The FDA has approved tramadol hydrochloride extended-release (Ryzolt – Purdue) for treatment of moderate to moderately severe chronic pain in adults. Tramadol is already available in another extended-release formulation (Ultram ER) and in immediate-release tablets alone (Ultram, and others) and combined with acetaminophen (Ultracet, and others).

ANALGESIC ACTIVITY — Tramadol is a weak opioid agonist that also inhibits serotonin and norepinephrine reuptake; it is not scheduled as a controlled substance by the FDA. Tramadol 100 mg is about as effective for pain as aspirin 650 mg plus codeine 60 mg.1

PHARMACOKINETICS — Tramadol is converted by CYP2D6 to an active metabolite, O-desmethyltramadol, which has a much higher affinity than the parent drug for mu-opioid receptors. Studies in healthy volunteers found that serum concentrations ... more      

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