安息香酸リザトリプタン

関: Maxalt、rizatriptan

WordNet

any salt or ester of benzoic acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/09/03 00:48:39」(JST)

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Rizatriptan (trade name Maxalt) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck & Co. for the treatment of migraine headaches.^[1] It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets (Maxalt-MLT).

Maxalt obtained approval by the United States Food and Drug Administration (FDA) on June 29, 1998. It is a second-generation triptan.

Rizatriptan is available only by prescription in Australia, Finland, the United States, Canada and New Zealand. Similarly, it is classed as a POM (Prescription Only Medicine) in the United Kingdom, Italy (as Rizaliv), Israel (as Rizalt), The Netherlands, Croatia and Spain (as Maxalt).

Indications

Rizatriptan is FDA-approved to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks.^[1] Rizatriptan is also used off-label to treat cluster headaches.

Contraindications

coronary artery disease
use of monoamine oxidase inhibitors

Adverse effects

Severe:

serotonin syndrome when used with MAOIs
coronary artery vasospasm
transient myocardial ischemia
myocardial infarction
ventricular tachycardia
ventricular fibrillation
hypertensive crisis

Atypical sensations:

paresthesia

Cardiovascular:

palpitations
syncope
hypertension
hypotension

Ear, nose, and throat:

tinnitus
sinusitis
allergic rhinitis
upper respiratory tract inflammation

Gastrointestinal:

diarrhea

Muscular:

myalgia

Neurological:

phonophobia
photophobia

Respiratory:

dyspnea

Skin:

sweating

Miscellaneous:

hypersensitivity

Mechanism of action

Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors.^[2] Like the other triptans sumatriptan and zolmitriptan, rizatriptan induces vasoconstriction—possibly by inhibiting the release of calcitonin gene-related peptide from sensory neurons in the trigeminal nerve.^[2]

References

^ ^a ^b "Rizatriptan". MedlinePlus. U.S. National Library of Medicine.
^ ^a ^b Wellington, K; Plosker, G. L. (2002). "Rizatriptan: An update of its use in the management of migraine". Drugs 62 (10): 1539–74. doi:10.2165/00003495-200262100-00007. PMID 12093318. edit

External links

Maxalt website by Merck & Co.

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. 患者情報：成人における片頭痛（詳細） migraine headaches in adults beyond the basics
2. 成人における片頭痛の急性期治療 acute treatment of migraine in adults
3. 小児における片頭痛のマネージメント management of migraine headache in children
4. 妊娠中の頭痛 headache in pregnancy
5. 性行為に伴う一次性頭痛 primary headache associated with sexual activity

English Journal

Efficacy of Parecoxib, Sumatriptan, and Rizatriptan in the Treatment of Acute Migraine Attacks.

Muller T, Lohse L.Source*Department of Neurology, St. Joseph Hospital Berlin-Weissensee, Berlin, Germany; and †MSFZ and NMVZ, Dresden, Germany.
Clinical neuropharmacology.Clin Neuropharmacol.2011 Oct 8. [Epub ahead of print]
Triptans and analgetic nonsteroidal inflammatory drugs reduce acute pain syndromes in migraine. A further treatment option for an acute headache attack in patients with migraine may be the application of cyclooxygenase-2-specific inhibitors, as they have anti-inflammatory and analgesic properties. T
PMID 21996647

An approach for rapid development of nasal delivery of analgesics-Identification of relevant features, in vitro screening and in vivo verification.

Wang S, Chow MS, Zuo Z.SourceSchool of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong Special Administrative Region.
International journal of pharmaceutics.Int J Pharm.2011 Aug 18. [Epub ahead of print]
Drug delivery via the nasal route is gaining increasing interest over the last two decades as an alternative to oral or parenteral drug administration. In the current study an approach for rapid identification of relevant features, screening and in vivo verification of potential therapeutic agents f
PMID 21871544

Japanese Journal

Development of Triptans in Japan : Bridging Strategy Based on the ICH-E5 Guideline

Shimazawa Rumiko,Ando Yuki,Hidaka Shinji,Saito Kazuyuki,Toyoshima Satoshi,Kobayashi Fumiaki
Journal of health science 52(4), 443-449, 2006-08-01
… Another was to conduct a placebo-controlled Phase III study in Japan in an attempt to extrapolate the data for efficacy from a repeated dose study (i.e., sumatriptan and rizatriptan benzoate). …
NAID 110006251401

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リンク元	「リザトリプタン」「Maxalt」
関連記事	「rizatriptan」

「リザトリプタン」

Rizatriptan
Systematic (IUPAC) name
	N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
Clinical data
Trade names	Maxalt
AHFS/Drugs.com	monograph
MedlinePlus	a601109
Pregnancy cat.	B1 (Au), C (U.S.)
Legal status	℞ Prescription only
Routes	Oral
Pharmacokinetic data
Bioavailability	45%
Protein binding	14%
Metabolism	by monoamine oxidase
Half-life	2–3 hours
Excretion	82% urine; 12% faeces
Identifiers
CAS number	145202-66-0
ATC code	N02CC04
PubChem	CID 5078
IUPHAR ligand	51
DrugBank	DB00953
ChemSpider	4900
UNII	WR978S7QHH
KEGG	D00675
ChEBI	CHEBI:48273
ChEMBL	CHEMBL905
Chemical data
Formula	C15H19N5
Mol. mass	269.345 g/mol
	SMILES n1cn(nc1)Cc2cc3c(cc2)ncc3CCN(C)C;
	InChI InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3 ; Key:ULFRLSNUDGIQQP-UHFFFAOYSA-N ;
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