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Drugs. 2013 Sep;73(13):1483-90. doi: 10.1007/s40265-013-0104-5.
The sumatriptan iontophoretic transdermal system (ZECUITY®) [hereafter referred to as sumatriptan TDS] is the first transdermal treatment for migraine to be approved by the US FDA. This article reviews the available pharmacologic properties of sumatriptan TDS and its clinical efficacy and tolerability for the acute treatment of adult patients with migraine with or without aura. Sumatriptan, a selective 5-hydroxy-tryptamine receptor subtype 1 (5-HT₁) agonist, is presumed to exert its therapeutic effect on migraine patients by binding to the 5-HT(1B/1D) receptors on intracranial blood vessels and sensory nerves of the trigeminal system, resulting in cranial vessel constriction and the inhibition of the release of pro-inflammatory neuropeptides and plasma extravasation. In a well designed, phase III clinical trial, sumatriptan TDS was shown to be more effective than placebo at treating a single migraine attack, with significantly more sumatriptan TDS than placebo recipients being headache pain free and nausea free at 2 hours. These data were supported by a long-term, repeat-use study over 12 months. Additionally, sumatriptan TDS was generally well tolerated in clinical trials; the most common adverse events were application-site reactions. The sumatriptan TDS formulation avoids the gastrointestinal tract, and has a controlled, sustained delivery, allowing for patients with migraine-associated nausea and vomiting to receive treatment without the risk of inconsistent absorption or avoidance of tablet use (associated with oral delivery of the drug in these patients). Moreover, it may offer a useful alternative to the nasal spray or subcutaneous sumatriptan formulations. However, definitive conclusions on the comparative efficacy and tolerability of sumatriptan TDS versus other sumatriptan formulations or other migraine drugs are not as yet possible, and data from comparative trials would be of great interest. Sumatriptan TDS is a useful addition to the treatment options available to migraine patients.
舒马曲坦离子电渗透贴剂(ZECUITY®)[以下简称舒马曲坦 TDS]是首个获得美国 FDA 批准的偏头痛透皮治疗药物。本文综述了舒马曲坦 TDS 的现有药理学特性及其在伴有或不伴有先兆的成人偏头痛急性治疗中的临床疗效和耐受性。舒马曲坦是一种选择性 5-羟色胺受体亚型 1(5-HT₁)激动剂,据推测其通过与颅内血管和三叉神经系统感觉神经上的 5-HT(1B/1D)受体结合,对偏头痛患者发挥治疗作用,导致颅血管收缩和抑制促炎神经肽的释放和血浆渗出。在一项精心设计的 III 期临床试验中,舒马曲坦 TDS 在治疗单次偏头痛发作方面比安慰剂更有效,接受舒马曲坦 TDS 治疗的患者在 2 小时时头痛无缓解和无恶心的比例显著高于安慰剂组。这些数据得到了一项为期 12 个月的长期重复使用研究的支持。此外,舒马曲坦 TDS 在临床试验中通常具有良好的耐受性;最常见的不良事件是贴剂部位反应。舒马曲坦 TDS 制剂避免了胃肠道,具有受控的、持续的释放,使伴有偏头痛相关恶心和呕吐的患者能够接受治疗,而不会有吸收不一致或避免使用片剂的风险(在这些患者中,药物的口服给药会出现这种情况)。此外,它可能是鼻喷雾剂或皮下注射舒马曲坦制剂的有效替代药物。然而,关于舒马曲坦 TDS 与其他舒马曲坦制剂或其他偏头痛药物的疗效和耐受性比较,目前尚无法得出明确的结论,并且比较试验的数据将非常有意义。舒马曲坦 TDS 是偏头痛患者可用治疗选择的有益补充。