title: Pharmacokinetics of a newly identified active metabolite of buspirone after administration of buspirone over its therapeutic dose range.
abstract: The objective of this study was to assess the pharmacokinetics of a newly identified active metabolite of buspirone, 6-hydroxybuspirone (6OHB), over the therapeutic dose range of buspirone. A 26-day, open-label, nonrandomized, single-sequence, dose-escalation study in normal healthy volunteers was conducted (N = 13). Subjects received escalating doses of buspirone with each dose administered for 5 days starting at a dose of 5 mg twice daily and increasing up to 30 mg twice daily. Plasma concentrations of 6OHB were approximately 40-fold greater than those of buspirone. 6OHB was rapidly formed following buspirone administration, and exposure increased proportionally with buspirone dose. Further research regarding the safety and efficacy of 6OHB itself is warranted.
authors.affiliation: Bristol-Myers Squibb Comapny, Princeton, NJ 08543, USA. randy.dockens@bms.com
authors.forename: Randy C
authors.initials: RC
authors.lastname: Dockens
authors.forename: Daniel E
authors.initials: DE
authors.lastname: Salazar
authors.forename: I Edgar
authors.initials: IE
authors.lastname: Fulmor
authors.forename: Michele
authors.initials: M
authors.lastname: Wehling
authors.forename: Mark E
authors.initials: ME
authors.lastname: Arnold
authors.forename: Robert
authors.initials: R
authors.lastname: Croop
mesh_terms: D000328:Adult; D014151:Anti-Anxiety Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D002065:Buspirone / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male
chemical_list: D014151:Anti-Anxiety Agents; C516840:6-hydroxybuspirone; D002065:Buspirone