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N5: Pharmacology > LESSON 2: Uses, Actions, & Interactions of Drugs in the Body > Flashcards

LESSON 2: Uses, Actions, & Interactions of Drugs in the Body Flashcards

1
Q

what refers to the long-term reductions in receptor number due to continuous agonist?

A

downregulation

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2
Q

what refers to what occurs when receptor activation is blocked for prolonged periods by pharmacologic antagonist or by denervation?

A

upregulation

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3
Q

what deals with a mathematical description of rates of drug movement into, within, and exit from the body, and tells us what dose to give to the patient in order to achieve a concentration that will elicit a response?

A

pharmacokinetics

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4
Q

pharmacokinetics helps to determine the correct dosage to give to achieve the correct therapeutic concentration so there will be ________ and ________.

A

less toxicity, excreted properly

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5
Q

the drug should enter _______ as they are the primary means of transport of various materials in the body.

A

blood vessels

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6
Q

what are the two things that prevent drug accumulation?

A

metabolism and excretion

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7
Q

as the drug enters the __________, it is distributed to different areas of the body depending on its selectivity before it exert its action at the target site.

A

systemic circulation.

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8
Q

what deals with relating the dose or concentration to the response?

A

pharmacodynamics

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9
Q

what deals with the relationship between the dose and the concentration that is achieved by the body?

A

pharmacokinetics

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10
Q

what is the percentage of the administered dose of a drug that reaches the circulation?

A

bioavailability

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11
Q

high bioavailability is when?

A

most of the administered dose goes to the systemic circulation

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12
Q

what are the three things that affect bioavailability?

A

type of drug, route through which it is given, the metabolic processes it undergoes before reaching the systemic circulation

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13
Q

what type of drugs are 100% bioavailable?

A

IV drugs

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14
Q

what is the name of the phenomenon when the drug is not yet in the systemic circulation and gets metabolized at a specific location in the body resulting in a reduced concentration of the active drug upon reaching its target site or the systemic circulation?

A

first pass effect

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15
Q

what are the 4 things that affect the distribution of drugs to its site of action?

A

its structure, lipophilicity or hydrohilicity, drug properties, affinity towards albumin or its transporter protein

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16
Q

what is the type of drug that is not attached to the binding site and is able to go to the target tissues where it would exert its action?

A

free drug

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17
Q

this is achieved between the distribution of the drug in the systemic circulation and the tissues up to a point where it reaches its organ of elimination?

A

equilibrium

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18
Q

metabolism usually occurs where?

A

liver

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19
Q

excretion usually occurs where?

A

kidneys

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20
Q

what is the movement of drug from the site of administration to systemic circulation?

A

absorption

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21
Q

what is the transport of drug in the bloodstream and into organs and tissues?

A

distribution

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22
Q

what is the biotransformation of drug in the body?

A

metabolism

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23
Q

what is the elimination of the drug or its compound from the body?

A

excretion

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24
Q

when you a drug _________, its concentration in the systemic circulation is already ________.

A

intravenously, high

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25
Q

what is the movement of drugs into the body, through Fick’s Law (Passive Diffusion)?

A

absorption

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26
Q

the movement of drugs into the body is dependent on what two things?

A

thickness of the membrane, permeability

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27
Q

what is the passive movement through membranes and other lipid structures?

A

lipid diffusion

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28
Q

in order for lipid diffusion to occur, the structure needs to be ______ meaning they can cross the membrane because they are lipophilic.

A

unionized

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29
Q

weak ______ are ionized in an acidic environment meaning they cannot cross membrane

A

bases

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30
Q

weak _____ are not ionized in an acidic environment meaning they can cross membrane.

A

acids

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31
Q

transport by special carriers are what?

A

not governed by Fick’s Law, capacity limited

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32
Q

what is it called when binding to receptors on cell membranes, internalization by infolding of membrane, and contents are released from intracellular vesicle happens?

A

endocytosis, pinocytosis

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33
Q

______ absorption until it is taken in to the systemic circulation.

A

slow

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34
Q

upon entering the blood vessels, the specific concentration should ideally fall where?

A

desired therapeutic range.

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35
Q

why is falling the desired therapeutic range ideal?

A

this range has been proven to elicit desired response.

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36
Q

at a certain time in the duration of action, the concentration should be ______ the desired therapeutic range.

A

within

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37
Q

the concentration should not be _______ as to be toxic, but not ______ as to be ineffective.

