Rizatriptan

Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches.[1] It should be used as soon as the headache starts.[2] It is taken by mouth.[1]

Rizatriptan
Clinical data
Trade namesMaxalt, others
AHFS/Drugs.comMonograph
MedlinePlusa601109
License data
Pregnancy
category
Routes of
administration		By mouth
Drug classTriptan
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability45%
Protein binding14%
Metabolismby monoamine oxidase
Elimination half-life2–3 hours
Excretion82% urine; 12% faeces
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.243.719
Chemical and physical data
FormulaC15H19N5
Molar mass269.352 g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

Common side effects include chest pain, dizziness, dry mouth, and tingling.[1] Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis.[1] Excessive use may result in medication overuse headaches.[1] Use is not recommended during pregnancy and breastfeeding is not recommended within 24 hours after taking a dose.[2] Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor.[1]

Rizatriptan was patented in 1991 and came into medical use in 1998.[3] It is available as a generic medication.[2] In 2017, it was the 204th most commonly prescribed medication in the United States, with more than two million prescriptions.[4][5]

Medical uses

Rizatriptan is used to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks.[6] A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.[7]

Contraindications

Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.[8]

Adverse effects

Frequent adverse effects (incidence less than 10%) are dizziness, drowsiness, asthenia/fatigue, and nausea. Clinical adverse experiences were typically mild and short-lasting (2–3 hours).[8]

Interactions

Mechanism of action
Further information: Serotonin receptor agonist and Triptan § Mechanism_of_action

Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors.[10] 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.[10]

Society and culture

It is typically by prescription except in Brazil.

Names

Brand names include Bizaliv, Rizalt, Rizact (India) and Maxalt.

References
  1. "Rizatriptan Benzoate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
  2. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 473. ISBN 9780857113382.
  3. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 531. ISBN 9783527607495.
  4. "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
  5. "Rizatriptan Benzoate - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
  6. "Rizatriptan". MedlinePlus. U.S. National Library of Medicine.
  7. Göbel H (2010). "Efficacy and tolerability of rizatriptan 10 mg compared with sumatriptan 100 mg: an evidence-based analysis". Expert Rev Neurother. 10 (4): 499–506. doi:10.1586/ern.10.24. PMID 20367203. S2CID 43395810.CS1 maint: uses authors parameter (link)
  8. Hargreaves RJ, Lines CR, Rapoport AM, Ho TW, Sheftell FD. (2009). "Ten years of rizatriptan: from development to clinical science and future directions". Headache. 49: S3–S20. doi:10.1111/j.1526-4610.2008.01335.x. PMID 19161563.CS1 maint: uses authors parameter (link)
  9. Millson DS, Tepper SJ, Rapoport AM (March 2000). "Migraine pharmacotherapy with oral triptans: a rational approach to clinical management". Expert Opinion on Pharmacotherapy. 1 (3): 391–404. doi:10.1517/14656566.1.3.391. PMID 11249525. S2CID 36053513.
  10. Wellington K, Plosker GL (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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