|Trade names||Maxalt, others|
|Defined daily dose||10 mg|
|Metabolism||by monoamine oxidase|
|Elimination half-life||2–3 hours|
|Excretion||82% urine; 12% faeces|
|Chemical and physical data|
|Molar mass||269.352 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. It should be used as soon as the headache starts. It is taken by mouth.
Common side effects include chest pain, dizziness, dry mouth, and tingling. Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis. Excessive use may result in medication overuse headaches. Use is not recommended during pregnancy and breastfeeding is not recommended within 24 hours after taking a dose. Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor.
Rizatriptan was patented in 1991 and came into medical use in 1998. It is available as a generic medication. A dose in the United Kingdom costs the NHS about 3.10 £ as of 2019. In the United States the wholesale cost of this amount is about US$0.73. In 2017, it was the 204th most commonly prescribed medication in the United States, with more than two million prescriptions.
Rizatriptan is used to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks. A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.
Frequent side effects (incidence less than 10%) are dizziness, drowsiness, asthenia/fatigue, and nausea. Clinical adverse experiences were typically mild and short-lasting (2–3 hours).
Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.
Mechanism of action
Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. 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.
Society and culture
A dose in the United Kingdom costs the NHS about 3.10 £ as of 2019. In the United States the wholesale cost of this amount is about US$0.73. In 2017, it was the 204th most commonly prescribed medication in the United States, with more than two million prescriptions.
Brandnames include Bizaliv, Rizalt, and Maxalt.
- "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 7 September 2020. CS1 maint: discouraged parameter (link)
- "Rizatriptan Benzoate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
- British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 473. ISBN 9780857113382.
- Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 531. ISBN 9783527607495. Unknown parameter
- "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
- "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
- "Rizatriptan Benzoate - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
- "Rizatriptan". MedlinePlus. U.S. National Library of Medicine.
- 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)
- 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)
- 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:10.1517/146565220.127.116.111. PMID 11249525.
- 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.
- "Rizatriptan benzoate". Drug Information Portal. U.S. National Library of Medicine.