5-HT3-Rezeptor-Antagonisten als Analgetika bei rheumatischen Erkrankungen

Abstract

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.

Pharmacological profile of dexketoprofen in orofacial pain

“…It has been proposed that 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 [21].…”

Immunomodulatory Effects Mediated by Serotonin

“…This has led to proposals that 5-HT is involved in the pathology, onset, and/or progression of the disease. Treating patients with 5-HT 3 antagonists combined with intra-articular glucocorticoids has analgesic effects [ 246 ]. While there have yet to be any reports on the responses of RA patient immune cells to 5-HT, the role of serotonergic system in arthritis or osteoarthritis has been studied in vitro and in vivo .…”

Identification of 5-HT3 receptors on human platelets: Increased surface immunoreactivity after activation with adenosine diphosphate (ADP) and thrombin receptor-activating peptide (TRAP)

“…The fact that5-HT3 receptors seem to be involved in the specificand unspecific immune response suggests abasic immunomodulatoryrole of 5-HT3 receptors. This is supported by clinical datashowing therapeuticallyeffectsof5-HT3 receptor antagonist in the treatment of chronic inflammatorydiseases (5,6,16,17).…”