Pharmacodynamics Flashcards

1
Q

what are the features of drug receptors?

A
  1. recognize and bind other molecules (ligands)
  2. propagate regulatory signals following ligand binding
  3. modulate ongoing cellular functions
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2
Q

estrogen receptor and vitamin A receptor are what types of receptors?

A

intracellular

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3
Q

what are two examples of intracellular receptors?

A

estrogen and vitamin A

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4
Q

EGFR, IR, and TGF-BR are what types of receptors?

A

intrinsic enzymatic activity

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5
Q

what are the typical targets for receptors with intrinsic enzymatic activity?

A

signal transduction - protein and lipid kinase cascades, protein phosphatases

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6
Q

what are examples of receptors with intrinsic activity?

A

EGFR, IR, TGF-BR

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7
Q

nicotinic Ach receptor is what type of receptor?

A

ligand gated ion channel

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8
Q

IL-3r, EPOr, and leptin receptor are what type of receptors?

A

directly associate with intracellular enzymes

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9
Q

which receptors directly associate with intracellular enzymes?

A

IL-3r, EPOr, and leptin receptor

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10
Q

B-adrenergic, rhodopsin, frizzled, and Smo receptors are what type of receptors?

A

GPCRs

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11
Q

what is the dissociation constant for drug binding affinity?

A

Kd = [R][L] / [RL]

or, Koff / Kon

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12
Q

what is the dissociation constant Kd equal to when the free receptor concentration equals the concentration of bound receptor?

A

ligand concentration (when half the receptors are occupied and half are free)

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13
Q

how does a small Kd value relate to binding affinity?

A

small Kd = greater binding affinity

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14
Q

definition: potency

A

measurement of drug dose used to compare the relative affinity and effectiveness of two or more drugs - done by comparing EC50s (more potent = more to the left)

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15
Q

definition: efficacy

A

the maximal effect a drug can induce

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16
Q

definition: competitive antagonist

A
  1. agonist and antagonist compete for same binding site
  2. shift to the right in the EC50
  3. maximal effect is still achievable
17
Q

definition: noncompetitive antagonist

A
  1. agonist and antagonist bind to different sites
  2. decrease in maximal effect
  3. agonist’s affinity for receptor may not change in presence of noncompetitive antagonist
18
Q

definition: partial agonist

A

drug that produces a lower maximal response as compared to the agonist

19
Q

definition: therapeutic index

A
  1. indicator
  2. ratio of TD50 / ED50
  3. the greater the ratio / window between the TD50 and ED50, the safer the drug is for a patient
20
Q

how does tolerance affect the dose-response curve?

A

shift to right

21
Q

how does sensitization affect the dose-response curve?

A

shift to left