Psychopharmacology

, 186:414

Pharmacokinetic and behavioral effects of allopregnanolone in healthy women

  • Erika Timby
  • Matts Balgård
  • Sigrid Nyberg
  • Olav Spigset
  • Agneta Andersson
  • Joanna Porankiewicz-Asplund
  • Robert H. Purdy
  • Di Zhu
  • Torbjörn Bäckström
  • Inger Sundström Poromaa
Original Investigation

DOI: 10.1007/s00213-005-0148-7

Cite this article as:
Timby, E., Balgård, M., Nyberg, S. et al. Psychopharmacology (2006) 186: 414. doi:10.1007/s00213-005-0148-7
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Abstract

Rationale

The behavioral effects of allopregnanolone (3α-hydroxy-5α-pregnan-20-one) in women are not known.

Objective

Allopregnanolone, a neuroactive steroid secreted by the mammalian ovary, exerts its anesthetic, anxiolytic, and sedative/hypnotic effects through potentiation of GABAA receptors. The purpose of this study was to evaluate the behavioral effects of allopregnanolone in healthy women.

Methods

Ten healthy women were given three increasing intravenous doses of allopregnanolone in the follicular phase of the menstrual cycle. Saccadic eye movement parameters and visual analogue scales of sedation were used to evaluate the behavioral response of allopregnanolone. Repeated blood samples for analyses of allopregnanolone were drawn throughout the study day.

Results

Exogenously administered allopregnanolone decreases saccadic eye movement parameters and increases subjective ratings of sedation that correlate with increased serum concentrations of this neuroactive steroid.

Conclusion

The behavioral effects of allopregnanolone are similar to that of its 5β-stereoisomer, pregnanolone (3α-hydroxy-5β-pregnan-20-one). Apart from fatigue and mild nausea, allopregnanolone given in a cumulative dose of 0.09 mg/kg did not have any adverse effects.

Keywords

AllopregnanoloneNeuroactive steroidBehavioralSaccadic eye velocityMenstrual cycle

Copyright information

© Springer-Verlag 2005

Authors and Affiliations

  • Erika Timby
    • 1
  • Matts Balgård
    • 2
  • Sigrid Nyberg
    • 1
  • Olav Spigset
    • 3
  • Agneta Andersson
    • 1
  • Joanna Porankiewicz-Asplund
    • 4
  • Robert H. Purdy
    • 5
  • Di Zhu
    • 1
  • Torbjörn Bäckström
    • 1
  • Inger Sundström Poromaa
    • 6
  1. 1.Department of Clinical Science, Obstetrics and GynecologyUmeå UniversityUmeåSweden
  2. 2.Hospital PharmacyUniversity HospitalUmeåSweden
  3. 3.Department of Clinical PharmacologyRegional and University Hospital of TrondheimTrondheimNorway
  4. 4.AgriSera ABVännäsSweden
  5. 5.Department of NeuropharmacologyThe Scripps Research InstituteLa JollaUSA
  6. 6.Department of Women's and Children's HealthUniversity Hospital, Uppsala UniversityUppsalaSweden