Lecchi Marzia, D'Alonzo Lidia, Negro Andrea, Martelletti Paolo
University of Milan, Department of Biotechnology and Biosciences , Bicocca, Milan , Italy.
Expert Opin Drug Metab Toxicol. 2014 Oct;10(10):1381-95. doi: 10.1517/17425255.2014.952631.
For more than a century, aspirin has been used for the acute treatment of primary headaches. However, the many formulations available are characterized by differences in the pharmacokinetic profile that could affect therapy effectiveness.
The formulations of aspirin affect the speed of absorption of the drug. This feature, in turn, moduates the peak plasmatic concentration (the faster the absorption, the higher the peak plasmatic concentration of aspirin). Recently, a new formulation, consisting in a micronized tablet with an effervescent nucleus, has been shown to be comparable to the formulations associated to the faster absorption. The efficacy of aspirin in migraine is well characterized: the drug is able to rapidly reduce pain and restore functionality, acting also on associated symptoms, in a manner comparable to that of oral sumatriptan. In tension-type headache, aspirin acts in a dose-dependent fashion. The safety profile of the drug is favorable: gastrointestinal complaints are generally mild in intensity and with an incidence comparable to that of ibuprofen and paracetamol.
According to international guidelines, aspirin should be considered as first-line therapy in primary headaches. Formulations that allow fast absorption, like the new micronized tablets, and portability, are to be preferred.
一个多世纪以来,阿司匹林一直用于原发性头痛的急性治疗。然而,现有的多种制剂在药代动力学特征上存在差异,这可能会影响治疗效果。
阿司匹林的制剂会影响药物的吸收速度。这一特性进而调节血浆峰值浓度(吸收越快,阿司匹林的血浆峰值浓度越高)。最近,一种新的制剂,即具有泡腾核的微粉化片剂,已被证明与吸收较快的制剂相当。阿司匹林在偏头痛中的疗效已得到充分表征:该药物能够迅速减轻疼痛并恢复功能,对相关症状也有作用,其作用方式与口服舒马曲坦相当。在紧张型头痛中,阿司匹林呈剂量依赖性发挥作用。该药物的安全性良好:胃肠道不适通常程度较轻,发生率与布洛芬和对乙酰氨基酚相当。
根据国际指南,阿司匹林应被视为原发性头痛的一线治疗药物。应首选能快速吸收的制剂,如新的微粉化片剂,以及便于携带的制剂。