Pharmacodynamic Principles

Question 1

what type of drug posses affinity and intrinsic efficacy

Answer 1

agonist

Question 2

what class of agonist binds to the same site as endogenous ligands

Answer 2

primary agonist

Question 3

what class of agonist binds to a different region of the receptor

Answer 3

allosteric agonist

Question 4

what is an example of an allosteric agonist

Answer 4

anaesthetic drug effects on GABA receptors

Question 5

what type of agonist produces maximal efficacy

Answer 5

full agonist

Question 6

what type of agonist can bind to and activate the receptor but produces a sub-maximal effect

Answer 6

partial agonist

Question 7

what opioid receptor acts a full agonist

Answer 7

morphine

Question 8

what opioid receptor is a partial agonist

Answer 8

buprenorphine

Question 9

what type of drug possess affinity but lacks intrinsic efficacy

Answer 9

antagonist

Question 10

what is the function of antagonistic drugs

Answer 10

prevent the action of natural agonists (neurotransmitters & hormones)

Question 11

what is an example of a drug that can act as an agonist and antagonist

Answer 11

butorphanol

Question 12

how does butorphanol act on mu receptors

Answer 12

antagonist

Question 13

how does butorphanol act on kappa receptors

Answer 13

agonist

Question 14

how does butorphanol act on kappa receptors

Answer 14

agonist

Question 15

what are the two types of antagonism

Answer 15

competitive & non-competitive

Question 16

what type of antagonism is present when the antagonistic drug acts on the SAME RECEPTOR as the agonist

Answer 16

competitive antagonism

Question 17

what type of antagonism is reversible when it can be over come by the agonist concentration

Answer 17

competitive antagonism

Question 18

what are examples of competitive antagonistic drugs

Answer 18

atropine
propranolol

Question 19

how will a competitive antagonist impact the potency of a drug

Answer 19

lowers potency

Question 20

how does competitive antagonism effect efficacy

Answer 20

efficacy remains constant

Question 21

which antagonism type is irreversible

Answer 21

non-competitive

Question 22

what type of bond is used by antagonistic non-competitive drugs?

Answer 22

covalent

Question 23

how does the use of a non-competitive antagonistic drug effect potency

Answer 23

decreases potency

Question 24

how does the use of a non-competitive antagonistic drug affect efficacy

Answer 24

decreases efficacy

Question 25

True or False: A non-competitive EMax will eventually equal that of the regular drug

Answer 25

FALSE there will always be a decrease in efficacy

Question 26

Besides comparing the efficacy of a drug with different amounts of antagonists, what else can those graphs be used for

Answer 26

determine antagonist strength

Question 27

what type of site does the non-competitive drug bind to

Answer 27

allosteric site because it causes change to the active site

Question 28

what type of agonist acts at the same receptors as an agonist but produces an opposite pharmacological effect

Answer 28

inverse agonist

Question 29

what are examples of inverse agonists

Answer 29

H1 receptor antihistaminergic drugs B-blockers / carvedilol antipsychotic drugs antihypertensive drugs

Question 30

which type of agonist would you expect to see to bind to only active receptors

Answer 30

full agonist competitive antagonist

Question 31

what agonist type would you expect to see occupying mostly active state receptors but some resting state

Answer 31

partial agonist

Question 32

what is the result of the partial agonist only occupying most but not all of the active state receptors

Answer 32

lowered max response / partial response

Question 33

what drug type do you expect to see occupying an equal amount of active and resting state receptors

Answer 33

antagonist

Question 34

what agonist type would you expect to see only occupying resting state receptors

Answer 34

inverse agonist competitive antagonist

Question 35

what is the effect of an inverse agonist only occupying resting state receptors

Answer 35

produces the opposite effect of the agonist

Question 36

True or False: Drug response is a linear function of drug occupancy

Answer 36

true

Question 37

what occurs when a drug occupies all available receptors

Answer 37

maximal response

Question 38

when is a response from a drug terminated

Answer 38

when it dissociated from the receptor

Question 39

what is occupancy theory of a drug

Answer 39

maximal response is proportional the the drug-receptor complex bindings

Question 40

when does max response of a drug occur

Answer 40

when all receptors are occupied at equilibrium

Question 41

when there is no ligand present, how is the equilibrium balanced

Answer 41

lies far to the left

Question 42

what state of receptor do agonists have a higher affinity for

Answer 42

active state

Question 43

which dose-response relationship describes a drug effect that increases in proportion to an increasing drug dose

Answer 43

graded dose-response

Question 44

which dose-response is used to measure the effect of a drug on an individual person

Answer 44

graded dose-response

Question 45

what can a graded dose-response be used to determine

Answer 45

efficacy of a drug over time

Question 46

which dose-response relationship is used to describe a drug effect as present or absent

Answer 46

quantal dose-response

Question 47

which dose-response relationship should be determined with a population of people

Answer 47

quantal dose-response

Question 48

what does a quantal dose-response graph plot

Answer 48

rate of an outcome occurrence in a population against a drug dose

Question 49

besides drug effects on a population, what else can a quantal dose-response graph determine

Answer 49

toxic levels of a drug

Question 50

which dose-response relationship results in a greater magnitude of response as the dose increases

Answer 50

graded dose-response

Question 51

True or False: Using Quantal dose-response, a higher percentage of the population will be affected as the dose is increased

Answer 51

true

Question 52

when is a drug considered unsafe/toxic in terms of standard safety margin

Answer 52

drug has a low safety margin

Question 53

what is used to determine the standard safety margin

Answer 53

ED (effective dose) LD (lethal dose)

Question 54

what is used to evaluate the safety of a certain drug

Answer 54

therapeutic index

Question 55

what kind of receptor regulation is present when there is a loss of receptors present

Answer 55

downregulation

Question 56

what kind of regulation is present when there is an increase of receptors present

Answer 56

upregulation

Question 57

what is the outcome of upregulation

Answer 57

more sensitive to a hormone or neurotransmitter

Question 58

how is upregulation created

Answer 58

long term administration of an antagonist

Question 59

explain the process of using prolonged antagonistic drugs on upregulation

Answer 59

all represent receptors become blocked forcing the cells to create new receptors for ligands to bind to

Question 60

what causes downregulation

Answer 60

long term exposure to agonists

Question 61

what is the result of downregulation

Answer 61

decreased responsiveness