ATC Group: N02C Antimigraine preparations

Almotriptan is a selective 5-HT_1B and 5-HT_1D receptor agonist. These receptors mediate vasoconstriction of certain cranial vessels, as demonstrated in studies using isolated human tissue preparations.

Atogepant is indicated for prophylaxis of migraine. Atogepant shows affinity to several receptors of the calcitonin/CGRP-receptor family. In view of the clinically relevant free plasma concentrations of atogepant and the fact that CGRP and amylin-1 receptors are considered to be involved in the pathophysiology of migraine, inhibitory effects of atogepant at these receptors could be of clinical relevance. However, the precise mechanism of action of atogepant in the prophylaxis of migraine remains to be established.

Clonidine has been shown to have both central and peripheral sites of action. With long-term treatment clonidine reduces the responsiveness of peripheral vessels to vasoconstrictor and vasodilator substances and to sympathetic nerve stimulation. Early in treatment, however, blood pressure reduction is associated with a central reduction of sympathetic outflow and increased vagal tone.

Dihydroergotamine binds with high affinity to 5-HT_1Dα and 5-HT_1Dβ receptors. It also binds with high affinity to serotonin 5-HT_1A, 5-HT_2A, and 5-HT_2C receptors. The therapeutic activity of dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT_1D receptors.

Eletriptan is a selective agonist at the vascular 5-HT_1B and neuronal 5-HT_1D receptors. Eletriptan also exhibits high affinity for the 5-HT_1F receptor which may contribute to its anti-migraine mechanism of action.

Erenumab is a human monoclonal antibody that binds to the calcitonin gene-related peptide (CGRP) receptor. CGRP is a neuropeptide that modulates nociceptive signalling and a vasodilator that has been associated with migraine pathophysiology. Inhibition of the effects of CGRP could theoretically attenuate compensatory vasodilation in ischaemic-related conditions.

Fremanezumab is a humanised IgG2Δa/kappa monoclonal antibody which selectively binds the calcitonin gene-related peptide (CGRP) ligand and blocks both CGRP isoforms (α- and β-CGRP) from binding to the CGRP receptor. It is believed that prevention of migraine is obtained by its effect modulating the trigeminal system.

Frovatriptan is a selective agonist for 5-HT receptors. Frovatriptan is believed to act selectively on extracerebral, intracranial arteries to inhibit the excessive dilatation of these vessels in migraine.

Galcanezumab is a humanised IgG4 monoclonal antibody that binds calcitonin gene-related peptide (CGRP) thus preventing its biological activity. Elevated blood concentrations of CGRP have been associated with migraine attacks.

Naratriptan has been shown to be a selective agonist for 5 hydroxytryptamine₁ (5-HT₁) receptors mediating vascular contraction. This receptor is found predominantly in intracranial (cerebral and dural) blood vessels. Naratriptan is indicated for the acute treatment of migraine attacks with or without aura.

Rizatriptan binds selectively with high affinity to human 5-HT_1B and 5-HT_1D receptors. The therapeutic activity of rizatriptan in treating migraine headache may be attributed to its agonist effects at 5-HT_1B and 5-HT_1D receptors on the extracerebral intracranial blood vessels that are thought to become dilated during an attack and on the trigeminal sensory nerves that innervate them.

Sumatriptan has been demonstrated to be a specific and selective 5-Hydroxytryptamine₁ (5HT_1D) receptor agonist with no effect on other 5HT receptor (5-HT₂ - 5-HT₇) subtypes. The vascular 5-HT_1D receptor is found predominantly in cranial blood vessels and mediates vasoconstriction.

Zolmitriptan has been demonstrated to be a selective agonist for the vascular human recombinant 5HT_1B and 5HT_1D receptor subtypes. Zolmitriptan is a high affinity 5HT_1B/1D receptor agonist with modest affinity for 5HT_1A receptors.