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PEDIATRICS

Pharmacokinetics of Buspirone in Autistic Children

David J. Edwards, PharmD, Diane C. Chugani, PhD, Harry T. Chugani, MD, Jamal Chehab, Monica Malian and Jacob V. Aranda, MD, PhD

From the Department of Pharmacy Practice (Dr Edwards), the Carman and Ann Adams Department of Pediatrics (Dr Edwards, Dr D. Chugani, Dr H. Chugani, Dr Aranda), the Department of Neurology (Dr H. Chugani), and the Department of Radiology (Dr D. Chugani, Dr. H. Chugani), Wayne State University, Detroit, Michigan; the Division of Clinical Pharmacology (Dr Edwards, Dr D. Chugani, Ms Chehab, Dr Aranda), PET Center (Dr D. Chugani, Dr H. Chugani), and the Department of Pharmacy Services (Ms Malian), Children's Hospital of Michigan and the NICHD-Pediatric Pharmacology Research Unit Network, Detroit, Michigan.

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.

Key Words: Buspirone • pediatrics • pharmacokinetics • gender • autism

Address for reprints: David J. Edwards, PharmD, Department of Pharmacy Practice, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201; e-mail: dje{at}wayne.edu.


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