Rizatriptan: Difference between revisions

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{{Short description|Medication used for the treatment of migraine headaches}}
{{Short description|Medication used for the treatment of migraine headaches}}
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{{Use dmy dates|date=December 2023}}
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<!-- Society and culture -->
<!-- Society and culture -->
Rizatriptan was patented in 1991 and came into medical use in 1998.<ref>{{cite web | title=Drug Approval Package: Maxalt/Rizatritan Benzoate NDA# 20864 & 20865 | website=U.S. [[Food and Drug Administration]] (FDA) | date=30 March 2001 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/98/20864-20865.cfm | access-date=25 December 2023 | archive-date=6 December 2022 | archive-url=https://web.archive.org/web/20221206085052/https://www.accessdata.fda.gov/drugsatfda_docs/nda/98/20864-20865.cfm | url-status=dead }}</ref><ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title= Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=531 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA531 }}</ref> It is available as a [[generic medication]].<ref name=BNF76>{{cite book|title=British National Formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=473|edition=76}}</ref> In 2022, it was the 190th most commonly prescribed medication in the United States, with more than 2{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Rizatriptan Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Rizatriptan | access-date = 30 August 2024 }}</ref> Rizatriptan is available in combination with meloxicam as [[meloxicam/rizatriptan]].
Rizatriptan was patented in 1991 and came into medical use in 1998.<ref>{{cite web |title=Drug Approval Package: Maxalt/Rizatritan Benzoate NDA# 20864 & 20865 |publisher=U.S. [[Food and Drug Administration]] (FDA) |date=30 March 2001 |url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/98/20864-20865.cfm |access-date=25 December 2023 |archive-date=6 December 2022 |archive-url=https://web.archive.org/web/20221206085052/https://www.accessdata.fda.gov/drugsatfda_docs/nda/98/20864-20865.cfm |url-status=dead }}</ref><ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title= Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=531 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA531 }}</ref> It is available as a [[generic medication]].<ref name=BNF76>{{cite book|title=British National Formulary: BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=473|edition=76}}</ref> In 2022, it was the 190th most commonly prescribed medication in the United States, with more than two million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Rizatriptan Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Rizatriptan | access-date = 30 August 2024 }}</ref> Rizatriptan is available in combination with [[meloxicam]] as [[meloxicam/rizatriptan]].


==Medical uses==
==Medical uses==
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* [[Propranolol]]<ref name="Millson 2000">{{cite journal | vauthors = Millson DS, Tepper SJ, Rapoport AM | title = Migraine pharmacotherapy with oral triptans: a rational approach to clinical management | journal = Expert Opinion on Pharmacotherapy | volume = 1 | issue = 3 | pages = 391–404 | date = March 2000 | pmid = 11249525 | doi = 10.1517/14656566.1.3.391 | s2cid = 36053513 }}</ref>{{Explain|date=October 2024}}
* [[Propranolol]]<ref name="Millson 2000">{{cite journal | vauthors = Millson DS, Tepper SJ, Rapoport AM | title = Migraine pharmacotherapy with oral triptans: a rational approach to clinical management | journal = Expert Opinion on Pharmacotherapy | volume = 1 | issue = 3 | pages = 391–404 | date = March 2000 | pmid = 11249525 | doi = 10.1517/14656566.1.3.391 | s2cid = 36053513 }}</ref>{{Explain|date=October 2024}}


==Mechanism of action==
==Pharmacology==
{{further|Serotonin receptor agonist|Triptan#Mechanism of action}}
===Mechanism of action===
{{Further|Serotonin receptor agonist|Triptan#Mechanism of action}}
 
Rizatriptan acts as an agonist at serotonin [[5-HT1B|5-HT<sub>1B</sub>]] and [[5-HT1D|5-HT<sub>1D</sub>]] receptors.<ref name="Wellington 2002">{{cite journal | vauthors = Wellington K, Plosker GL | title = Rizatriptan: an update of its use in the management of migraine | journal = Drugs | volume = 62 | issue = 10 | pages = 1539–74 | year = 2002 | pmid = 12093318 | doi = 10.2165/00003495-200262100-00007 | s2cid = 195693597 }}</ref> 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]].<ref name="Wellington 2002"/>
Rizatriptan acts as an agonist at serotonin [[5-HT1B|5-HT<sub>1B</sub>]] and [[5-HT1D|5-HT<sub>1D</sub>]] receptors.<ref name="Wellington 2002">{{cite journal | vauthors = Wellington K, Plosker GL | title = Rizatriptan: an update of its use in the management of migraine | journal = Drugs | volume = 62 | issue = 10 | pages = 1539–74 | year = 2002 | pmid = 12093318 | doi = 10.2165/00003495-200262100-00007 | s2cid = 195693597 }}</ref> 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]].<ref name="Wellington 2002"/>
==Chemistry==
The experimental [[log P]] is 1.4 and its predicted log P is 1.67 to 1.77.<ref name="PubChem">{{cite web | title=Rizatriptan | website=PubChem | url=https://pubchem.ncbi.nlm.nih.gov/compound/5078 | access-date=27 June 2025}}</ref><ref name="DrugBank">{{cite web | title=Rizatriptan: Uses, Interactions, Mechanism of Action | website=DrugBank Online | date=14 June 2012 | url=https://go.drugbank.com/drugs/DB00953 | access-date=27 June 2025}}</ref>


== Society and culture ==
== Society and culture ==

Latest revision as of 22:33, 27 June 2025

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Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches.[1][2] It is taken by mouth.[1][2] It can also be applied on the tongue.[3] It is a serotonin (5-HT) 1B/1D receptor agonist (triptan).[1][3]

Common side effects include chest pain, dizziness, dry mouth, and tingling.[2] Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis.[2] Excessive use may result in medication overuse headaches.[2] 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.[2]

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 two million prescriptions.[7][8] Rizatriptan is available in combination with meloxicam as meloxicam/rizatriptan.

Medical uses

Rizatriptan is indicated to treat acute migraine attacks with or without aura.[1][3] It does not prevent future migraine attacks.[9] A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.[10]

Contraindications

Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.[11]

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).[11]

Interactions

Pharmacology

Mechanism of action

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Rizatriptan 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]

Chemistry

The experimental log P is 1.4 and its predicted log P is 1.67 to 1.77.[14][15]

Society and culture

Brand names

Brand names include Rizalt, Rizalt RPD, Rizact (India), Rizafilm,[3] Maxalt,[1] and Maxalt-MLT.[1][16][17][18]

References

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