A

too high; too low

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38
Q

concentration should be above the _____________________ which is determined by the dose and the elimination of the drug.

A

minimum effective concentration.

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39
Q

what is the area called when the entire concentration of the drug inside the body that will have an effect and elicit a specific response, and is important in calculating bioavailability?

A

area under the curve (AUC)

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40
Q

what is it called when 2 drugs that have been marketed at different times need to have the same bioavailability?

A

bioequivalence

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41
Q

what route has 75 to ≤100% bioavailability, where large volumes are often feasible but may be painful?

A

intramuscular (IM)

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42
Q

what route has 75 to ≤100% bioavailability, where it is given at smaller volume than intramuscular, and may be painful?

A

subcutaneous (SC)

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43
Q

what route has 5 to <100% bioavailability, and it is most convenient, and first pass may be significant?

A

oral (PO)

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44
Q

what route has 30 to <100% bioavailability, and has less first pass compared to oral?

A

rectal (PR)

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45
Q

what route has 5 to <100% bioavailability, and is often very rapid onset?

A

inhalation

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46
Q

what route has 80 to ≤100% bioavailability, and is used for lack of first pass effect, and usually very slow absorption?

A

transdermal

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47
Q

the form of medication will determine what?

A

its route of administration

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48
Q

the composition of medication is designed to enhance its what?

A

absorption and metabolism

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49
Q

what refers to the volume of where the drug is distributed in the body, and the ration of the amount of drug in the body to its concentration in the plasma or blood?

A

volume of distribution

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50
Q

if there is ___ initial concentration or concentration in the blood, the volume of distribution is ____ because the drug travels to different areas.

A

low; high

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51
Q

what type of drugs usually have a high volume of distribution?

A

lipophilic drugs

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52
Q

drugs are distributed to areas that have _____, such as the heart, liver, kidneys, and brain?

A

extensive blood supplies

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53
Q

why are sites like bone and brain difficult for drugs to reach?

A

due to either poor blood supply or barriers

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54
Q

what are the three areas of slower drug distribution?

A

muscles, skin, fat

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55
Q

what drugs are the ones that get access to the tissues where they will exert their effects?

A

free drugs

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56
Q

what drugs will not exert any effect?

A

protein-bound drugs

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57
Q

what are the 4 determinants of distribution?

A

size of the organ, blood flow, solubility, binding

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58
Q

what is the biochemical reaction involving a parent drug, and takes place mainly in the liver and produces: an inactive metabolite, a more soluble compound, and a more potent metabolite?

A

biotransformation

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59
Q
  1. what phase reaction includes Cytochrome P450 enzymes, and oxidation, deamination, desulfuration, reduction, and hydrolysis?
A

phase I reaction

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60
Q

what phase reaction includes conjugation, glucuronidation, acetylation, and sulfation, and usually renders drug polar and excretable?

A

phase II reactions

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61
Q

which labs will the nurse review if there is a concern about the patient’s ability to metabolize drugs?

A

liver

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62
Q

what are the 3 organs that contribute to the important process of eliminating drugs from the body?

A

kidneys, liver, bowel

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63
Q

what is the term that refers to the volume of drug that is cleared of the drug, and reveals the function of a kidney?

A

clearance

64
Q

what is the rate of elimination that is proportionate to the drug concentration. and where clearance is constant?

A

first-order elimination

65
Q

what is the rate of elimination that is proportionate to the drug concentration. and where clearance is constant?

A

first-order elimination

66
Q

what is it called when the amount of drug eliminated is constant regardless of concentration?

A

zero-order elimination

67
Q

what is the condition in which the rate of the drug elimination is equals the rate of administration, determines dosing intervals, and is reached after 4-5 half-lives?

A

steady-state concentration

68
Q

what is the measure of the rate at which drugs are removed from the body?

A

half-life

69
Q

most drugs are considered to be effectively removed after about how many half-lives?

A

five half-lives

70
Q

a drug should be ______ minimum effective concentration, and ______ toxic dose.

A

above; below

71
Q

what is the time it takes for the drug to elicit a therapeutic response?

A

onset of action

72
Q

what is the time it takes for the drug to elicit a therapeutic response?

A

onset of action

73
Q

what is the time it takes for a drug to reach its maximum therapeutic response?

A

peak effect

74
Q

what is the time a drug concentration is sufficient to elicit a therapeutic response?

A

duration

75
Q

what is the lowest blood level of a drug?

