Pharmacokinetics of a newly identified active metabolite of buspirone after administration of buspirone over its therapeutic dose range.
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.
Dockens
Randy C
RC
Bristol-Myers Squibb Comapny, Princeton, NJ 08543, USA. randy.dockens@bms.com
Salazar
Daniel E
DE
Fulmor
I Edgar
IE
Wehling
Michele
M
Arnold
Mark E
ME
Croop
Robert
R
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
D014151:Anti-Anxiety Agents; C516840:6-hydroxybuspirone; D002065:Buspirone