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BFCP 1 FINAL > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

Gs

A

Activates Ca2+ channels
Increased AC, cAMP and calcium

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1
Q

Gi

A

Activates K+ channels
Decreased AC, cAMP
Increased potassium

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2
Q

Gq

A

Increased PLC, IP3, DAG and calcium

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3
Q

Beta adrenergic receptor

A

Example of GCPR

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4
Q

Insulin receptor

A

Example of receptor tyrosine kinase

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5
Q

Non-receptor tyrosine kinase

A

No enzymatic domain

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6
Q

TGF-B receptor

A

Example of receptor serine and threonine kinase

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7
Q

Intracellular receptors

A

Lipid soluble ligand
Slower effect but longer lasting effect
Ex. thyroid receptor

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8
Q

Tachyphylaxis

A

Repeated admin - diminishing effect

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9
Q

Desensitization

A

Decreased ability of receptor to respond

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10
Q

Inactivation

A

Loss of ability of receptor to respond

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11
Q

Refractory

A

Period of time required before ligand-receptor can respond

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12
Q

Down regulation

A

Removal of receptor after repeated exposure to ligand

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13
Q

Graded response

A

Individual

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14
Q

Quantal response

A

Population

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15
Q

Potency

A

Location of curve on x-axis
Closer to y, more potent
Decreased EC50

16
Q

Efficacy

A

Maximal height of curve
Emax
Drug occupies all receptors, no response to higher dose of drug

17
Q

Therapeutic index

A

Measure of drug’s saftety
Large value = wider window/margin

18
Q

Agonist

A

Can be drug or endogenous

19
Q

Full agonist

A

Activates receptor with max efficacy
Stabilizes receptor

20
Q

Partial agonist

A

Activates receptor but not max efficacy (less efficacious)
Can bind to same receptor

21
Q

Inverse agonist

A

Inactivates constitutively active receptor
Acts in absence of agonist

22
Q

Antagonist

A

Binds to allosteric site (change conformation to prevent binding of agonist) or active site (prevent binding of agonist)

23
Q

Competitive antagonist

A

Decreases agonist potency
Binds reversibly to active
Can be overcome by increasing [agonist]
Agonist must be present

24
Q

Noncompetitive active site agonist

A

Reduces efficacy
Binds irreversibly to active site (can’t be outcompeted)

25
Q

Noncompetitive allosteric antagonist

A

Reduces efficacy
Does not bind active site
Prevents conformation change/activation

26
Q

Nonreceptor antagonist

A

Inhibits agonist but doesn’t affect same receptor
Can be chemical or physiologic (insulin and glucagon)

27
Q

Nicotinic ACh receptor

A

Ligand gated ion channel, allows sodium influx for muscle contraction

BFCP 1 FINAL (13 decks)

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