Loder Elizabeth W, Dowson Andrew J, Spierings Egilius L H
Spaulding Rehabilitation Hospital, Harvard Medical School, Boston, MA 02114, USA.
Curr Med Res Opin. 2005;21 Suppl 3:S8-12. doi: 10.1185/030079905x46278.
Controlled clinical trials and extensive clinical use of conventional oral tablets of zolmitriptan, a selective agonist of serotonin1B/1D receptors, have proven the compound to be fast-acting, highly effective, and well-tolerated in the acute treatment of migraine. An orally disintegrating tablet (ODT) of zolmitriptan that dissolves on the tongue without the need for fluid intake has been developed in order to provide an acceptable, convenient alternative for patients who prefer not to, or cannot, take conventional tablets. A fast onset of effective, sustained pain relief was predicted for zolmitriptan ODT on the basis of its bioequivalence with the conventional tablet, which has been confirmed in three randomised, double-blind, placebo-controlled trials of zolmitriptan ODT in the acute treatment of migraine. Compared with placebo, significantly higher proportions of patients treated with zolmitriptan ODT responded to treatment (reduction of moderate or severe headache to mild or no pain) as early as 30 minutes after dosing. Headache response was maintained at 24 hours in significantly higher proportions of patients receiving zolmitriptan ODT compared with placebo. Zolmitriptan ODT also resulted in significantly greater pain-free rates than placebo as early as 1 hour after dosing. Zolmitriptan ODT relieved patients of other migraine-associated symptoms, including nausea, photophobia and phonophobia, and enabled >50% of patients to resume normal daily activities 2 hours after dosing. Adverse events observed with zolmitriptan ODT were similar to those associated with the serotonin1B/1D agonists as a class, and were generally transient and of mild or moderate intensity.
舒马曲坦是一种5-羟色胺1B/1D受体的选择性激动剂，其普通口服片剂的对照临床试验和广泛临床应用已证明该化合物在偏头痛急性治疗中起效快、疗效高且耐受性良好。已研发出一种舒马曲坦口腔崩解片（ODT），该片剂可在舌上溶解，无需饮水，以便为不愿或不能服用普通片剂的患者提供一种可接受的、方便的替代选择。基于舒马曲坦ODT与普通片剂的生物等效性，预计其可快速起效并持续缓解疼痛，这已在三项舒马曲坦ODT急性治疗偏头痛的随机、双盲、安慰剂对照试验中得到证实。与安慰剂相比，服用舒马曲坦ODT的患者中，早在给药后30分钟就有显著更高比例的患者对治疗有反应（中度或重度头痛减轻至轻度或无痛）。与安慰剂相比，接受舒马曲坦ODT的患者中，在24小时时头痛缓解的比例显著更高。舒马曲坦ODT早在给药后1小时就导致无痛率显著高于安慰剂。舒马曲坦ODT还缓解了患者的其他偏头痛相关症状，包括恶心、畏光和畏声，并使超过50%的患者在给药后2小时能够恢复正常日常活动。观察到的舒马曲坦ODT的不良事件与5-羟色胺1B/1D激动剂类药物相关的不良事件相似，通常是短暂的，强度为轻度或中度。