A

trough

76
Q

half-life is constant in ____ order kinetics, while not useful in _____ order kinetics.

A

first; zero

77
Q

TRUE OR FALSE. Furosemide, Dobutamine, and Milrinone are drugs for heart failure.

A

TRUE

78
Q

antiviral drug with potential to treat SARS-CoV-2 infections; decrease the length of stay in the hospital

A

Remdesivir

79
Q

addresses cytokine storm and an IL-6 inhibitor

A

Tocilizumab

80
Q

an anticoagulant that addresses the potential thromboembolism in the patient

A

Enoxaparin

81
Q

what deals with therapeutic uses and effects of drugs?

A

pharmacotherapeutics

82
Q

ordered by the physician and administered by the nurse

A

drugs in the treatment of disease

83
Q

concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease especially in humans

A

Medical Pharmacology

84
Q

any substance that can affect or lead to a biological response through chemical action

A

drug

85
Q

drugs that end on “-mab”

A

monoclonal antibodies

86
Q

drugs that are chemically derived

A

small molecules or small molecule drugs

87
Q

big drugs with a lot of protein components; produced through a biologic system or a living organism

A

biologic agents or biologic agent drugs or biologics

88
Q

frontline in detecting adverse drug events and possible drug interactions

A

nurses

89
Q

what are the steps in prescribing a drug?

A

Step 1: Define the patient’s problem
Step 2: Specify the therapeutic objective/s
Step 3: Verify the sustainability of the P-treatment / Select appropriate P-Drug
Step 4: Start the treatment / Initiate Therapy (Write a Prescription)
Step 5: Give information, instructions, and warnings
Step 6: Monitor and/or stop treatment

90
Q

what are the goals of therapy?

A. eradicate disease and minimize the impact of disease in the patient’s life
B. relieve symptoms and minimize the potential for adverse effects of the medication
C. prevent disease progression and prevent morbidity and mortality
D. all of the above

A

D.

91
Q

what is the aim of minimizing the impact of disease in the patient’s life?

A

fewer complications

92
Q

what are the five therapeutic objectives?

A
  1. eradication of virus
  2. relief of symptoms
  3. decrease morbidity and mortality
  4. prevent complications
  5. minimize drug adverse effects
93
Q

basis of this concern would be pharmacodynamics

A

efficacy

94
Q

basis of this concern would be pharmacodynamics and pharmacokinetics

A

safety

95
Q

give the seven problems in pharmacotherapeutics

A
  1. medication errors
  2. suboptimal use
  3. unnecessary therapy
  4. therapeutic duplication
  5. unrecognized interactions
  6. drug allergies
  7. adverse effects
96
Q

when do medication errors occur?

A

during prescribing, transcribing, administration of medication

97
Q

a reaction between two (or more) drugs

A

drug-drug interaction

98
Q

what causes adverse effects of drugs?

A

individual variation of responses to drugs

99
Q

what are the two factors that affect response to medication?

A

(1) drug factors pharmacologic properties and (2) patient factors

100
Q

TRUE OR FALSE. Drug factors pharmacologic properties corresponds to the following questions:
Right Drug? Right Route? Right Dose?

A

TRUE

101
Q

what are the physiologic variables that can affect specific drugs?

A

age, sex, genetic pattern

102
Q

what are the pathophysiologic differences that can affect specific drugs?

A

disease state and severity, comorbidities, concurrent medications

103
Q

what is the effect of drug on the body?

A

pharmacodynamics

104
Q

integration of molecular actions into effect on the body

A

mechanism of action

105
Q

dose-response relationship

A

quantitative terms

106
Q

can either be receptor-mediated or non-receptor-mediated

A

chemical action

107
Q

TRUE OR FALSE. Rarely, the actions of drugs are receptor-mediated.

A

FALSE. The actions of drugs are MOSTLY receptor-mediated.

108
Q

pharmacodynamics is largely based on the concept of __________

A

drug-receptor binding

109
Q

drug gets to the _______ circulation and to the site of action once administered.

A

systemic

110
Q

TRUE OR FALSE. A lot of drugs in the same target of action can increase effectiveness.

A

FALSE. A lot of drugs in the same target of action can increase toxicity.

111
Q

receptors largely determine the quantitative relations between ________ of drug and ________

A

dose or concentration; pharmacologic effects

112
Q

specific molecules in a biologic system with which drugs interact to produce changes in the function of the system

A

receptors

113
Q

where are receptors found?

