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Polymorphic CYP2D6 mediates O-demethylation of the opioid analgesic tramadol

  • PHARMACOKINETICS AND DISPOSITION
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Abstract

Objective: This study was designed to investigate whether the in vivo metabolism of tramadol was influenced by CYP2D6 polymorphism. Methods: The extent of tramadol O- and N-demethylation was calculated by determining the amounts of tramadol and O- and N-desmethyltramadol in 24 h urine after ingestion of a test dose of tramadol. The O- and N-demethylation rates were calculated by dividing the 24-h urinary excretion amount of tramadol by that of O-and N-desmethyltramadol. Volunteers were phenotyped for CYP2D6 polymorphism using sparteine as an in vivo probe. Results and conclusion: High correlation was found between tramadol-O-demethylation and sparteine oxidation in 71 extensive metabolizers of sparteine (r s= 0.544). The mean metabolic ratio of tramadol O-demethylation was significantly higher in poor metabolizers of sparteine than in extensive metabolizers (4.4 vs 0.8). These in vivo results confirm that tramadol O-demethylation is carried out to a large extent by the polymorphic CYP2D6.

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Received: 9 January 1997 / Accepted in revised form: 23 July 1997

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Paar, W., Poche, S., Gerloff, J. et al. Polymorphic CYP2D6 mediates O-demethylation of the opioid analgesic tramadol. E J Clin Pharmacol 53, 235–239 (1997). https://doi.org/10.1007/s002280050368

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  • DOI: https://doi.org/10.1007/s002280050368

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