Review Note

Last Update: 01/30/2025 05:17 PM

Current Deck: A Villanova CRNA::Advanced Pharmacology Class::Exam 1

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Pharmacokinetic changes
  • Pseudocholinesterase deficiency can be caused by mutations in the BCHE (butrylcholinesterase) gene. 
    • Defects in this enzyme alters the metabolism of choline ester drugs like {{c1::succinylcholine}} or procaine;
  • there are examples of BCHE genetic disorders in which this enzyme is absent or defective and a patient’s sensitivity to succinylcholine become exaggerated (duration of action is extended from 5 minutes to {{c1::8 hours}})

Pharmacogenetics of CYPs is complex and can be a major cause of biological variation in drug responses in the human population   
  • Patients with variants in the gene that codes for CYP2D6 experience reduced benefits of tamoxifen that is used in the treatment of  breast cancer.
  • In order to be effective, tamoxifen is metabolized to its active form endoxifen by CYP2D6.  Women with an inherited deficiency in this enzyme receive minimal benefit from tamoxifen and they are 9.5 times more likely to experience a recurrence of cancer than effective metabolizers that have a normal form of CYP2D6. 
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So CYP variations could mean different things for different drugs

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