Rapoport Alan M, Tepper Stewart J, Bigal Marcelo E, Sheftell Fred D
Department of Neurology, College of Physicians and Surgeons, Columbia University, New York, New York, USA.
CNS Drugs. 2003;17(6):431-47. doi: 10.2165/00023210-200317060-00005.
The 5-HT(1B/1D) receptor agonists (the 'triptans') are migraine-specific agents that have revolutionised the treatment of migraine. They are usually the drugs of choice to treat a migraine attack in progress. Different triptans are available in various strengths and formulations, including oral tablets, orally disintegrating tablets, nasal sprays and subcutaneous injections. In Europe, sumatriptan is also available as a suppository. Specific differences among the triptans exist, as evidenced by different pharmacological profiles including half-life, time to peak plasma concentrations, peak plasma concentrations, area under the concentration-time curve, metabolism and drug-drug interaction profiles. How or whether these differences translate to clinical efficacy and tolerability advantages for one agent over another is not well differentiated. However, delivery systems may play an important role in onset of action. Given that the clinical distinctions among these agents are subtle, identification of the most appropriate triptan for an individual patient requires consideration of the specific characteristics of the patient and knowledge of patient preference, an accurate history of the efficacy of previous acute-care medications and individual features of the drug being considered. The selection of an acute antimigraine drug also depends upon the stratification of the patient's migraine attack by peak intensity, time to peak intensity, level of associated symptoms such as nausea and vomiting, time to associated symptoms, comorbid diseases and concomitant treatments that might cause drug-drug interactions. Individual patient response to the triptans seems to be idiosyncratic and possibly genetically determined. Therefore, a set of specific questions can be used to determine whether a currently used triptan is optimally effective, whether the dose needs to be increased or whether another triptan should be tried. The clinician has in his/her armamentarium an ever-expanding variety of triptans, available in multiple formulations and dosages, which have good safety and tolerability profiles. Continued clinical use will yield familiarity with the various triptans, and it should become possible for the interested physician to match individual patient needs with the specific characteristics of a triptan to optimise therapeutic benefit. Use of the methods outlined in this review in choosing a triptan for an individual patient is probably more likely to lead to migraine relief than making an educated guess as to which triptan is most appropriate.
5-羟色胺（1B/1D）受体激动剂（“曲坦类药物”）是偏头痛特异性药物，彻底改变了偏头痛的治疗方式。它们通常是治疗正在发作的偏头痛的首选药物。不同的曲坦类药物有各种不同的强度和剂型，包括口服片剂、口腔崩解片、鼻喷雾剂和皮下注射剂。在欧洲，舒马曲坦也有栓剂剂型。曲坦类药物之间存在特定差异，不同的药理学特征可以证明这一点，包括半衰期、血浆浓度达峰时间、血浆峰浓度、浓度-时间曲线下面积、代谢以及药物相互作用情况。这些差异如何或是否会转化为一种药物相对于另一种药物在临床疗效和耐受性方面的优势，目前还没有明确区分。然而，给药系统可能在起效方面发挥重要作用。鉴于这些药物之间的临床差异很细微，为个体患者确定最合适的曲坦类药物需要考虑患者的具体特征、了解患者偏好、准确掌握既往急性治疗药物的疗效史以及所考虑药物的个体特性。选择急性偏头痛药物还取决于根据患者偏头痛发作的峰值强度、达到峰值强度的时间、恶心和呕吐等相关症状的程度、出现相关症状的时间、合并疾病以及可能导致药物相互作用的伴随治疗来对患者的偏头痛发作进行分层。个体患者对曲坦类药物的反应似乎具有特异性，可能由基因决定。因此，可以使用一组特定问题来确定当前使用的曲坦类药物是否效果最佳、剂量是否需要增加或者是否应该尝试另一种曲坦类药物。临床医生拥有越来越多的曲坦类药物，有多种剂型和剂量可供选择，这些药物具有良好的安全性和耐受性。持续的临床使用将使人熟悉各种曲坦类药物，感兴趣的医生应该能够将个体患者的需求与曲坦类药物的具体特征相匹配，以优化治疗效果。使用本综述中概述的方法为个体患者选择曲坦类药物，可能比凭经验猜测哪种曲坦类药物最合适更有可能缓解偏头痛。
