Triptan efficacy in migraine attacks: from appropriate diagnosis to metabolic profiles and pharmacogenomics

Abstract

A major, revolutionary advance in acute migraine therapy was the development of sumatriptan, a selective 5-HT1B/1D receptor agonist. After sumatriptan, the so-called second generationtriptans have become available and at present 7 triptans are on the market. Activation of the trigeminal nerve is a key component of the cascade that leads to, and perpetuates, a migraine attack. Sumatriptan and the other triptans currently on the market (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, zolmitriptan) are potent agonists of the 5-HT1B and 5-HT1D receptors, and some are potent 5-HT1F agonists. The use of a variety of endpoints for a certain drug, measuring treatment success in terms of both efficacy and tolerability, should aid in the selection of agents that can offer patients the highest likelihood of consistent treatment success. Further possibilities are offered by studying metabolic profiles of molecules in order to tailor the best treatment option for each patient, and obtain the best efficacy profiles and the lower rate of drug-adverse events. Drug Dev Res 68: 335-340, 2007.

Chemical and pharmacological characterization of triptans

“…Az injekciós (s.c.) sumatriptant kivéve a többi triptánok metabolizmusában a máj is szerepet játszik, így májbetegség a használatukat korlátozza [46][47][48][49]. A triptánok farmakokinetikai tulajdonságai a (4. táblázatban) van összefoglalva [50][51][52].…”