Cited by 134Menopause: Health Impacts and TreatmentsAnesthesia and Sedative AgentsEstrogen and related hormone effects

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Sedative and hypnotic effects of oral administration of micronized progesterone may be mediated through its metabolites

Arafat, ElSayed S., Hargrove, Joel T., Maxson, Wayne S., Desiderio, Dominic M., Wentz, Anne Colston, Andersen, Richard N.·1988·American Journal of Obstetrics and Gynecology

DOI 10.1016/0002-9378(88)90448-6

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Abstract

Progesterone and its metabolites were measured in serum extracts by radioimmunoassay and gas chromatography-mass spectrometry, respectively, after ingestion of micronized progesterone by eight postmenopausal women. One subject received 400 mg of micronized progesterone orally that induced a hypnotic state that lasted for approximately 2 hours. Blood samples were drawn periodically from all subjects for measurement of progesterone and its metabolites in serum. Levels of serum progesterone and its metabolites increased significantly from baseline values and reached a peak between 2 and 6 hours after oral progesterone administration. Significant quantities of five compounds (progesterone, 5 alpha-pregnan-3 alpha-ol-20-one, 5 beta-pregnan-3 alpha-ol-20-one, 5 beta-pregnan-3 alpha,20 beta-diol, and 5 beta-pregnan-3 alpha-ol-11,20-dione) that have been reported to possess anesthetic qualities were identified. The sedative and hypnotic effects of oral administration of progesterone may be mediated through those compounds.

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Authors: Arafat, E. S., Hargrove, J. T., Maxson, W. S., Desiderio, D. M., Wentz, A. C., & Andersen, R. N.
Affiliations: Rust College (US)
Vanderbilt University Medical Center (US)
University of Tennessee Health Science Center (US)
Corresponding author: Hargrove, Joel T.
Venue: American Journal of Obstetrics and Gynecology
Publisher: Elsevier BV
Published: 1988-11
Volume: 159
Issue: 5
Pages: 1203-1209
ISSN: 0002-9378 (ISSN-L)
DOI: 10.1016/0002-9378(88)90448-6
OpenAlex: W2042977357
Cited by: 134
References: 22
Citations by year: 2026: 1 · 2023: 1 · 2022: 3 · 2021: 2 · 2020: 1 · 2019: 2 · 2018: 2 · 2016: 2 · 2015: 1 · 2013: 4 · 2012: 2
FWCI: 1.87
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: American Journal of Obstetrics and Gynecology (publishedVersion)
PubMed (publishedVersion)
Funders: National Institutes of Health (2s14rr002866-04)
National Institute of General Medical Sciences (GM26666)
National Center for Research Resources (5S14RR02866)
Topics: Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
Health Sciences › Medicine › Anesthesiology and Pain Medicine › Anesthesia and Sedative Agents
Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
Keywords: micronized progesterone, sedative effects, hypnotic effects, progesterone metabolites, postmenopausal women, oral administration, serum progesterone, 5alpha-pregnan-3alpha-ol-20-one, sleep induction
MeSH terms: Administration, Oral, Blood Chemical Analysis, Chromatography, Gas, Dose-Response Relationship, Drug, Female, Humans, Hypnotics and Sedatives, Middle Aged, Powders, Progesterone, Mass Spectrometry, Time Factors

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Sedative and hypnotic effects of oral administration of micronized progesterone may be mediated through its metabolites

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