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Namespace Prefixes

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Statements

Subject Item
n2:DB00953
rdf:type
n3:Drug
n3:description
Rizatriptan is a triptan drug used for the treatment of migraine headaches. It is a selective 5-hydroxytryptamine1 receptor subtype agonist.
n3:dosage
n6:271B41C7-363D-11E5-9242-09173F13E4C5 n6:271B41C8-363D-11E5-9242-09173F13E4C5 n6:271B41C9-363D-11E5-9242-09173F13E4C5 n6:271B41CA-363D-11E5-9242-09173F13E4C5 n6:271B41CB-363D-11E5-9242-09173F13E4C5 n6:271B41CC-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Wellington K, Plosker GL: Rizatriptan: an update of its use in the management of migraine. Drugs. 2002;62(10):1539-74. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12093318 # Wellington K, Jarvis B: Spotlight on rizatriptan in migraine. CNS Drugs. 2002;16(10):715-20. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12269863 # Ikemoto F, Toru T, Aijima H, Natsumeda Y: [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance] Nippon Yakurigaku Zasshi. 2004 Apr;123(4):295-302. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15056946 # Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12434581 # Tfelt-Hansen P, De Vries P, Saxena PR: Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs. 2000 Dec;60(6):1259-87. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11152011
n3:group
approved
n3:halfLife
2-3 hours
n3:indication
For treatment of acute migraine attacks with or without aura.
n3:manufacturer
n4:271B41BC-363D-11E5-9242-09173F13E4C5
owl:sameAs
n14:DB00953 n23:DB00953
dcterms:title
Rizatriptan
adms:identifier
n8:Rizatriptan n19:D00675 n20:0006-0266-12 n21:51 n22:51 n24:DB00953 n27:48273 n28:4900 n29:46506557 n30:PA451264 n31:5078
n3:mechanismOfAction
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.
n3:packager
n4:271B41B7-363D-11E5-9242-09173F13E4C5 n4:271B41B4-363D-11E5-9242-09173F13E4C5 n4:271B41B5-363D-11E5-9242-09173F13E4C5 n4:271B41BA-363D-11E5-9242-09173F13E4C5 n4:271B41BB-363D-11E5-9242-09173F13E4C5 n4:271B41B6-363D-11E5-9242-09173F13E4C5 n4:271B41B9-363D-11E5-9242-09173F13E4C5 n4:271B41B8-363D-11E5-9242-09173F13E4C5
n3:patent
n9:5602162 n9:5298520 n9:2060139
n3:routeOfElimination
Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.
n3:synonym
N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]-ethanamine Rizatriptanum MK 462 free base Rizatriptan benzoate Rizatriptan benzoat Risatriptan
n3:toxicity
Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.
n3:volumeOfDistribution
* 140 L [male] * 110 L [female]
n25:hasAHFSCode
n26:28-32-28
n3:proteinBinding
14%
n3:synthesisReference
Montserrat Armengol Asparo, Pere Dalmases Barjoan, "Process for preparing a rizatriptan." U.S. Patent US20050148778, issued July 07, 2005.
n11:hasConcept
n12:M0246872
foaf:page
n17:rizatrip.htm n18:max1248.shtml n32:rizatriptan.html
n3:IUPAC-Name
n15:271B41D1-363D-11E5-9242-09173F13E4C5
n3:InChI
n15:271B41D7-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n15:271B41D6-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n15:271B41D3-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n15:271B41D4-363D-11E5-9242-09173F13E4C5
n3:SMILES
n15:271B41D5-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n15:271B41CF-363D-11E5-9242-09173F13E4C5 n15:271B41E7-363D-11E5-9242-09173F13E4C5
n3:logP
n15:271B41CD-363D-11E5-9242-09173F13E4C5 n15:271B41D0-363D-11E5-9242-09173F13E4C5 n15:271B41E9-363D-11E5-9242-09173F13E4C5
n3:logS
n15:271B41CE-363D-11E5-9242-09173F13E4C5
n25:hasATCCode
n33:N02CC04
n3:H-Bond-Acceptor-Count
n15:271B41DD-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n15:271B41DE-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n15:271B41D8-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n15:271B41D9-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n15:271B41DB-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n15:271B41DA-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n15:271B41DC-363D-11E5-9242-09173F13E4C5
n3:absorption
Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
145202-66-0
n3:category
n3:containedIn
n5:271B41C2-363D-11E5-9242-09173F13E4C5 n5:271B41BD-363D-11E5-9242-09173F13E4C5 n5:271B41C0-363D-11E5-9242-09173F13E4C5 n5:271B41C3-363D-11E5-9242-09173F13E4C5 n5:271B41BE-363D-11E5-9242-09173F13E4C5 n5:271B41BF-363D-11E5-9242-09173F13E4C5 n5:271B41C6-363D-11E5-9242-09173F13E4C5 n5:271B41C4-363D-11E5-9242-09173F13E4C5 n5:271B41C5-363D-11E5-9242-09173F13E4C5 n5:271B41C1-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n15:271B41E3-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n15:271B41E5-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n15:271B41E6-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n15:271B41E8-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n15:271B41E2-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n15:271B41E1-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n15:271B41E4-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n15:271B41D2-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n15:271B41DF-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n15:271B41E0-363D-11E5-9242-09173F13E4C5