Jun 2, 2020

ADME and toxicity considerations for tramadol: from basic research to clinical implications

Expert Opinion on Drug Metabolism & Toxicology
Mohsen Doostmohammadi, Hamid-Reza Rahimi


Tramadol is widely used in chronic pain management for improving patients' quality of life and reducing trauma. Although it is listed in several medicinal guidelines, its use is controversial because of the conflicting results obtained in pharmacokinetic/pharmacodynamic studies. It is a multi-receptor targeting drug which acts as a µ1 opioid receptor agonist, monoamine reuptake inhibitor, and inhibitor of ligand gated ion channels and some special protein-coupled receptors. This review provides a comprehensive view on the pharmacokinetic, pharmacodynamic, and toxicity of tramadol with a deep look on its side effects, biochemical and pathological changes, and possible drug interactions. In addition, the main ways of tramadol poisoning management are described according to in vivo and clinical trial studies. Given the broad spectrum of targets, an increase in the cases of overdoses and toxicity, and probable interaction with other drugs, it is necessary to take another look at the pharmacology of tramadol. Regarding the adverse effects of tramadol on different tissues, especially the nervous system and liver tissue, more attentions to tramadol and its metabolites, their interaction with other drugs, and active agents seems critic...Continue Reading

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Mentioned in this Paper

Pain Management
Nervous System Structure
Clinical Research
Pharmacologic Substance
Administration Procedure
G-Protein-Coupled Receptors

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