Neuroendocrine effects of naltrexone versus nalmefene in humans.
ACTH
cortisol
nalmefene
naltrexone
neuroendocrine
prolactin
Journal
Human psychopharmacology
ISSN: 1099-1077
Titre abrégé: Hum Psychopharmacol
Pays: England
ID NLM: 8702539
Informations de publication
Date de publication:
03 2020
03 2020
Historique:
received:
12
08
2019
revised:
14
01
2020
accepted:
20
01
2020
pubmed:
13
2
2020
medline:
30
1
2021
entrez:
13
2
2020
Statut:
ppublish
Résumé
Naltrexone and nalmefene are approved for the treatment of alcohol use disorders, in different countries. Naltrexone is also approved for the treatment for opioid use disorders, most recently in a depot formulation. These compounds target primarily μ(mu)- and κ(kappa)-opioid receptor systems, which are involved in the downstream neurobiological effects of alcohol and in the modulation of neuroendocrine stress systems. The study objective was to compare the neuroendocrine effects of naltrexone and nalmefene on adrenocorticotropic hormone (ACTH), cortisol, and prolactin, in normal volunteers. Adult normal volunteers (n = 11 male and n = 9 female) were studied in a stress-minimized inpatient setting on three consecutive days, after intravenous saline, naltrexone HCl (10 mg), or nalmefene HCl (10 mg), in fixed order. ACTH, cortisol, and prolactin were analyzed pre-injection and up to 180 min post-injection. Naltrexone and nalmefene caused elevations in ACTH and cortisol compared with saline. Nalmefene had a greater effect on ACTH and cortisol, compared with naltrexone. Both compounds also caused elevations in prolactin in males (females were not examined, due to the influence of menstrual cycle on prolactin). This study suggests that both nalmefene and naltrexone have effects potentially due to κ-partial agonism in humans, as well as antagonist effects at μ-receptors.
Substances chimiques
Narcotic Antagonists
0
Naltrexone
5S6W795CQM
Adrenocorticotropic Hormone
9002-60-2
Prolactin
9002-62-4
nalmefene
TOV02TDP9I
Hydrocortisone
WI4X0X7BPJ
Types de publication
Controlled Clinical Trial
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
e2726Subventions
Organisme : National Institutes of Health NIH-NCATS
ID : 5UL1TR001866-04
Pays : International
Organisme : NIH-NIDA
ID : RO1 DA018151
Pays : International
Informations de copyright
© 2020 John Wiley & Sons Ltd.
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