potency, efficacy, and the therapeutic index

Question 1

pharmacokinetics

Answer 1

study of drug movement through the body aka absorption, distribution etc.

Question 2

pharmacodynamics

Answer 2

study of how a drug changes the body

Question 3

quantal effects

Answer 3

yes/no response, this when when we are trying to indicate whether or not a drug achieves a certain response e.g does this medication alleviate a headache

Question 4

what is the ED50 median effective response

Answer 4

this is the dose required to produce a specific therapeutic response in 50% of patients

Question 5

what is the ED50 response also referred to as

Answer 5

standard dose

Question 6

what is the therapeutic index

Answer 6

this is the ratio of a drugs T50 to its ED50

Question 7

what is the median lethal dose LD50

Answer 7

this is the amount of drug that would be lethal in 50% of test animals

Question 8

median toxic dose TD50

Answer 8

this is the dose that will produce a given toxicity in 50% of patients

Question 9

what is a therapeutic window

Answer 9

range based on the minimum effective therapeutic concentration and the minimum toxic concentration for a specific toxic effect

Question 10

the bigger the therapeutic index..

Answer 10

the safer the drug

Question 11

what makes a drug more safe

Answer 11

the therapeutic window

Question 12

medications with a very small therapeutic window are considered what medications

Answer 12

high alert medications

Question 13

what are graded effects

Answer 13

not yes or no, asks how much. e.g how much can this medication drop my pt blood pressure

Question 14

phase 1 of graded effects

Answer 14

very little medications, very little effect

Question 15

phase 2 of graded effects

Answer 15

there is now a relationship between the dose of the drug administered and the degree of client response

Question 16

what phase has a linear relationship between amount of drug administered and degree of client response

Answer 16

phase 2

Question 17

phase 3 of graded effects

Answer 17

when the plateau is reached. no therapeutic effects

Question 18

potency

Answer 18

comparing doses of medications to respect how much drug is needed to produce a specific response

Question 19

if a drug is highly potent, how much of the drug is needed fro a therapeutic response

Answer 19

not much

Question 20

efficacy

Answer 20

the greater the efficacy the greater the capacity of the drug to exert its full biological effects

Question 21

do we want a drug with a big efficacy or small

Answer 21

big

Question 21

if three drugs are equally efficacious how should you choose

Answer 21

choose the one that is most cost efficient

Question 22

rate of association

Answer 22

the rate at which a drug binds to a receptor

Question 23

what is k-1

Answer 23

this is the rate at which a drug binds to a receptor and lets go

Question 24

what kind fo drugs do we want when considering recpetor binding

Answer 24

we want drugs with a high affinity for drug binding

Question 25

what does it mean when a drug has an high affinity

Answer 25

it means that it binds to a receptor quickly and dissociates slowly

Question 26

what is a low affinity

Answer 26

it will have a low association and fast dissociation

Question 27

low affinity is how potent

Answer 27

poorly potent

Question 28

high affinity is how potent

Answer 28

very potent

Question 29

agonist types

Answer 29

full, partial, inverse

Question 30

antagonist types

Answer 30

reversible, competitive, non competitive, irreversible

Question 31

agonists act as what

Answer 31

they act as a replacement for the hormone or a endogenous ligand or drug that is insufficient

Question 32

full agonists

Answer 32

able to achieve the full biological effect at the endogenous ligand receptor

Question 33

what kind of drug is identical to what the body would be producing on its own

Answer 33

full agonist

Question 34

dexamethasone produces the same response as what

Answer 34

cortisol

Question 35

partial agonist

Answer 35

will only achieve a fraction of the biological effect

Question 36

the efficacy will always be what of partial agonist

Answer 36

lower efficacy than a full agonist

Question 37

inverse agonist and intrinsic activity

Answer 37

when alone, they physically change the physiology of a cell

Question 38

what kind of efficacy do inverse agonists have?

Answer 38

negative efficacy

Question 39

when can we use a inverse agonists

Answer 39

when someone is nervous/anxious GABAa receptor stimulation making the person more relaxed

Question 40

what agonists bind to a receptor and cause the receptor to be less than what it usually is

Answer 40

inverse

Question 41

antagonists do what

Answer 41

they bind to the receptor site as the endogenous ligand, but do not produce a billogical repsonse

Question 42

what efficacy do antagonists have

Answer 42

they dont have any, because they stop the drug

Question 43

irreversible antagonists

Answer 43

cannot be reversed unless the cell is destroyed and replaced with a new one

Question 44

competitive antagonism

Answer 44

competes for the same receptor binding site as the endogenous ligand

Question 45

once the competitive antagonist is binded what happens

Answer 45

it blocks the endogenous ligand from binding

Question 46

non-competitive antagonism

Answer 46

binds to a site other than the endogenous receptor

Question 47

what does the competitive antagonist bind to

Answer 47

binds to the enzyme, changing the conformation of the receptor so the endogenous ligand cant bind

Question 48

what antagonist changes the confirmation of the enzyme

Answer 48

non-competitive antagonist

Question 49

examples of non-competitive antagonists

Answer 49

PCP, ketamine

Question 50

what is the k-1 and kd of a irreversible antagonist

Answer 50

k-1 is equal to 0

KD is very low, affinity is very low