Sedative and hypnotic effects of oral administration of micronized progesterone may be mediated through its metabolites
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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Progesterone produces its anxiolytic and hypnotic effects via allopregnanolone binding to GABAA receptors.
“Progesterone produces its anxiolytic/hypnotic effects via allopregnanolone's binding to GABAA-receptors [96, 97]”
From Sleep, hormones, and circadian rhythms throughout the menstrual cycle in healthy women and women with premenstrual dysphoric disorder (2010) · cites this paper as [96]
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The Rebirth of Progesterone in the Prevention of Preterm Labor
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Is Bio-Identical Hormone Replacement Therapy Safer than Traditional Hormone Replacement Therapy?
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Antiproliferative effects of low-dose micronized progesterone
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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)
- 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
- 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 › Genetics › 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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