Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches.[1][3] It is taken by mouth.[1][3] It can also be applied on the tongue.[2] It is a serotonin (5-HT) 1B/1D receptor agonist (triptan).[1][2]
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| Trade names | Maxalt, Maxalt-MLT, Rizafilm, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601109 |
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| Routes of administration | By mouth |
| Drug class | Triptan |
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| Pharmacokinetic data | |
| Bioavailability | 45% |
| Protein binding | 14% |
| Metabolism | By monoamine oxidase |
| Elimination half-life | 2–3 hours |
| Excretion | 82% urine; 12% feces |
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| ECHA InfoCard | 100.243.719 |
| Chemical and physical data | |
| Formula | C15H19N5 |
| Molar mass | 269.352 g·mol−1 |
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Common side effects include chest pain, dizziness, dry mouth, and tingling.[3] Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis.[3] Excessive use may result in medication overuse headaches.[3] Use is not recommended during pregnancy and breastfeeding is not recommended within 24 hours after taking a dose.[4] Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor.[3]
Rizatriptan was patented in 1991 and came into medical use in 1998.[5][6] It is available as a generic medication.[4] In 2022, it was the 190th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[7][8]
Medical uses
editRizatriptan is indicated to treat acute migraine attacks with or without aura.[1][2] It does not prevent future migraine attacks.[9] A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.[10]
Contraindications
editRizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.[11]
Adverse effects
editFrequent 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).[11]
Interactions
editMechanism of action
editRizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors.[13] 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.[13]
Society and culture
editBrand names
editBrand names include Rizalt, Rizalt RPD, Rizact (India), Rizafilm,[2] Maxalt,[1] and Maxalt-MLT.[1][14][15][16]
References
edit- ^ a b c d e f g "Maxalt- rizatriptan benzoate tablet; Maxalt-MLT- rizatriptan benzoate tablet, orally disintegrating". DailyMed. 1 June 2022. Archived from the original on 23 March 2023. Retrieved 25 December 2023.
- ^ a b c d e "Archived copy" (PDF). Archived (PDF) from the original on 2 August 2023. Retrieved 25 December 2023.
{{cite web}}: CS1 maint: archived copy as title (link) - ^ a b c d e f "Rizatriptan Benzoate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 23 October 2020. Retrieved 18 March 2019.
- ^ a b British National Formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 473. ISBN 9780857113382.
- ^ "Drug Approval Package: Maxalt/Rizatritan Benzoate NDA# 20864 & 20865". U.S. Food and Drug Administration (FDA). 30 March 2001. Archived from the original on 6 December 2022. Retrieved 25 December 2023.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 531. ISBN 9783527607495.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Rizatriptan Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
- ^ "Rizatriptan". MedlinePlus. U.S. National Library of Medicine. Archived from the original on 5 July 2016. Retrieved 21 March 2018.
- ^ 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.
- ^ a b 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. S2CID 23587019.
- ^ 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.
- ^ a b 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. S2CID 195693597.
- ^ "Rishum01_5_982075622.pdf" (PDF). Mohpublic.z6.web.core.windows.net. Retrieved 21 December 2023.
- ^ "Maxalt Oral: Uses, Side Effects, Interactions, Pictures, Warnings & More". WebMD. Archived from the original on 21 December 2023. Retrieved 21 December 2023.
- ^ "Rizact 10 mg Tablet - Uses, Dosage, Side Effects, Composition". Practo. Archived from the original on 21 December 2023. Retrieved 21 December 2023.