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Updated: Jun 22, 2026

High-throughput and Comprehensive Drug Surveillance Using Multisegment Injection-Capillary Electrophoresis-Mass Spectrometry
Published on: April 23, 2019
Opioid metabolism
1Department of Anesthesiology, Albany Medical College, Albany, NY 12208, USA. smithh@mail.amc.edu
Abstract:
Clinicians understand that individual patients differ in their response to specific opioid analgesics and that patients may require trials of several opioids before finding an agent that provides effective analgesia with acceptable tolerability. Reasons for this variability include factors that are not clearly understood, such as allelic variants that dictate the complement of opioid receptors and subtle differences in the receptor-binding profiles of opioids. However, altered opioid metabolism may also influence response in terms of efficacy and tolerability, and several factors contributing to this metabolic variability have been identified. For example, the risk of drug interactions with an opioid is determined largely by which enzyme systems metabolize the opioid. The rate and pathways of opioid metabolism may also be influenced by genetic factors, race, and medical conditions (most notably liver or kidney disease). This review describes the basics of opioid metabolism as well as the factors influencing it and provides recommendations for addressing metabolic issues that may compromise effective pain management. Articles cited in this review were identified via a search of MEDLINE, EMBASE, and PubMed. Articles selected for inclusion discussed general physiologic aspects of opioid metabolism, metabolic characteristics of specific opioids, patient-specific factors influencing drug metabolism, drug interactions, and adverse events.
Insights
Patient response to opioid analgesics varies due to differences in metabolism. Understanding opioid metabolism factors is key to effective pain management and minimizing adverse drug interactions.
Area of Science:
- Pharmacology
- Pain Management
- Drug Metabolism
Background:
- Individual patient responses to opioid analgesics vary significantly.
- Factors influencing opioid response include genetic variations and receptor binding profiles.
- Altered opioid metabolism is a key contributor to variability in efficacy and tolerability.
Purpose of the Study:
- To review the fundamentals of opioid metabolism.
- To identify factors influencing opioid metabolic variability.
- To provide recommendations for managing metabolic issues in pain management.
Main Methods:
- Literature search of MEDLINE, EMBASE, and PubMed.
- Inclusion of articles discussing opioid metabolism physiology, drug characteristics, patient factors, interactions, and adverse events.
Main Results:
- Opioid metabolism is influenced by enzyme systems, genetic factors, race, and medical conditions (liver/kidney disease).
- Drug interaction risk is determined by the metabolizing enzyme systems of opioids.
- Metabolic variability impacts both the effectiveness and tolerability of opioid analgesics.
Conclusions:
- Understanding opioid metabolism is crucial for optimizing pain management.
- Addressing metabolic variability can improve analgesic efficacy and patient tolerability.
- Recommendations are provided to guide clinicians in managing opioid metabolism-related challenges.
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