Drugs Acting on Serotonin Receptors

Key points

• 5-HT agonists are used ACUTELY in migraine; 5-HT antagonists in prophylaxis.
• Sumatriptan: 5-HT1D agonist — acute migraine treatment.
• Pizotifen: 5-HT2 antagonist — migraine prophylaxis; methysergide rarely used (retroperitoneal fibrosis).
• Cyproheptadine: 5-HT2 antagonist — controls diarrhoea in carcinoid syndrome (also used in serotonin syndrome).
• Ondansetron/granisetron: 5-HT3 antagonists — antiemetics; most common side effect constipation.