Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine.
Frovatriptan succinate is one of the most recent serotonin receptor agonists to receive FDA, approved labelling for use in the acute management of migraine with or without aura in adults. The mechanism of action of frovatriptan is thought to be similar to that of a serotonin agonist. However, frovatriptan has distinctive pharmacokinetic and pharmacologic properties, chiefly, a high affinity for serotonin receptors 1B and 1D and a long elimination half-life; frovatriptan was shown to be more selective for cerebral than coronary arteries, a property which makes frovatriptan more favourable in patients at risk of coronary artery disease. Additionally, frovatriptan has a half-life of approximately 25 h, substantially longer than that of any other agent within its class. This property makes frovatriptan suitable for patients who typically suffer migraines of long duration and/or those who suffer migraine recurrence. The efficacy of frovatriptan in the treatment of acute migraine was demonstrated in five double-blind, randomised, placebo-controlled trials. At 2h, headache response rates for frovatriptan 2.5 mg ranged from 38 to 40% compared to 22-35% for placebo. Headache recurrence for frovatriptan 2.5 mg at 24h ranged from 9 to 14% compared with 18% in placebo subjects. Frovatriptan has no clinically significant pharmacokinetic interactions with drugs used for migraine prophylaxis or with commonly prescribed medications. Adverse effects of frovatriptan including dizziness, paresthesia, dry mouth, fatigue and flushing were generally mild and well tolerated. Given the fact that patient response to serotonin agonists is individualised, and selecting an effective agent may involve trial and error, frovatriptan is a welcome alternative in the acute management of migraine.
St John's University, College of Pharmacy and Allied Health Professions, and Ambulatory Medicine, Queens Hospital Center, jamaica, New York 11439, USA. balbisie@stjohns.edu
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Balbisi
D002227:Carbazoles / Q000494:pharmacology / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D008297:Male; D008599:Menstruation Disturbances / Q000150:complications; D008881:Migraine Disorders / Q000188:drug therapy* / Q000209:etiology; D015337:Multicenter Studies as Topic; D016032:Randomized Controlled Trials as Topic; D012008:Recurrence; D012307:Risk Factors; D017366:Serotonin Receptor Agonists / Q000627:therapeutic use*; D018170:Sumatriptan / Q000009:adverse effects / Q000627:therapeutic use*; D016896:Treatment Outcome; D014363:Tryptamines
D002227:Carbazoles; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; D018170:Sumatriptan; C108128:frovatriptan