• Jörn Lötsch.
• Institute of Clinical Pharmacology, Johann Wolfgang Goethe-University, Frankfurt, Germany. j.loetsch@em.uni-frankfurt.de
• Curr Opin Anaesthesiol. 2004 Oct 1;17(5):449-53.

Purpose Of ReviewMorphine metabolites have attracted continuing interest for their contribution to the desired and unwanted effects of morphine. Among the metabolites of morphine, morphine-6-glucuronide has been given most scientific attention. It accounts for 10% of the morphine metabolism, acts as an agonist at mu-opioid receptors and exerts antinociceptive effects. This review summarizes the recent findings on morphine-6-glucuronide and discusses its potential use as an analgesic.Recent FindingsMorphine-6-glucuronide has a very long delay between the time course of its plasma concentrations and the time course of its central nervous effects, with 6-8 h probably the longest transfer half-life between plasma and effect site of all opioids administered in humans. This complicates the control of morphine-6-glucuronide therapy when used as an intravenous analgesic, and the long duration of action confers no advantage over other opioids because long-lasting opioid analgesia can be readily obtained with sustained release formulations of other opioids. During acute treatment, however, morphine-6-glucuronide appears to be sufficiently potent to exert peripheral analgesic effects, without exerting major central nervous opioid side effects for a short period of time. The side effects profile does not clearly separate morphine-6-glucuronide from morphine, with reports of similar side effects. There are contrasting reports, however, about similar or less respiratory depression and other side effects compared with morphine after systemic injection.SummaryMorphine-6-glucuronide might qualify as an analgesic but it has several pharmacological properties that make it far from ideal for therapeutic use. Whether it will be a useful addition to the currently established analgesics has yet to be demonstrated.

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