title: Current and emerging second-generation triptans in acute migraine therapy: a comparative review.
abstract: Sterile neurogenic inflammation within cephalic tissue, involving vasodilation and plasma protein extravasation, has been proposed as a pathophysiological mechanism in acute migraine. The action of 5-hydroxytryptamine (5-HT1B/1D) agonists--so-called triptans--on receptors located in meningeal arteries (5-HT1B) and trigeminovascular fiber endings (5-HT1D) has an inhibitory effect on this neurogenic inflammation. Recently, a series of second-generation 5-HT1B/1D agonists (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, and zolmitriptan) have been developed and are reviewed in this article. Their in vitro pharmacological properties, pharmacokinetics, clinical efficacy, drug interactions, and adverse effects are evaluated and compared to the golden standard in the treatment of acute migraine, sumatriptan.
authors.affiliation: Department of Clinical Pharmacology, College of Medicine, Sultan Qaboos University Hospital, Sultanate of Oman.
authors.forename: D
authors.initials: D
authors.lastname: Deleu
authors.forename: Y
authors.initials: Y
authors.lastname: Hanssens
mesh_terms: D000208:Acute Disease; D002227:Carbazoles / Q000627:therapeutic use; D006801:Humans; D007211:Indoles / Q000627:therapeutic use; D008881:Migraine Disorders / Q000188:drug therapy*; D010080:Oxazoles / Q000627:therapeutic use; D023303:Oxazolidinones; D010880:Piperidines / Q000627:therapeutic use; D011759:Pyrrolidines / Q000627:therapeutic use; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000627:therapeutic use*; D014230:Triazoles / Q000627:therapeutic use; D014363:Tryptamines
chemical_list: D002227:Carbazoles; C470302:HTR1B protein, human; D007211:Indoles; D010080:Oxazoles; D023303:Oxazolidinones; D010880:Piperidines; D011759:Pyrrolidines; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D014230:Triazoles; D014363:Tryptamines; C409045:almotriptan; C115647:eletriptan; C089750:zolmitriptan; C093622:rizatriptan; C108128:frovatriptan; C106783:naratriptan