Department of Dermatology, Arida Municipal Hospital, Arida, Japan.
J Dermatol. 2012 Jun;39(6):536-40. doi: 10.1111/j.1346-8138.2011.01432.x. Epub 2011 Nov 14.
5-Hydroxytryptamine 2A serotonin receptor (5-HT(2A) ) is associated with the contraction of vascular smooth muscle, platelet aggregation and thrombus formation and coronary artery spasms. Sarpogrelate hydrochloride (sarpogrelate) is a selective 5-HT(2A) antagonist and was supposed to be effective for Raynaud's phenomenon with collagen disease. Sarpogrelate has not been investigated regarding the effects, safety and quality of life (QOL) in patient with skin ulcers of collagen disease. Eleven patients with skin ulcers and systemic sclerosis (SSc) were administrated sarpogrelate p.o. three times a day for 3-6 months. The area (mean ± standard error) of skin ulcer at the pretreatment, and after 3 and 6 months of sarpogrelate intake was 2.1 ± 0.8, 0.2 ± 0.1 and 0.1 ± 0.1 mm(2), respectively. The reduction of skin ulcer area was significant after 3 months of sarpogrelate intake. In assessment of QOL, scores of symptoms and emotions but not of functioning were significantly improved after sarpogrelate intake. The global score (mean ± SE) of Skindex-16 at pretreatment, and after 3 and 6 months of sarpogrelate intake was 31.8 ± 8.7, 23.7 ± 8.3 and 10.9 ± 4.6, respectively. The score was significantly improved after 6 months of sarpogrelate intake. There were no obvious side-effects during this study. Sarpogrelate was considered to be a useful drug to improve skin ulcers and QOL in patients with SSc.
5-羟色胺 2A 受体（5-HT（2A））与血管平滑肌收缩、血小板聚集和血栓形成以及冠状动脉痉挛有关。盐酸沙格雷酯（沙格雷酯）是一种选择性 5-HT（2A）拮抗剂，据推测对胶原病引起的雷诺现象有效。尚未研究沙格雷酯对胶原病皮肤溃疡患者的疗效、安全性和生活质量（QOL）。11 例皮肤溃疡和系统性硬化症（SSc）患者每天口服沙格雷酯 3 次，持续 3-6 个月。治疗前、治疗 3 个月和 6 个月时皮肤溃疡的面积（平均值±标准误差）分别为 2.1±0.8、0.2±0.1 和 0.1±0.1mm2。治疗 3 个月后皮肤溃疡面积明显缩小。在 QOL 评估中，症状和情绪评分而非功能评分显著改善。治疗前、治疗 3 个月和 6 个月时 Skindex-16 的全球评分（平均值±SE）分别为 31.8±8.7、23.7±8.3 和 10.9±4.6。治疗 6 个月后评分显著改善。研究期间无明显不良反应。沙格雷酯被认为是一种改善 SSc 患者皮肤溃疡和 QOL 的有效药物。
