Related Experiment Video
Updated: May 31, 2026

14:56
An Experimental Paradigm for the Prediction of Post-Operative Pain (PPOP)
Published on: January 27, 2010
CYP2D6 polymorphisms and codeine analgesia in postpartum pain management: a pilot study
Sondra VanderVaart1, Howard Berger, Johanna Sistonen
1Department of Pharmaceutical Sciences, University of Toronto, Ontario, Canada.
Therapeutic Drug Monitoring
|July 12, 2011
Summary
Codeine
Area of Science:
- Pharmacogenomics
- Pain Management
- Postoperative Care
Background:
- Codeine is a common analgesic after cesarean section (c-section).
- Codeine metabolism varies significantly due to Cytochrome P450 enzyme 2D6 (CYP2D6) genetic variations.
- CYP2D6 ultrarapid metabolizers (UMs) convert more codeine to morphine, while poor metabolizers (PMs) convert very little.
Purpose of the Study:
- To investigate the association between CYP2D6 genotype and codeine's effectiveness for pain relief in women after c-section.
- To explore how genetic variations in CYP2D6 influence pain scores and the need for analgesia.
Main Methods:
- Collected blood samples for CYP2D6 genotyping from 45 mothers post-c-section.
- Monitored pain levels, codeine usage, and adverse events for three days.
- Estimated theoretical morphine dosage based on individual CYP2D6 genotype.
Main Results:
- Poor metabolizers (PMs) reported no pain relief from codeine.
- Ultrarapid metabolizers (UMs) experienced rapid pain relief but reported side effects like dizziness and constipation.
- Further research with larger cohorts is needed for intermediate metabolizer genotypes.
Conclusions:
- Extreme CYP2D6 genotypes (PMs and UMs) appear to predict codeine response and adverse events post-c-section.
- This pilot study highlights the potential of pharmacogenomics in tailoring postoperative pain management.
- Larger studies are required to establish genotype-phenotype correlations across the full spectrum of CYP2D6 metabolizers.
Related Concept Videos
Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes
Cytochrome P450 (CYP450) enzymes are a superfamily of heme-containing monooxygenases that play a pivotal role in Phase I drug metabolism by catalyzing oxidation and reduction reactions.These enzymes transform lipophilic xenobiotics into more hydrophilic metabolites, facilitating subsequent Phase II conjugation and eventual excretion. The CYP450 family is classified into families (e.g., CYP1–CYP3) and subfamilies (e.g., CYP2A, CYP2C), based on amino acid sequence homology.CYP450 isoenzymes,...
Opioid Analgesics: Synthetic and Semisynthetic Opioids
Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Opioid Analgesics: Morphine and Other Natural Cogeners
Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
Analgesia and Pain Management
Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Genetic variations significantly influence drug response through pharmacokinetics, receptor interactions, and biologic milieu modifications. Pharmacokinetic alterations impact drug metabolism and clearance, affecting efficacy and toxicity. Variants in drug-metabolizing enzymes, such as CYP2C9 and CYP2C19, alter drug activation and elimination. For example, CYP2C9 loss-of-function variants require lower warfarin doses to prevent excessive bleeding, while CYP2C19 variants reduce clopidogrel...
Pharmacogenetics of Drug Metabolism: Overview
Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...