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Triptan
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===Comparison=== {| class="wikitable" style="margin: 1em auto 1em auto;" |+ Comparative pharmacology of triptans, oral formulations<ref name="Goodman" /><ref name="Bigal"/><ref name="Armstrong"/><ref name="Mathew"/> |- ! Drug !! Brand !! Company !! Receptor agonist !! 5-HT<sub>1D</sub> affinity<br/>(pKI in [[nanomolar|nM]])<ref name="Deleu">{{cite journal|title=Current and emerging second-generation triptans in acute migraine therapy: a comparative review|journal=J Clin Pharmacol|author1=Deleu, D. |author2=Hanssens Y. |year=2000|volume=40|issue=7|pages=687β700|pmid=10883409|doi=10.1177/00912700022009431|s2cid=15585554}}</ref> !! [[Bioavailability|Bioavail­ability]] (%) !! [[Partition coefficient|log D<sub>pH 7.4</sub>]] !! [[Cmax (pharmacology)|T<sub>max</sub>]] (h) !! [[Elimination half-life|T<sub>1/2</sub>]] (h) !! Metab­olism !! Dose (mg) |- | [[Sumatriptan]] | align="center"| Imitrex | align="center"| [[Glaxo Smith Kline]] | align="center"| 5-HT<sub>1B/D</sub> | align="center"| 7.9β8.5 | align="center"| 14β17 | align="center"| β1.3 | align="center"| 2β2.5 | align="center"| 2.5 | align="center"| [[MAO-A]] | align="center"| 25, <br /> 50, <br /> 100 |- | [[Zolmitriptan]] | align="center"| Zomig | align="center"| [https://www.astrazeneca.com/media-centre/press-releases/2017/astrazeneca-enters-agreement-with-grunenthal-to-divest-rights-to-migraine-treatment-zomig-07062017.html GrΓΌnenthal]<ref>{{Cite web|url=https://www.astrazeneca.com/media-centre/press-releases/2017/astrazeneca-enters-agreement-with-grunenthal-to-divest-rights-to-migraine-treatment-zomig-07062017.html|title=AstraZeneca enters agreement with GrΓΌnenthal to divest rights to migraine treatment Zomig|website=www.astrazeneca.com|date=7 June 2017 |language=en|access-date=2018-03-22|url-status=live|archive-url=https://web.archive.org/web/20180322204845/https://www.astrazeneca.com/media-centre/press-releases/2017/astrazeneca-enters-agreement-with-grunenthal-to-divest-rights-to-migraine-treatment-zomig-07062017.html|archive-date=2018-03-22}}</ref> | align="center"| 5-HT<sub>1B/D</sub> | align="center"| 9.2 | align="center"| 40 | align="center"| β0.7 | align="center"| 1.5β2 | align="center"| 2β3 | align="center"| [[MAO-A]] <br /> [[CYP1A2]] | align="center"| 2.5, <br /> 5 |- | [[Naratriptan]] | align="center"| Amerge | align="center"| [[Glaxo Smith Kline]] | align="center"| 5-HT<sub>1B/D</sub> | align="center"| 8.3 | align="center"| 70 | align="center"| β0.2 | align="center"| 2β3 | align="center"| 6 | align="center"| many CYPs <br /> [[MAO-A]] | align="center"| 1, <br /> 2.5 |- | [[Rizatriptan]] | align="center"| Maxalt | align="center"| Merck | align="center"| 5-HT<sub>1B/D</sub> | align="center"| 7.7 | align="center"| 45 | align="center"| β0.7 | align="center"| 1β1.5 | align="center"| 2β2.5 | align="center"| [[MAO-A]] | align="center"| 5, <br /> 10 |- | [[Almotriptan]] | align="center"| Axert | align="center"| Almirall-Prodesfarma | align="center"| 5-HT<sub>1B/D</sub> <br /> 5-HT<sub>1F</sub>{{citation needed|date=October 2016}} | align="center"| 7.8 | align="center"| 70 | align="center"| +0.35 | align="center"| 2.5 | align="center"| 3.6 | align="center"| [[CYP2D6]] <br /> [[CYP3A4]] <br /> [[MAO-A]] | align="center"| 6.25, <br /> 12.5 |- | [[Eletriptan]] | align="center"| Relpax | align="center"| [[Pfizer]] | align="center"| 5-HT<sub>1B/D</sub> <br /> 5-HT<sub>1F</sub><ref name=relpax_spc>{{cite web | title= Relpax β 20 mg and 40 mg | url= http://emc.medicines.org.uk/emc/assets/c/html/DisplayDoc.asp?DocumentID=8195 | access-date= 2008-11-09 | url-status= live | archive-url= https://web.archive.org/web/20040620163458/http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=8195 | archive-date= 2004-06-20 }}</ref> | align="center"| 8.9 | align="center"| 50 | align="center"| +0.5 | align="center"| 1β2 | align="center"| 3.6β5.5 | align="center"| [[CYP3A4]] | align="center"| 20, <br /> 40, <br /> 80 |- | [[Frovatriptan]] | align="center"| Frova | align="center"| Vernalis | align="center"| 5-HT<sub>1B/D</sub> | align="center"| 8.4 | align="center"| 24β30 | align="center"| | align="center"| 2β4 | align="center"| 26 | align="center"| [[CYP1A2]] | align="center"| 2.5 |} Zolmitriptan is different from the other triptans because it is converted to an active N-desmethyl metabolite which has higher affinity for the 5-HT<sub>1D</sub> and 5-HT<sub>1B</sub> receptors; both substances have a biological half-life of 2 to 3 hours.<ref name="Goodman" /> In studies, newer triptans are mostly compared to sumatriptan.<ref name="Ferrari">{{cite journal | last1 = Ferrari | first1 = M. D. | last2 = Goadsby | first2 = P. J. | last3 = Roon | first3 = K. I. | last4 = Lipton | first4 = R. B. | year = 2002 | title = Triptan (serotonin, 5-HT1D/1B agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials | journal = Cephalalgia | volume = 22 | issue = 8| pages = 633β658 | doi = 10.1046/j.1468-2982.2002.00404.x | pmid=12383060| s2cid = 2368571 }}</ref> They are better than sumatriptan for their longer half-life in plasma and higher oral [[bioavailability]],<ref name="Foyes" /> but have a higher potential for [[central nervous]] side effects.<ref name="Mutschler" /> [[Donitriptan]] and [[avitriptan]] were never marketed.
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