Brion N, Bons J, Plas J, Bayliss E M, Advenier C
Laboratoire de Pharmacologie, Hôpital Andre Mignot, Versailles.
Cephalalgia. 1989;9 Suppl 9:79-82. doi: 10.1111/J.1468-2982.1989.TB00077.X.
Subcutaneous GR43175 was examined in patients with acute migraine for efficacy, tolerability and safety in an open, controlled, dose-ranging study. Ten patients with acute, non-medicated, migraine (15 attacks) were assessed for severity of headache and associated symptoms (nausea, vomiting and photophobia). GR43175 plasma samples were monitored serially after dosing. Doses of 2 mg or 3 mg gave rapid relief of all migraine symptoms. Thirteen attacks (86%) had either resolved completely or improved to a mild non-migraine residual headache within 40 min. Treatment was well tolerated at all doses, the only adverse effects being transient pain on injection. Peak plasma concentrations were obtained within 10-20 min; a decline in plasma drug concentration did not result in a relapse in headache severity.
在一项开放、对照、剂量范围研究中,对急性偏头痛患者皮下注射GR43175的疗效、耐受性和安全性进行了研究。对10例急性、未用药的偏头痛患者(15次发作)的头痛严重程度及相关症状(恶心、呕吐和畏光)进行了评估。给药后连续监测GR43175血浆样本。2毫克或3毫克的剂量能迅速缓解所有偏头痛症状。13次发作(86%)在40分钟内完全缓解或改善为轻度非偏头痛残留头痛。所有剂量的治疗耐受性良好,唯一的不良反应是注射时的短暂疼痛。血浆浓度在10 - 20分钟内达到峰值;血浆药物浓度下降并未导致头痛严重程度复发。