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Its principal metabolite, tapentadol-O-gluroronide has no activity on opioid tapentadol receptors, reuptake systems in synapses or other junctures .
Tramadol is metabolized almost tapentadol entirely by the enzyme of the P450, CYP26 cytochrome .
CYP2D6 gene mutations occur in approximately 1 to 7% of the Caucasian tapentadol population and can increase or decrease enzymatic activity and produce alterations of opioid analgesia .
Aside of the potential differences in individual responses to opioids metabolized by the P450 cytochrome there is a high-risk tapentadol of pharmacological interactions as some of the substrates of CYP2D6 are antiarrhythmic medications, antidepressants, antipsychotics anti-parasite medications and tamoxifen .
The analgesic activity of tramadol is affected by the inhibition of CYP2D6 as its analgesic effects are produced by its metabolite tapentadol not working nucynta rebate nucynta official website tapentadol presentacion tapentadol M1 (O-desmetiltramadol) In vitro studies to assess the inhibitory or inductor effects of tapentadol over the main seven isoforms of CYP implicated in the metabolism of medications (CYP2D6, CYP3A4, CYP1A2, CYP2A6, CYP2C9, CYP2C19 y CYP2E1) have revealed that tapentadol is not significantly metabolized by the CYP enzymes, and does not inhibit or induce the activity of any of the CYP isoforms assessed, except for the CYP2D6, which, however, is considered clinically irrelevant (12,24,26,41) .
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