Methysergide

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Methysergide
Systematic (IUPAC) name
1-Methyl-d-lysergic acid-(1-hydroxybut-2-yl)amide
Identifiers
CAS number	361-37-5
ATC code	N02CA04
PubChem	9681
DrugBank	APRD00463
Chemical data
Formula	C21H27N3O2
Mol. mass	353.458 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	X
Legal status
Routes	?

Methysergide (UML-491) is a prescription drug used for prophylaxis of migraine headaches and is sold under the brand names Sansert and Deseril in 2mg dosages. Methysergide was approved by the FDA in 1962. Its molecular structure is closely related to that of LSD. It is a 5-HT (serotonin) antagonist. It is a receptor antagonist for the 5-HT receptor 2C^[1].

Methysergide is one of the most effective^[2] medications for the prevention of migraine, but not for the treatment of an acute attack. It has a known side effect, retroperitoneal fibrosis^[3], which is severe, although uncommon. In addition, there is an increased risk of left-sided cardiac valve dysfunction.^[2][4]

Novartis withdrew it from the U.S. market after taking over Sandoz, but currently lists it as a product.

Like LSD, methysergide also produces psychedelic and hallucinogenic effects above a dosage of about 4mg.^[5] Full effects are felt with dosages of 8-20mg.^{[citation needed]}

[edit] See also

Triptan

[edit] References

1. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 187
2. ^ ^{a b} Joseph T, Tam SK, Kamat BR, Mangion JR (2003). "Successful repair of aortic and mitral incompetence induced by methylsergide maleate: confirmation by intraoperative transesophageal echocardiography". Echocardiography 20 (3): 283–7. PMID 12848667. 
3. ^ emedicine.com (2002)
4. ^ 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine
5. ^ L. Bender (1970): "Children's Reactions to Psychotomimetic Drugs", Psychotomimetic Drugs, pp. 265-273]

[edit] External links

• Novartis Sansert site.
• Novartis Sansert product description.
• Migraines.org More detailed information on methysergide.
• neurologychannel.com, general information on migraines.

v • d • e Ergolines Lysergic acid derivatives Bromocriptine, Cabergoline, Ergine, Ergonovine, Ergotamine, Lysergic acid, Lysergol, LSD, D-Lysergic acid hydroxyethylamide, Lisuride, Methergine, Methysergide, Pergolide Hallucinogenic lysergamides AL-LAD, ALD-52, BU-LAD, CYP-LAD, DAL, DAM-57, Ergonovine, ETH-LAD, LAE-32, LSD, LPD-824, LSM-775, D-Lysergic acid N-(α-hydroxyethyl)amide, Methylergonovine, MLD-41, PARGY-LAD, PRO-LAD Other ergolines Ergoline Natural sources Argyreia nervosa, Claviceps spp., Ipomoea tricolor, Ipomoea violacea, Rivea corymbosa

v • d • e Antimigraine preparations (N02C) Ergot alkaloids Dihydroergotamine • Ergotamine • Methysergide • Lisuride Corticosteroid derivatives Flumedroxone Selective serotonin (5-HT1) agonists Triptans (Almotriptan, Eletriptan, Frovatriptan, Naratriptan, Rizatriptan, Sumatriptan, Zolmitriptan) Other antimigraine preparations Pizotifen • Clonidine • Topiramate • Amidrine • Iprazochrome • Dimetotiazine • Oxetorone