title: Profiles of 5-HT 1B/1D agonists in acute migraine with special reference to second generation agents.
abstract: The efficacy of 5-hydroxytryptamine 1B/1D (5-HT 1B/1D) agonists is related to their inhibitory effects on neurogenic inflammation, mediated through serotoninergic control mechanisms. Recently, a series of oral second generation 5-HT 1B/1D agonists (eletriptan, naratriptan, rizatriptan and zolmitriptan) have been developed and are reviewed in this paper. Their in vitro and in vivo pharmacological properties, clinical efficacy, drug interactions, and adverse effects are evaluated and compared to the gold standard in the treatment of acute migraine, sumatriptan.
authors.affiliation: Department of Clinical Pharmacology, College of Medicine, Sultan Qaboos University.
authors.forename: D
authors.initials: D
authors.lastname: Deleu
authors.forename: Y
authors.initials: Y
authors.lastname: Hanssens
mesh_terms: D000208:Acute Disease; D000818:Animals; D002986:Clinical Trials as Topic; D003326:Coronary Circulation / Q000187:drug effects; D003329:Coronary Vasospasm / Q000139:chemically induced; D015195:Drug Design; D004347:Drug Interactions; D006801:Humans; D008658:Inactivation, Metabolic; D007211:Indoles / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D008578:Meninges / Q000098:blood supply; D008881:Migraine Disorders / Q000188:drug therapy* / Q000503:physiopathology; D015394:Molecular Structure; D009619:Nociceptors / Q000502:physiology; D010080:Oxazoles / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D023303:Oxazolidinones; D010880:Piperidines / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D011433:Propranolol / Q000494:pharmacology; D011759:Pyrrolidines / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic; D051381:Rats; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000502:physiology; D012008:Recurrence; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000145:classification / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013329:Structure-Activity Relationship; D018170:Sumatriptan / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D016896:Treatment Outcome; D014230:Triazoles / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D014363:Tryptamines; D014662:Vasoconstrictor Agents / Q000009:adverse effects / Q000627:therapeutic use
chemical_list: 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; D014662:Vasoconstrictor Agents; C115647:eletriptan; C089750:zolmitriptan; C093622:rizatriptan; D018170:Sumatriptan; D011433:Propranolol; C106783:naratriptan