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奥洛他定:一种针对肥大细胞的过敏性结膜炎药物。

Olopatadine: a drug for allergic conjunctivitis targeting the mast cell.

机构信息

Department of Neuroscience, Ophthalmology Unit, University of Padua, Via Giustiniani 2, 35128 Padova, Italy.

出版信息

Expert Opin Pharmacother. 2010 Apr;11(6):969-81. doi: 10.1517/14656561003694643.

DOI:10.1517/14656561003694643
PMID:20307221
Abstract

IMPORTANCE OF THE FIELD

Ocular allergic diseases are characterized by specific activation of conjunctival mast cells with subsequent release of preformed and newly formed mediators. Mast cells are thus the first therapeutic target of ocular anti-allergic treatments.

AREAS COVERED IN THIS REVIEW

In this review, a Medline literature search was conducted on conjunctival mast cells, their role in ocular allergy and mast cell stabilization by ocular anti-allergic compounds.

WHAT THE READER WILL GAIN

Olopatadine hydrochloride, a mast cell stabilizer and histamine receptor antagonist, has been shown to inhibit mast cell activation in an in vitro model of human mast cell culture, reducing histamine and TNF-alpha release and upregulating proinflammatory mediators in conjunctival epithelial cells. In the in vivo conjunctival allergen challenge (CAC) model in allergic subjects, combined with objective evaluations of tear mediators and cytology, olopatadine reduced histamine tear levels and all aspects of allergic inflammation, confirming the positive clinical effects observed in active allergic patients.

TAKE HOME MESSAGE

Mast cells play a central role in the pathogenesis of ocular allergy. The CAC model is ideal for assessing the mast cell stabilizing effects of anti-allergic compounds. This review of clinical studies demonstrates the superiority of olopatadine compared with other topical allergic drugs.

摘要

重要性的领域

眼部过敏疾病的特点是特定的结膜肥大细胞的激活,随后释放预先形成的和新形成的介质。肥大细胞因此是眼部抗过敏治疗的第一个治疗靶点。

本篇综述涵盖

在这篇综述中,对结膜肥大细胞进行了 Medline 文献检索,以及它们在眼部过敏中的作用和眼部抗过敏化合物对肥大细胞的稳定作用。

读者将获得的信息

盐酸奥洛他定是一种肥大细胞稳定剂和组胺受体拮抗剂,已被证明可抑制体外人肥大细胞培养模型中的肥大细胞激活,减少组胺和 TNF-α 的释放,并在上皮细胞中上调促炎介质。在过敏受试者的体内结膜变应原挑战 (CAC) 模型中,结合对泪液介质和细胞学的客观评估,奥洛他定可降低组胺的泪液水平和过敏炎症的各个方面,证实了在活跃过敏患者中观察到的积极临床效果。

结论

肥大细胞在眼部过敏发病机制中起核心作用。CAC 模型是评估抗过敏化合物稳定肥大细胞作用的理想模型。对临床研究的综述表明,奥洛他定优于其他局部过敏药物。

相似文献

1
Olopatadine: a drug for allergic conjunctivitis targeting the mast cell.奥洛他定:一种针对肥大细胞的过敏性结膜炎药物。
Expert Opin Pharmacother. 2010 Apr;11(6):969-81. doi: 10.1517/14656561003694643.
2
Mast cell stabilization and anti-histamine effects of olopatadine ophthalmic solution: a review of pre-clinical and clinical research.奥洛他定滴眼液的肥大细胞稳定作用和抗组胺作用:临床前和临床研究综述
Curr Med Res Opin. 2005 Sep;21(9):1377-87. doi: 10.1185/030079905X56547.
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A comparison of the clinical efficacy of pheniramine maleate/naphazoline hydrochloride ophthalmic solution and olopatadine hydrochloride ophthalmic solution in the conjunctival allergen challenge model.马来酸氯苯那敏/盐酸萘甲唑啉滴眼液与盐酸奥洛他定滴眼液在结膜过敏原激发模型中的临床疗效比较。
Clin Ther. 2005 May;27(5):568-77. doi: 10.1016/j.clinthera.2005.04.011.
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Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo.眼部抗过敏化合物在体外可选择性抑制人肥大细胞细胞因子,在体内可抑制结膜细胞浸润。
Clin Exp Allergy. 2007 Nov;37(11):1648-56. doi: 10.1111/j.1365-2222.2007.02782.x. Epub 2007 Sep 17.
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Comparison of the effects of ketotifen fumarate 0.025% and olopatadine HCl 0.1% ophthalmic solutions in seasonal allergic conjunctivities: a 30-day, randomized, double-masked, artificial tear substitute-controlled trial.富马酸酮替芬0.025%滴眼液与盐酸奥洛他定0.1%滴眼液治疗季节性变应性结膜炎的疗效比较:一项为期30天的随机双盲人工泪液替代对照试验。
Clin Ther. 2005 Sep;27(9):1392-402. doi: 10.1016/j.clinthera.2005.09.013.
6
Efficacy of once-daily olopatadine 0.2% ophthalmic solution compared to twice-daily olopatadine 0.1% ophthalmic solution for the treatment of ocular itching induced by conjunctival allergen challenge.与每日两次使用0.1%奥洛他定滴眼液相比,每日一次使用0.2%奥洛他定滴眼液治疗结膜过敏原激发引起的眼部瘙痒的疗效。
Curr Eye Res. 2007 Dec;32(12):1017-22. doi: 10.1080/02713680701736558.
7
Comparative effects of topical ocular anti-allergy drugs on human conjunctival mast cells.局部眼部抗过敏药物对人结膜肥大细胞的比较作用。
Ann Allergy Asthma Immunol. 1997 Dec;79(6):541-5. doi: 10.1016/S1081-1206(10)63063-3.
8
Double-masked, randomized, placebo-controlled clinical study of the mast cell-stabilizing effects of treatment with olopatadine in the conjunctival allergen challenge model in humans.奥洛他定治疗对人结膜过敏原激发模型肥大细胞稳定作用的双盲、随机、安慰剂对照临床研究。
Clin Ther. 2003 Oct;25(10):2539-52. doi: 10.1016/s0149-2918(03)80315-6.
9
Characterization of the ocular antiallergic and antihistaminic effects of olopatadine (AL-4943A), a novel drug for treating ocular allergic diseases.奥洛他定(AL-4943A)是一种治疗眼部过敏性疾病的新型药物,对其眼部抗过敏和抗组胺作用的表征。
J Pharmacol Exp Ther. 1996 Sep;278(3):1252-61.
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Comparative efficacy of olopatadine 0.1% ophthalmic solution versus levocabastine 0.05% ophthalmic suspension using the conjunctival allergen challenge model.使用结膜过敏原激发模型比较0.1%奥洛他定滴眼液与0.05%左卡巴斯汀眼用混悬液的疗效
Curr Med Res Opin. 2004 Dec;20(12):1953-8. doi: 10.1185/030079904X5724.

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