Intro To Pharmacology (Test 1) Lectures 2-8

Front 1

What does drug selectivity depend on?

Back 1

-Dose
-Drug Distribution
-Receptor Distribution
-Receptor Selectivity (specificity)

Front 2

What are the major types of receptors?

Back 2

-Tyrosine Kinase linked receptors
-G protein linked receptors
-Ligand Gated ion channel receptors
-Intracellular receptors

Front 3

Give examples of Tyrosine Kinase Receptors?

Back 3

-Insulin, EGF, GH, PDGF, VEGF

Front 4

Give examples of G protein linked receptors?

Back 4

-Serotonin, MUSCARINE, Dopaminergic, Noradrenergic

Front 5

Give examples of ligand gated ion channel receptors?

Back 5

-NICOTINIC, GABA, Glutamate

Front 6

What mediates the actions of pharmacologic antagonists?

Back 6

Receptors

Front 7

What binds to a receptor but does not activate it?

Back 7

Antagonist

Front 8

What binds to a receptor, does not activate it, and is concentration dependent?

Back 8

Competitive antagonist

Front 9

In the presence of a competitive antagonist, _____ concentrations of an agonist are required to produce the same effect of agonist alone.

Back 9

HIGHER

Front 10

What changes the receptor to decrease efficacy of the agonist?

Back 10

Noncompetitive Antagonist

Front 11

What causes the same effect as eliminating a fraction of total receptors from the response?

Back 11

Noncompetitive Antagonist

Front 12

Is the Potency of noncompetitive antagonists dependent or independent of dose and relative affinity of the agonist?

Back 12

INDEPENDENT

Front 13

What binds covalently to a receptor, which causes the duration of the action to be the rate of turnover of the receptor molecules?

Back 13

Irreversible Antagonists

Front 14

What is the difference between Ligand specificity and affinity?

Back 14

-Specificity: ligand binding to specific receptors
-Affinity: The extent to which the ligand is capable of binding and remains bound to a receptor

Front 15

What is intrinsic activity?

Back 15

-The extent to which a bound ligand activates a receptor
-This distinguishes agonist from antagonist
-(Receptor efficacy)

Front 16

What will an Agonist have?

Back 16

Affinity and Activity

Front 17

What will an Antagonist have?

Back 17

Only Affinity, NO Activity

Front 18

What does the Vmax value represent?

Back 18

Max velocity due to saturatability

Front 19

What does Km equal?

Back 19

-The concentration of substrate needed to reach 1/2 Vmax
-Essentially a measure of affinity for the substrate

Front 20

What does Kd equal?

Back 20

THe concentration at which BINDING is half saturated

Front 21

What is Potency related to?

Back 21

Drug Binding Affinity

Front 22

What is Efficacy related to?

Back 22

The Rate and Extent of receptor activation AFTER drug binding

Front 23

In a "system", drug response increases _____ with dose?

Back 23

Proportionally

Front 24

______ is related to affinity for the receptor.

Back 24

Potency

Front 25

What does Emax represent?

Back 25

Maximal response that can be produced (EFFICACY!!!)

Front 26

What does EC50 represent?

Back 26

The CONCENTRATION that produces 50% of the maximal effect (POTENCY!!!!!)

Front 27

If Kd is low, then binding affinity is ____?

Back 27

High

Front 28

Drugs that produce a FULL effect on a system are called?

Back 28

Full Agonists

Front 29

Drugs that interact with a receptor but cannot produce the same maximal effect are called?

Back 29

Partial agonists

Front 30

What determines potency?

Back 30

Affinity and Efficacy

Front 31

What are the 3 types of Antagonism?

Back 31

-Chemical
-Pharmacological
-Physiological

Front 32

Describe a Chemical antagonist?

Back 32

-Does NOT require a receptor
-It is a Chemical interaction of two substances

Front 33

Describe a Pharmacological antagonist?

Back 33

-Binds to receptors, but does NOT activate signal transduction mechanism
-Prevents Agonist binding!

Front 34

Describe Physiological antagonists?

Back 34

-Opposing effects by 2 agonists
-Ex. Insulin and GLucagon

Front 35

Are Pharmacological antagonists competitive?

Back 35

Yes, they effect potency and can be both reversible or irreversible

Front 36

What is an advantage of an irreversible inhibitor?

Back 36

Its duration of action is dependent on the rate of TURNOVER!!!! (NOT elimination)

Front 37

What is a disadvantage of an irreversible inhibitor?

Back 37

Easier to overdose!

Front 38

What do non-competitive Pharmacological antagonists primarily effect?

Back 38

Efficacy! (downward shift in curve)
-Binds to a different site then the agonist

Front 39

Can you compete off a non-competitive Pharmacological antagonists?

Back 39

No!!!!

Front 40

How do you stop the effect of a non-competitive Pharmacological antagonists?

Back 40

-Take the patient off the drug, this shift in concentration will shift the drug off its binding site!!

Front 41

What allows an increase in sensitivity of target cells to activation by low levels of ligand?

Back 41

SPARE RECEPTORS!!

Front 42

In a system with NO spare receptors, is ED50 <, >, or = Kd?

Back 42

(=) Equal to

Front 43

What effect do spare receptors have on noncompetitive antagonists?

Back 43

-Decrease their initial effect!
-They will function as "competitive" antagonists