Distribution of Venlafaxine, O-desmethylvenlafaxine, and O-desmethylvenlafaxine to Venlafaxine Ratio in Postmortem Human Brain Tissue

• NCJ Number: 246848
• Journal: Journal of Forensic Sciences Volume: 59 Issue: 3 Dated: May 2014 Pages: 683-689
• Author(s): Meredith D. Murrell M.S.; Dianne A. Cruz M.S.; Martin A. Javors Ph.D.; Peter M. Thompson M.D.
• Date Published: May 2014
• Length: 7 pages
• Publication Format: Article
• Publication Type: Report (Study/Research)
• Language: English
• Country: United States of America

Annotation

Venlafaxine VEN and its metabolite O-desmethylvenlafaxine ODV inhibit reuptake of serotonin and norepinephrine.

Abstract

Venlafaxine VEN and its metabolite O-desmethylvenlafaxine ODV inhibit reuptake of serotonin and norepinephrine. This study examines whether VEN is differentially distributed in postmortem brain and examines relationships between brain and femoral blood concentrations from donors prescribed VEN for treatment of depression. Using high-pressure liquid chromatography-ultraviolet detection, VEN and ODV concentrations were measured in temporal, occipital, and cerebellar cortex of six postmortem brains. The ODV/VEN ratio was calculated as a relative measure of drug metabolism within each region where higher ratios indicated a greater conversion of VEN to ODV. Compared to the other regions examined, the cerebellum showed decreased VEN p = 0.056, ODV p = 0.006, and ODV/VEN p = 0.027 ratios. In parts per million, VEN was higher in temporal and occipital cortex, but not cerebellum, as compared to femoral blood concentration. These observations suggest that VEN and ODV are differentially distributed in the brain, and metabolism of VEN to ODV may vary across brain regions.