Tapentadol and oxycodone reduce cingulate glutamate in healthy volunteers.
glutamate
magnetic resonance spectroscopy
opioid
oxycodone
tapentadol
Journal
British journal of clinical pharmacology
ISSN: 1365-2125
Titre abrégé: Br J Clin Pharmacol
Pays: England
ID NLM: 7503323
Informations de publication
Date de publication:
03 2022
03 2022
Historique:
revised:
30
06
2021
received:
18
02
2021
accepted:
03
07
2021
pubmed:
25
8
2021
medline:
27
4
2022
entrez:
24
8
2021
Statut:
ppublish
Résumé
Tapentadol and oxycodone are commonly used analgesics. Preclinical studies have shown that oxycodone modulates brain metabolites related to opioid pathways, whereas tapentadol also affects noradrenergic activity. However, knowledge about the function of the medications in the human brain is limited. The aim was to investigate effects of tapentadol and oxycodone on brain glutamate, the most important neurotransmitter in pain processing. Magnetic resonance spectroscopy was obtained in 21 healthy subjects from the anterior cingulate cortex, prefrontal cortex, and insula at baseline and after 14 days of treatment with either 50 mg tapentadol, 10 mg oxycodone (equipotent dose, both extended release) or placebo twice daily in a randomized double-blind cross-over study. Compared to baseline, decreased glutamate/creatine levels were identified in anterior cingulate cortex after tapentadol (1.26 ± 0.14 vs. 1.35 ± 0.18, P = .04) and oxycodone (1.26 ± 0.10 vs. 1.35 ± 0.12, P = .05) treatments, both with 7% reduction. This indicates that both analgesics modulate the glutamatergic system at the supraspinal level in humans.
Substances chimiques
Analgesics
0
Analgesics, Opioid
0
Phenols
0
Glutamic Acid
3KX376GY7L
Oxycodone
CD35PMG570
Tapentadol
H8A007M585
Types de publication
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1358-1364Informations de copyright
© 2021 British Pharmacological Society.
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