Methysergide
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Methysergide
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| Systematic (IUPAC) name | |
| 1-Methyl- d-lysergic acid- (1-hydroxybut- 2-yl) amide | |
| Identifiers | |
| CAS number | |
| ATC code | N02 |
| PubChem | |
| DrugBank | |
| 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.
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[edit] Pharmacology
It is an antagonist at the 5-HT2C receptor[1]. It also is a 5-HT1A receptor antagonist.[2] It is known to have partial agonist effects on some of the other 5-HT receptors as well.[3]
[edit] Uses
Methysergide is one of the most effective[4] medications for the prevention of migraine, but not for the treatment of an acute attack.
[edit] Side effects
It has a known side effect, retroperitoneal fibrosis[5], 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.[4][6]
[edit] 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.
[edit] Related compounds
Its molecular structure is closely related to that of LSD.
Like LSD, methysergide also produces psychedelic and hallucinogenic effects.
About 4 mg is equal to 25mcg of LSD.[7]
[edit] See also
[edit] References
- ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 187
- ^ 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. PMID 2933009.
- ^ 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. doi:. PMID 510385.
- ^ 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. doi:. PMID 12848667.
- ^ emedicine.com (2002)
- ^ 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine
- ^ 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. doi:. PMID 5318626.
[edit] External links
- Novartis Sansert site.
- Novartis Sansert product description.
- Migraines.org More detailed information on methysergide.
- neurologychannel.com, general information on migraines.
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