1. what are the steps to induce effects (4)
    • delivery of molecule to tissue cell
    • complex formation with receptor (site of action)
    • molecular event causing an effect
    • mechanism of action
  2. drug molecules move in ____ ____ motion, _____ then ______ the bond and then ______ again according to the _______ of the molecule and _______ from other drug molecules
    • constant random
    • binding
    • releasing
    • binding
    • affinity
    • competition
  3. t/f drug molecules move in constant organized motions
    false constant random
  4. what affects the binding of a drug molecule to a receptor?
    • affinity of the molecule
    • competition from other drug molecules
  5. what type of chemical bond is weak and easily reversed?
    ionic bonds
  6. what type of chemical bonds are weaker than ionic
    hydrogen bonds
  7. what type of chemical bond is often irreversible and is the strong bond? give an dental example
    • covalent bonds
    • tetracycline + dentin
  8. what chemical bond contributes to mutual attraction between molecules
    van der Waals forces
  9. what are the two most common bonds between drugs and receptors? why?
    • hydrogen and ionic
    • because they are easily reversed
  10. t/f hydrogen and ionic bonds are the most common bond between drugs and receptors because they are irreversible and the strongest
    FALSE-they are the most common because they are easily reversed
  11. The most common type of chemical bond
    between a drug molecule and receptor is
    1) Hydrogen bond
    2) Covalent bond
    3) Ionic
    4) van der Waals forces

    • D) 1 and 3
    • Hydrogen binding and ionic binding are the most common types of binding between drugs and receptors
  12. good affinity is directly related to greater _____
  13. ____ dose and _____ dose are both related to their chemical structure
    • ceiling dose
    • threshold dose
  14. what is the maximum response produced by a drug called?
    ceiling dose
  15. what is the lowest dose to produce an effect called?
    threshold dose
  16. efficacy is related to the _____ ____ of the drug once a drug receptor complex is formed
    intrinsic activity
  17. The term that describes the maximum response produced by a drug is:

    E) Potency
    • C) Efficacy
    • Efficacy is the magnitude of response obtained from optimal receptor site occupancy by a drug
  18. a competitive antagonist as affinity but no intrinsic activity what effect does it have on the agonist?
    reduces the potency of the agonist
  19. toxicity can occur because of undesirable effects associated with administration of _______ dosages of drugs
  20. what are some undesirable effects associated with administration of therapeutic dosages of drugs?
    • exaggeration of direct effects at higher dosages
    • multiple concurrent adverse effects at therapeutic dosage level
  21. toxicity can occur in two ways what are they?
    overdose or side effect
  22. what is used during drug development to identify safe and effective doses?
    therapeutic index or TI
  23. t/f the lower the numeric value of the TI the safer the drug
    false- the HIGHER the number the safer the drug
  24. what is the ratio used to figure the TI?
    ratio of LD50 and ED50
  25. Two similar drugs (A and B) are being compared. The therapeutic index (TI) is computed for both of them. The TI for drug A is 8.5, and the TI for drug B is 5.0. Which drug is relatively more safe?

    • B) Drug A
    • The therapeutic index is used to compare the relative
    • safety of a drug. The higher the numeric value, the safer the drug.
  26. what is the movement of drugs through the body called?
  27. what five things does pharmacokinetics relate to?
    • drug's absorption
    • distribution in the body
    • distribution to site of action
    • Metabolism of drug
    • Excretion of drug
  28. what are the six factors influencing the rate of absorption?
    • degree of ionization and pH of tissues
    • formulation of the drug (liquid or solid form)
    • drug concentration
    • degree of blood circulation to the area
    • area of absorptive surface (larger area more absorption)
    • rout of drug administration (enteral or parenteral)
  29. the six factors influencing the rate of absorption are: degree of _______ and ____ of tissues, ______ of the drug (liquid or solid form), drug ______, degree of blood _______ to the area, ______ of absorptive surface, _____ of drug ________ (enteral or parenteral)
    • ionization and pH
    • formulation
    • concentration
    • circulation
    • area
    • route
    • administration
  30. t/f nonpolar, nonionized drugs will cross biologic membrane easier
  31. what is the purpose of the enteric coating? (3)
    delay dissolution of drug in the stomach, so that it will dissolve in the upper intestines instead of the stomach and reduces the adverse gastric side effects
  32. a greater concentration of the same drug means it will _____ faster than a lower concentration
  33. greater blood flow to an area = ?
    faster rate of absorption
  34. what organs have the greatest blood circulation?
    • liver
    • heart
    • GI tract
  35. where is the site of absorption for most oral drugs?
    upper small intestine
  36. what route is the safest most common, convenient and most unpredictable?
    oral (enteral)
  37. what effect may reduce concentration of drug molecules (hint the liver breaks it down first)
    first pass
  38. the _____ metabolizes most of the drug and the concentration is reduced this is called what?
    • liver
    • first pass
  39. what route of administration is the most predictable?
    IV route
  40. where does the majority of metabolism occur?
  41. t/f the majority of metabolism occurs in the upper small intestines
  42. what are the enzymatic reactions known as phase I and phase II known as?
  43. biotransformation can alter drugs 4 ways what are they? (4 conversions)
    • convert active drug into inactive drug
    • convert active drug to an active drug or toxic metabolite
    • convert inactive drug to active drug
    • convert unexcretable (more lipophilic) drug into excretable (more hydrophilic) metabolite
  44. which phase is it when the chemical structure is modified through oxidation, reduction or hydrolysis
    phase I
  45. what phase is it when it changes the drug so it is not active
    phase II
  46. what is responsible for many adverse drug reactions?
    cytochrome P450
  47. what is the most common means to eliminate drug molecules?
    renal excretion
  48. where in the kidney does excretion take place?
  49. what are the two types of glomerular filtration?
    • active tubular secretion
    • passive tubular reabsorption
  50. how many half lives are there to eliminate a drug?
  51. what is zero order kinetics?
    constant amount eliminated per unit of time
  52. t/f a constant fraction of the drug is eliminated per unit of time
  53. The enzymatic reactions, classified as phase I and phase II processes, are known together as:

    • B) Biotransformation
    • Biotransformation is the set of enzymatic reactions that can convert an active drug to inactive, an active drug to metabolite, an inactive drug into an active drug, or an unexcretable drug into an excretable metabolite
Card Set
ch 2 general principles of pharmacology