Success and failure of triptans

Sumatriptan and the newer triptans (zolmitriptan, naratriptan, rizatriptan, eletriptan, almotriptan, frovatriptan and donitriptan) display high agonist activity at 5-HT(1B) and 5-HT(1D) receptors. Most triptans, but not all (donitriptan, frovatriptan and rizatriptan), also have a high affinity at the 5-ht(1F) receptor. In anaesthesisted animals, triptans decrease the arteriovenous anastomotic fraction of carotid blood flow. In isolated blood vessels, triptans cause contraction and this effect is more marked on cranial arteries. The 5-HT(1B) receptors and not 5-HT(1D) or 5-ht(1F) receptors mediate the vascoconstrictor effect of triptans. In animal studies, the triptans exert an inhibitory effect within the trigeminovascular system. The therapeutic effect of triptans is mediated mainly by their cranial vasoconstrictor property. Whether the inhibitory effects of the triptans on the trigeminovascular system contribute to their efficacy in migraine is still a moot point. The biggest success of triptans is that they provide an excellent therapeutic option for migraine therapy. This success has generated awareness for migraine in patients, clinicians and researchers alike. This, in turn, has increased our knowledge of the disease pathophysiology, which will ultimately lead to even better drugs in future. Among the failures of triptans, one may mention that a minority of patients respond poorly and others may have headache recurrence and chest syndromes. Overall, however, the advantages of triptans far outweigh their disadvantages and they represent a significant advance in medical therapy.