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QuickView for Rizatriptan (compound)

Name: rizatriptan
PubChem Compound ID: 5078
Molecular formula: C15H19N5
Molecular weight: 269.345 g/mol
N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine; 144034-80-0; 1H-Indole-3-ethanamine, N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-; Rizatriptan; MK 462 free base; Risatriptan
Name: rizatriptan
Name (isomeric): DB00953
Drug Type: small molecule
Rizatriptan benzoate; Rizatriptan benzoat; MK 462 Free Base; Risatriptan
Brand: Maxalt MLT, Maxalt, Maxalt-MLT
Category: Serotonin Agonists, Selective Serotonin Agonists, Vasoconstrictor Agents, Anti-migraine Agents, Anti-inflammatory Agents
CAS number: 145202-66-0
Indication: For treatment of acute migraine attacks with or without aura.
Rizatriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological act...
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Mechanism of Action:
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) vasoconstricti...
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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.
Protein binding: 14%
Biotransformation: Rizatriptan is metabolized by monoamine oxidase A isoenzyme (MAO-A) to an inactive indole acetic acid metabolite. In addition, several other inactive metabolites are formed. An active metabolite, N-monodesmethyl-rizatriptan, with pharmacological activity similar to that of the parent compound has been identified in small concentrations (14%) in the plasma.
Route of elimination: 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.
Half Life: 2-3 hours
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.
Affected organisms: Humans and other mammals
Drug interaction:
ErgotaminePossible severe and prolonged vasoconstriction
FluvoxamineIncreased risk of CNS adverse effects
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
NefazodoneIncreased risk of CNS adverse effects
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