Link Andrea Stephanie, Kuris Anikó, Edvinsson Lars
Biomedical Center Lund, Lund, Sweden.
J Headache Pain. 2008 Feb;9(1):5-12. doi: 10.1007/s10194-008-0011-4. Epub 2008 Jan 23.
Primary headaches such as migraine are among the most prevalent neurological disorders, affecting up to one-fifth of the adult population. The scientific work in the last decade has unraveled much of the pathophysiological background of migraine, which is now considered to be a neurovascular disorder. It has been discovered that the trigemino-cerebrovascular system plays a key role in migraine headache pathophysiology by releasing the potent vasodilator calcitonin gene-related peptide (CGRP). This neuropeptide is released in parallel with the pain and its concentration correlates well with the intensity of the headache. The development of drugs of the triptan class has provided relief for the acute attacks but at the cost of, mainly cardiovascular, side effects. Thus, the intention to improve treatment led to the development of small CGRP receptor antagonists such as olcegepant (BIBN4096BS) and MK-0974 that alleviate the acute migraine attack without acute side events. The purpose of this review is to give a short overview of the pathological background of migraine headache and to illustrate the mechanisms behind the actions of triptans and the promising CGRP receptor blockers.
偏头痛等原发性头痛是最常见的神经系统疾病之一，影响着多达五分之一的成年人口。过去十年的科学研究揭示了偏头痛的许多病理生理背景，目前认为偏头痛是一种神经血管疾病。现已发现，三叉神经血管系统通过释放强效血管舒张剂降钙素基因相关肽（CGRP）在偏头痛性头痛的病理生理学中起关键作用。这种神经肽与疼痛同时释放，其浓度与头痛强度密切相关。曲坦类药物的开发为急性发作提供了缓解，但主要以心血管副作用为代价。因此，为改善治疗而研发了小型CGRP受体拮抗剂，如olcegepant（BIBN4096BS）和MK-0974，它们可缓解急性偏头痛发作且无急性副作用。本综述的目的是简要概述偏头痛性头痛的病理背景，并阐明曲坦类药物和有前景的CGRP受体阻滞剂的作用机制。
