Wilkinson M, Pfaffenrath V, Schoenen J, Diener H C, Steiner T J
City of London Migraine Clinic, UK.
Cephalalgia. 1995 Oct;15(5):337-57. doi: 10.1046/j.1468-2982.1995.1505337.x.
Sumatriptan is a potent and selective agonist at the vascular 5HT1 receptor which mediates constriction of certain large cranial blood vessels and/or inhibits the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater following activation of the trigeminovascular system. The mode of action of this drug in migraine and cluster headache is discussed. On the basis of a detailed review of all published trials and available data from post-marketing studies, the efficacy, safety, tolerability and the place of oral and subcutaneous sumatriptan in the treatment of both conditions are assessed. A number of double-blind clinical trials have demonstrated that sumatriptan 100 mg administered orally is clearly superior to placebo in the acute treatment of migraine headache and achieves significantly greater response rates than ergotamine or aspirin. In other studies, 70 to 80% of patients receiving sumatriptan 6 mg sc experienced relief of migraine headaches by 1 or 2 h after administration, and patients consistently required less rescue medication for unresolved symptoms. Sumatriptan was also effective in relieving associated migraine symptoms like nausea and vomiting. Sumatriptan was equally effective regardless of migraine type or duration of migraine symptoms. Overall, approximately 40% of patients who initially responded to oral or subcutaneous sumatriptan experienced recurrence of their headache usually within 24 h, effectively treated by a further dose of this drug. In 75% of patients with cluster headache treated with sumatriptan 6 mg sc, relief was achieved within 15 min. Based on pooled study data, sumatriptan is generally well tolerated and most adverse events are transient. Adverse events following oral administration include nausea, vomiting, malaise, fatigue and dizziness. With the subcutaneous injection, injection site reactions occur in approximately 30%. Chest syumptoms are reported in 3 to 5% but have been associated with myocardial ischaemia only in rare isolated cases. The recommended dosage of sumatriptan at the onset of migraine symptoms is 100 mg orally or 6 mg subcutaneously. The recommended dosage for cluster headache is 6 mg sumatriptan sc. Sumatriptan must not be given together with vasoconstrictive substances, e.g., ergotamines, or with migraine prophylactics with similar properties, e.g., methysergide. Sumatriptan should not be given during the migraine aura. It is contraindicated in patients with ischaemic heart disease, previous myocardial infarction, Prinzmetal (variant) angina and uncontrolled hypertension.
舒马曲坦是一种强效且具有选择性的血管5HT1受体激动剂,该受体介导某些大的颅脑血管收缩和/或在三叉神经血管系统激活后抑制硬脑膜中血管周围三叉神经轴突释放血管活性神经肽。本文讨论了该药物在偏头痛和丛集性头痛中的作用方式。在对所有已发表试验和上市后研究的可用数据进行详细综述的基础上,评估了口服和皮下注射舒马曲坦在治疗这两种疾病中的疗效、安全性、耐受性及地位。多项双盲临床试验表明,口服100mg舒马曲坦在偏头痛急性治疗中明显优于安慰剂,且缓解率显著高于麦角胺或阿司匹林。在其他研究中,70%至80%接受6mg皮下注射舒马曲坦的患者在给药后1至2小时偏头痛症状得到缓解,且患者持续需要较少的缓解症状的急救药物。舒马曲坦在缓解恶心和呕吐等相关偏头痛症状方面也有效。无论偏头痛类型或偏头痛症状持续时间如何,舒马曲坦均同样有效。总体而言,最初对口服或皮下注射舒马曲坦有反应的患者中,约40%通常在24小时内头痛复发,再次服用该药物可有效治疗。在75%接受6mg皮下注射舒马曲坦治疗的丛集性头痛患者中,15分钟内症状得到缓解。根据汇总研究数据,舒马曲坦一般耐受性良好,且大多数不良事件是短暂的。口服后的不良事件包括恶心、呕吐、不适、疲劳和头晕。皮下注射时,约30%会出现注射部位反应。3%至5%的患者报告有胸部症状,但仅在极少数孤立病例中与心肌缺血有关。偏头痛症状发作时舒马曲坦的推荐剂量为口服100mg或皮下注射6mg。丛集性头痛的推荐剂量为皮下注射6mg舒马曲坦。舒马曲坦不得与血管收缩物质(如麦角胺)或具有类似性质的偏头痛预防性药物(如美西麦角)同时使用。偏头痛先兆期不应使用舒马曲坦。缺血性心脏病、既往心肌梗死、变异型心绞痛和未控制的高血压患者禁用。