Term
|
Definition
| drug that binds to same site as ligand and creates same signal |
|
|
Term
| define allosteric agonist |
|
Definition
| drug binds to different site than ligand creating no signal but causing ligand to be more effective |
|
|
Term
|
Definition
| drug produces lesser response than ligand and competes for ligand sites competetivly |
|
|
Term
|
Definition
| drug binds to ligands receptor and inhibits it leading to no signal within the cell |
|
|
Term
| define competitive agonist |
|
Definition
| drug binds irreversibly to the receptor and prevents agonist from binding and producing max effect |
|
|
Term
| define chemical antagonist |
|
Definition
| drug binds to another drug to antagonize its action. no receptor involved |
|
|
Term
| define physiological antagonist |
|
Definition
antagonist makes physiological action that is opposite of agonist and by separate mechanism
opposing drugs compete effects but go for different receptors |
|
|
Term
| compared to the agonist, what receptor and signal does an allosteric agonist have, what response does it ilict |
|
Definition
receptor: different
signal: same
response: increased (assuming agonist present) |
|
|
Term
| compared to the agonist, what receptor and signal does an partial agonist have, what response does it ilict |
|
Definition
receptor: same
signal: same
response: less than agonist |
|
|
Term
| compared to the agonist, what receptor and signal does an antagonist have, what response does it ilict |
|
Definition
receptor: same
signal: none
response: less than agonist |
|
|
Term
| how can the drug dose relationship, in a general statement, serve as a guidline for perscribing |
|
Definition
dont perscribe over the minimum dose it takes to produce the maximum response
increase in dose generally means an increase in response, at some point the response will max out though |
|
|
Term
| how is the drug dose relationship calculated |
|
Definition
E=(Emax x C) / (C + EC50)
E = effect
C = concentration
Emax = max response
EC50 = concentration that produces 50% of max effect |
|
|
Term
| what is a similar theory that the drug dose relationship equation can be used for, what is the equation |
|
Definition
B = (Bmax x C) / (C + Kd)
B = number of receptors
Kd = concentration of free drug producing half max binding to receptors |
|
|
Term
|
Definition
|
|
Term
| what does it mean if Kd = EC50 |
|
Definition
nothing much,
at 50% of drug binding, you get 50% of drug max effect |
|
|
Term
| where are Kd and EC50 found on a percent bound/max effect vs drug concentration graph |
|
Definition
| on the x axis at 50% binding or 50% max effect |
|
|
Term
| explain where an agonist + allosteric agonist, a partial agonist, a non-competitive agonist, and an agonist + antagonist are on a graph in comparison to just an agonist |
|
Definition
agonist + allosteric agonist: shift left
partial agonist: shorter
non-competitive agonist: much like partial agonist, progressivly decreases
agonist + antagonist: shift right |
|
|
Term
| define pharmacological antagonism, what antagonists fit into this category, which dont |
|
Definition
2 drugs with opposite effects go for the same receptor
pharmacological antagonists: competitive and non-competitive agonists
not: chemical and physiological agonists |
|
|
Term
|
Definition
concentration needed to produce 50% of the drug max response
the dose, how much you need to take, the size of the pill |
|
|
Term
| how is potency determined on a graph |
|
Definition
by looking at the Y axis, the more left the more potent
if curve on the left is taller than the right every dose is more potent |
|
|
Term
|
Definition
upper limit of the dose response curve
the higher the more effective the drug |
|
|
Term
| what is the most important thing about a drug |
|
Definition
|
|
Term
| how is efficacy determine on a graph |
|
Definition
| look at the X axis, the higher the curve the more effective |
|
|
Term
| what is clinical effectiveness dependent on |
|
Definition
| potency, max efficacy, ability to reach receptors |
|
|
Term
| why are there spare receptors |
|
Definition
max effect was achieved without filling all the receptors because there are more receptors than effectors to signal within the cell
OR
receptors, although without ligand, are still occupied with the signaling process so are empty until finished |
|
|
Term
| what can spare receptors tell us about drug sensitivity |
|
Definition
| if max effect is achieve with few receptors occupied, the drug is more sensitive |
|
|
Term
| on a graph, where is the drug response curve depicting spare receptors |
|
Definition
| to the left of receptor binding |
|
|
Term
| what can indicate to you that at the time there are no spare receptors |
|
Definition
|
|
Term
| if there are 11 receptors and 4 receptors how many spare receptors are there, what is the relationship of EC50 to Kd |
|
Definition
|
|
Term
| what information does a quantal dose effect plot give us |
|
Definition
| EC50, LD50 (leathal dose in 50% of popultation), TD50 (toxic dose in 50% of the population) |
|
|
Term
| what do we want our drugs to show on a quantal effective dose plot |
|
Definition
| ED50 far away from TD50 and REALLY far from LD50 |
|
|
Term
| what are the reasons for drug response variations (3) |
|
Definition
pharmakinetics: alterations in the drug concentrations that reach the receptor
variation in receptors due to physiological differences (obease, genetics, athletic)
altered number of receptors due to up or down regulation due to body status |
|
|
Term
| when choosing a dose of a drug, what is our goal. what if we need a higher dose how can we achieve that and avoid side effects |
|
Definition
use lowest dose needed to produce desired effects and minimise undesired effects
if you need a higher dose use two different drugs with different mechanisms to lower chance of undesired effects
alter the method of delivery |
|
|
Term
| what are the two types of non-competitive inhibition, explain them |
|
Definition
irreversible: more common, same receptor as drug
allosteric: different receptor than drug |
|
|
