Codeine Essay

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Codeine is naturally occurring opiate from the poppy plant and is an agonist of µ opioid receptors in the central nervous system, leading to analgesic effects. There are three other opioid receptors (delta, kappa, and the nociceptin orphanin peptide receptor). Opioids acting at the µ receptor have demonstrated significant decreases in pain (Fields, 2011). Codeine is typically prescribed as an oral medication to treat mild to moderate pain, such as cancer pain (Bernard et al., 2006). It is also used as a cough suppressant and as an antidiarrheal medication. Although the main effect of this drug is analgesia, side effects include respiratory depression, constipation, nausea, vomiting, skin rashes, and euphoria followed by dysphoria. In the present day, codeine is mainly synthesized by pharmacological companies and as a pro-drug of morphine. Most of the metabolites of codeine have similar affinities for the µ receptor, except for morphine and its metabolite, morphine-6-glucuronide (Caraco et al., 1996). Morphine has an affinity 200-fold higher to this receptor than codeine, which may help explain the addictive characteristic. Other opioids that act on this receptor include heroin and oxycodone, also having high addiction potential (Fields, 2011). Heroin is more potent than both codeine and morphine.
Like other weak organic bases, codeine is well absorbed from the gastrointestinal tract. However, much of the drug is excreted by the kidneys or undergoes clearance by the liver (Fig. 1). In the liver a large percent of the codeine is metabolized to codeine-6-glucuronide, a smaller percent undergoes nitrogen-demethylation and is converted to norcodeine, and an even smaller percent is metabolized to morphine via oxygen-demethylation (Chen...

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...rtant that tests are designed to address the issue. Examples of CYP2D6 assays available are the AmpliChip, the Luminex, and AutoGenomics. These assays test for common alleles in the population , therefore rare alleles can go unreported. The AmpliChip test uses about 240 probes to screen for 30 different alleles, including all of the ones mentioned above. Similarly, the Luminex array screens for 22 SNPs, representing 17 of the common alleles and the AutoGenomics assay screens for over 20 alleles (Lyon et al., 2012). When prescribing medications, doctors should be aware of an individual’s metabolism type in order to avoid toxicity or inefficient treatment. For instance, in the case of poor and ultra rapid metabolizers, codeine should not be administered. Instead, doctors should consider prescribing another opiate such as morphine, since it bypasses the CYP2D6 pathway.

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