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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 C 21H27N3O2  
Mol. mass 353.458 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat. X
Legal status
Routes  ?
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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.

Contents

Pharmacology

Methysergide interacts with of serotonin (5-HT) receptors. Its therapeutic effect in migraine prophylaxis has been associated with its antagonism at the 5-HT2B receptor.[1] Furthermore, it is an antagonist at the 5-HT2C receptor and at the 5-HT1A receptor.[2][3] It is known to have partial agonist effects on some of the other 5-HT receptors as well.[4]

Uses

Methysergide is used to treat headaches such as migraine and other recurrent throbbing headaches.[5] Methysergide is one of the most effective[6] 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 diarrhoea.[7]

Side effects

It has a known side effect, retroperitoneal fibrosis[8], 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.[6][9]

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.

Related compounds

Its molecular structure is closely related to that of LSD.

Like LSD, methysergide also produces psychedelic and hallucinogenic effects. [* reference needed]

About 4 mg is equal to 25mcg of LSD.[10]

See also

Triptan

References

  1. ^ Schmuck K, Ullmer C, Kalkman HO, Probst A, Lubbert H (May 1996). "Activation of meningeal 5-HT2B receptors: an early step in the generation of migraine headache?". Eur. J. Neurosci. 8 (5): 959–67. PMID 8743744.  
  2. ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.   Page 187
  3. ^ 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.  
  4. ^ 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:10.1016/0014-2999(79)90326-1. PMID 510385.  
  5. ^ http://www.patient.co.uk/medicine/Methysergide.htm
  6. ^ 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:10.1046/j.1540-8175.2003.03027.x. PMID 12848667.  
  7. ^ http://www.patient.co.uk/medicine/Methysergide.htm
  8. ^ emedicine.com (2002)
  9. ^ 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine
  10. ^ 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:10.3109/02770906509106904. PMID 5318626.  

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