Biotransformation

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Author:
phxtopher
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102084
Filename:
Biotransformation
Updated:
2011-09-16 04:13:47
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Biotransformation
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Biotransformation
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  1. biotransformation reactions are significant
    because
    • they are often the first step in eliminating drugs
    • from the body
  2. Enzymes are also responsible for
    Metabolism or biotransformation
  3. xenobiotics
    • The metabolism (biotransformation) of foreign drugs
    • from the body
  4. What are the 2 primary ways drugs are excreted
    from the body?

    2
    1.) Urine/Feces --> Unexcreted

    2.) Metabolized/biotransformed then excreted
  5. What are other ways that drugs can be excreted
    after being metabolized or biotransformed?

    2
    Sweating

    Respriation
  6. Most drugs are biotransformed when and why
    prior to excretion because they are not polar enough

    ie not water soluble enough
  7. What is the major object of biotransformation?
    • Make non polar drugs more polar to be more readily
    • excreted
  8. Drugs are biotransformed by what
    Enzymes
  9. The products of biotransformation results in
    what
    • a compound that is less active or inactive that
    • the parent drug
  10. Biotransformation makes a drug more soluble or
    less soluble?
    Makes the drug more soluble for excretion
  11. After biotransformation what is produced that is
    no longer of therapeutic value
    a metabolite
  12. Prodrugs
    • the biotransformation creates the metabolite that
    • produces the therapeutic response
  13. Prodrugs
    Biotransformation produces the active drug
  14. Where does biotransformation primarily occur
    in the liver, but other places as well
  15. 1.
    Other
    places biotransformation can occur

    KGSL
    o Kidneys

    o GI Tract

    o Skin

    o Lungs
  16. How are drugs ingected orally entered into the
    bloodstream?
    Absorbed in the GI Tract to enter the bloodstream
  17. What is the primary organ for biotransformation
    the liver
  18. How are drugs transported to the liver
    hepatic portal vein
  19. Once the drugs are absorbed into the
    bloodstream, are the drugs directly or indirectly delivered to the liver and
    how
    directly delivered

    via the hepatic protal vein
  20. First pass effect
    • the percentage loss of how much a drug is loss due to
    • absorption into the GI tract
  21. Possible Pathways of Elimination for a Drug
    1) excreted unchanged,

    • 2) biotransformed (structurally
    • modified) to metabolites that are:
    • a) excreted
    • b) further biotransformed.
  22. Prodrugs take advantage of what to produce a
    therapeutic effect
    the metabolism
  23. Prodrugs are the same or different as drugs
    the same, just use metabolism to produce effect
  24. Only between prodrugs and drugs
    prodrugs are activated by the metabolic process
  25. 1.
    Properities
    of Metabolites

    PHIL
    • Polar
    • Hydrophilic
    • Inactive
    • Less Active
  26. Drugs are AKA
    Xenobiotics
  27. heme-containing membrane proteins
    cytochrome P450 enzymes
  28. cytochrome P450 enzymes are found in high
    concentrations where
    the liver
  29. 1.
    cytochrome
    P450 enzymes are found in lower concentrations where?

    BLIK
    • Brian
    • Lungs
    • Intestine
    • Kidneys
  30. most important enzymes for drug metabolism are
    cytochrome P450 monooxygenases
  31. 1.
    cytochrome
    P450 are capable of catalyzing what type of reactions

    7
    • Aromatic and aliphatic hydroxylations
    • N-, O-, and S- dealkylation
    • N-oxidation
    • Sulfoxidation
    • N-hydroxylation
    • Deamination
  32. CYP 450 interactions generally result from what
    of two processes

    II
    Induction

    Inhibition
  33. Induction
    a drug stimulates the synthesis of the enzyme OR

    • reduces its degradation and the metabolic capacity for the isoenzyme is
    • increased
  34. reduces its degradation and the metabolic
    capacity for the isoenzyme is increased
    Induction

    1 of the 2 processes of P450 Enzyme
  35. Inhibition
    Competitive binding at an enzyme's binding sites(s)

    • A drug with a high affinity for an enzyme with SLOW the
    • metabolism of any low affinity drug that produces a particular enzyme
  36. A drug with a high affinity for an enzyme with SLOW the metabolism of any low affinity drug that produces a particular enzyme
    Inhibition
  37. designed to take advantage of absorption or
    metabolic properties to provide more optimal drug therapy
    Prodrugs
  38. Prodrugs
    • designed to take advantage of
    • absorption or

    • metabolic properties to provide
    • more optimal drug therapy
  39. an inactive compound that is administered and
    then transformed into an active substance by either chemical or metabolic means
    Prodrugs
  40. designed to take advantage of absorption or
    metabolic properties to provide more optimal drug therapy
    Prodrugs
  41. Prodrugs
    • designed to take advantage of
    • absorption or

    • metabolic properties to provide
    • more optimal drug therapy
  42. Biotransformation Reactions are broken into what
    two groups
    Phase I Rxns

    Phase II Rxns
  43. Phase I rxns are
    Functionalization Rxns
  44. How do Phase I rxns work?
    make a compound more hydrophilic

    by introducing or exposing a polar functional group
  45. reactions that introduce or expose a functional
    group on a compound
    Phase I Rxns
  46. Phase I Rxns
    reactions that introduce or expose a functional group on a compound
  47. in some cases, these reactions enhance or retain
    the activity of the parent compound.
    Phase I Reactions
  48. biosynthetic reactions
    Phase II Rxns
  49. result in covalent linkage between a functional group on the parent drug and a highly polar conjugate.
    Phase II Rxns

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