Antimigraine drugs

Abstract

Migraine is a paroxysmal disorder characterized by attacks of headache, nausea, vomiting, photophobia, phonophobia, and malaise. This review summarizes new treatment options for therapy of the acute attack. Mild or moderate migraine attacks are treated with antiemetics followed by analgesics such as aspirin, paracetamol, nonsteroidal anti-inflammatory drugs, or antiemetics combined with ergotamine or dihydroergotamine. Sumatriptan, a specific serotonin (5-HT)1B/D agonist is used when attacks do not respond to ergotamine, or when intolerable side effects occur. The new migraine drugs zolmitriptan, naratriptan, rizatriptan, and eletriptan differ slightly in their pharmacological profiles, which translates into minor differences in efficacy, headache recurrence, and side effects. New drugs in migraine prophylaxis include cyclandelate, valproic acid and magnesium.

Mechanisms of Action of the 5-HT1B/1D Receptor Agonists

“…32 Comparative trials have shown that 2.5 mg of naratriptan is less effective than 100 mg of sumatriptan in terms of the likelihood of achieving headache relief, but has almost no adverse effects. 45 Naratriptan has a lower headache recurrence rate than sumatriptan and rizatriptan when directly compared, but the time to recurrence is not longer with naratriptan. 29 Rizatriptan has a rapid onset of action, high bioavailability, and a favorable adverse effects profile.…”

High performance liquid chromatographic method for the determination of sumatriptan with fluorescence detection in human plasma

“…1) is a 5-hydroxytryptamine (5-HT1B/1D) receptor agonist, efficacious in the treatment of migraine. The mechanism of action of the (5-HT1B/1D) receptor agonist has been thoroughly studied [1][2][3][4] and leads to two main theories. Sumatriptan acts as a vasoconstrictor of dilated intracranial blood vessels and, also as an inhibitor of the pro-inflammatory neuropeptide release which leads to headache relief.…”

Colonic Ischemia Associated With Naratriptan Use

“…4 Though the premarketing experience failed to demonstrate its ischemic potential, we report on a case of ischemic colitis associated with the use of naratriptan. 5 This suggests that the development of ischemic colitis may be a class effect of the triptans.…”