Codeine, Potentially Unpredictably Lethal

Frequently used in the pediatric population, codeine is a narcotic analgesic in prodrug form.  In the body, codeine is metabolized to morphine through the CYP2D6 pathway.  In the general population, it is estimated that approximate 10% of codeine undergoes conversion to morphine.

We’re generally familiar with the concept that a certain percentage of the population is ineffective at metabolizing codeine, and therefore receives no additional analgesic effect.  However, the flip side, as these authors report, is a CYP2D6 genotype of over-metabolizers.  In this case series, the over-metabolism of codeine in three post-surgical children likely resulted in supra-therapeutic conversion to morphine, leading to respiratory arrest.

The short summary – when possible, avoid medications that are unpredictably metabolized – such as codeine.

“More Codeine Fatalities After Tonsillectomy in North American Children”
www.ncbi.nlm.nih.gov/pubmed/22492761

2 thoughts on “Codeine, Potentially Unpredictably Lethal”

  1. CYP2D6, I believe. Wonder how common a duplicate cyp2D6 gene is? Any idea?
    Mary Shue, ED RPh
    University of Michigan Health System

  2. Aha, you found a typo! – now corrected.

    Regarding the CYP2D6 variability, I have copied and pasted directly from Wikipedia:
    "Ethnicity is a factor in the occurrence of CYP2D6 variability. The prevalence of CYP2D6 poor metabolizers is approximately 6–10% in white populations, but is lower in most other ethnic groups such as Asians (2%).[6] In blacks, the frequency of poor metabolizers is greater than for whites.[7] The occurrence of CYP2D6 ultrarapid metabolisers appears to be greater among Middle Eastern and North African populations.[8]

    This variability is accounted for by the differences in the prevalence of various CYP2D6 alleles among the populations–approximately 10% of whites appear to have the non-functional CYP2D6*4 allele,[5] while approximately 50% of Asians possess the CYP2D6*10 allele,[5] which should produce decreased CYP2D6 function; however this still appears to be within the normal range and are still grouped as intermediate metabolisers."

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