期刊
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
卷 88, 期 3, 页码 1358-1364出版社
WILEY
DOI: 10.1111/bcp.15050
关键词
glutamate; magnetic resonance spectroscopy; opioid; oxycodone; tapentadol
资金
- Grunenthal GmbH
Research shows that both tapentadol and oxycodone can modulate the glutamatergic system at the supraspinal level in humans, leading to decreased glutamate/creatine levels in the brain regions studied.
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.
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