2013
DOI: 10.1517/17425255.2013.779669
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Contribution of oxycodone and its metabolites to the overall analgesic effect after oxycodone administration

Abstract: This article's calculations demonstrate that OC itself is responsible for the analgesic effect. Although OM and noroxymorphone have much higher µ-receptor affinity than the parent drug, the metabolite concentrations at the site of action are very low. This suggests that there is a minimal analgesic effect from these metabolites.

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Cited by 47 publications
(35 citation statements)
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“…This variant affects about 3% of northern Europeans, 5 to 10% of southern Europeans, 1 to 2 % of Asians, and 10 to 30% of individuals from Arabian and northeast African countries [168]. However, it appears that oxycodone is unlikely to result in this reaction [169,170]. In addition to affecting the mother, opioids can result in sedation of the breastfed infant [171][172][173].…”
Section: Dopaminergicsmentioning
confidence: 99%
“…This variant affects about 3% of northern Europeans, 5 to 10% of southern Europeans, 1 to 2 % of Asians, and 10 to 30% of individuals from Arabian and northeast African countries [168]. However, it appears that oxycodone is unlikely to result in this reaction [169,170]. In addition to affecting the mother, opioids can result in sedation of the breastfed infant [171][172][173].…”
Section: Dopaminergicsmentioning
confidence: 99%
“…More recently, Klimas and coworkers [46] demonstrated that OC itself is responsible for its analgesic effects. They found that although OCM and NOM have much higher affinity than OC for the μ‐opioid receptor, the OCM and NOM metabolite concentrations at the site of action are very low.…”
Section: Discussionmentioning
confidence: 99%
“…Oxycodone is eliminated by hepatic metabolism . While oxycodone has three pharmacologically active metabolites (oxymorphone, noroxymorphone, and noroxycodone), the parent drug appears to be the source of its analgesic effects . Intrathecal but not systemic administration of noroxymorphone may have analgesic effect .…”
Section: Oxycodone Pharmacologymentioning
confidence: 99%