Differential tramadol and O‐desmethyl metabolite levels in brain vs. plasma of mice and rats administered tramadol hydrochloride orally

@article{Tao2002DifferentialTA,
  title={Differential tramadol and O‐desmethyl metabolite levels in brain vs. plasma of mice and rats administered tramadol hydrochloride orally},
  author={Qiu Tao and Dennis J. Stone and Michael R. Borenstein and Ellen E. Codd and Timothy P. Coogan and Daksha Desai-Krieger and Sha Liao and Robert B Raffa},
  journal={Journal of Clinical Pharmacy and Therapeutics},
  year={2002},
  volume={27}
}
  • Q. Tao, D. Stone, R. Raffa
  • Published 1 April 2002
  • Medicine
  • Journal of Clinical Pharmacy and Therapeutics
Objective: To investigate a possible differential brain uptake of tramadol vs. its major metabolite (O‐desmethyl tramadol; M1) in mice and rats. 
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40 Citations
Background Citations
21
Results Citations
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40 Citations

Citation Type

Citation Type

Regulation of cerebral CYP2D alters tramadol metabolism in the brain: interactions of tramadol with propranolol and nicotine
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The results suggest that the regulation of brain CYP2D by xenobiotics may cause drug–drug interactions (DDIs) of tramadol, and brain CYPs may play an important role in DDIs of centrally active substances.
Brain disposition, metabolism and behavioral effects of the synthetic opioid AH-7921 in rats
Uptake and Metabolism of Human Pharmaceuticals by Fish: A Case Study with the Opioid Analgesic Tramadol.
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The pharmacokinetic data of tramadol in fish help bridge the gap between widely available mammalian pharmacological data and potential effects on aquatic organisms and highlight the importance of understanding drug uptake and metabolism in fish to enable the full implementation of predictive toxicology approaches.
Lack of evidence for involvement of P-glycoprotein in brain uptake of the centrally acting analgesic, tramadol in the rat.
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It seems that the brain accumulation of tramadol is not affected by P-gp inhibition which implies that there may be some other transport mechanisms involved in BBB transport of tramadol.
Basic pharmacology relevant to drug abuse assessment: tramadol as example
  • R. Raffa
  • Medicine
    Journal of clinical pharmacy and therapeutics
  • 2008
TLDR
Its multimodal mechanism of action, pharmacologically active enantiomers, and active metabolite make it a particularly instructive and relevant example of a centrally acting analgesic.
Toxicity of Liver and Kidney Induced by Different Concentrations of Tramadol in Young and Adult Mice
TLDR
The infiltration of inflammatory cells and its aggregation were detected within the kidney and liver tissue of adult and young mice group that consumed TM, indicating Tramadol could have dangerous side effects even when its total dose doesn’t exceed 400mg daily.
Distribution, pharmacokinetics and primary metabolism model of tramadol in zebrafish.
TLDR
A simple and high throughput analytical procedure was developed and validated to determine the distribution and pharmacokinetic profiles of tramadol, and its primary metabolites in tissues of zebrafish.
Histopathological and Molecular Studies on Tramadol Mediated Hepato-Renal Toxicity in Rats
Tramadol, a broadly used opioid in recent years, is an effective analgesic agent for the treatment of moderately severe acute or chronic pain. The liver and kidneys are responsible for the metabolism…
Pharmacokinetics of tramadol and the metabolite O-desmethyltramadol in dogs.
TLDR
Simulated oral dosing regimens predict tramadol and M1 plasma concentrations consistent with analgesia in humans; however, studies are needed to establish the safety and efficacy of these doses.
Clinical Pharmacology of Tramadol
TLDR
Tramadol is an effective and well tolerated agent to reduce pain resulting from trauma, renal or biliary colic and labour, and also for the management of chronic pain of malignant or nonmalignant origin, particularly neuropathic pain.
...
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  • Q. Tao, D. Stone, R. Raffa
  • Chemistry
    Journal of chromatography. B, Biomedical sciences and applications
  • 2001
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