Dowson Andrew J
The King's Headache Service, King's College Hospital, Denmark Hill, London, SE5 9RS, UK.
Expert Rev Neurother. 2004 May;4(3):339-48. doi: 10.1586/14737175.4.3.339.
Almotriptan (Almogran, Lundbeck; Almirall Prodesfarma; Axert, Ortho-McNeil) is a novel 5-HT(1B/1D) receptor agonist (triptan) that is widely available on prescription for the acute treatment of migraine. Almotriptan has pharmacodynamic and pharmacokinetic profiles that make it suitable for use in this indication. It is a potent agonist at 5-HT(1B), (1D) and (1F) receptors, while having a low affinity for other 5-HT receptors. It is also a potent inhibitor of neurogenic inflammation. Almotriptan has a high oral bioavailability, is absorbed rapidly, has a relatively short plasma half-life and its route of elimination presents few potential problems. Placebo-controlled dose-finding studies have demonstrated that almotriptan tablets are effective and well-tolerated in the acute treatment of migraine, with a 12.5 mg dose providing the best balance between efficacy and tolerability. Large placebo-controlled studies show that the efficacy of oral almotriptan is comparable with that of the other oral triptans. In direct comparator-controlled studies, almotriptan was as effective as sumatriptan 50 and 100 mg but had a superior tolerability profile. Furthermore, the efficacy and tolerability of almotriptan is sustained in the long term following open-label administration. Meta-analyses and post hoc analyses of clinical data confirm these findings. In conclusion, almotriptan 12.5 mg is a good therapeutic choice for the symptomatic treatment of acute migraine attacks.
阿莫曲坦(Almogran,灵北公司;Almirall Prodesfarma公司;Axert,奥多-麦尼尔公司)是一种新型5-羟色胺(5-HT)(1B/1D)受体激动剂(曲坦类药物),可凭处方广泛获取,用于偏头痛的急性治疗。阿莫曲坦具有使其适用于该适应症的药效学和药代动力学特征。它是5-HT(1B)、(1D)和(1F)受体的强效激动剂,而对其他5-HT受体的亲和力较低。它也是神经源性炎症的强效抑制剂。阿莫曲坦具有高口服生物利用度,吸收迅速,血浆半衰期相对较短,其消除途径几乎没有潜在问题。安慰剂对照剂量探索研究表明,阿莫曲坦片在偏头痛的急性治疗中有效且耐受性良好,12.5毫克剂量在疗效和耐受性之间提供了最佳平衡。大型安慰剂对照研究表明,口服阿莫曲坦的疗效与其他口服曲坦类药物相当。在直接对照比较研究中,阿莫曲坦与50毫克和100毫克舒马曲坦效果相当,但耐受性更佳。此外,开放标签给药后,阿莫曲坦的疗效和耐受性在长期内得以维持。临床数据的荟萃分析和事后分析证实了这些发现。总之,12.5毫克阿莫曲坦是急性偏头痛发作症状性治疗的良好治疗选择。