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Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is a triptan, used in the acute treatment of migraine attacks with or without aura and cluster headaches.

Zolmitriptan is marketed by AstraZeneca with the brand names Zomig, Zomigon (Argentina, Canada & Greece), AscoTop (Germany) and Zomigoro (France). In 2008, Zomig generated nearly $154 million in sales.^[1]

AstraZeneca's U.S. patent on Zomig tablets expired on November 14, 2012, and its pediatric exclusivity extension expired on May 14, 2013.^[2] The patent in certain European countries has already expired too, and generic drug maker Actavis released a generic version in those countries, starting in March 2012.^[3]

Description

Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is partially soluble in water.

Indications

Zolmitriptan is used for the acute treatment of migraines with or without aura in adults. Zolmitriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine.

Zolmitriptan is available as a swallowable tablet, an oral disintegrating tablet, and a nasal spray, in doses of 2.5 and 5 mg. People who get migraines from aspartame should not use the disintegrating tablet (Zomig ZMT), which contains aspartame.^[4]

According to a study of healthy volunteers, food intake seems to have no significant effect on the effectiveness of Zolmitriptan in both men and women. ^[5]

Contraindications and precautions

Zolmitriptan should not be given to patients with ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) or to patients who have symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm, including Prinzmetal's angina, or other significant underlying cardiovascular disease.

Zolmitriptan may increase blood pressure, it should not be given to patients with uncontrolled hypertension, should not be used within 24 hours of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide, and should not be administered to patients with hemiplegic or basilar migraine.

Concurrent administration of MAOI or use of zolmitriptan within 2 weeks of discontinuation of MAO-A inhibitor therapy is contraindicated.

Adverse reactions

The Zomig ZMT dissolvable pill contains aspartame, and should be avoided by anyone sensitive to that ingredient and by those suffering from phenylketonuria.

Rarely, serious cardiac events, including myocardial infarction, have been associated with zolmitriptan.

Reported minor adverse reactions include: hypesthesia, paresthesia (all types), warm and cold sensations, chest pain, throat and jaw tightness, dry mouth, dyspepsia, dysphagia, nausea, somnolence, vertigo, asthenia, myalgia, myasthenia and sweating.

Drug Interactions: see Zomig package insert for complete list: [1]

Following administration of cimetidine, the half-life and AUC of zolmitriptan and its active metabolites were approximately doubled (see CLINICAL PHARMACOLOGY in product pamphlet). Cimetidine (INN) (/sᵻˈmɛtᵻdiːn/ or /saɪˈmɛtᵻdiːn/) is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach.

References

^ "2008 Top 200 generic drugs by retail dollars" PDF (332 KB). Drug Topics (May 26, 2009). Retrieved on August 25, 2009.
^ http://www.drugs.com/availability/generic-zomig-zmt.html
^ http://www.actavis.com/en/media+center/newsroom/articles/migraine_zolmitriptan_eu.htm
^ Newman LC, Lipton RB (2001). "Migraine MLT-Down: An Unusual Presentation of Migraine in Patients With Aspartame-Triggered Headaches". Headache: the Journal of Head and Face Pain (abstract) 41 (9): 899–901. doi:10.1046/j.1526-4610.2001.01164.x. |access-date= requires |url= (help)
^ Emma J. Seaber, Richard W. Peck, Deborah A. Smith, John Allanson, Nanco R. Hefting, Jan J. van Lier, Frans A.E. Sollie, Johan Wemer, Jan H.G. Jonkman (1998). "The absolute bioavailability and effect of food on the pharmacokinetics of zolmitriptan in healthy volunteers.". British Journal of Clinical Pharmacology (abstract) 46 (5): 433–439. doi:10.1046/j.1365-2125.1998.00809.x. |access-date= requires |url= (help)

MacGregor, E.A. (1998). "Zolmitriptan clinical studies". Drugs Today 34 (12): 1027–1033. doi:10.1358/dot.1998.34.12.487488. PMID 14743270.

External links

Zomig Information Site (USA)

UpToDate Contents

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1. 小児における片頭痛の急性期治療 acute treatment of migraine in children
2. 成人における片頭痛の急性期治療 acute treatment of migraine in adults
3. 群発頭痛：治療および予後 cluster headache treatment and prognosis
4. 性行為に伴う一次性頭痛 primary headache associated with sexual activity
5. エストロゲン関連片頭痛 estrogen associated migraine

English Journal

Efficacy of frovatriptan as compared to other triptans in migraine with aura.

