Gladstone Jonathan Paul, Gawel Marek
Sunnybrook & Women's College Health Sciences Centre, University of Toronto, Toronto, Ontario, Canada.
Drugs. 2003;63(21):2285-305. doi: 10.2165/00003495-200363210-00002.
Migraine is a common, frequently incapacitating, headache disorder that imposes a substantial burden on both the individual patient and society. The last two decades have witnessed an explosion in our understanding of the pathophysiology of migraine, and in our development of an efficacious and diverse therapeutic armamentarium. There are several routes of drug administration available to patients with migraine. All the serotonin 5-HT(1B/1D) receptor agonists (triptans) are available as oral tablets (sumatriptan, rizatriptan, zolmitriptan, naratriptan, almotriptan, frovatriptan and eletriptan). Only sumatriptan is available as a subcutaneous injection. Some triptans are also available via newer routes of administration, including orally disintegrating tablets (rizatriptan and zolmitriptan), rectal suppositories (sumatriptan) and intranasal sprays (sumatriptan and zolmitriptan). Oral disintegrating tablets and other non-oral triptan routes (subcutaneous, intranasal, rectal) are a useful alternative to conventional oral tablets for patients who have difficulty swallowing pills or prefer not to do so, and for patients whose nausea and/or vomiting precludes swallowing tablets and/or makes the likelihood of complete absorption unpredictable. This is important because epidemiological studies in migraine reveal that the vast majority of patients (>90%) have experienced nausea during a migraine attack and more than 50% have nausea with the majority of attacks. Similarly, most (almost 70%) have vomited at some time during an attack and of these patients, almost one-third vomit in the majority of attacks. The newer formulations, rapidly dissolving tablets and intranasal sprays, afford patients the opportunity to use abortive therapy without the need for liquids, at anytime and anywhere, at the onset of a migraine attack. Furthermore, the intranasal sprays are absorbed rapidly and have a prompt onset of action allowing for significant pain free rates versus placebo as early as 15 minutes post administration. The ability to administer treatment early in a migraine attack and have a rapid onset of action is particularly important in acute migraine treatment in order to prevent the development of central sensitisation. While many patients and physicians choose conventional oral tablets because of familiarity and ease of administration, the newer formulations, oral disintegrating tablets and intranasal sprays, should be given consideration as first-line agents in selected patients.
偏头痛是一种常见的、常常使人丧失能力的头痛疾病,给患者个人和社会都带来了沉重负担。在过去二十年里,我们对偏头痛病理生理学的理解以及有效且多样的治疗手段的发展都有了飞跃。偏头痛患者有多种给药途径。所有5-羟色胺5-HT(1B/1D)受体激动剂(曲坦类药物)都有口服片剂(舒马曲坦、利扎曲坦、佐米曲坦、那拉曲坦、阿莫曲坦、夫罗曲坦和依立曲坦)。只有舒马曲坦有皮下注射剂型。一些曲坦类药物也有更新的给药途径,包括口腔崩解片(利扎曲坦和佐米曲坦)、直肠栓剂(舒马曲坦)和鼻喷雾剂(舒马曲坦和佐米曲坦)。口腔崩解片和其他非口服曲坦类药物给药途径(皮下、鼻内、直肠)对于吞咽药片有困难或不愿吞咽的患者,以及恶心和/或呕吐导致无法吞咽片剂和/或使完全吸收的可能性不可预测的患者来说,是传统口服片剂的有用替代方法。这很重要,因为偏头痛的流行病学研究表明,绝大多数患者(>90%)在偏头痛发作期间经历过恶心,超过50%的患者在大多数发作时伴有恶心。同样,大多数(近70%)患者在发作期间的某个时候呕吐过,在这些患者中,近三分之一在大多数发作时呕吐。更新的剂型,即速溶片和鼻喷雾剂,使患者有机会在偏头痛发作开始时随时随地无需用水就能使用缓解治疗。此外,鼻喷雾剂吸收迅速,起效迅速,与安慰剂相比,给药后15分钟就有显著的无痛率。在偏头痛发作早期给药并迅速起效的能力在急性偏头痛治疗中尤为重要,以防止中枢敏化的发展。虽然许多患者和医生因为熟悉和易于给药而选择传统口服片剂,但更新的剂型,即口腔崩解片和鼻喷雾剂,在特定患者中应被视为一线药物。