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Serotonin receptors and valvular heart disease
Published in Demetrius Pertsemlidis, William B. Inabnet III, Michel Gagner, Endocrine Surgery, 2017
Javier G. Castillo, David H. Adams
Ergot derivatives have been similarly linked to DIHVD [32]. Ergotamine and methysergide (classically prescribed for the treatment and prophylaxis of migraine), as well as nonspecific dopamine agonists such as pergolide and cabergoline (routinely recommended for the treatment of Parkinson’s disease), share a similar chemical structure with 5-HT and therefore can interact with its receptors, particularly 5-HT2B receptors [34]. Accordingly, the incidence of valve disease (on echocardiography) in patients taking pergolide or cabergoline has been published to be 23% and 28%, respectively, versus none in those patients on nonergot dopamine agonists [35]. Interestingly, those ergot derivatives with more affinity for 5-HT2A receptors, such as lisuride, bromocriptine, and terguride, have not been associated with DIHVD. These findings lead to support for the specific implication of 5-HT2B receptors in the development of valvulopathies [36]. As a consequence, multiple drugs have been tested for agonist activity at the 5-HT2B receptor, including guanfacine, oxymetazoline, quinidine, xylometazoline, and fenoldopam. Among the latter, although still under investigation, guanfacine (antihypertensive agent in adults and recently indicated to treat attention deficit in infants) and quinidine (antiarrhythmic) are of special concern.
Serotonin and valvular heart disease
Published in Expert Opinion on Therapeutic Targets, 2022
Helge Waldum, Rune Wiseth, Alexander Wahba
There are thus strong indications that serotonin may be central in the pathogenesis of all types of progressive heart valve disease and play an important role in pulmonal hypertension as well as systemic sclerosis. A selective 5-HT2B antagonist like terguride should therefore be evaluated particularly in the treatment of valvular heart disease, but also in pulmonal hypertension at least as part of systemic sclerosis. It is a sad fact that until now no efficient drug therapy of any of these conditions exists due to imperfect understanding of their pathogenesis.
Current immunosuppressive and antifibrotic therapies of systemic sclerosis and emerging therapeutic strategies
Published in Expert Review of Clinical Pharmacology, 2020
Bénédict Fallet, Ulrich A. Walker
Terguride is a 5-HT2B antagonist. In a small open-label study of 12 SSc patients, terguride induced a downregulation of fibrosis-related biomarkers. Skin fibrosis as measured by the mRSS also improved significantly in the treatment group as compared to the control group [136].