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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. Methysergide was approved by the FDA in 1962. Its molecular structure is closely related to that of LSD. 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]
Methysergide is one of the most effective[4] medications for the prevention of migraine, but not for the treatment of an acute attack. 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]
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.[7] Full effects are felt with dosages of 8-20mg.citation needed
About 4 mg is equal to 25mcg of LSD.[8]
See also
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. 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. PMID 12848667.
- ^ emedicine.com (2002)
- ^ 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine
- ^ L. Bender (1970): "Children's Reactions to Psychotomimetic Drugs", Psychotomimetic Drugs, pp. 265-273]
- ^ 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. PMID 5318626.
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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Wikipedia content modification information:
- This page was last modified on 5 August 2008, at 13:49.
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