PHRD5915 Drug Design - Winston Lectures Review

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daynuhmay
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265403
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PHRD5915 Drug Design - Winston Lectures Review
Updated:
2014-03-07 04:19:43
Tags:
adme phasei phaseii cyp450
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drug design
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  1. pharmacokinetic phase of drug action
    ADME
  2. pharmacodynamic phase of drug action
    pharmacological & toxicological effects (interactions w/ biological targets)
  3. how most drugs pass through lipid membranes for absorption & distribution to occur
    passive diffusion
  4. 2 requirements for most drugs to pass through lipid membranes
    • 1) drugs must have lipophilicity
    • 2) concentration gradient
  5. faces outside of lipid bilayers
    polar, hydrophilic heads
  6. faces inside of lipid bilayers
    nonpolar, hydrophobic fatty acid tails
  7. saturated or unsaturated tails increase fluidity
    unsaturated
  8. 4 factors controlling drug distribution
    • 1) size
    • 2) lipophilicity/hydrophilicity
    • 3) polarity
    • 4) ionic state (pKa)
  9. imine
  10. toxic metabolite of APAP
    N-acetyl-p-benzoquinone imine (NAPQI)
  11. Phenol2.svg
    phenol
  12. ester
  13. carbonyl
  14. carboxylic acid
  15.  or 
    aldehyde
  16. ether
  17. ketone
  18. amide
  19. pH > pKa
    deprotonated
  20. pH < pKa
    protonated
  21. carboxylic acid + alcohol
    ester + H2O
  22. carboxylic acid + amine
    amide + H2O
  23. thiol

    (important fcnal group in cysteine)
  24. sulfide
  25. sulfoxide
  26. sulfone
  27. sulfonic acid
  28. Henderson-Hasselbalch Equation
    pH = pKa - log([HA]/[A-])
  29. [A-] > [HA]
    non-ionized
  30. e- withdrawing groups in R ____ (raise/lower) pKa
    lower

    (weaken the base)
  31. e- donating groups in R ____ (raise/lower) pKa
    raise

    (make a stronger base)
  32. substrate binds close to P450 heme. spectrum?
    Type 1 

    (high @ 410nm)
  33. substrate binds directly to P450 heme. spectrum?
    Type II

    (high @ 440nm)
  34. where does P450 get its electrons?
    from NADPH via CYP450 reductase
  35. biotransformation
    changes properties of a xenobiotic from lipophilic to hydrophilic
  36. characteristics of Phase I products (2)
    • 1) inactivation
    • 2) conversion of active drug to another active one
  37. example of Phase 1 conversion of an active drug to another active drug
    codeine, heroine -> morphine
  38. 4 compartments alcohol detoxification takes place in
    • 1) microsomes (CYP2E1)
    • 2) cytosol (ADH)
    • 3) mitochondria (ALDH)
    • 4) peroxisomes (catalase)
  39. products of CCl4 breakdown (4)
    • 1) carbon monoxide
    • 2) carbon dioxide
    • 3) phosgene
    • 4) HCl
  40. coupling of reduction of H2O2 & lipid hydroperoxides to the oxidation of other substances
    cooxidation

    (used by peroxidases, instead of using NADPH or NADH)
  41. universal sulfonate donor for all sulfotransferase reactions
    PAPS (3'phosphoadenosine-5'phosphosulfate)
  42. APS + ATP =
    PAPS

    (sulfation reaction)
  43. sulfotransferase + PAPS =
    PAP

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