Tamura T, Matsubara M, Takada C, Hasegawa K, Suzuki K, Ohmori K, Karasawa A
Pharmaceutical Research Center, Kyowa Hakko Kogyo Co. Ltd, 1188 Shimotogari, Nagaizumi-cho, Sunto-gun, Shizuoka 411-8731, Japan.
Br J Dermatol. 2004 Dec;151(6):1133-42. doi: 10.1111/j.1365-2133.2004.06172.x.
Olopatadine hydrochloride (olopatadine) is one of the second-generation antihistamines, which is prescribed for allergic disorders such as rhinitis, urticaria and eczema dermatitis.
To investigate the possible anti-inflammatory effect of olopatadine on the chronic contact hypersensitivity response to repeated topical application of oxazolone in mice.
The preventive and therapeutic effects of oral olopatadine were quantified by measurements of ear swelling, cytokine protein and mRNA expression in the ear lesion, and were compared with those of topical betamethasone 17-valerate (betamethasone).
The ear receiving repeated applications of oxazolone exhibited erythema, oedema and abrasion. Both preventive and therapeutic administration of olopatadine (10 mg kg(-1) day(-1)) significantly inhibited the ear swelling and the increased production of interleukin (IL)-4, IL-1beta, granulocyte-macrophage colony-stimulating factor (GM-CSF) and nerve growth factor. In the histopathological analysis, olopatadine ameliorated epidermal hyperplasia and infiltration of inflammatory cells. Consistent with these results, olopatadine significantly reduced the increased expression of interferon-gamma and IL-4 mRNA. Although betamethasone (0.012 mg ear(-1) day(-1)) showed similar activities to olopatadine against these responses, it caused atrophy of the ear skin.
These results indicate that olopatadine is an antihistamine agent having inhibitory activities against chronic inflammatory dermatitis, possibly resulting from its diminishing effect on elevated cytokines.
盐酸奥洛他定是第二代抗组胺药之一,用于治疗鼻炎、荨麻疹和湿疹性皮炎等过敏性疾病。
研究奥洛他定对小鼠反复局部应用恶唑酮所致慢性接触性超敏反应的可能抗炎作用。
通过测量耳部肿胀、耳部病变中细胞因子蛋白和mRNA表达,对口服奥洛他定的预防和治疗效果进行量化,并与外用17-戊酸倍他米松(倍他米松)进行比较。
反复应用恶唑酮的耳部出现红斑、水肿和擦伤。奥洛他定(10 mg kg⁻¹ 天⁻¹)的预防和治疗给药均显著抑制耳部肿胀以及白细胞介素(IL)-4、IL-1β、粒细胞-巨噬细胞集落刺激因子(GM-CSF)和神经生长因子的产生增加。在组织病理学分析中,奥洛他定改善了表皮增生和炎症细胞浸润。与这些结果一致,奥洛他定显著降低了干扰素-γ和IL-4 mRNA的表达增加。尽管倍他米松(0.012 mg 耳⁻¹ 天⁻¹)对这些反应表现出与奥洛他定相似的活性,但它导致了耳部皮肤萎缩。
这些结果表明,奥洛他定是一种对慢性炎症性皮炎具有抑制活性作用的抗组胺药,这可能是由于其对升高的细胞因子的减弱作用所致。