Rizatriptan

Rizatriptan
Clinical data
Trade names Maxalt
AHFS/Drugs.com Monograph
MedlinePlus a601109
Pregnancy
category
Routes of
administration		 Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 45%
Protein binding 14%
Metabolism by monoamine oxidase
Elimination half-life 2–3 hours
Excretion 82% urine; 12% faeces
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.119.030 Edit this at Wikidata
Chemical and physical data
Formula C15H19N5
Molar mass 269.345 g/mol
3D model (JSmol)
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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), France, Israel (as Rizalt), The Netherlands, Croatia and Spain (as Maxalt). It is classified as OTC (over-the-counter) in Brazil (also 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

Drug Interactions

Adverse effects

Mechanism of action

Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors.[3] 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.[3]

References

  1. 1 2 "Rizatriptan". MedlinePlus. U.S. National Library of Medicine.
  2. ↑ Millson, D; Tepper, S (2000). "Migraine pharmacotherapy with oral triptans: a rational approach to clinical management". Expert Opin Pharmacother. 1 (3): 391–404. doi:10.1517/14656566.1.3.391. PMID 11249525.
  3. 1 2 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.
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