Term
T/F
According to the Occupation theory, a maximum response is reached when the majority of receptors are occupied 

Definition
FALSE
When all receptors are occupied 


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 

Definition
FALSE
the stimulus is decreased gradually after the drug is removed 


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 


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) 


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 


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 


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 xaxis 


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)) 

