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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/01/23 16:16:39」(JST)

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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 2 mg dosages.

Pharmacology

Methysergide interacts with serotonin (5-HT) receptors. Its therapeutic effect in migraine prophylaxis has been associated with its antagonism at the 5-HT_2B receptor.^[1] Furthermore, it is an antagonist at the 5-HT_2C receptor and at the 5-HT_1A receptor.^[2]^[3] It is known to have partial agonist effects on some of the other 5-HT receptors as well.^[4] Methysergide is metabolised into methylergometrine in humans, which is responsible for its psychedelic effects.^[5]

Uses

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

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.^[7]^[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.

References

^ 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. doi:10.1111/j.1460-9568.1996.tb01583.x. PMID 8743744.
^ 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:10.1016/0014-2999(79)90326-1. PMID 510385.
^ Bredberg, U.; Eyjolfsdottir, G. S., Paalzow, L., Tfelt-Hansen, P., Tfelt-Hansen, V. (1 January 1986). "Pharmacokinetics of methysergide and its metabolite methylergometrine in man". European Journal of Clinical Pharmacology 30 (1): 75–77. doi:10.1007/BF00614199. PMID 3709634.
^ ^a ^b http://www.patient.co.uk/medicine/Methysergide.htm
^ ^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.
^ emedicine.com (2002)
^ 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine

External links

Novartis Sansert site.
Novartis Sansert product description.
Migraines.org More detailed information on methysergide.
neurologychannel.com, general information on migraines.
History of methysergide in migraine.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 群発頭痛：治療および予後 cluster headache treatment and prognosis
2. 成人における片頭痛の予防的治療 preventive treatment of migraine in adults
3. 薬剤誘発性の弁膜症 valvular heart disease induced by drugs
4. 後腹膜線維症の臨床症状および診断 clinical manifestations and diagnosis of retroperitoneal fibrosis
5. 頭痛、片頭痛、および脳卒中 headache migraine and stroke

English Journal

Neuropeptide AF induces anxiety-like and antidepressant-like behavior in mice.

Palotai M1, Telegdy G2, Tanaka M3, Bagosi Z1, Jászberényi M1.
Behavioural brain research.Behav Brain Res.2014 Nov 1;274:264-9. doi: 10.1016/j.bbr.2014.08.007. Epub 2014 Aug 10.
Little is known about the action of neuropeptide AF (NPAF) on anxiety and depression. Only our previous study provides evidence that NPAF induces anxiety-like behavior in rats. Therefore, the aim of the present study was to investigate the action of NPAF on depression-like behavior and the underlyin
PMID 25116251

Chronic resveratrol treatment exerts antihyperalgesic effect and corrects co-morbid depressive like behaviors in mice with mononeuropathy: involvement of serotonergic system.

Zhao X1, Yu C2, Wang C3, Zhang JF3, Zhou WH3, Cui WG3, Ye F4, Xu Y5.
Neuropharmacology.Neuropharmacology.2014 Oct;85:131-41. doi: 10.1016/j.neuropharm.2014.04.021. Epub 2014 May 14.
Patients suffering from chronic neuropathic pain are at high risk of co-morbid depression, which burdens healthcare. This work aimed to investigate the effects of resveratrol, a phenolic monomer enriched in red wine and grapes, on pain-related and depressive-like behaviors in mice with mononeuropath
PMID 24835468

Breastfeeding and migraine drugs.

Davanzo R1, Bua J, Paloni G, Facchina G.
European journal of clinical pharmacology.Eur J Clin Pharmacol.2014 Sep 13. [Epub ahead of print]
PURPOSE: Breastfeeding women may suffer from migraine. While we have many drugs for its treatment and prophylaxis, the majority are poorly studied in breastfeeding women. We conducted a review of the most common anti-migraine drugs (AMDs) and we determined their lactation risk.METHODS: For each AMD,
PMID 25217187

Japanese Journal

Effect of Peripheral 5-HT on Glucose and Lipid Metabolism in Wether Sheep

PLOS ONE 9(2), e88058, 2014-02
NAID 120005435471

Antinociceptive Profiles and Mechanisms of Orally Administered Coumarin in Mice

Biological and Pharmaceutical Bulletin 36(6), 925-930, 2013
NAID 130003361436

Pharmacological Characterization of Itch-Associated Response Induced by Repeated Application of Oxazolone in Mice

Journal of pharmacological sciences 113(3), 255-262, 2010-07-20
NAID 10029889358

Related Pictures

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リンク元

「メチセルギド」

Methysergide
Systematic (IUPAC) name
	1-Methyl- d-lysergic acid- (1-hydroxybut- 2-yl) amide
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a603022
Pregnancy cat.	X
Legal status	?
Identifiers
CAS number	361-37-5
ATC code	N02CA04
PubChem	CID 9681
IUPHAR ligand	134
DrugBank	DB00247
ChemSpider	9300
UNII	XZA9HY6Z98
KEGG	D02357
ChEMBL	CHEMBL1065
Chemical data
Formula	C21H27N3O2
Mol. mass	353.458 g/mol
	SMILES O=C(N[C@@H](CC)CO)[C@@H]3/C=C2/c4cccc1c4c(cn1C)C[C@H]2N(C3)C;
	InChI InChI=1S/C21H27N3O2/c1-4-15(12-25)22-21(26)14-8-17-16-6-5-7-18-20(16)13(10-23(18)2)9-19(17)24(3)11-14/h5-8,10,14-15,19,25H,4,9,11-12H2,1-3H3,(H,22,26)/t14-,15+,19-/m1/s1 ; Key:KPJZHOPZRAFDTN-ZRGWGRIASA-N ;
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英: methysergide
同: メチセルジド
関: 片頭痛

[show details]

メチセルギド : 約 1,310 件
メチセルジド : 約 1,180 件

日本で発売はされていないらしい。
麦角アルカロイド誘導体で片頭痛の治療薬として用いられる

[pmid8743744-1] 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. doi:10.1111/j.1460-9568.1996.tb01583.x. PMID 8743744.

[Rang187-2] Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 187

[pmid2933009-3] 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.

[pmid510385-4] 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] Bredberg, U.; Eyjolfsdottir, G. S., Paalzow, L., Tfelt-Hansen, P., Tfelt-Hansen, V. (1 January 1986). "Pharmacokinetics of methysergide and its metabolite methylergometrine in man". European Journal of Clinical Pharmacology 30 (1): 75–77. doi:10.1007/BF00614199. PMID 3709634.

[patient.co.uk-6] ttp://www.patient.co.uk/medicine/Methysergide.htm

[Tam-7] 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.

[8] .com (2002)

[mayo-9] 1997 Mayo Clinic study linking heart disease to Fen Phen Valvular heart disease associated with fenfluramine-phentermine

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methysergide