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Pharmacology I > Test 1 Part II > Flashcards

Test 1 Part II Flashcards

1
Q

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

A

weak; strong

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2
Q

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

A

hydrophobic

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3
Q

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

A

weak

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4
Q

most receptors are _______________

A

proteins

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5
Q

receptors determine:

A
  1. relationship between dose and effect
  2. selectivity of drug action
  3. actions of agonist and antagonists
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6
Q

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

A
  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
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7
Q

what are the different types of receptors

A

ligands
regulatory proteins
enzymes
transport proteins
structural proteins
spare receptors

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8
Q

ligand receptor type

A

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

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9
Q

regulatory protein receptor types

A

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

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10
Q

what receptor types do we know the most about

A

regulatory proteins

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11
Q

enzyme receptor type

A

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

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12
Q

spare receptor type

A

available receptors after the max effect of a drug is achieved

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13
Q

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

A

affinity

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14
Q

what is affinity?

A

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

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15
Q

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

A

high affinity

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16
Q

increased affinity = ___________ potency

A

increased

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17
Q

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

A

potency

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18
Q

Drugs are defined by their _____________

A

potency

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19
Q

increased potency = ____________ EC50

A

decreased

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20
Q

what is EC50

A

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

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21
Q

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

A

concentration (of the drug)

22
Q

increased affinity = ___________ potency = ____________EC50

A

increased; decreased

23
Q

define potency

A

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

24
Q

define efficacy

A

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

25
Q

what is efficacy dependent upon?

A

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

26
Q

drug choices are made based on ______________ rather than ______________

A

efficacy; potency

27
Q

what is intrinsic activity

A

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

28
Q

intrinsic activity is independent from _________________

A

affinity

29
Q

maximal attainable response is represented by what numerical value?

A

1.0

30
Q

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 _______________

A

agonist; antagonist

31
Q

_____________________ is used to classify drugs as agonist or antagonists

A

intrinsic activity

32
Q

intended/therapeutic response

A

response given to a drug that is observed in most patients

33
Q

idiosyncratic response

A

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

34
Q

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

A

idiosyncratic

35
Q

hyporeactive response

A

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

36
Q

hyperreactive response

A

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

37
Q

hypersensitive response

A

allergic or immunological response to a drug

38
Q

tolerance (drug response)

A

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

39
Q

tachyphylaxis (drug response)

A

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

40
Q

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?

A

tachyphylaxis

41
Q

paradoxical effect of a drug

A

opposite effect than intended

42
Q

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

A

paradoxical

43
Q

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

A
  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
44
Q

a patients response to a drug can be altered by

A
  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)
45
Q

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

A

upregulation

46
Q

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 ____________________

A

up-regulation

47
Q

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

A

down-regulation

48
Q

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

A

selectivity

49
Q

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

A

selectivity

50
Q

T/F: side effects are a category of selectivity

A

false

Pharmacology I (16 decks)

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