A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action of serotonin and serotonergic drugs at serotonin (5-HT) receptors. Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include, but are not limited to: Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis. Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors. Risperidone antipsychotic Trazodone Nefazodone Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. They are efficacious in treating chemotherapy-induced emesis and postoperative nausea and vomiting. They include, but are not limited to: Dolasetron Granisetron Ondansetron Palonosetron Tropisetron Other 5-HT3 antagonists have been considered for use in the treatment of irritable bowel syndrome: Alosetron Cilansetron Also, the antidepressant mirtazapine acts as a 5-HT3 antagonist. Although some non-selective serotonin antagonists may have a particular affinity for a specific 5-HT receptor (and thus may be listed below e.g., methysergide), they still may also possess a generalised non-selective action. They include, but are not limited to: Chlorpromazine Cyproheptadine Metergoline Methysergide Mianserin Mirtazapine Oxetorone Pizotifen Propranolol Ritanserin Spiperone Carbinoxamine Cinnarizine Cyproheptadine Hydroxyzine Methdilazine Pizotifen Promethazine Pizotifen is a 5-HT2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis. Also used in the treatment of migrane. Oxatomide Oxetorone Also used in the treatment of migrane.
Silvestro Micera, Stefano Lai, Maria Pasquini, Sara Conti, Marco Mainardi
Heinrich Hofmann, Marijana Mionic Ebersold, Débora Bonvin