Trade names Deseril, Sansert ATC code N02CA04 (WHO) CAS ID 361-37-5 | MedlinePlus a603022 Molar mass 353.458 g/mol | |
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AHFS/Drugs.com Micromedex Detailed Consumer Information Pregnancy
category AU: C
US: X (Contraindicated) Legal status AU: S4 (Prescription only)
CA: ℞-only
UK: POM (Prescription only)
US: ℞-only | ||
Methysergide (1-methyl-D-lysergic acid butanolamide or UML-491) is a prescription drug formerly used for prophylaxis of cluster headaches/migraine headaches, but is no longer recommended due to retroperitoneal/retropulmonary fibrosis.
Contents
Medical uses
Methysergide is used to treat headaches such as migraine and other recurrent throbbing headaches. Methysergide is one of the most effective medications for the prevention of migraine, but not for the treatment of an acute attack.
It is also used in carcinoid syndrome to treat severe diarrhea. It may also be used in the treatment of serotonin syndrome.
Side effects
It has a known side effect, retroperitoneal fibrosis, which is severe, although uncommon. Other severe but uncommon side effects include pleural fibrosis, and subendocardial fibrosis.
In addition, there is an increased risk of left-sided cardiac valve dysfunction.
Pharmacology
Methysergide interacts with serotonin (5-HT) receptors. Its therapeutic effect in migraine prophylaxis has been associated with its antagonism at the 5-HT2B receptor. Furthermore, it is an antagonist at the 5-HT2C receptor, while at the 5-HT1A receptor it serves as a partial agonist. It is known to have partial agonist effects on some of the other 5-HT receptors as well. Methysergide is metabolised into methylergometrine in humans, which is responsible for its psychedelic effects.
History
Methysergide was approved by the U.S. Food and Drug Administration (FDA) in 1962.
Novartis withdrew it from the U.S. market after taking over Sandoz, but currently lists it as a product.