9.12 Pharmacology 3

Question 1

components on or within the cell to which a substance binds

Answer 1

receptors

Question 2

How do surface receptors act as ion channels?

Answer 2

directly alter membrane permeability

Question 3

How do surface receptors act to directly influence cell function?

Answer 3

enzymatically

Question 4

Purpose of surface receptors linking to regulatory proteins

Answer 4

regulatory proteins control other chemical or enzymatic processes

Question 5

affinity

Answer 5

• attraction of a drug to a receptor

- determines how it will bind and react

Question 6

efficacy

Answer 6

How well a drug binds and reacts to with a receptor

Question 7

How do drugs affect change through binding?

Answer 7

The drug finds and occupies a receptor, then somehow interacts with it to change cell function

Question 8

agonist

Answer 8

drug that can bind to a receptor and initiate a change

Question 9

What do agonist drugs have?

Answer 9

• affinity

- efficacy

Question 10

Antagonists ONLY have

Answer 10

affinity

Question 11

How do antagonists work?

Answer 11

• binds to receptor
• does not initiate a change
• blocks the effect of another chemical and prevents action

Question 12

antagonists aka

Answer 12

blockers

Question 13

beta blockers are used to treat

Answer 13

HTN

Question 14

competitive antagonist

Answer 14

both the agonist and the antagonist have an equal opportunity to occupy the receptor

Question 15

For a competitive antagonist vs. an agonist, which will win out for receptor spots?

Answer 15

whichever has the highest concentration

Question 16

What happens if a competitive antagonist “wins”?

Answer 16

inhibition

Question 17

Competitive antagonists generally require a (higher/lower) concentration. Why?

Answer 17

• higher concentration

- weak bones

Question 18

noncompetitive antagonist

Answer 18

• irreversible
• strong bonds formed
• cannot be displaced by the agonist

Question 19

How long do noncompetitive antagonist drugs last?

Answer 19

• entire lifespan of the cell

- usually several days

Question 20

partial agonist

Answer 20

• don’t get a full response

Question 21

Partial agonists have:

Answer 21

• affinity

- don’t have full efficacy

Question 22

Clinical advantage to partial agonist drugs?

Answer 22

fewer side effects

i.e. cardiovascular and antipsychotics

Question 23

mixed agonist-antagonist

Answer 23

can stimulate certain receptors while blocking others

Question 24

Example of mixed agonist-antagonist

Answer 24

selective estrogen receptor modulator (ex. tamoxifen used in breast cancer)

Question 25

How does tamoxifen work as a mixed agonist-antagonist?

Answer 25

• stimulates estrogen receptors to prevent osteoporosis

- blocks effects on breast tissue to prevent cancer

Question 26

inverse agonist

Answer 26

• binds to same receptor as an agonist

- has opposite effect

Question 27

Uses for inverse agonists?

Answer 27

• could slow down overstimlulated receptors

- research in antipsychotics and beta blockers

Question 28

desensitization

Answer 28

• cell becomes less responsive

- can decrease active receptors

Question 29

down-regulation

Answer 29

slower version of desensitization

Question 30

super sensitivity

Answer 30

cell becomes more responsive