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Pharmacokinetics of a Newly Identified Active Metabolite of Buspirone After Administration of Buspirone Over Its Therapeutic Dose Range
Author(s) -
Dockens Randy C.,
Salazar Daniel E.,
Fulmor I. Edgar,
Wehling Michele,
Arnold Mark E.,
Croop Robert
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006292250
Subject(s) - buspirone , pharmacokinetics , active metabolite , pharmacology , metabolite , medicine , therapeutic index , oral administration , drug , agonist , receptor
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.