A

inside the lipid membrane, within the lipid membrane, or inside the cell

114
Q

what are receptors responsible for?

A

selectivity (LOCK AND KEY fashion) of drug actions

115
Q

receptor and ligand would be selective

A

LOCK AND KEY fashion

116
Q

a physiologic response is elicited from the LOCK AND KEY fashion

A

agonist/activator

117
Q

inhibit the binding of the ligand which can activate the receptor, and thus, in a way, the receptor is deactivated

A

antagonist

118
Q

molecular interactions by which drugs exert their effects

A

drug-receptor interaction

119
Q

molecule to which a drug may bind without changing any function, e.g. albumin binding

A

inert binding molecule or site

120
Q

binds drugs

A

albumin

121
Q

receptors determine the quantitative relations between drug concentration and pharmacologic response

A

occupational theory of drug action

122
Q

many drugs are classified on the basis of their ________.

A

primary receptor affinity

123
Q

TRUE OR FALSE. Drug receptors are coupled with effectors.

A

TRUE

124
Q

molecules that translate the drug-receptor interaction into a change in cellular activity

A

effectors

125
Q

what are the four types of receptors?

A

Ligand-regulated ion channel, G protein-coupled receptors, Receptor Protein Kinases, Intracellular receptor

126
Q

a type of receptor that contribute to synaptic plasticity; effect in milliseconds

A

Ligand-regulated ion channel

127
Q

are metabotropic receptors

A

G protein-coupled receptors

128
Q

what is the receptor of drugs that are lipophilic (non-polar) and can cross the membrane easiest?

A

Intracellular receptor

129
Q

how long is the lag period of intracellular receptors?

A

30 minutes to 1 hour

130
Q

______ can open the area in the DNA-binding domain and cause the transcription of specific genes

A

binding of the steroid

131
Q

what will lead to the release of a heat shock protein that’s inhibiting the transcription of DNA-binding domain?

A

activating or binding to the intracellular receptor

132
Q

what makes proteins and leads to specific physiologic responses?

A

translation

133
Q

the receptor itself is in the membrane and it is an enzyme

A

receptors on membrane spanning enzymes

134
Q

bind separate tyrosine kinase molecules; associated with an enzyme inside the cell

A

receptors located on membrane-spanning molecules

135
Q

based on chemical or physical properties

A

non-receptor mediated drug action

136
Q

what are the four types of non-receptor mediated drug action?

A

metal chelators, alkalinizing drugs, acidifying drug, osmotic diuretcs

137
Q

the response to a drug is proportional to the concentration of the receptors that are bound (occupied) by the drug

A

dose-response relationships

138
Q

two major types of dose-response relationships

A

(1) graded and (2) quantal

139
Q

concentration (log) during graded-dose relationships

A

X-axis

140
Q

response during graded-dose relationships

A

Y-axis

141
Q

concentration at which the drug elicits 50% of its maximal response

A

Potency (EC50)

142
Q

maximal response produced by the drug

A

Efficacy (Emax)

143
Q

equal to the concentration of drug that binds 50% of the receptors in the system

A

Kd

144
Q

maximal response is possible without 100% receptor occupancy

A

spare receptors

145
Q

relating the concentration and the number of the population that responds to a specific or determined response

A

quantal dose-response graph

146
Q

the concentration or dose that causes a specified response in
50% of the population under study

A

ED 50

147
Q

median toxic dose; dose required to produce a particular toxic
effect in 50% of animals

A

TD50

148
Q

median lethal dose; dose required to produce a particular toxic

A

LD50

149
Q

Activates receptor with maximal efficacy

A

full agonist

150
Q

activates receptor, but not with maximal efficacy

A

partial agonist

151
Q

inactivates constitutively active receptor

A

inverse agonist

152
Q

decreases agonist potency by binding reversibly to active site of receptor

A

competitive agonist

153
Q

decreases agonist efficacy by binding to site other than active site of the receptor

A

noncompetitive allosteric antagonist

154
Q

decreases agonist efficacy by binding irreversibly to active site of receptor

A

noncompetitive active site antagonist

155
Q

Receptors are dynamically regulated in

A

location, and sensitivity

156
Q

loss of response of tissues following repeated or continuous administration of drugs

A

tachyphylaxis

157
Q

agonist-bound receptors may be internalized by _____________.

A

endocytosis

N5: Pharmacology (7 decks)

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