PHRD5915 Drug Design Lecture 2 - ADME

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daynuhmay
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PHRD5915 Drug Design Lecture 2 - ADME
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2014-02-14 12:30:02
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ADME
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ADME
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  1. pharmacokinetic phase of drug action
    ADME
  2. pharmacodynamic phase of drug action
    pharmacological & toxicological effects
  3. MW of most drugs
    100-1000 Daltons
  4. most common route of drug absorption
    passive diffusion
  5. IUPAC definition of lipophilic
    having an affinity for fat and high lipid solubilty
  6. what lipophilicity correlates with
    bioaccumulation
  7. a measure of lipophilicity
    relative solubility of a substance in water and an organic solvent (water-immiscible)
  8. important property of a drug that influences passive transport across cell membranes
    lipophilicity
  9. after oral administration, what must a drug first do?
    dissolve in the aqueous phase of the stomach
  10. for absorption & distribution to occur, what must drugs do?
    pass through lipid membranes to move between compartments
  11. alternative mechanisms for absorption/distribution (2)
    • 1) pass through pores in membranes (small molecules)
    • 2) membrane transporters
  12. factors controlling drug distribution (4)
    • 1) size
    • 2) lipophilicity/hydrophobicity
    • 3) polarity
    • 4) ionic state (pKa)
  13. partition coefficient
    • ratio of drug in the organic layer vs drug in the aqueous layer
    • (drug in organic layer)/(drug in aqueous layer)
  14. P>1
    increasing lipophilicity
  15. P<1
    decreasing lipophilicity
  16. phospholipid structure
    polar head group, hydrocarbon (apolar lipid) tail
  17. why lipophilic/hydrophobic groups are more soluble in organic solvents
    hydrocarbons can't bind to water
  18. most drugs are ____ (weak/strong) acids/bases that partially ionize when dissolved in water
    weak
  19. protonation status if:
    pH>pKa
    deprotonated
  20. protonation status if:
    pH<pKa
    protonated
  21. proton donor in a reaction
    acid
  22. affects the proportion of molecular and ionized forms of the drug
    pH of the aqueous solution
  23. distribution constant is dependent on...
    pH
  24. when logD=logP
    range in which distribution is NOT pH dependent
  25. decreasing pH = _____ molecular drug form and _____ ionized drug form in water
    increasing; decreasing
  26. decreasing P = ____ solubility in H2O
    increasing
  27. imine vs amine
    N is double bonded
  28. esterification
    carboxylic acid + ROH -> ester + H2O
  29. reverse reaction of esterification
    hydrolysis
  30. amidation
    carboxylic acid + RNH2 -> amide + H2O
  31. reverse reaction of amidation reaction
    hydrolysis
  32. R-SH
    thiol
  33. R-S-R
    sulfide
  34. R-S=O
       |
       R'
    sulfoxide
  35. ...R
        |
    O=S=O
        |
        R'
    sulfone
  36. ...R
        |
    O=S=O
        |
        OH
    (R-SO3H)
    sulfonic acid
  37. ...R
        |
    O=S=O
        |
        NR
    sulfonamide
  38. key component to allergic response to sulfonamide abx (sulfanethoxazole, sulfasalazine, sulfadiazine)
    arylamine group at N4
  39. COOH -> COO

    which is the acid? conjugate base?
    • acid: COOH
    • conjugate base: COO-
  40. equation for isoelectric point (pH of a neutral zwitterion)
    pH = 1/2 (pK1 + pK2)
  41. for polyprotic acids:
    isoelectric point  __ (>/</=) isoionic point
    ~=
  42. when pH=pKa
    when acid is 50% ionized (when HA = A-)
  43. given the pKa & pH, determine the ratio of nonionized to ionized in a body compartment
    pH = pKa - log ([HA]/[A-])
  44. if [HA/A-] = 10-1, what percent is nonionized?
    1/10 = 1 of 10 (or 10 of 100) is nonionized = 10%
  45. AUC
    • area under the curve
    • function of the fraction of drug dose that enters the systemic circulation & clearance

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