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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]
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]
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] In spite of acting as an agonist of the serotonin 5-HT 2A receptor, DHE has been described as non-hallucinogenic. [16]
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.
Eletriptan is a serotonin receptor agonist, specifically an agonist of certain 5-HT 1 family receptors. Eletriptan binds with high affinity to the 5-HT [1B , 1D , 1F] receptors. It has a modest affinity to the 5-HT [1A , 1E , 2B , 7] receptors, and little to no affinity at the 5-HT [2A , 2C , 3 , 4 , 5A , 6] receptors.
Like all triptans, almotriptan has a high and specific affinity for serotonin 5-HT 1B/1D receptors. Binding of the drug to the receptor leads to vasoconstriction of the cranial (brain) blood vessels and thus affects the redistribution of blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through ...
[5] [6] [4] Whereas methysergide is a mixed agonist of some serotonin receptors (e.g., the 5-HT 1 receptors) and antagonist of other serotonin receptors (e.g., the 5-HT 2 receptors), methylergonovine is a non-selective agonist of most of the serotonin receptors, including of both the serotonin 5-HT 1 and 5-HT 2 receptor subgroups. [7]
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