Drug intelligence / Profile preview

cyproheptadine

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Cyproheptadine is a first-generation antihistamine and serotonin antagonist used primarily to treat allergic symptoms such as sneezing, runny nose, itching, red or watery eyes, and other manifestations of seasonal allergies. It is also used for appetite stimulation and has off-label uses in the treatment of serotonin syndrome and certain types of headaches, including migraines. Cyproheptadine acts as a potent competitive antagonist at both histamine H1 receptor and several serotonin (5-HT) receptors. Its antagonism at the hypothalamic appetite center may explain its ability to stimulate appetite. Additionally, it exhibits anticholinergic and sedative effects and has been reported to block calcium channels at the pituitary level.

Brand names
Periactin
Other names
cyproheptadine
02

Targets

mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)

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