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5-HT2B agonist

• May induce fibrotic changes in multiple organs
• The forbidden mechanism: new drug development is halted for drugs found to activate 5-HT2B
• Vasoconstriction → pulmonary hypertension risk

Drugs with this mechanism (5)

• Cabergoline — Long-acting dopamine agonist for prolactinomas; valvulopathy at high dose.
• Dihydro­ ergotamine — Injectable or intranasal ergot for refractory migraine; never combine closely with a triptan.
• Ergotamine — Ergot alkaloid for migraine; vasoconstrictive, largely supplanted by triptans.
• Fenfluramine — Serotonin releaser once in "fen-phen"; now for Dravet seizures, valvulopathy risk.
• Serotonin — Endogenous monoamine neurotransmitter (5-HT).

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