Gomez-Mancilla B, Cutler N R, Leibowitz M T, Spierings E L, Klapper J A, Diamond S, Goldstein J, Smith T, Couch J R, Fleishaker J, Azie N, Blunt D E
Pharmacia & Upjohn Company, Kalamazoo, MI 491001-0199, USA.
Cephalalgia. 2001 Sep;21(7):727-32. doi: 10.1046/j.1468-2982.2001.00208.x.
In this randomized, double-blind, placebo-controlled, parallel-group study, patients received a single 50-mg oral dose of a 5-HT(1D) agonist, PNU-142633 (n = 34), or matching placebo (n = 35) during an acute migraine attack. No statistically significant treatment effects were observed at 1 and 2 h after dosing, even after stratifying by baseline headache intensity. At 1 and 2 h post-dose, 8.8% and 29.4% of the PNU-142633 group, respectively, and 8.6% and 40.0% of the placebo group, respectively, experienced headache relief; 2.9% and 8.8% of the PNU-142633 group and 0% and 5.7% of the placebo group were free of headache pain. Adverse events associated with PNU-142633 treatment included chest pain (two patients) and QTc prolongation (three patients). Results from this study suggest that anti-migraine efficacy is not mediated solely through the 5-HT(1D) receptor subtype, although this receptor may contribute, at least in part, to the adverse cardiovascular effects observed with 5-HT agonist medications.
在这项随机、双盲、安慰剂对照、平行组研究中，患者在急性偏头痛发作期间接受了单次50毫克口服剂量的5-羟色胺（5-HT）（1D）激动剂PNU-142633（n = 34）或匹配的安慰剂（n = 35）。给药后1小时和2小时未观察到统计学上显著的治疗效果，即使按基线头痛强度分层后也是如此。给药后1小时和2小时，PNU-142633组分别有8.8%和29.4%的患者头痛缓解，安慰剂组分别有8.6%和40.0%的患者头痛缓解；PNU-142633组分别有2.9%和8.8%的患者无头痛疼痛，安慰剂组分别有0%和5.7%的患者无头痛疼痛。与PNU-142633治疗相关的不良事件包括胸痛（两名患者）和QTc延长（三名患者）。这项研究的结果表明，抗偏头痛疗效并非仅通过5-HT（1D）受体亚型介导，尽管该受体可能至少部分导致了5-HT激动剂药物所观察到的不良心血管效应。
