GEN #30 & 31 Phase I Drug Metabolism

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  1. Pharmacogenomics allows for the individualization of drug treatment by assessing the potential that a drug agent will be efficacious due to ______ considerations and prevent toxicities due to _____ considerations
    • PD
    • PK
  2. Biotransformation via the_______ represents one of the most common elimination mechanisms
    cytochrome P450s
  3. 15-30% of the most commonly used drugs are metabolized by the _______ isoform alone
  4. Tamoxifen is metabolized by 9 CYP isoforms, as well as the ______________
    flavin monooxygenase
  5. _____________ reduces excess superoxide anion
    Superoxide dismutase
  6. Oxygen binds to CYP via a __________________________
    non-covalent iron-protoporphyrin IX ring (heme)
  7. ________________ compares evolution of different families across species
    phylogenic tree
  8. What organ contains the most diverse array of CYP450 proteins
  9. The CYP4B1 isoform is located in which tissue
  10. In what tissue is the CYP4F8 isoform located
  11. CYP11A, 11B1, 11B2 isoforms are found in the
    adrenal glands
  12. The CYP24 isoform is located where
  13. Which CYP isoform preferentially binds polar heterocyclic compounds and aryl amines
  14. The majority of the CYPs expressed on the intestines & liver belong to which sub-family
  15. Gene sequence changes shown in CYP450 genes that impact enzymatic activity
    Phenotypic Variation
  16. The phenotype that has no function alleles present
    poor metabolizer
  17. The phenotype that has either one funtionsl and one mutant/deficient allele or two partially active/deficient alleles present
    intermediate metabolizer
  18. The phenotype that has either 2 active alleles or a combination of one active and one partially active allele present
    extensive metabolizer
  19. The phenotype that has 3 or more active alleles present
    ultrarapid metabolizer
  20. Which phenotypic metabolizer should be able to achieve therapeutic effects at normal dosing?
    (I know this is poorly worded)
    extensive metabolizer
  21. What non-CYP450 super family of phase I enzymes are expressed in the liver, intestines, and ER membranes
    flavin monooxygenase
  22. What is an alternative to genotyping CYP450 alleles
  23. The assays for phenotyping are based on the ________ of substrate drugs that have been labeled with a stable or radioactive carbon
  24. What substrate is used for a CYP3A4 breath test
  25. What substrate is used for a CYP1A2 breath test
  26. What substrate is used for a CYP2C19 breath test
  27. erythromycin will undergo ____________ by CYP3A4
  28. CYP1A2 is aslo known as
    Aryl hydrocarbon hydroxylase
  29. CYP2D6 aka
    debrisoquine/sparteine hydroxylase
  30. CYP2C19 aka
    S-mephenytoin hydroxylase
  31. Smoking has what effect on CYP1A2
  32. theophylline, clozapine, & olanzapine are metabolized by which CYP
  33. clopidogrel, proton pump inhibitors, and phenytoin are metabolized by which CYP
  34. phenytoin, warfarin, and sulfonylureas are metabolized by which CYP
  35. bupropion, cyclophosphamide, methadone, & nevirapine are metabolized by which CYP
  36. What is the most frequent allele of the CYP2B6 isoform
  37. Mutant alleles generally have _________ catalytic activity of the expressed protein
  38. Preferential substrates of CYP2C9 are _______ compounds having 1 or more ____________
    • weakly acidic
    • aromatic rings
  39. Patients with the poor metabolizer alleles will show a 5X greater instance of _________ upon starting an oral sulfonylurea antihyperglycemic agent.
  40. Ultra-rapid metabolizers will have _____________ levels of the oral sulfonylurea antihyperglycemic agents
  41. The FDA recommends _____ & _____ genotyping for warfarin
    • CYP2C9
    • VKORC1
  42. CYP2C19 is also know as
    S-mephenytoin hydroxylase
  43. Beta blockers are deactivated by CYP2D6 therefore which phenotype would result in a higher risk for therapeutic failure
    ultra-rapid metabolizer
  44. Poor metaboliazer alleles for CYP2C19 are
    *2 & *3
Card Set
GEN #30 & 31 Phase I Drug Metabolism
GEN #30 & 31 Phase I Drug Metabolism
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