Evers S1, Savi L, Omboni S, Lisotto C, Zanchin G, Pinessi L.
The journal of headache and pain.J Headache Pain.2015 Dec;16(1):514. doi: 10.1186/s10194-015-0514-8. Epub 2015 Apr 1.
BACKGROUND: The treatment of migraine attacks with aura by triptans is difficult since triptans most probably are not efficacious when taken during the aura phase. Moreover, there are insufficient data from randomised studies whether triptans are efficacious in migraine attacks with aura when taken
PMID 25916333

SLCO1A2-MDCKII: a Promising in vitro System to Understand the Role of OATP1A2 in Blood Brain Barrier Drug Penetration.

Liu H1, Yu N1, Lu S1, Ito S2, Zhang X2, Prasad B3, He E1, Lu X1, Li Y1, Wang F1, Xu H1, An G1, Unadkat JD3, Kusuhara H4, Sugiyama Y5, Sahi J6.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2015 Apr 23. pii: dmd.115.064170. [Epub ahead of print]
OATP1A2 has the potential to be a target for CNS drug delivery due to its luminal localization at the human blood-brain barrier and broad substrate specificity. We confirmed greater OATP1A2 mRNA expression in human brain relative to other tissues and report OATP1A2 expression comparable to BCRP and
PMID 25908246

Acute Migraine Treatment in Adults.

Becker WJ1.
Headache.Headache.2015 Apr 15. doi: 10.1111/head.12550. [Epub ahead of print]
There are many options for acute migraine attack treatment, but none is ideal for all patients. This study aims to review current medical office-based acute migraine therapy in adults and provides readers with an organized approach to this important facet of migraine treatment. A general literature
PMID 25877672

Japanese Journal

群発頭痛の治療に関する最近の進歩

臨床神経学 53(11), 1131-1133, 2013
NAID 130004505360

脳神経外科医が知っておくべき頭痛の知識

脳神経外科ジャーナル = Japanese journal of neurosurgery 21(10), 771-778, 2012-10-20
NAID 10031131642

トリプタンおよびCGRP受容体アンタゴニスト

臨床神経学 52(11), 971-972, 2012
NAID 130004505228

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★リンクテーブル★

リンク元	「ゾルミトリプタン」

「ゾルミトリプタン」

Zolmitriptan
Systematic (IUPAC) name
	(S)-4-({3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
Clinical data
Trade names	Zomig
AHFS/Drugs.com	monograph
Pregnancy; category	AU: B3; US: C (Risk not ruled out); ;
Routes of; administration	Oral, nasal spray
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	40% (oral)
Protein binding	25%
Metabolism	Hepatic (CYP1A2-mediated, to active metabolite)
Biological half-life	3 hours
Excretion	Renal (65%) and fecal (35%)
Identifiers
CAS Number	139264-17-8
ATC code	N02CC03 (WHO)
PubChem	CID 60857
IUPHAR/BPS	60
DrugBank	DB00315
ChemSpider	54844
UNII	2FS66TH3YW
KEGG	D00415
ChEBI	CHEBI:10124
ChEMBL	CHEMBL1185
Chemical data
Formula	C16H21N3O2
Molar mass	287.357 g/mol
	SMILES O=C1OC[C@@H](N1)Cc2ccc3c(c2)c(c[nH]3)CCN(C)C ;
	InChI InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1 ; Key:ULSDMUVEXKOYBU-ZDUSSCGKSA-N ;
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　　[★]

英: zolmitriptan
商: ゾーミッグ Zomig
関: 血管収縮剤

[1] "2008 Top 200 generic drugs by retail dollars" PDF (332 KB). Drug Topics (May 26, 2009). Retrieved on August 25, 2009.

[2] ttp://www.drugs.com/availability/generic-zomig-zmt.html

[3] ttp://www.actavis.com/en/media+center/newsroom/articles/migraine_zolmitriptan_eu.htm

[4] Newman LC, Lipton RB (2001). "Migraine MLT-Down: An Unusual Presentation of Migraine in Patients With Aspartame-Triggered Headaches". Headache: the Journal of Head and Face Pain (abstract) 41 (9): 899–901. doi:10.1046/j.1526-4610.2001.01164.x. |access-date= requires |url= (help)

[5] Emma J. Seaber, Richard W. Peck, Deborah A. Smith, John Allanson, Nanco R. Hefting, Jan J. van Lier, Frans A.E. Sollie, Johan Wemer, Jan H.G. Jonkman (1998). "The absolute bioavailability and effect of food on the pharmacokinetics of zolmitriptan in healthy volunteers.". British Journal of Clinical Pharmacology (abstract) 46 (5): 433–439. doi:10.1046/j.1365-2125.1998.00809.x. |access-date= requires |url= (help)

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zolmitriptan