In this article, we explore the fascinating history of triptans and their significant impact on migraine management. Triptans, a cornerstone in migraine treatment, have a surprising origin story that traces back to a fungus known as Claviceps purpurea. This fungus, which grows on rye, forms structures resembling a hen’s foot, called ergots. Historically, rye was a staple food, and when it became contaminated with this fungus, it led to ergotism in those who consumed it. Ergotism caused severe symptoms like hallucinations and gangrene due to the alkaloids in the fungus binding to serotonin receptors. The condition was so severe that it earned the name “St. Anthony’s fire.” Discover how these origins led to the development of effective migraine treatments.
The Medieval Impact of Rye Ergot
In medieval times, people consumed a lot of rye, and if the rye was contaminated, ergotism could result. The hallucinations were due to the overstimulation of serotonin receptors in the brain, similar to the effects of LSD. Gangrene occurred because the alkaloids caused such severe constriction of blood vessels that the flesh would become necrotic.
Medicinal Use of Rye Ergot
Despite its dangers, rye ergot was known for its potent medicinal properties. By the 18th century, it was used in paste form to stop uterine bleeding after childbirth. This use inspired further study, and in the 1940s, scientists discovered serotonin, a compound named for its role in increasing blood vessel tone. The understanding of serotonin’s functions evolved, revealing its significant impact on the brain.
The Development of Ergotamine
Ergotamine, discovered in 1918, was initially used to treat migraine by constricting blood vessels, a sensible approach given the theory that migraine was caused by blood vessel dilation. However, ergotamine had severe side effects, including high blood pressure and the risk of gangrene. This led researchers to seek a milder alternative. The quest for a safer migraine treatment culminated in the 1970s with the development of sumatriptan by Glaxo, which was marketed in the USA in 1993. Sumatriptan revolutionized migraine treatment with its effectiveness and shifted the perception of migraine from a psychiatric issue to a neurological condition.
Risks Associated with Triptans
While triptans were a breakthrough, they are not without risks. They should be avoided by individuals with coronary heart disease due to their constriction of cranial arteries. However, recent evidence suggests triptans do not significantly constrict brain blood vessels, alleviating some concerns about stroke risk.
How Triptans Relieve Migraine Pain
The exact mechanism by which triptans relieve migraine pain is still not fully understood. Initially believed to work by constricting blood vessels, it is now thought that they act on serotonin receptors in the brain, influencing neurological pathways rather than just the vascular system.
Fun Fact: Even if we have focused on the role of serotonin on the brain and blood vessels, 90% of the serotonin in the human body is stored in the gut. In the digestive tract, serotonin plays an important role in motility.
References
- Eadie MJ. Ergot of rye-the first specific for migraine. Journal of clinical neuroscience : official journal of the Neurosurgical Society of Australasia. 2004;11(1):4-7.
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