Review Article

The Journal of Headache and Pain

, Volume 12, Issue 1, pp 5-12

Open Access This content is freely available online to anyone, anywhere at any time.

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

  • Anna FerrariAffiliated withHeadache and Drug Abuse Inter-Dep. Research Centre, Division of Toxicology and Clinical Pharmacology, University of Modena and Reggio Emilia Email author 
  • , Ilaria TiraferriAffiliated withSchool of Medical Toxicology, University of Modena and Reggio Emilia
  • , Laura NeriAffiliated withSchool of Clinical Pharmacology, University of Modena and Reggio Emilia
  • , Emilio SternieriAffiliated withHeadache and Drug Abuse Inter-Dep. Research Centre, Division of Toxicology and Clinical Pharmacology, University of Modena and Reggio Emilia

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.

Keywords

Acute treatment Disposition Headache Pharmacokinetics Triptan Variability