| Morphine in postoperative patients: pharmacokinetics and pharmacodynamics of metabolites. | |
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MedLine Citation:
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PMID: 17578959 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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BACKGROUND: There is great variability in the need for morphine in the postoperative period. We performed a pharmacokinetic-pharmacodynamic study considering the potential effect of the two main metabolites of morphine. METHODS: Fifty patients with moderate to severe pain received morphine as an IV titration, followed by IM administration postoperatively. The plasma concentration of morphine, morphine-6-glucuronide (M-6-G), morphine-3-glucuronide (M-3-G), and pain intensity were measured at frequent intervals. Pharmacokinetic and pharmacodynamic fitting was performed with the software NONMEM. RESULTS: The pharmacokinetics were largely predictable. M-6-G and M-3-G clearances were markedly decreased in patients with renal failure. The pharmacodynamics was less predictable, with an important interindividual variability. M-6-G was 7.8 times more potent than morphine, but the average time to peak concentration in the effect compartment after a bolus injection of morphine was 4.25 h for M-6-G, when compared to 0.33 h for morphine. M-3-G showed mild inhibition of the analgesic properties of morphine and of M-6-G. The time to M-3-G peak concentration in the effect compartment after a bolus injection of morphine was 10 h. CONCLUSIONS: M-6-G is a potent opioid agonist and M-3-G a mild opioid antagonist. Both are poorly excreted in patients with renal failure. However, the metabolism of morphine was rapid when compared to the transfer of metabolites through the blood-brain barrier, which appears to be the limiting process. Because poor analgesia due to M-3-G's effect may occur in some patients after 1 or 2 days, a switch to other molecules should be considered. |
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Authors:
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Jean Xavier Mazoit; Karin Butscher; Kamran Samii |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Anesthesia and analgesia Volume: 105 ISSN: 1526-7598 ISO Abbreviation: Anesth. Analg. Publication Date: 2007 Jul |
Date Detail:
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Created Date: 2007-06-20 Completed Date: 2007-07-19 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 1310650 Medline TA: Anesth Analg Country: United States |
Other Details:
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Languages: eng Pagination: 70-8 Citation Subset: AIM; IM |
Affiliation:
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Univ Paris-Sud, Laboratoire d'Anesthésie UPRES 3540, Faculté de Médecine, Le Kremlin Bicêtre, France. jean-xavier.mazoit@u-psud.fr |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adult Aged Female Humans Male Metabolic Networks and Pathways / drug effects, physiology Middle Aged Morphine / metabolism*, pharmacology*, therapeutic use Morphine Derivatives / metabolism Pain, Postoperative / drug therapy, metabolism Postoperative Period* |
| Chemical | |
Reg. No./Substance:
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0/Morphine Derivatives; 20290-09-9/morphine-3-glucuronide; 20290-10-2/morphine-6-glucuronide; 57-27-2/Morphine |
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