Spencer C M, Gunasekara N S, Hills C
Adis International Limited, Auckland, New Zealand.
Drugs. 1999 Aug;58(2):347-74. doi: 10.2165/00003495-199958020-00016.
Zolmitriptan is a selective serotonin 5-HT1B/1D receptor agonist ('triptan'). Its efficacy and tolerability have been assessed in a number of randomised, placebo-controlled, double-blind trials in large numbers of adults with moderate to severe migraine attacks. Oral zolmitriptan 2.5 and 5mg has a rapid onset of action (significant headache relief is observed at 45 minutes) and efficacy is sustained in most patients who respond at 2 hours. The drug is significantly more effective than placebo as measured by a number of parameters including 2-hour headache response rates and pain-free response rates. Other symptoms of migraine, including nausea, photophobia and phonophobia are also alleviated with zolmitriptan. Zolmitriptan is effective in the treatment of migraine associated with menses and migraine with aura. There is some evidence to support the use of zolmitriptan in patients with migraine who have had a poor response to previous therapy. The efficacy of zolmitriptan appears to be maintained, with no tachyphylaxis, following repeated administration for multiple attacks of migraine over a prolonged period of time, with high headache response rates reported over all attacks. In comparison with placebo, the incidence of persistent migraine headache is reduced by zolmitriptan and recurrent migraine headache occurs less frequently with the active treatment. Zolmitriptan has also demonstrated efficacy in the treatment of persistent and/or recurrent migraine headache. For relief of migraine headache, zolmitriptan 5mg had similar efficacy to sumatriptan 100mg for a single attack, but generally was more effective than sumatriptan 25 and 50mg for multiple attacks, in single trials. The incidence of recurrent headache with zolmitriptan was similar to that with sumatriptan. Zolmitriptan is generally well tolerated with most adverse events being mild to moderate, transient and resolving without intervention or the need for treatment withdrawal. The most common adverse events with zolmitriptan therapy are asthenia, heaviness other than that of the chest or neck, dry mouth, nausea, dizziness, somnolence, paraesthesia, warm sensation, tightness, vasodilation and chest pain.
Zolmitriptan is effective across a wide range of migraine subtypes, maintains efficacy when used in the long term and is generally well tolerated. Further clinical experience is necessary to define the position of zolmitriptan among other currently or soon to be available selective 5-HT1B/1D receptor agonists. However, on the basis of available data, zolmitriptan should emerge as a useful treatment option in the management of patients with moderate to severe migraine.
佐米曲普坦是一种选择性5-羟色胺5-HT1B/1D受体激动剂(“曲坦类药物”)。在大量患有中度至重度偏头痛发作的成年人中进行的多项随机、安慰剂对照、双盲试验中,已对其疗效和耐受性进行了评估。口服2.5毫克和5毫克的佐米曲普坦起效迅速(45分钟时可观察到头痛明显缓解),且大多数在2小时时有反应的患者疗效得以持续。通过包括2小时头痛缓解率和无痛缓解率在内的多个参数衡量,该药物比安慰剂显著更有效。佐米曲普坦还可缓解偏头痛的其他症状,包括恶心、畏光和畏声。佐米曲普坦对与月经相关的偏头痛和伴有先兆的偏头痛有效。有一些证据支持在对先前治疗反应不佳的偏头痛患者中使用佐米曲普坦。在长时间内多次偏头痛发作重复给药后,佐米曲普坦的疗效似乎得以维持,无快速耐受性,所有发作的头痛缓解率均较高。与安慰剂相比,佐米曲普坦可降低持续性偏头痛头痛的发生率,积极治疗时复发性偏头痛头痛的发生频率更低。佐米曲普坦在治疗持续性和/或复发性偏头痛头痛方面也已证明有效。为缓解偏头痛头痛,单次发作时5毫克佐米曲普坦与100毫克舒马曲坦疗效相似,但在单项试验中,多次发作时佐米曲普坦通常比25毫克和50毫克舒马曲坦更有效。佐米曲普坦复发性头痛的发生率与舒马曲坦相似。佐米曲普坦一般耐受性良好,大多数不良事件为轻至中度、短暂性,无需干预或停药即可缓解。佐米曲普坦治疗最常见的不良事件为乏力、非胸部或颈部的沉重感、口干、恶心、头晕、嗜睡、感觉异常、温热感、紧绷感、血管扩张和胸痛。
佐米曲普坦对多种偏头痛亚型均有效,长期使用时疗效得以维持,且一般耐受性良好。需要更多临床经验来确定佐米曲普坦在其他现有或即将上市的选择性5-HT1B/1D受体激动剂中的地位。然而,根据现有数据,佐米曲普坦应成为治疗中度至重度偏头痛患者的一种有用选择。