Triptans

K K Jain MD (Dr. Jain is a consultant in neurology and has no relevant financial relationships to disclose.)
Originally released June 15, 2009; last updated July 23, 2017; expires July 23, 2020

Overview

Triptans, selective serotonin receptor (5-HT) agonists, are used in the treatment of acute migraine attacks as well as non-migraine headaches. In this article, the author describes the pharmacology of triptans and compares 7 approved triptans: almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan. Clinical trials of triptans and personalized treatment of migraine with triptans are also described.

Key points

 

• Triptans are selective serotonin receptor agonists used in the treatment of acute migraine attacks.

 

• The beneficial effect of triptans in migraine is related to their multiple mechanisms of action at sites implicated in the pathophysiology of migraine, eg, vasoconstriction.

 

• Several triptans with different methods of delivery are available.

 

• It may be possible to match individual patient needs with the specific characteristics of the individual triptans to optimize therapeutic benefit.

Historical note and terminology

Triptans, belonging to a family of tryptamine-based drug, are selective serotonin receptor (5-HT) agonists used in the treatment of acute migraine attacks and cluster headaches. Basis for the discovery of triptans was laid in 1960s by observations that vasoconstriction produced by 5-HT, ergotamine, and noradrenaline reduced migraine attacks. Platelet 5-HT levels were found to be reduced during migraine. As 5-HT itself could not be researched, efforts were focused on the receptors of 5-HT to discover and develop a more specific agonist for 5-HT receptors. This led to discovery of several types and subtypes of 5-HT. Several compounds were tested and discarded because of low bioavailability. Continued research led to the discovery of the first triptan drug, sumatriptan, which had both vasoconstriction effect as well as better oral bioavailability. Sumatriptan was first launched in Europe in 1991 and became available 1993 in the United States. Several other triptans have been developed since then. Marketed triptans for migraine are:

 

• Almotriptan
• Eletriptan
• Frovatriptan
• Naratriptan
• Rizatriptan
• Sumatriptan
• Zolmitriptan

Sumatriptan/naproxen, combination of a triptan with a long-acting nonsteroidal antiinflammatory drug, is approved for acute treatment and sustained relief of migraine.

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