Triptans and migraine: advances in use, administration, formulation, and development

Abstract

Recent triptan development has focused on new administration methods and formulations, triptan combination therapies, treatment in menstrually related migraines, and novel serotonin receptor subtype agonists (5HTf). Areas covered: Clinical triptan research related to migraine was reviewed, analyzing EMBASE and PUBMED data bases from 01/01/2011 to 06/29/2016, with a focus on clinical trials of class 1 or 2 level of evidence. There have been advances in drug combination therapies, as well as administration devices that aid in ease of use, increase efficacy, and decrease adverse reactions. Some new agents and devices have similar or less efficacy compared to previous generic triptan formulations. New agents have action at the 5HTf receptor subtype, and avoid vascular side effects of classic 5Ht1b/d agonists, however adverse reactions may limit their clinic use. Long half-life triptans, frovatriptan and naratriptan, do appear to have good benefit in menstral related migraine. Expert opinion: Recent advances in triptan development can offer some advantages to migraine therapy and patient preferences, but have a much higher cost compared to individual generic triptan agents. In the coming years, triptan advances with high efficacy, limiting ADRs and cost are welcomed, in this regard the 5HT1b/d triptans are already well established.

No additive effect of combining sumatriptan and olcegepant in the GTN mouse model of migraine

“…Triptans are 5-HT 1B/1D/1F agonists (7) inhibiting trigeminal calcitonin gene-related peptide (CGRP) release by hyperpolarizing nerve endings (8) and causing cranial vasoconstriction (9,10). Although beneficial in many patients, lack of effect and a relatively high incidence of side effects cause limitations (11–13). A meta-analysis of 53 high-quality, placebo-controlled randomized clinical trials showed an average sumatriptan (100 mg per oral) response rate of 59% (95% CI 57–61) for any headache response, 29% (95% CI 27–31) for pain freedom and 20% (95% CI 18–21) for sustained pain freedom (14), showing that sumatriptan often results in pain reduction and not pain freedom.…”

Targeted 5-HT1F Therapies for Migraine

“…Triptans were introduced as a migraine treatment in the 1990s, implicating a major step forward in the better treatment for this disorder [ 17 ]. Since then, new research has focused on new administration methods and formulations, including triptan combination therapies with NSAIDs [ 18 , 19 ].…”

Chemical and pharmacological characterization of triptans

“…Triptánok: A migrén kezelésében 1973-ban egy új szakasz kezdődött, amikor megpróbáltak az ergot származékoknál szelektívebb szerotonin agonistát szintetizálni, figyelembe véve a szerotonin jelenlétét a migrénes rohamok esetén [18][19][20].…”