素E2诱导的眼部炎症的疗效及安全性:技术说明
AAPS PharmSciTech. 2006;7(4):96. doi: 10.1208/pt070496.
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In vivo ocular availability of ketorolac following ocular instillations of aqueous, oil, and ointment formulations to normal corneas of rabbits: a technical note.
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AAPS PharmSciTech. 2005 Oct 24;6(3):E523-6. doi: 10.1208/pt060365.
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The emerging roles of topical non-steroidal anti-inflammatory agents in ophthalmology.局部用非甾体抗炎药在眼科领域的新作用
Br J Ophthalmol. 1996 May;80(5):480-5. doi: 10.1136/bjo.80.5.480.
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Ketorolac. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential.酮咯酸。对其药效学和药代动力学特性以及治疗潜力的综述。
Drugs. 1990 Jan;39(1):86-109. doi: 10.2165/00003495-199039010-00008.