Müller W, Fiebich B L, Stratz T
Hochrhein-Institut für Rehabilitationsforschung, Bad Säckingen.
Z Rheumatol. 2006 Oct;65(6):546, 548-52. doi: 10.1007/s00393-005-0014-3.
Various rheumatic diseases like fibromyalgia, systemic inflammatory rheumatic disorders and localized diseases, such as arthritides and activated arthroses, tendinopathies and periarthropathies, as well as trigger points can be improved considerably by treatment with the 5-HT3 receptor antagonist tropisetron. Particularly in the latter group of diseases, local injections have done surprisingly rapid analgesic action. This effect matches that of local anesthetics, but lasts considerably longer and is comparable to local injections of local anesthetics combined with corticosteroids. The action of the 5-HT3 receptor antagonists can be attributed to an antinociceptive effect that occurs at the same time as an antiphlogistic and probably also an immunosuppressive effect. Whereas an inhibited release of substance P from the nociceptors, and possibly some other neurokins as well, seems to be the most likely explanation for the antinociceptive action, the antiphlogistic effect is primarily due to an inhibited formation of various different phlogistic substances; in some conditions, like systemic inflammatory rheumatic diseases, for example, the 5-HT3 receptor antagonists may exert an immunosuppressive effect in addition to this.
多种风湿性疾病，如纤维肌痛、全身性炎症性风湿性疾病以及局部性疾病，如关节炎和活动性关节病、肌腱病和关节周围疾病，还有触发点，通过使用5-羟色胺3（5-HT3）受体拮抗剂托烷司琼进行治疗可得到显著改善。特别是在后一组疾病中，局部注射具有惊人的快速镇痛作用。这种效果与局部麻醉剂相当，但持续时间长得多，并且与局部注射局部麻醉剂加皮质类固醇的效果相当。5-HT3受体拮抗剂的作用可归因于一种与抗炎作用同时出现的抗伤害感受作用，可能还有免疫抑制作用。伤害感受器中P物质释放受抑制，可能还有其他一些神经激肽释放受抑制，似乎是抗伤害感受作用最可能的解释，而抗炎作用主要是由于多种不同炎症物质的形成受抑制；在某些情况下，如全身性炎症性风湿性疾病，例如，5-HT3受体拮抗剂除此之外可能还发挥免疫抑制作用。
