Occupancy of brain serotonin transporters during treatment with paroxetine in patients with social phobia: a positron emission tomography study with 11C McN 5652

Psychopharmacology (Berl). 2002 Dec;164(4):341-8. doi: 10.1007/s00213-002-1218-8. Epub 2002 Sep 11.

Abstract

Rationale: Although selective serotonin reuptake inhibitors (SSRIs) are widely used in the treatment of anxiety and depressive disorders, the occupancy of the serotonin reuptake transporter (SERT) achieved in humans at typical clinical doses by these agents remains poorly characterized.

Objective: The purpose of this study was to determine the occupancy of the SERT achieved in vivo by the SSRI paroxetine in social phobia patients at typical antianxiety doses.

Methods: Measures of SERT availability were obtained with positron emission tomography and the SERT radiotracer [(11)C](+)-McN 5652 in five patients with social phobia before and during treatment with paroxetine at usual therapeutic doses (20-40 mg per day).

Results: Occupancy of the SERT by paroxetine was high in all subjects and in all regions measured after 3-6 months of continuous treatment.

Conclusions: The results of this study in an anxiety disorder sample are consistent with previously reported results in a depressed sample and suggest that paroxetine at therapeutic doses achieves very high occupancy levels of the SERT.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Brain / diagnostic imaging
  • Brain / drug effects*
  • Brain Mapping
  • Carrier Proteins / drug effects*
  • Carrier Proteins / physiology
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Image Processing, Computer-Assisted
  • Isoquinolines / pharmacokinetics
  • Magnetic Resonance Imaging
  • Male
  • Membrane Glycoproteins / drug effects*
  • Membrane Glycoproteins / physiology
  • Membrane Transport Proteins*
  • Middle Aged
  • Nerve Tissue Proteins*
  • Paroxetine / pharmacokinetics
  • Paroxetine / therapeutic use*
  • Personality Inventory
  • Phobic Disorders / diagnostic imaging
  • Phobic Disorders / drug therapy*
  • Selective Serotonin Reuptake Inhibitors / pharmacokinetics
  • Selective Serotonin Reuptake Inhibitors / therapeutic use*
  • Serotonin Plasma Membrane Transport Proteins
  • Tomography, Emission-Computed*

Substances

  • Carrier Proteins
  • Isoquinolines
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • SLC6A4 protein, human
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • Paroxetine
  • McN 5652