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Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. [1] [3] It is taken by mouth. [1] [3] It can also be applied on the tongue. [2] It is a serotonin (5-HT) 1B/1D receptor agonist (triptan). [1] [2] Common side effects include chest pain, dizziness, dry mouth, and tingling. [3]
The drugs of this class act as agonists for serotonin 5-HT 1B and 5-HT 1D receptors at blood vessels and nerve endings in the brain. The first clinically available triptan was sumatriptan, which has been marketed since 1991. Triptans have largely replaced ergotamines, an older class of medications used to relieve migraine and cluster headaches. [3]
The neurotransmitter serotonin (illustration) has various receptors. A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin (5-hydroxytryptamine; 5-HT), a neurotransmitter and hormone and the endogenous ligand of the serotonin receptors.
Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They are selective 5-hydroxytryptamine/serotonin 1B/1D (5-HT 1B/1D) agonists. [1] Migraine is a complex disease which affects about 15% of the population and can be highly disabling. [2]
Sumatriptan is molecularly similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT 1D and 5-HT 1B [17]) agonist. Sumatriptan's primary therapeutic effect is related in its inhibition of the release of Calcitonin gene-related peptide (CGRP), likely through its 5-HT 1D/1B receptor-agonist action. [18]
DHE's antimigraine activity is due to its action as an agonist at the serotonin 5-HT 1B, 5-HT 1D, and 5-HT 1F receptors. It also interacts with other serotonin, adrenergic, and dopamine receptors. [14] DHE is an agonist of the serotonin 5-HT 2B receptor and has been associated with cardiac valvulopathy. [15]
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