Pharmicodynamics - Answers What the body does to a drug
What is the advantage to expressing drug dose as a log? - Answers -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? - Answers -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 - Answers when we express the response on the y axis as an absolute value
-numbers that can assume values across a scale
quantal response - Answers -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? - Answers
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? - Answers Drug A
What does it mean if one drug is more potent than another? - Answers You need less of that drug than
the other drug to achieve the same effect
ED50 - Answers the dose that produces a response equal to half of the maximum response
Efficacy - Answers 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? - Answers 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? - Answers Drug B
How do you calculate therapeutic index? - Answers TI = TD50/ED50
Is it better to have a high or low therapeutic index? - Answers High
stereoisomer - Answers same structural formula, atoms arranged differently in space - this could cause a
drug to not be a good complimentary of fit
Enantiomers - Answers isomers that are mirror images of each other
What is the benefit of having a drug that is just the active enantiomer? - Answers 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 - Answers equal mixture of enantiomers
Ka - Answers Ka is the volume needed to get one mole of unbound drug when 50% of the receptors are
occupied
Kd - Answers Kd is the concentration of drug in the plasma when 50% of the receptors are occupied
full agonist - Answers Ability of a drug to produce 100% of the maximum response regardless of the
potency
partial agonist - Answers Medication that produces a weaker, or less efficacious, response than an
agonist.
receptor antagonist - Answers a drug that binds to a receptor and inhibits its function
competitive (reversible) antagonist - Answers the antagonist is competing with the agonist and it is
reversible - this means that they have equal affinities for the receptor because if one had an advantage
or higher Ka it would not be competitive it would just take the receptor site
what would make an antagonist irreversible? - Answers a higher Ka
How can competitive antagonists be overcome? - Answers by increasing the dose of the agonist
If you compare the LDR curve for the agonist alone and the agonist plus the competitive reversible
antagonist the curve is shifted to the right and is parallel which means you can still achieve the same
magnitude of effect but you need more dose
irreversible antagonist - Answers Affinity is so high that receptor is unavailable to bind agonist. Duration
of action independent of rate of elimination and more dependent on rate of turnover of receptor
molecules
binds to receptors with a covalent bond which can't be broken will be bound to that receptor site for the
life of the cell