What do excitatory NT bind to? - - ligand gated sodium channels and open them up
If it reaches -55 then it will fire
What do inhibitory NT bind to? - - potassium gated ion channel
Potassium then leaves the cell taking its positive current with it and takes the voltage inside the cell further...
Pharmacodynamics - ✔✔✔ - What the body does to a drug
What is the advantage to expressing drug dose as a log? - ✔✔✔ - -we can go from 0.01 ug to 100 ug
in one graph
-it allows us to express drug doses across a very wide range
-it expands the concentration at the lower axis - our ability to look at the body's response at the lower
doses - because all of the action is happening at the left side of the graph we want to be able to finely
grade the graph on the side of the graph where the response is happening
-Ability to compare graphs for different drugs - overlay
What do the three areas of an LDR curve represent? - ✔✔✔ - -it begins as flat where there is no
difference from one integer to the next - no response at this dose
-The area where it rises is called the linear part of the graph - this is where we start seeing effects by
increasing the dose
-the next part is called the plateau because increasing the dose gives no further effects
Graded response - ✔✔✔ - when we express the response on the y axis as an absolute value
-numbers that can assume values across a scale
Quantal response - ✔✔✔ - -when the response is expressed on the y axis as whether or not the person
is a responder
-expressed as % of people that respond or don't respond
What is an example of a response expressed as a percentage that is not a quantal response? - ✔✔✔ -
A1C - expressed as a percentage - measurable as a graded value on the y axis
, On an LDR curve where Drug B falls to the right of Drug A, Which drug is more potent? - ✔✔✔ - Drug
A
What does it mean if one drug is more potent than another? - ✔✔✔ - You need less of that drug than
the other drug to achieve the same effect
ED50 - ✔✔✔ - the dose that produces a response equal to half of the maximum response
Efficacy - ✔✔✔ - the maximum response that a drug is capable of achieving
(This is where the drug plateaus on the curve
What is an example of when it would be bad to get to the top of the maximum dose? - ✔✔✔ - Imagine
giving a drug to get a response of drop in systolic blood pressure. We don't want it to be 90% effective
On an LDR curve where Drug B is higher than Drug A, Which drug has more efficacy? - ✔✔✔ - Drug
B
How do you calculate therapeutic index? - ✔✔✔ - TI = TD50/ED50
Is it better to have a high or low therapeutic index? - ✔✔✔ - High
Stereoisomer - ✔✔✔ - same structural formula, atoms arranged differently in space - this could cause
a drug to not be a good complimentary of fit
Enantiomers - ✔✔✔ - isomers that are mirror images of each other
What is the benefit of having a drug that is just the active enantiomer? - ✔✔✔ - the drug that is the
pure form of the active enantiomer and not a mix should in theory only bind at the active site - you're
not getting unwanted bindings
Racemic mixture - ✔✔✔ - equal mixture of enantiomers
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