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Why pharmacokinetic differences among oral triptans have little clinical importance: a comment

Triptans, selective 5-HT1B/1D receptor agonists, are specific drugs for the acute treatment of migraine that have the same mechanism of action. Here, it is discussed why the differences among kinetic parameters of oral triptans have proved not to be very important in clinical practice. There are thr...

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Detalles Bibliográficos
Autores principales: Ferrari, Anna, Tiraferri, Ilaria, Neri, Laura, Sternieri, Emilio
Formato: Texto
Lenguaje:English
Publicado: Springer Milan 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3072488/
https://www.ncbi.nlm.nih.gov/pubmed/20878535
http://dx.doi.org/10.1007/s10194-010-0258-4
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author Ferrari, Anna
Tiraferri, Ilaria
Neri, Laura
Sternieri, Emilio
author_facet Ferrari, Anna
Tiraferri, Ilaria
Neri, Laura
Sternieri, Emilio
author_sort Ferrari, Anna
collection PubMed
description Triptans, selective 5-HT1B/1D receptor agonists, are specific drugs for the acute treatment of migraine that have the same mechanism of action. Here, it is discussed why the differences among kinetic parameters of oral triptans have proved not to be very important in clinical practice. There are three main reasons: (1) the differences among the kinetic parameters of oral triptans are smaller than what appears from their average values; (2) there is a large inter-subject, gender-dependent, and intra-subject (outside/during the attack) variability of kinetic parameters related to the rate and extent of absorption, i.e., those which are considered as critical for the response; (3) no dose-concentration–response curves have been defined and it is, therefore, impossible both to compare the kinetics of triptans, and to verify the objective importance of kinetic differences; (4) the importance of kinetic differences is outweighed by non-kinetic factors of variability of response to triptans. If no oral formulations are found that can allow more predictable pharmacokinetics, the same problems will probably also arise with new classes of drugs for the acute treatment of migraine.
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spelling pubmed-30724882011-05-18 Why pharmacokinetic differences among oral triptans have little clinical importance: a comment Ferrari, Anna Tiraferri, Ilaria Neri, Laura Sternieri, Emilio J Headache Pain Review Article Triptans, selective 5-HT1B/1D receptor agonists, are specific drugs for the acute treatment of migraine that have the same mechanism of action. Here, it is discussed why the differences among kinetic parameters of oral triptans have proved not to be very important in clinical practice. There are three main reasons: (1) the differences among the kinetic parameters of oral triptans are smaller than what appears from their average values; (2) there is a large inter-subject, gender-dependent, and intra-subject (outside/during the attack) variability of kinetic parameters related to the rate and extent of absorption, i.e., those which are considered as critical for the response; (3) no dose-concentration–response curves have been defined and it is, therefore, impossible both to compare the kinetics of triptans, and to verify the objective importance of kinetic differences; (4) the importance of kinetic differences is outweighed by non-kinetic factors of variability of response to triptans. If no oral formulations are found that can allow more predictable pharmacokinetics, the same problems will probably also arise with new classes of drugs for the acute treatment of migraine. Springer Milan 2010-09-29 2011-02 /pmc/articles/PMC3072488/ /pubmed/20878535 http://dx.doi.org/10.1007/s10194-010-0258-4 Text en © Springer-Verlag 2010
spellingShingle Review Article
Ferrari, Anna
Tiraferri, Ilaria
Neri, Laura
Sternieri, Emilio
Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title_full Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title_fullStr Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title_full_unstemmed Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title_short Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
title_sort why pharmacokinetic differences among oral triptans have little clinical importance: a comment
topic Review Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3072488/
https://www.ncbi.nlm.nih.gov/pubmed/20878535
http://dx.doi.org/10.1007/s10194-010-0258-4
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