PHRD5915 Drug Design Lecture 10 - Pharmacodynamics

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  1. function of antagonist
    prevents agonist from binding to the receptor
  2. M1 expressing tissue
    parietal cells
  3. M2 expressing tissue
    nerve terminals
  4. M3 expressing tissues
    smooth muscle
  5. NN expressing tissue
    post ganglionic cell bodies
  6. Nexpressing tissue
    skeletal muscle cells
  7. occupation theory
    receptor is activated as long is it is occupied by the agonist
  8. rate theory
    frequency of interaction between agonist & R dictates R activation (in freq -> inc response)
  9. an inverse agonist has a higher affinity for the receptor in the _______ state.
  10. agonist receptor affinity/actions can be modulated allosterically by... (3)
    • 1) other membrane-assoc'd proteins
    • 2) agents binding at other sites on the R
    • 3) intracellular proteins (eg G-proteins)
  11. binds to a site adjacent to the R & decreases ability of R to be activated by agonist
    non-competitive antagonist
  12. partial agonist ______ (do/don't) have spare receptors
  13. receptors usually ID'd using irreversible inhibitors
    spare receptors
  14. receptor-independent drug mechanisms (2)
    • 1) inhibition of biosynthetic/degradative enzymes
    • 2) binding agents
  15. physostigmine MOA
    cholinesterase inhibitor decreases ACh metabolism to inc cholinergic responses
  16. cholestyramine resin MOA
    binds cholesterol to decrease GI absorption
  17. Sugammadex MOA
    binds steroidal paralytic agents to inc speed of recovery from paralysis
  18. tachyphylaxis
    receptor desensitization
  19. tachyphylaxis occurs as a result of...
    • 1) R number
    • 2) R-effector coupling
  20. pharmacokinetic tolerance
    repeated exposure to a drug leads to increased induction of metabolic enzymes
  21. pharmacodynamic tolerance
    repeated exposure to drug leads to change in signal transduction pathways or other adaptive responses (reduced responsiveness)
  22. additive effect
    the effect of 2 drugs is equal to the sum of the individual effects (eg alcohol & barbituates)
  23. synergistic effect
    the effect of 2 drugs is greater than the sum of their individual effects (eg sulfamethoxazol & trimethoprim)
  24. potentiation
    a drug which alone has not effect enhances the potency of a drug which does not have an effect (eg penicillin & probenecid)
  25. functional antagonism
    effect of one agonist opposes the effect of another agonist (on different tissues)
  26. median effective dose (ED50)
    dose of drug at which 50% of individuals demonstrate the desired therapeutic effect
  27. what does ED50 provide a measure of? (2)
    • 1) clinical potency
    • 2) therapeutic selectivity
  28. median lethal dose (LD50)
    dose of drug causing deaht in 50% of subjects
  29. therapeutic index (TI)
    provides an estimate of the margin of safety (inc TI -> inc margin of safety)

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  30. physiological antagonism
    effect of one agonist opposes the effect of another agonist on different tissues
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PHRD5915 Drug Design Lecture 10 - Pharmacodynamics
2014-05-12 08:22:05

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