Term
T/F
According to the Occupation theory, a maximum response is reached when the majority of receptors are occupied |
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Definition
FALSE
When all receptors are occupied |
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Term
T/F
According to the Occupation theory, the stimulus increases gradually when a drug is introduced and stops abruptly when the drug is removed |
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Definition
FALSE
the stimulus is decreased gradually after the drug is removed |
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Term
Match
full agonist α=0
partial agonist 0<α<1
antagonist α<0
inverse agonist α=1
|
|
Definition
full agonist α=1
partial agonist 0<α<1
antagonist α=0
inverse agonist α<0 |
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Term
T/F
you can get a max response without maximum binding |
|
Definition
|
|
Term
Which acts more slowly?
agonist
antagonist
Why? |
|
Definition
Antagonist
because it must displace the agonist before it can bind |
|
|
Term
| The rate of dissociation is directly related to____ and inversely related to _____ |
|
Definition
directly related to AGONIST POTENCY and inversely related to ANTAGONIST POTENCY
(see Rate Theory) |
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Term
| If the Occupation theory is true, how to Kd and EC50 compare? |
|
Definition
They should be the same
Kd is the concentration at which you get 50% binding
EC50 is the concentration at which you get 50% of a response
OT is 1:1 meaning %bound=%response |
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Term
T/F
Measuring antagonist activity is difficult but possible |
|
Definition
FALSE
antagonists dont give a response so there is nothing to measure.
Must be measured in terms of the agonist |
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|
Term
T/F
antagonist binding may be reversible or irreversible |
|
Definition
|
|
Term
T/F
For competitive antagonism the affinity of the agonist=affinity of antagonist |
|
Definition
|
|
Term
Competitive Antagonist
As you put in more antagonist what happens to the EC50? |
|
Definition
It increases
(need more agonist to get 50% response) |
|
|
Term
Competitive Antagonist
T/F
Dumping more agonist will eventually give 100% response |
|
Definition
TRUE
it does not change the Emax |
|
|
Term
Which plot defines binding?
Scatchard or Schild |
|
Definition
|
|
Term
T/F
The dose response curve shifts to the left as more antagonist is present |
|
Definition
|
|
Term
[image]
Which has the greatest EC50?
What does this mean in terms of the agonist? |
|
Definition
A4 has the greatest EC50
It takes most agonists to get maximum response
|
|
|
Term
|
Definition
pA2 is the [antagonist] needed to decrease the agonist resonse by 50%
AKA
the [antagonist] that increases the [agonist] by 2 to get the same response if there were no antagonist present |
|
|
Term
| Where do you look for the pA2 on a graph? |
|
Definition
| Where the line crosses the x-axis |
|
|
Term
|
Definition
| pA2= -log Ka= -log [agonist] |
|
|
Term
Which is the more potent antagonist?
pA2= 4
pA2=12 |
|
Definition
pA2=12
Think pA2= 10^-12 (smaller than10^-4) so it takes a smaller [Antagonist] to decrease the agonist response by 50% |
|
|
Term
|
Definition
[drug] with antagonist present
[drug] w/o antagonist present |
|
|
Term
Irreversible Antagonism
T/F
Can be reversed by increasing [agonist] |
|
Definition
FALSE
Not reversible no matter how much agnonist, must create a new receptor |
|
|
Term
Irreversible Antagonism
T/F
Emax is decreased |
|
Definition
|
|
Term
Irreversible Antagonism
T/F
Time dependent |
|
Definition
|
|
Term
T/F
Occupation Theory is not always correct |
|
Definition
TRUE
Even though an antagonist is present you may still get 100% response...see pg 13 |
|
|
Term
Irreversible Antagonism
Increasing the amount of antagonist _____the EC50
increase
decrease
no effect |
|
Definition
|
|
Term
Noncompetitive Antagonism
T/F
behaves as a competitive antagonist at low concentration |
|
Definition
|
|
Term
| What happens to the agonist and the response once a noncompetitive antagonist binds? |
|
Definition
| The agonist can still bind to it's site but will not initiate a response |
|
|
Term
| Where does a noncompetitive antagonist bind? |
|
Definition
| To a site different from where the agonist binds |
|
|
Term
Noncompetitive Antagonist
As you add more antagonist what happens to the Emax
increase
decrease
no effect |
|
Definition
|
|
Term
Partial agonist have_____binding but____effect
partial
full
no |
|
Definition
| Full binding and partial effect |
|
|
Term
Partial agonist
T/F
Bmax=Emax |
|
Definition
FALSE
Bmax ≠Emax
You can get maximum binding(Bmax) but you will not get full effect (Emax) |
|
|
Term
Partial agonist
As you increase the concentration of partial agonist what happens to the concentration of full agonist |
|
Definition
| The receptors get occupied by the PA and the [A] decreases |
|
|
Term
T/F
When creating drugs they will always be partial agonists with respect to te natural ligand |
|
Definition
TRUE
The natural ligand will always have more of an effect |
|
|
Term
Partial Agonist
What happens to the response if you have full receptor occupancy of partial agonists? |
|
Definition
| Will not get a full response |
|
|
Term
|
Definition
| Dose that gives the maximum pharmacological effect |
|
|
Term
T/F
you can always increase the effect wanted by administerng higher doses of the drug |
|
Definition
FALSE
there is a ceiling dose!
Once this is reached no matter how much drug is given the effect will not change |
|
|
Term
[image]
T/F
C is more potent than B |
|
Definition
TRUE
(draw line across the 50% mark and verticle lines down to the concentration...takes less of C to have same effect as B, therefore more potent) |
|
|
Term
[image]
Which is more effective, A or B? |
|
Definition
| Both are equally effect, both give a maximum response |
|
|
Term
[image]
How does D compare to the rest of the curves? |
|
Definition
It is the least potent and least effective
It doesnt even give enough of a response to reach 50% and never reaches maximum response |
|
|
Term
T/F
Graded responses are gradual |
|
Definition
|
|
Term
T/F
Using a less potent drug is preferable because there are less side effects |
|
Definition
FALSE
using a less potent drug increases the chance of offset reactions because you must administer more of the drug to get a response |
|
|
Term
T/F
Quantal Dose Responses are gradual |
|
Definition
|
|
Term
| Quantal Dose responses follow which type of distribution |
|
Definition
| Normal Distribution (Bell shaped Curve) |
|
|
Term
| What is the therapeutic index? |
|
Definition
| The ratio of lethal dose to therapeutic dose |
|
|
Term
| What is the median effective dose aka ED50? |
|
Definition
| The dose of drug required to produce specific intensity in 50% of the population |
|
|
Term
| What is the lethal dose aka LD50? |
|
Definition
| The effective dose producing death in 50% of the population |
|
|
Term
| Having a LD50 is not really preferable....what is used instead and why? |
|
Definition
| Standard safety Margin is used because the Lethal Dose is now set at 1% and the Effective Dose is set at 99% |
|
|
Term
| What does a Therapeutic Index of 2.62 mean? |
|
Definition
| You need to give 2.62 times as much (or 262%) of the dose to get the lethal effect |
|
|
Term
| Using the Standard Safety Margin with LD set at 1%, what does a SSM of 34% mean? |
|
Definition
| You need to give 34% times as much of the drug to get a lethal effect |
|
|
Term
[image]
a) what is the time to onset for the smallest curve
b) what is the time to peak for the highest curve
c) What is the duration of action for the middle curve |
|
Definition
a) about 2 hrs (from 0 til measurable)
b) about 2 hrs (from 0 to its highest measurable point)
c) about 3 hrs (from onset (1) til no measurable amount(4)) |
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