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Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential
Migraine is an important socioeconomic burden and is ranked the sixth cause of years of life lost because of disability in the general population and the third cause of years of life lost in people younger than 50 years. The cornerstone of pharmacological treatment is represented by the acute therap...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Dove Medical Press
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5848843/ https://www.ncbi.nlm.nih.gov/pubmed/29563831 http://dx.doi.org/10.2147/JPR.S132833 |
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author | Negro, Andrea Koverech, Angela Martelletti, Paolo |
author_facet | Negro, Andrea Koverech, Angela Martelletti, Paolo |
author_sort | Negro, Andrea |
collection | PubMed |
description | Migraine is an important socioeconomic burden and is ranked the sixth cause of years of life lost because of disability in the general population and the third cause of years of life lost in people younger than 50 years. The cornerstone of pharmacological treatment is represented by the acute therapy. The serotonin (5-hydroxytryptamine [5-HT]) receptor subtype 1(B)/1(D) agonists, called triptans, are nowadays the first-line acute therapy for patients who experience moderate-to-severe migraine attacks. Unfortunately, a high percentage of patients are not satisfied with this acute treatment, either for lack of response or side effects. Moreover, their mechanism of action based on vasoconstriction makes them unsuitable for patients with previous cardio- and cerebrovascular diseases and for those with uncontrolled hypertension. Since the introduction of triptans, no other acute drug class has passed all developmental stages. The research for a new drug lacking vasoconstrictive effects led to the development of lasmiditan, a highly selective 5-HT1(F) receptor agonist with minimized interactions with other 5-HT receptor subtypes. Lasmiditan is considered to be the first member of a new drug category, the neurally acting anti-migraine agent (NAAMA). Phase II and III trials had shown superiority compared to placebo and absence of typical triptan-associated adverse events (AEs). Most of the AEs were related to the central nervous system, depending on the high permeability through the blood–brain barrier and mild to moderate severity. The results of ongoing long-term Phase III trials will determine whether lasmiditan will become available in the market, and then active triptan comparator studies will assess patients’ preference. Future studies could then explore the safety during pregnancy and breastfeeding or the risk that overuse of lasmiditan leads to medication overuse headache. |
format | Online Article Text |
id | pubmed-5848843 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-58488432018-03-21 Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential Negro, Andrea Koverech, Angela Martelletti, Paolo J Pain Res Review Migraine is an important socioeconomic burden and is ranked the sixth cause of years of life lost because of disability in the general population and the third cause of years of life lost in people younger than 50 years. The cornerstone of pharmacological treatment is represented by the acute therapy. The serotonin (5-hydroxytryptamine [5-HT]) receptor subtype 1(B)/1(D) agonists, called triptans, are nowadays the first-line acute therapy for patients who experience moderate-to-severe migraine attacks. Unfortunately, a high percentage of patients are not satisfied with this acute treatment, either for lack of response or side effects. Moreover, their mechanism of action based on vasoconstriction makes them unsuitable for patients with previous cardio- and cerebrovascular diseases and for those with uncontrolled hypertension. Since the introduction of triptans, no other acute drug class has passed all developmental stages. The research for a new drug lacking vasoconstrictive effects led to the development of lasmiditan, a highly selective 5-HT1(F) receptor agonist with minimized interactions with other 5-HT receptor subtypes. Lasmiditan is considered to be the first member of a new drug category, the neurally acting anti-migraine agent (NAAMA). Phase II and III trials had shown superiority compared to placebo and absence of typical triptan-associated adverse events (AEs). Most of the AEs were related to the central nervous system, depending on the high permeability through the blood–brain barrier and mild to moderate severity. The results of ongoing long-term Phase III trials will determine whether lasmiditan will become available in the market, and then active triptan comparator studies will assess patients’ preference. Future studies could then explore the safety during pregnancy and breastfeeding or the risk that overuse of lasmiditan leads to medication overuse headache. Dove Medical Press 2018-03-08 /pmc/articles/PMC5848843/ /pubmed/29563831 http://dx.doi.org/10.2147/JPR.S132833 Text en © 2018 Negro et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Review Negro, Andrea Koverech, Angela Martelletti, Paolo Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title | Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title_full | Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title_fullStr | Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title_full_unstemmed | Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title_short | Serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
title_sort | serotonin receptor agonists in the acute treatment of migraine: a review on their therapeutic potential |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5848843/ https://www.ncbi.nlm.nih.gov/pubmed/29563831 http://dx.doi.org/10.2147/JPR.S132833 |
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