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Comparative study of the neurotoxicological effects of tramadol and tapentadol ...

Faria, J; Barbosa, J; Queiros, O; Moreira, R; Felix Carvalho; Ricardo Jorge Dinis Oliveira

Opioid therapy and abuse are increasing, justifying the need to study their toxicity and underlying mechanisms. Given opioid pharmacodynamics at the central nervous system, the analysis of toxic effects in neuronal models gains particular relevance. The aim of this study was to compare the toxicological effects of acute exposure to tramadol and tapentadol in the undifferentiated human SH-SY5Y neuroblastoma cell...


Comparative metabolism of tramadol and tapentadol: a toxicological perspective

Barbosa, J; Faria, J; Queiros, O; Moreira, R; Felix Carvalho; Ricardo Jorge Dinis Oliveira

Tramadol and tapentadol are centrally acting, synthetic opioid analgesics used in the treatment of moderate to severe pain. Main metabolic patterns for these drugs in humans are well characterized. Tramadol is mainly metabolized by cytochrome P450 CYP2D6 to O-desmethyltramadol (M1), its main active metabolite. M1 and tapentadol undergo mainly glucuronidation reactions. On the other hand, the pharmacokinetics of...


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