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Methysergide

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Methysergide chemical structure
Methysergide

1-Methyl-d-lysergic acid-(1-hydroxybut-2-yl)amide
IUPAC name
CAS number
361-37-5
ATC code

N02CA04

PubChem
9681
DrugBank
APRD00463
Chemical formula {{{chemical_formula}}}
Molecular weight 353.458 g/mol
Bioavailability
Metabolism
Elimination half-life
Excretion {{{excretion}}}
Pregnancy category X
Legal status
Routes of administration


Main article: Serotonin antagonists

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.

PharmacologyEdit

It is a receptor antagonist for the 5-HT receptor 2C[1]. It also is a 5-HT1A receptor antagonist.[2]

It is known to have partial agonists effects on 5-HT receptors as well.[3]

UsesEdit

Methysergide is one of the most effective[4] medications for the prevention of migraine, but not for the treatment of an acute attack.

Side effectsEdit

It has a known side effect, retroperitoneal fibrosis[5], which is severe, although uncommon.

In addition, there is an increased risk of left-sided cardiac valve dysfunction.[4][6]

HistoryEdit

Methysergide was approved by the FDA in 1962.

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

Related compoundsEdit

Its molecular structure is closely related to that of LSD.

Like LSD, methysergide also produces psychedelic and hallucinogenic effects above a dosage of about 4mg.[7] Full effects are felt with dosages of 8-20mg.[How to reference and link to summary or text]

About 4 mg is equal to 25mcg of LSD.[8]

See alsoEdit

Triptan

ReferencesEdit

  1. Rang, H. P. (2003). Pharmacology, Edinburgh: Churchill Livingstone. Page 187
  2. Saxena PR, Lawang A (October 1985). A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors. Arch Int Pharmacodyn Ther 277 (2): 235–52.
  3. Colpaert FC, Niemegeers CJ, Janssen PA (October 1979). In vivo evidence of partial agonist activity exerted by purported 5-hydroxytryptamine antagonists. Eur. J. Pharmacol. 58 (4): 505–9.
  4. 4.0 4.1 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.
  5. emedicine.com (2002)
  6. 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine
  7. L. Bender (1970): "Children's Reactions to Psychotomimetic Drugs", Psychotomimetic Drugs, pp. 265-273]
  8. Abramson HA, Rolo A (September 1965). Lysergic acid diethylamide (LSD-25). 38. Comparison with action of methysergide and psilocybin on test subjects. J Asthma Res 3 (1): 81–96.

External linksEdit

Template:Serotonin antagonists

Template:Antimigraine preparations

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