Test 1 Part II

Question 1

drugs that bind via __________ bonds are more selective than drugs that bind via _________________ bonds

Answer 1

weak; strong

Question 2

which drug-receptor bond is important to the interactions of highly lipid-soluble drugs

Answer 2

hydrophobic

Question 3

_____________ drug-receptor bonds require a very precise fit in order for a reaction to occur

Answer 3

weak

Question 4

most receptors are _______________

Answer 4

proteins

Question 5

receptors determine:

Answer 5

1. relationship between dose and effect
2. selectivity of drug action
3. actions of agonist and antagonists

Question 6

how do receptors determine the relationship between dose and effect of a drug?

Answer 6

1. affinity for binding determines the concentration of the drug required for a biological response
2. Total # of receptors may limit the maximal effect a drug can produce

Question 7

what are the different types of receptors

Answer 7

ligands
regulatory proteins
enzymes
transport proteins
structural proteins
spare receptors

Question 8

ligand receptor type

Answer 8

a signal triggering molecule binding to a site on a target protein to serve a biological purpose

Question 9

regulatory protein receptor types

Answer 9

mediate the actions of endogenous chemical signals from NT, autocoids, and hormones

Question 10

what receptor types do we know the most about

Answer 10

regulatory proteins

Question 11

enzyme receptor type

Answer 11

an endogenous receptor that may be inhibited or activated by binding to a drug

Question 12

spare receptor type

Answer 12

available receptors after the max effect of a drug is achieved

Question 13

_______________ is measured by the concentration of drug that is needed for drug-receptor binding

Answer 13

affinity

Question 14

what is affinity?

Answer 14

the lowest concentration of drug to occupy 50% of the receptors

Question 15

______________ = presence of low concentration of drug that produced drug - receptor binding

Answer 15

high affinity

Question 16

increased affinity = ___________ potency

Answer 16

increased

Question 17

binding affinity can be related to drug ________________, as seen in dose-response curves

Answer 17

potency

Question 18

Drugs are defined by their _____________

Answer 18

potency

Question 19

increased potency = ____________ EC50

Answer 19

decreased

Question 20

what is EC50

Answer 20

the effective concentration required to produce 50% of that drugs maximal response

Question 21

the higher the affinity of a drug to its receptor, the less ______________ required

Answer 21

concentration (of the drug)

Question 22

increased affinity = ___________ potency = ____________EC50

Answer 22

increased; decreased

Question 23

define potency

Answer 23

Very closely related to EC50. Just the concentration or dose required for 50% of the drugs max response. As EC50 drop potency goes up.

Question 24

define efficacy

Answer 24

the ability of the drug-receptor complex to activate signal transduction –> biological response

Question 25

what is efficacy dependent upon?

Answer 25

the ability of a drug to induce conformation change in the shape of the receptor that leads to ST and BR

Question 26

drug choices are made based on ______________ rather than ______________

Answer 26

efficacy; potency

Question 27

what is intrinsic activity

Answer 27

the measure of the magnitude/intensity of a biologic response produced by the EC100 relative to the maximal attainable response produced in target tissues

Question 28

intrinsic activity is independent from _________________

Answer 28

affinity

Question 29

maximal attainable response is represented by what numerical value?

Answer 29

1.0

Question 30

the closer an alpha value of drug is to 1.0 is more of a _______________; while closer to 0.0 it is more of a _______________

Answer 30

agonist; antagonist

Question 31

_____________________ is used to classify drugs as agonist or antagonists

Answer 31

intrinsic activity

Question 32

intended/therapeutic response

Answer 32

response given to a drug that is observed in most patients

Question 33

idiosyncratic response

Answer 33

infrequently observed and unintended response to a drug. usually caused by genetic differences in metabolism of drug

Question 34

give a medication to make patient stop sneezing, and it makes them stop coughing instead. This is an example of what type of response

Answer 34

idiosyncratic

Question 35

hyporeactive response

Answer 35

quantifiable response to a given dose of a drug that is diminished when compared to the response observed in most patients

Question 36

hyperreactive response

Answer 36

quantifiable response to a given dose of a drug that is increased when compared to the response observed in most patients

Question 37

hypersensitive response

Answer 37

allergic or immunological response to a drug

Question 38

tolerance (drug response)

Answer 38

decreased response to a drug as a consequence of continued administration/usage

Question 39

tachyphylaxis (drug response)

Answer 39

a rapid decline in response to administration of a drug. give once works great, then 2nd exposure does not work at all

Question 40

you give a patient a steroid injection for pain in the back. the first time you do it the patient claims it worked great, so they come back to get another when it flared up again. This time; however, the patient claims there was no relief, like it didnt work. This would be an example of what type of drug response?

Answer 40

tachyphylaxis

Question 41

paradoxical effect of a drug

Answer 41

opposite effect than intended

Question 42

you give propranolol to decrease a patients heart rate, but it causes the patients heart rate to rise more. This is an example of what type of drug effect

Answer 42

paradoxical

Question 43

what are all the things a provider should consider when choosing a drug to administer?

Answer 43

1. age of pt 2. sex of pt 3. body size of pt 4. disease state (liver/kidney compromise?) 5. genetic factors 6. simulatneous administration of other drugs

Question 44

a patients response to a drug can be altered by

Answer 44

1. inherited drug metabolizing enzymes 2. interruptions in the active transport of the drug from the cytoplasm 3. physiologic conditions that alter the endogenous receptor ligands (runner/athlete, pheochromocytoma, htn) 4. alterations in the # or function of receptors 5. changes in the components responsible for completing the DR complex (wrong dx, compensatory mechanism activity)

Question 45

antagonist binds to receptor causing hypostimulation, then the body compensates for the depressive effect by generating more receptors, this is called ___________________

Answer 45

upregulation

Question 46

propranolol fx as antagonist to decrease HR, if you abruptly withdraw this medication from the patient, it can result in rebound effects, like SVT, this is due to ____________________

Answer 46

up-regulation

Question 47

_____________________ is when the body recognizes the stimulation of an agonist and tries to compensate for the increased effects by removing some of the receptors

Answer 47

down-regulation

Question 48

the ________________ of a drug is what identifies its usefulness in medicine

Answer 48

selectivity

Question 49

the action of a drug binding to one or a few types of receptors more tightly than others describes its __________________

Answer 49

selectivity

Question 50

T/F: side effects are a category of selectivity

Answer 50

false