Combining an oral opioid-receptor agonist and the antagonist naloxone: A smart drug design that removes some but not all adverse effects of the opioid analgesic

Combining an oral opioid-receptor agonist and the antagonist naloxone: A smart drug design that... In the present issue of the Scandinavian Journal of Pain Sabine Hesselbarth and co-workers publish the results of a study from “real life” on the outcome of patients treated with a strong opioid of any kind, compared with oxycodone controlled released with naloxone added [1]. The rationale behind this combination is that naloxone taken by mouth is absorbed from the gastrointestinal tract into the portal circulation, but on first passage through the liver most of the naloxone (about 97–99%) is metabolized to inactive metabolites. The minute part of the naloxone that reaches the systemic circulation and crosses the blood–brain barrier is too small to precipitate any anti-analgesic effects.1Naloxone in depot-opioid tablets, binds to intestinal wall receptors in the entire GI-tractOn its passage through the GI-tract, the naloxone, gradually released from the controlled release oxycodone tablet, binds to opioid-receptors in the intestinal wall, reducing the effects of the opioid agonist on smooth muscle and secretory function of the intestinal wall. This co-administration of opioid agonist and antagonist is well documented to reduce the most common of the problematic adverse effects of opioids: the obstinate opioid-induced constipation [2,3].2Laxative regimens relieve opioid induced constipation, but not other opioid-induced dysfunctions in the GI-tractIt http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Scandinavian Journal of Pain de Gruyter

Combining an oral opioid-receptor agonist and the antagonist naloxone: A smart drug design that removes some but not all adverse effects of the opioid analgesic

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Publisher
De Gruyter
Copyright
© 2014 Scandinavian Association for the Study of Pain
ISSN
1877-8860
eISSN
1877-8879
D.O.I.
10.1016/j.sjpain.2014.02.004
Publisher site
See Article on Publisher Site

Abstract

In the present issue of the Scandinavian Journal of Pain Sabine Hesselbarth and co-workers publish the results of a study from “real life” on the outcome of patients treated with a strong opioid of any kind, compared with oxycodone controlled released with naloxone added [1]. The rationale behind this combination is that naloxone taken by mouth is absorbed from the gastrointestinal tract into the portal circulation, but on first passage through the liver most of the naloxone (about 97–99%) is metabolized to inactive metabolites. The minute part of the naloxone that reaches the systemic circulation and crosses the blood–brain barrier is too small to precipitate any anti-analgesic effects.1Naloxone in depot-opioid tablets, binds to intestinal wall receptors in the entire GI-tractOn its passage through the GI-tract, the naloxone, gradually released from the controlled release oxycodone tablet, binds to opioid-receptors in the intestinal wall, reducing the effects of the opioid agonist on smooth muscle and secretory function of the intestinal wall. This co-administration of opioid agonist and antagonist is well documented to reduce the most common of the problematic adverse effects of opioids: the obstinate opioid-induced constipation [2,3].2Laxative regimens relieve opioid induced constipation, but not other opioid-induced dysfunctions in the GI-tractIt

Journal

Scandinavian Journal of Painde Gruyter

Published: Dec 29, 2017

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