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
[[File:Rizatriptan 3D ball-and-stick.png a|frameless]]
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] A dose in the United Kingdom costs the NHS about 3.10 £ as of 2019.[2] In the United States the wholesale cost of this amount is about US$0.73.[4] In 2017, it was the 204th most commonly prescribed medication in the United States, with more than two million prescriptions.[5][6]

Medical uses

Rizatriptan is used to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks.[7] A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.[8]

Contraindications

Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.[9]

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).[9]

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.[11] 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.[11]

Society and culture

It is typically by prescription except in Brazil.

Names

Brandnames include Bizaliv, Rizalt, and Maxalt.

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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. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  5. "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
  6. "Rizatriptan Benzoate - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
  7. "Rizatriptan". MedlinePlus. U.S. National Library of Medicine.
  8. 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.CS1 maint: uses authors parameter (link)
  9. Hargreaves RJ, Lines CR, Rapoport AM, Ho TW, Sheftell FD. (2009). "Ten years of rizatriptan: from development to clinical science and future directions". Headache. doi:10.1111/j.1526-4610.2008.01335.x. PMID 19161563.CS1 maint: uses authors parameter (link)
  10. 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.
  11. 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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