title: Overview of initial clinical studies with intravenous and oral GR43175 in acute migraine.
abstract: The novel 5-HT 1-like receptor agonist GR43175 has been evaluated as a treatment for acute migraine in a series of open, dose-ranging and controlled clinical trials. Patients with severe attacks of migraine have attended special pain or headache clinics for treatment and assessment. Given intravenously as a bolus, GR43175 is capable of aborting all migraine symptoms within 10-30 min in over 90% of cases at a dose of 64 micrograms/kg. Characteristic transient and reversible side effects with such a regimen include feelings of heaviness, pressure and occasionally warmth or tingling which can be diminished by extending the duration of drug administration to a short infusion. Initial dose-ranging studies with a dispersible tablet formulation of GR43175 have revealed an efficacy of 70-85% within 2 h with doses of 70-280 mg. Furthermore, tolerability is excellent. These encouraging early results warrant larger-scale controlled studies of GR43175 in acute migraine.
authors.affiliation: Medical Division, Glaxo Group Research Limited, Greenford, Middlesex, UK.
authors.forename: V L
authors.initials: VL
authors.lastname: Perrin
authors.forename: M
authors.initials: M
authors.lastname: Färkkilä
authors.forename: J
authors.initials: J
authors.lastname: Goasguen
authors.forename: A
authors.initials: A
authors.lastname: Doenicke
authors.forename: J
authors.initials: J
authors.lastname: Brand
authors.forename: P
authors.initials: P
authors.lastname: Tfelt-Hansen
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000368:Aged; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D007211:Indoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D007275:Injections, Intravenous; D008297:Male; D008875:Middle Aged; D008881:Migraine Disorders / Q000188:drug therapy*; D013449:Sulfonamides / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018170:Sumatriptan
chemical_list: D007211:Indoles; D013449:Sulfonamides; D018170:Sumatriptan