###### Created: 2023-10-22 15:53 ###### Areas & Topics: #medicine #pharmacology ###### Note Type: #permanent ###### Connected to: [[Migraine]] - The triptans are a group of medications specifically indicated for the treatment of migraines. - The initial research into the development of anti-migraine medication was by Glaxo in the 1960's, which eventually led to the development of sumatriptan as the first antimigraine drug, being first released in The Netherlands in 1991. - The chemical structure of triptans is identical to that of serotonin (5-HT). - The main difference in the structure of each of the triptans is the side chain attached to them, which can slightly vary their effect and half-life (an important consideration for prescribing) ![[Pasted image 20231022164321.png]] ### Mechanism of Action - Triptans are a family of tryptamine-based drugs (tryptamine being a metabolite of tryptophan, the precursor to serotonin) - They work as agonists of 5HT-1B and 5HT-1D receptors and selectively bind to them when ingested. - Agonism of 5HT-1B is thought to cause vasoconstriction, which may reduce pain from vasodilation of the cranial blood vessels during migraine. - Agonism of 5HT-1D is thought to inhibit activation of the trigeminal nerve, stopping nociception and release of vasoactive neuropeptides. So, the main three ways triptans act to reduce migraine is: - Vascular (causing vasoconstriction to prevent painful dilation) - Trigeminovascular (inhibition of nociceptive neurotransmission in the trigeminal nerve) - Central (inhibiting the release of vasoactive neuropeptides produced b the trigeminal nerve that affect nociceptive brain structures) ### Adverse Effects - The main adverse effects of triptans are known as 'triptan sensations' - It is not fully understood what causes these effects, but it is likely to be from the stimulation of the 5HT receptors centrally and vasoconstriction Examples of common adverse effects include: - Flushing - Paraesthesia (tingling, burning etc.) - Tightness (mainly in the throat and chest possibly due to vasoconstriction) - Dizziness (possibly due to vasoconstriction) - Nausea ### Examples - Sumatriptan - Rizatriptan - Frovatriptan - Zolmitriptan ### Resources https://www.ncbi.nlm.nih.gov/books/NBK554507/ https://en.wikipedia.org/wiki/Discovery_and_development_of_triptans https://en.wikipedia.org/wiki/Triptan https://bnf.nice.org.uk/drugs/sumatriptan/#side-effects https://go.drugbank.com/drugs/DB00669