斑块状银屑病是一种影响成人和儿童的慢性皮肤自身免疫性疾病。 0.3% 罗氟司特乳膏是目前唯一适用于治疗 12 岁或以上患者斑块状银屑病的外用磷酸二酯酶 4 抑制剂。罗氟司特抑制磷酸二酯酶 4 抑制剂酶，导致环磷酸腺苷的积累，从而抑制炎症介质干扰素 γ 和肿瘤坏死因子-α。罗氟司特每天使用一次，在第 15 天达到稳定状态，在成人中的半衰期约为 4 天。罗氟司特通过细胞色素 P450 酶和结合作用进行广泛的肝脏代谢。罗氟司特 99% 与血浆蛋白结合。罗氟司特的功效和安全性在 DERMIS-1 和 DERMIS-2 临床试验中进行了评估。这些设计相同的双盲、载体对照 3 期试验将 881 名患者随机分配至 0.3% 罗氟司特乳膏或载体，每日一次，持续 8 周。在 DERMIS-1 中，使用 0.3% 罗氟司特乳膏的研究者总体评估成功率为 42.4%，而使用赋形剂的成功率为 6.1%（32.3%-46.9%；P <0.001）。同样，在 DERMIS-2 中，使用 0.3% 罗氟司特乳膏的研究者总体评估成功率为 37.5%，而使用赋形剂的成功率为 6.9%（20.8%-36.9%；P <0.001）。在 881 名参与者中，1% 的参与者因不良反应而停止使用罗氟司特乳膏治疗，而使用赋形剂治疗的参与者为 1.3%。施用部位的荨麻疹（0.3%）是导致罗氟司特停药的最常见不良反应。迄今为止，外用皮质类固醇是治疗轻度斑块型银屑病最常用的药物。敏感区域通常很难用现有的局部疗法（包括皮质类固醇）来治疗。外用罗氟司特已被证明可有效治疗敏感区域，包括皮肤皱褶，并且可能成为某些患者全身治疗的替代方案。美国食品和药物管理局批准外用罗氟司特用于治疗 12 岁或以上患者的斑块状银屑病，包括擦擦部位。版权所有 © 2023 Wolters Kluwer Health, Inc. 保留所有权利。

Plaque psoriasis is a chronic dermatologic autoimmune disease that affects adults and children. Roflumilast 0.3% cream is currently the only topical phosphodiesterase 4 inhibitor indicated for the treatment of plaque psoriasis in patients 12 years or older.Roflumilast inhibits phosphodiesterase 4 inhibitor enzyme leading to the accumulation of cyclic adenosine monophosphate, which suppresses the inflammatory mediators interferon-γ and tumor necrosis factor-α. Roflumilast, applied once daily, reaches steady state by day 15 and has a half life of approximately 4 days in adults. Roflumilast undergoes extensive hepatic metabolism by cytochrome P450 enzymes and conjugation. Roflumilast is 99% bound to plasma proteins.Roflumilast efficacy and safety were evaluated in the DERMIS-1 and DERMIS-2 clinical trials. These identically designed, double-blind, vehicle-controlled phase 3 trials randomized 881 patients to roflumilast 0.3% cream or vehicle, applied once daily for 8 weeks. In DERMIS-1, the Investigator Global Assessment success rate was 42.4% with roflumilast 0.3% cream compared with 6.1% with the vehicle (32.3%-46.9%; P <0.001). Similarly, in DERMIS-2, the Investigator Global Assessment success rate was 37.5% with roflumilast 0.3% cream compared with 6.9% with the vehicle (20.8%-36.9%; P <0.001). Of 881 participants, 1% discontinued treatment with roflumilast cream due to adverse reactions compared with 1.3% treated with vehicle. Urticaria at the application site (0.3%) was the most common adverse reaction that led to discontinuation of roflumilast.To date, topical corticosteroids are the most commonly used agents to treat mild plaque psoriasis. Sensitive areas are often challenging to treat with existing topical therapy, including corticosteroids. Topical roflumilast has shown to be effective in treating sensitive areas, including skin folds, and may be an alternative to systemic therapy for some patients. The Food and Drug Administration approved topical roflumilast for the treatment of plaque psoriasis, including intertriginous areas, for patients 12 years or older.Copyright © 2023 Wolters Kluwer Health, Inc. All rights reserved.