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Cycle 3 > Quantitative Pharmacodynamics > Flashcards

Quantitative Pharmacodynamics Flashcards

1
Q

What is Pharmacokinetics?

A

relationship between drug administration and exposure to drug

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2
Q

What is Pharmacodynamics?

A

relationship between exposure to drug and effect

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3
Q

What are receptor agonisms?

A
  • agonists bind to receptors
  • activate transmembrane events
  • conc need to have % effect differs
  • max response may differ
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4
Q

What are receptor antagonisms?

A
  • bind to receptors
  • do not signal transduction
  • low [antagonist] little inhibition
  • zero efficacy as it does not activate a receptor
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5
Q

What is efficacy?

A

how well drugs/ligands activate receptors once its bound

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6
Q

What are the quantitative aspects go drug-receptor interactions?

A
  • noncov
  • reversible
  • competitive
  • specific
  • selective
  • ligand
  • reversibility (how easily the ligand bind and dissociate from receptors
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7
Q

What is the rate of dissociation?

A
  • number of molecules dissociating per second proportional to the conc of receptor ligand complexes
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8
Q

What is the rate of association?

A
  • number of molecules association er second proportional to the conc of receptor and ligand
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9
Q

What is Kd?

A

The concentration of ligands resulting in half receptors being occupied by ligand
EC50 is the drug conc thats gives 50% response
(See equation 1)

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10
Q

How do we measure Kd?

A
  • receptor binding sites
  • measure binding to cell membranes
  • total binding = specific binding + non specific binding
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11
Q

What is specific binding?

A

binding to receptors

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12
Q

What is non-specific binding?

A

binding to anything else present

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13
Q

How does an agonist binding to a receptor lead to biological effect?

A
  • law of mass action applies
  • response related to receptor occupancy
  • max tissue response obtained at lower occupancy or higher occupancy
  • see equation 2
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14
Q

What is the Hill Equation?

A

See equation 3

  • predicts what we should see most of effect over approximately 100 fold difference in conc
  • reflects range of drug conc over which response occurs
  • important because allows us to view consequences of using 3 drugs on a patient
  • allows for calculation of EC50 and nH
  • allows us to obtain KD for ligand binding
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15
Q

How does the Hill Equation explain partial agonism?

A
  • isoprenaline and prenalterol activate beta adrenergic receptors
  • isoprenaline = full agonist
  • prenalterol = partial agonist
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16
Q

What are partial agonists?

A
  • fully occupy all receptors
  • cannot activate large enough proportion to elicit max response
  • some tissues, this may be sufficient
  • dependent on receptor reserve
17
Q

What are spar receptors?

A
  • full agonists elicit max response without all receptors being occupied
  • Kd > EC50
18
Q

How can receptor number and efficacy determine response?

A
  • drugs are tested for max response in 2 diff. tissues

- two tissues have different number of receptors present needed to obtain max response

19
Q

What is competitive antagonism?

A
  • reversible
  • agonist and antagonist cannot bind at the same time
  • effect of antagonist overcome with higher conc of agonist
  • increase EC50
  • more agonists = overcome antagonist
  • Kd increased by (1+ [B]/kB )
  • dependent on [antagonist]
  • see equation 3
20
Q

What is the cheng prustoff equation?

A

see equation 4

21
Q

What is irreversible antagonism?

A
  • antagonists bind covalently to same site as agonist
  • not dissociate
  • receptors become inactivated
  • reduces max response
  • increases [Agonist] not overcome blockade
  • KD unchanged
22
Q

How does antagonism by partial agonists work?

A
  • partial agonist competes with full agonist
  • high [partial agonist] activity of partial agonist predominates
  • add partial agonist on top of full agonist, antagonises the effect
23
Q

What is allosteric antagonism?

A
  • antagonist binds to diff. site on receptors
  • receptors activated if binds to agonist alone
  • effect on response curve is complicated and depends on receptor reserve
24
Q

What are inverse agonists?

A
  • receptors are constitutively active
  • drugs bind to R to reduced amount of receptor available to spontaneously activate and reduce resting response of tissue

Cycle 3 (4 decks)

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