Tramadol is a centrally acting opioid analgesic, used in treating moderate to severe pain. Tramadol possesses weak agonist actions at the μ-opioid receptor, releases serotonin, and inhibits the reuptake of norepinephrine. Tramadol undergoes hepatic metabolism, being O- and N- demethylated to five different metabolites. Of these, O-desmethyltramadol is the most significant. Approximately 30% of the dose is excreted in the urine as unchanged drug, whereas 60% of the dose is excreted as metabolites, the remainder is excreted either as unidentified or an unextractable metabolites.
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