title: Pharmacokinetics of buspirone in autistic children.
abstract: Buspirone is used to treat generalized anxiety disorder in children and may be useful in developmental disorders in which brain serotonin synthesis is altered. Autistic children (13 boys, 7 girls) were given a single oral dose of 2.5 mg (2-3 years) or 5.0 mg (4-6 years). Blood was collected for 8 hours, and plasma was assayed for buspirone and its metabolite 1-pyrimidinylpiperazine (1-PP). The peak concentration of buspirone averaged 1141 +/- 748 pg/mL with a time to maximum concentration of 0.8 hours. Half-life was 1.6 +/- 0.3 hours. Peak concentrations of 1-PP were 4.5-fold higher than for buspirone. Girls had higher peak concentrations (1876 vs 746 pg/mL) for buspirone and a lower peak 1-PP/buspirone concentration ratio. These results suggest that buspirone is rapidly absorbed and eliminated in young children with extensive metabolism to 1-PP. Plasma concentrations with 2.5- to 5.0-mg doses were similar to those observed in older children receiving 7.5- to 15-mg doses.
authors.affiliation: Department of Pharmacy Practice, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA. dje@wayne.edu
authors.forename: David J
authors.initials: DJ
authors.lastname: Edwards
authors.forename: Diane C
authors.initials: DC
authors.lastname: Chugani
authors.forename: Harry T
authors.initials: HT
authors.lastname: Chugani
authors.forename: Jamal
authors.initials: J
authors.lastname: Chehab
authors.forename: Monica
authors.initials: M
authors.lastname: Malian
authors.forename: Jacob V
authors.initials: JV
authors.lastname: Aranda
mesh_terms: D014151:Anti-Anxiety Agents / Q000097:blood / Q000493:pharmacokinetics*; D001321:Autistic Disorder / Q000378:metabolism*; D002065:Buspirone / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics*; D002648:Child; D002675:Child, Preschool; D005260:Female; D006801:Humans; D008297:Male; D017366:Serotonin Receptor Agonists / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D014151:Anti-Anxiety Agents; D017366:Serotonin Receptor Agonists; C037921:1-(2-pyrimidinyl)piperazine; D002065:Buspirone