Triptans are medicines used in the treatment of migraine and cluster headaches. They are not used to prevent either of these conditions, nor are they considered a cure. However, they do provide significant symptomatic treatment. Below, we review triptans pharmacology in terms of indications, mechanism, side effects, and drug interactions.
Triptans have been around since the 1990s, largely replacing ergotamine drugs in the relief of patients with cluster headaches or migraine.
Sumatriptan, the first FDA approved triptan, was made available to the public in 1993. It was long believed that activity at serotonin receptors led to reduced incidence of migraine attacks, but it was not precisely known why. Triptans filled the gap and became an instant success.
Examples of widely prescribed triptans:
Though triptans are used to treat cluster headaches and migraines, they are not used to treat other types of headache. For example – they are not used to treat tension headaches. Note that triptans are not prophylactic agents and do not prevent migraines and cluster headaches.
Instead, triptans are abortive agents – meaning that they help to hasten the end of an ongoing event.
As we alluded to earlier, researchers long knew that a connection existed between migraine and its relief via activity at serotonergic receptors. This research commenced in the 1940s, but it was only in the 1990s that triptans became widely used.
Specifically, triptans work as agonists at 5-HT1B and 5-HT1D receptors. They have activity at other receptor sites, but it’s through their activity at these two receptor sites that primarily accounts for their therapeutic impact.
Agonism at 5-HT1B / 5-HT1D receptors causes vasoconstriction of blood vessels surrounding the brain.
However, triptans also have two other modes of effect:
These are the three primary ways in which triptans exert their therapeutic impact.
Side effects with triptans include:
Though triptans are linked to these effects, it’s worth emphasizing that triptans are very well-tolerated drugs.
More rarely, triptans are linked to cardiovascular events, not least because triptans are linked to the risk of high blood pressure.
Sumatriptan overdose is linked to sulfhemoglobinemia – an effect which causes blood to change from red to green. However, once sumatriptan is discontinued from use, the change reverses within a matter of weeks. The condition arises due to the presence of a sulfur group within the hemoglobin molecule.
When we think about the clinical pharmacology of triptans, we need to talk about the following factors:
That concludes our rapid revision of triptans pharmacology. They remain a widely prescribed, and highly effective, drug class. Check back to our PharmaFactz blog soon for even more exclusive content to help you master the science of medicines!