Pharmacology - General

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Pharmacology - General
2014-12-08 11:15:28

Pharmacology PAP-570
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  1. Class of drugs that bind directly to DNA (CA)
    Alkylating agents
  2. Renal toxicity
  3. Inhibit microtubule function
    Natural products-plants
  4. Mechanism of resistance=gene amplification
    Methotrexate (meth heads have to amp their dose to get high)
  5. Most widely used drug for Breast CA
  6. MOA: inhibit thymidylate synthetase
  7. Ceiling effect
    Used to describe the maximal response obtainable from a drug
  8. Lung toxicity (single drug)
  9. MOA: inhibits dihydrofolate reductase
  10. Mechanism of resistance=DNA repair enzymes
    Alkylating agents
  11. Site of action of most therapeutic agents
  12. Group of drugs that target S phase
    Natural products-plants
  13. MOA: inhibit lymphocyte proliferation
  14. Non-natural product drug that targets s-phase
    • Methotrexate
    • (meth heads like to have sex)
  15. Target M-phase of cell cycle
    Natural products-plants
  16. Largest family of receptors
    G-protein-Coupled Receptors
  17. Prodrug Alkylating agent
  18. Increased GI toxicity
  19. How are steroid transported in the blood?
    Bound to CBG (capillary blood glucose)
  20. Inhibits purine anabolism
    6-mercaptopurine (6 letters in purine)
  21. What is the Kd of a drug?
    The concentration of drug that occupies 50% of receptors
  22. Turns urine red
  23. What is the overall objective of drug therapy?
    Use of proper dose of drug to achieve the desired therapeutic action with minimal amount of side effects
  24. Causes uterine hyperplasia
  25. Heart toxicity (single drug)
    Adriamycin (Adrian Peterson has my heart racing ;) )
  26. Lipid-soluble alkylating agent
  27. Plotting drug dose on x-axis and amount of response on y-axis describes what type of curve
    Log-dose response curve
  28. Toxicity: sodium retention, osteoporosis
  29. MOA: Intercalates DNA (2 drugs)
    Actinomycin, Adriamycin
  30. Neurological toxicity (single drug name)
  31. A strong drug-receptor interaction when only small amount of the drug is present is said to have high or low affinity?
  32. Drug-receptor interaction results in a response of the cell/tissue
  33. Drug binds to the receptor and does not stimulate a response
  34. Competitive antagonist is an example of what type of receptor
    Ligand-gated ion channels
  35. Can an allosteric modulator have its own effect?
    No-it only enhances/inhibits an effect
  36. Fractional occupancy is synonymous to…
    % receptors occupied
  37. Which type of receptor is activated by phosphorylation?
    Tyrosine kinase
  38. What do tyrosine kinase receptors do?
    Turn on other signaling molecules such as JAK and STAT
  39. What is special about the steroid hormone receptors?
    They bind inside the nucleus
  40. When do we use Kd values?
    To compare drugs
  41. What is Kd
    Equilibrium dissociation constant
  42. Occupancy equation=(actual equation)
    D/(D + Kd)
  43. EC50 vs LD50
    EC50-“test tube” experimental value of the effective conc, LD50-effective dose in a clinical/physiological setting
  44. On an LDR curve, how do you determine which drug is the most potent?
    The one furthest left is the most potent
  45. Efficacy-define it
    Maximal level of response produced by the drug
  46. Potency-define it
    Amount of drug that produces a give level of response
  47. Potency vs. efficacy
    Potency refers to the amount of drug, efficacy refers to the amount of response
  48. What does it mean if drug A is more potent than drug B?
    To achieve any level of response, less of drug A is needed than of drug B
  49. How do you determine the maximal response
    Testing increasing levels of a drug until the response reaches a constant value (top of the LDR curve) and it plateaus
  50. Idiosyncrasy
    An unusual effect of the drug that occurs in a small percentage of people
  51. Loss of responsiveness to a drug treatment over time
  52. Pharmacokinetic vs pharmacodynamics
    • Kinetic=dose-concentration
    • Dynamic=concentration-effect
  53. Bioavailability
    Rate and extent of absorption of a drug