Pharmacodynamics

Question 1

Gs

Answer 1

Activates Ca2+ channels
Increased AC, cAMP and calcium

Question 1

Gi

Answer 1

Activates K+ channels
Decreased AC, cAMP
Increased potassium

Question 2

Gq

Answer 2

Increased PLC, IP3, DAG and calcium

Question 3

Beta adrenergic receptor

Answer 3

Example of GCPR

Question 4

Insulin receptor

Answer 4

Example of receptor tyrosine kinase

Question 5

Non-receptor tyrosine kinase

Answer 5

No enzymatic domain

Question 6

TGF-B receptor

Answer 6

Example of receptor serine and threonine kinase

Question 7

Intracellular receptors

Answer 7

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

Question 8

Tachyphylaxis

Answer 8

Repeated admin - diminishing effect

Question 9

Desensitization

Answer 9

Decreased ability of receptor to respond

Question 10

Inactivation

Answer 10

Loss of ability of receptor to respond

Question 11

Refractory

Answer 11

Period of time required before ligand-receptor can respond

Question 12

Down regulation

Answer 12

Removal of receptor after repeated exposure to ligand

Question 13

Graded response

Answer 13

Individual

Question 14

Quantal response

Answer 14

Population

Question 15

Potency

Answer 15

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

Question 16

Efficacy

Answer 16

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

Question 17

Therapeutic index

Answer 17

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

Question 18

Agonist

Answer 18

Can be drug or endogenous

Question 19

Full agonist

Answer 19

Activates receptor with max efficacy
Stabilizes receptor

Question 20

Partial agonist

Answer 20

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

Question 21

Inverse agonist

Answer 21

Inactivates constitutively active receptor
Acts in absence of agonist

Question 22

Antagonist

Answer 22

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

Question 23

Competitive antagonist

Answer 23

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

Question 24

Noncompetitive active site agonist

Answer 24

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

Question 25

Noncompetitive allosteric antagonist

Answer 25

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

Question 26

Nonreceptor antagonist

Answer 26

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

Question 27

Nicotinic ACh receptor

Answer 27

Ligand gated ion channel, allows sodium influx for muscle contraction