TU Munich, Dermatology , Biedersteiner Straße 29, Munich 80802 , Germany
Expert Opin Drug Metab Toxicol. 2013 Nov;9(11):1507-16. doi: 10.1517/17425255.2013.819343. Epub 2013 Jul 22.
Pimecrolimus , a calcineurin inhibitor, is a non-steroidal treatment option in patients aged ≥ 2 years with mild-to-moderate atopic eczema (AE). It was approved as a viable therapeutic option by the FDA in 2001 and in the European Union a year later in 2002. Calcineurin inhibitors inhibit the synthesis of inflammatory cytokines released from T cells and mast cells. In contrast to corticosteroids, calcineurin inhibitors act specifically on proinflammatory cells. Pimecrolimus shows comparative efficacy to mild topical corticosteroids and a special antipruritic effect. Furthermore, examinations of the systemic absorption of pimecrolimus implicated no systemic immunosuppression. In 2006, the FDA set a black box warning in the packaging materials of pimecrolimus alluding to the risk of skin malignancy or lymphomas due to theoretical consideration.
The authors provide a review of pimecrolimus as a treatment for AE. Specifically, the authors present the pharmacokinetic and pharmacodynamic information on pimecrolimus and also review its efficacy. The authors also discuss pimecrolimus' safety and tolerability profile.
Pimecrolimus represents a valuable part of active and proactive therapy in AE. That being said, the long-term safety of topical calcineurin inhibitors remains to be investigated. Given the results from experimental photocarcinogenicity studies, effective sun protection should be employed during the therapy, although an increased risk for skin malignancies and lymphomas was not found in recent studies. Pimecrolimus should be considered as an alternative therapeutic approach in AE treatment management going along with a corticoid-sparing effect.
他克莫司是一种钙调磷酸酶抑制剂,是一种非甾体治疗药物,适用于年龄≥ 2 岁的轻至中度特应性皮炎(AD)患者。2001 年,美国食品药品监督管理局(FDA)批准他克莫司作为一种可行的治疗选择,次年 2002 年,在欧盟也获得批准。钙调磷酸酶抑制剂可抑制 T 细胞和肥大细胞释放的炎症细胞因子的合成。与皮质类固醇不同,钙调磷酸酶抑制剂专门作用于促炎细胞。他克莫司的疗效与轻度局部皮质类固醇相当,且具有特殊的止痒作用。此外,对他克莫司全身吸收的检查表明,他克莫司没有全身免疫抑制作用。2006 年,美国食品药品监督管理局(FDA)在他克莫司的包装材料上添加了黑框警告,暗示由于理论上的考虑,他克莫司存在皮肤恶性肿瘤或淋巴瘤的风险。
作者对他克莫司治疗 AD 进行了综述。具体而言,作者介绍了他克莫司的药代动力学和药效学信息,并对其疗效进行了综述。作者还讨论了他克莫司的安全性和耐受性概况。
他克莫司是 AD 积极主动治疗的有价值的一部分。话虽如此,局部钙调磷酸酶抑制剂的长期安全性仍有待研究。鉴于光致癌性实验研究的结果,在治疗期间应采取有效的防晒措施,尽管最近的研究并未发现皮肤恶性肿瘤和淋巴瘤的风险增加。在 AD 治疗管理中,他克莫司应被视为皮质类固醇节省效应的替代治疗方法。