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Published in: The Journal of Headache and Pain 1/2011

Open Access 01-02-2011 | Review Article

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

Authors: Anna Ferrari, Ilaria Tiraferri, Laura Neri, Emilio Sternieri

Published in: The Journal of Headache and Pain | Issue 1/2011

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Abstract

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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Metadata
Title
Why pharmacokinetic differences among oral triptans have little clinical importance: a comment
Authors
Anna Ferrari
Ilaria Tiraferri
Laura Neri
Emilio Sternieri
Publication date
01-02-2011
Publisher
Springer Milan
Published in
The Journal of Headache and Pain / Issue 1/2011
Print ISSN: 1129-2369
Electronic ISSN: 1129-2377
DOI
https://doi.org/10.1007/s10194-010-0258-4

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