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10 Cards in this Set
- Front
- Back
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What gene associated with redheads is aso associated with increased response to painful stimuli and decrease response to analgesics?
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MC1R
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What are the contrasting dynamics associated with administering Coumadin?
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Coumadin has a low therapeutic window and is metabolized by CYP2C9. The gene product it inhibits (VKORC1--encoudes for vitamin K epoxide) is responsible for pharmacodynamic properties. So for people with deficient forms of CYP2C9 and a low-dose haplotype of VKORC1 (or other combinations), it can be difficult to predict proper dosing levels.
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Which gene codes for a protein that is important for converting the prodrug codeine into morphine?
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CYP2D6. About 5-10% of Caucasians are poor metabolizers of Codeine (80 to 90% of total poor metabolizers). Multiple copies of this gene can also occur leading to ultrarapid metabolizers.
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If someone is a poor metabolizer of Codeine, what other considerations may be relevant with other medications?
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CYP2D6, the gene product from Xsome 22 that metabolizes protein is a high-affinity, lowcapcity enzyme. People receiving medications such as tricyclic antidepressants, SSRIs, beta blocker, antipsychotics, tamoxifen, tramadol, and hydrocodone should be aware of potential drug interactions.
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What phase II enzyme (from Xsome 4) conjugates codeine and morphine for elimination?
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UGT2B7 glucuronidates morphine to M6G (very analgesic) and M3G (anti-analgesic). Polymorphisms have been noted in Caucasians and the Japanese.
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What efflux transporter has polymorphisms that limit pumping of morphine out of the CNS leading to a greater analgesic effect?
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ABCB1 (polymorphism is a SNP C3435T). It can also be upregulated in chronic use.
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What receptor mutation can lead to a decreased efficacy of morphine?
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Variability in the mu opiod receptor (MOR1) can lead to greater binding of endogenous opiods such as beta-endorphin, lessening the response to morphine.
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What genetic polymorphism leads to a greater increase in pain sensitivity (and anxiety) due to a deficient breakdown of catecholamines?
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Catecholamine-O-methyltransferase (COMT)--a gene product from Chromosome 22. Most common SnP is val158met. Can also affect chronic pain.
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What happens in a knee injury that allows for a response to morphine during chronic inflammation?
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Mu-opioid receptors are not normally present in the knee joint, but under states of chronic inflammation they will be expressed and transported to the joint after a few weeks.
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What immune response system has associated polymorphisms that are important in the management of pain?
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Interleukin-1 is an initial induce or a proinflammatory state. IL-1A (IL-1 receptor antagonist) is an antagonist that downregulats IL-1alpha and beta. People with higher IL1-RA levels need less morphine.
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