Lecture 1 Pharmacodynamics Flashcards

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1
Q

Drug Receptor

A

Specific macromolecule that recognizes the drug

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2
Q

What is required for drug to affect a specific action?

A

Drug Receptor

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3
Q

Ability for drug to bind depends on which two factors?

A
  • drug size
  • shape relative to binding site
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4
Q

Degree of affinity

A

degree of attraction or binding power a given drug has for the receptors

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5
Q

Receptor

A

component on or within a cell that a substance can bind to

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6
Q

Receptors on the cell surface

A
  • Receptor sites on exterior of cell
  • Will not specifically allow substance to enter cell
  • Receptors are “transmembrane” proteins: Relay information from binding site to intracellular mechanism to cause change
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7
Q

Proteins may have which two sites

A
  • extracellular receptor site: binding domain
  • intracellular enzymatic component: catalytic domain
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8
Q

Example of insulin

A
  • Binds to extracellular component of protein
  • Activates protein enzymatic activity on inner surface of cell membrane
  • Leads to glucose uptake in muscle cells
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9
Q

Affinity

A
  • Amount of attraction between the drug and the receptor
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10
Q

Selective

A
  • a type of drug that affects only one type of cell or tissue and produces a specific physiological response
  • no drug produces only one effect
  • example: Cardioselectivve drugs vs. GI system
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11
Q

Dose Response

A
  • Shape of curve is related to number of receptors bound by the drug
  • Response is proportional to number of receptors occupied by the drug
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12
Q

What happens as dosage increases?

A
  • more receptors become occupied
  • Dose response increases
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13
Q

Agonist drug

A
  • binds to a receptor and produces an action
  • Affinity and efficacy
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14
Q

Antagonist drug

A
  • binds to a receptor and does not produce an action
  • Only affinity
  • can be called a blocker
    example: Benadryl
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15
Q

Partial Agonists

A
  • do not evoke a maximal response
  • often have high affinity for a receptor
  • may not completely activate the receptor
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16
Q

Agonist-Antagonist

A
  • can stimulate certain receptors while blocking effects of endogenous substances on other receptors
  • example: SERMs
17
Q

Inverse agonists

A
  • bind to the same receptor as the agonist but have the opposite effect on cell function
  • *opposite effect but same receptor
18
Q

Receptor Regulation

A
  • not static
  • regulated by exogenous and endogenous factors
  • can decrease and increase their sensitivity to stimulation
19
Q

Overstimulation of postsynaptic receptors may lead to?

A
  • functional decrease in appropriate receptor population
  • endogenous: Neurotransmitters/ Hormones
  • exogenous: Medications
20
Q

Result of Receptor Desensitization

A

Cell becomes less responsive

21
Q

Receptor Desensitization: “Down-Regulation”

A
  • slower, more prolonged process in which the number of available receptors is diminished
22
Q

Prolonged exposure of Receptor Desensitization can cause?

A
  • Receptor removal
  • Decreased receptor synthesis
  • Combination of both
23
Q

Receptor Desensitization or Decrease in receptor function can protect against?

A
  • Acute CNS injury
  • Cardiac diagnoses
  • Viral infections
24
Q
A