Product Code Database
Eletriptan, sold under the brand name Relpax and used in the form of eletriptan hydrobromide, is a second-generation triptan medication intended for treatment of migraine . It is used as an abortive medication, blocking a migraine attack which is already in progress. Eletriptan is marketed and manufactured by Pfizer.
| + | |
| 1.9–45 (Ki) 417–1,820 () | |
| 0.52–15.1 (Ki) 8.1–60 () 83% () | |
| 0.10–1.5 (Ki) 0.63–0.91 () | |
| 56–62 (Ki) 30–126 () | |
| 10–20 (Ki) 7.4–132 () | |
| 1,150–>3,160 (Ki) 851 () | |
| 447 (Ki) 155 () | |
| >3,160 (Ki) () | |
| >3,160 (mouse) | |
| >3,160 (guinea pig) | |
| 977–1,584 (rat) | |
| 525 | |
| 200 (Ki) 355 () | |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: (2025). 9780128233573 ISBN 9780128233573 | |
Eletriptan is believed to reduce swelling of the blood vessels surrounding the brain. This swelling is associated with the head pain of a migraine attack. Eletriptan blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound. It is thought that these actions contribute to relief of symptoms by eletriptan.
Eletriptan is a serotonin receptor agonist, specifically an agonist of certain 5-HT1 family receptors. Eletriptan binds with high affinity to the 5-HT1B,]] receptors. It has a modest affinity to the 5-HT1A,]] receptors, and little to no affinity at the 5-HT2A,]] receptors.
Eletriptan has no significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic D1 or D2; muscarinic; or . Eletriptan could be efficiently co-administered with nitric oxide synthase (NOS's) inhibitors for the treatment of NOS-dependent diseases (US patent US 2007/0254940).
Two theories have been proposed to explain the efficacy of 5-HT1 receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
The drug is also notable in being a weak serotonin 5-HT2A receptor agonist ( = 851nM), albeit with about two to three orders of magnitude lower activational potency than at the serotonin 5-HT1B and 5-HT1D receptors.
In the United States, Relpax is marketed by Viatris after Upjohn was spun off from Pfizer.
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