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Pharmacology Exam 1 > Units 1-2 > Flashcards

Units 1-2 Flashcards

1
Q

Define absorption:

A

The movement of a drug from its site of administration int the blood

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2
Q

When drugs are being absorbed what effects the onset and intensity of effects?

A

The route it is administered because each route has different barriers to absorption

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3
Q

What to categories signify the route or medications?

A
  • Enteral (via GI tract)

- Parenteral (outside of GI tract via “injection”)

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4
Q

Is oral (PO) administration Enteral or Parenteral?

A

Enteral

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5
Q

What routes of administration fall under parenteral?

A
  • IV
  • IM
  • Sub Q
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6
Q

How are oral drugs absorbed?

A

From intestine, stomach, or both

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7
Q

What does P-glycoprotein do in relation to oral administration?

A

-Can effect intestinal absorption by pumping drug back out

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8
Q

What are barriers to absorption with oral administration?

A
  1. layer of epithelial cells that lines GI tract

2. Capillary wall

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9
Q

Why is the layer of epithelial cells that lines the GI tract a barrier to oral administration of drug absorption?

A

Drugs absorbed from sites along GI tract must pass through liver before general circulation can occur

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10
Q

What are factors that determine the absorption of a drug administered orally?

A
  • Solubility and stability of drug
  • Gastric and intestinal pH
  • Food in gut
  • Co-administration of other drugs
  • Special coatings on drug preparation
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11
Q

What is important about IV drug absorption?

A

-No barrier to absorption

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12
Q

What is the only barrier to IM drug absorption?

A

-Capillary wall is only barrier

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13
Q

How do Sub Q drug get absorbed?

A

Enters blood by passing through spaces between cells of capillary wall

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14
Q

Why is there no barrier to absorption of IV drugs?

A

drug directly in blood stream

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15
Q

Is IV drug absorption instantaneous and complete?

A

Yes

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16
Q

The water solubility of a drug given IM and blood flow at site of IM injection determine what?

A

Rapid or slow absorption

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17
Q

Are there any significant barriers to Sub Q drug absorption?

A

No, similar to IM

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18
Q

Solubility of Sub Q drug and blood flow at Sub Q injection site are major determinants of what?

A

Rapid or slow absorption

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19
Q

The rate at which a drug undergoes absorption is influenced by what?

A
  • Physical and chemical properties of drug itself

- Physiologic and anatomic factors at absorption site

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20
Q

What are factors that impact absorption of a drug?

A
  • Rate of dissolution
  • Surface area
  • Blood flow
  • Lipid solubility
  • pH partitioning
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21
Q

How does the rate of dissolution effect drug absorption?

A

Drug must dissolve first, which determines rate of absorption

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22
Q

How does surface area effect dug absorption?

A

Larger surface area= faster absorption

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23
Q

How does blood flow effect drug absorption?

A

-more blood flow = quicker absorption

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24
Q

What is a concentration gradient in relation to drug absorption?

A

Amount of drug outside of the blood and amount drug in blood

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25
Q

How does lipid solubility effect the absorption of a drug?

A

Highly lipid-soluble drugs= quicker absorption

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26
Q

Why are lipid soluble drugs absorbed quicker?

A

Can easily cross membranes

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27
Q

Bioavailability is the amount of active drug that what?

A

Reaches the systemic circulation from its site of administration

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28
Q

Can different formulations of the same drug vary bioavailability?

A

Yes

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29
Q

What factors effect the bioavailability of a drug?

A
  • Tablet disintegration time
  • Enteric coating of tablet
  • Sustained release formulation (can make drug response variable)
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30
Q

Small spheres containing drug that release at different times is what type of drug?

A

Sustained Release (SR) drug

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31
Q

Protective coating absorbed in small intestine is what type of drug?

A

Enteric Coating (EC)

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32
Q

Differences in bioavailability occur primarily in what?

A

Oral preparations (usually too small to lack clinical importance)

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33
Q

Differences in bioavailability is the biggest concern with drug that have what?

A

A small therapeutic range

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34
Q

Why do drug with a small therapeutic range have bioavailability concerns?

A

Small changes can produce significant change in response (toxicity or therapeutic failure)

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35
Q

What are factors that impact distribution of a drug?

A
  • Albumin levels
  • Blood flow to tissues
  • Ability to exit vascular system
  • Ability to enter cells
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36
Q

Albumin is the main protein used in drug binging which made in the liver, if poor liver function what can happen to distribution of a drug?

A

Theres not enough albumin for drug to bind to and carry out desired effect

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37
Q

How does blood flow to tissued impact drug absorption?

A

Drugs are carried by blood flow to tissues and organs

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38
Q

Why is regional blood flow not typically an issue in drug distribution?

A

Most tissues are well perfused

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39
Q

Why are abscess and tumors a complication in the distribution of drugs?

A

They have limited blood supply

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40
Q

What is a drugs next step after being received from the blood?

A

Exiting the vascular system

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41
Q

Why is exiting the vascular system important for drug distribution?

A

Most drugs do not produce their effect in the blood need to get to site of action

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42
Q

Why is exiting the vascular system important for a drug in order to complete metabolism and excretion?

A

Yes

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43
Q

How do drugs leave the vascular system?

A

Via capillary beds (typically pass between not through_

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44
Q

What is the BBB?

A

Blood brain barrier

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45
Q

What is the name for unique capillaries in CNS?

A

BBB

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46
Q

Is the placenta a absolute barrier to drug distribution in the fetus?

A

No

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47
Q

Is protein binding important for a drug to leave the vascular system,?

A

Yes

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48
Q

What does BBB do?

A

Protect certain drug from effecting CNS

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49
Q

Why most some drugs enter cells during distribution?

A

To reach site of action

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50
Q

Why must all drugs enter cells during distribution at some point?

A

To undergo metabolism and excretion

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51
Q

The factors that allow drugs to enter cells are same as what allows them to cross membranes, what are these factors?

A
  • Lipid solubility
  • Presence of transport system
  • Or both
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52
Q

Many drugs do produce their action by binding with receptors on external surfaces of a cell and do not need to do what?

A

Cross the cell membrane to act

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53
Q

Is the liver one of the most important organs for protein making?

A

Yes

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54
Q

What is the most common/important protein?

A

Albumin

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55
Q

What is the name of the protein that is a large molecule which is forced to remain in the blood stream?

A

Albumin

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56
Q

Does albumin impact drug distribution?

A

Yes

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57
Q

Can drugs make reversible bonds with various proteins/

A

Yes

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58
Q

Can drugs be bound or unbound?

A

Yes

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59
Q

Even though drug can bind to albumin, only what will occur?

A

Only some drugs will be bound at any moment

60
Q

What does the percentage of drug molecules that are bound depend on?

A

Strength of attraction between albumin and the drug

61
Q

What is a consequence of protein binding?

A

Restriction of drug distribution

62
Q

Drugs bound to albumin can’t do what?

A

Leave bloodstream

63
Q

Because when drugs are bound to albumin they can’t leave the blood stream, what does this prolong and increase?

A
  • Distribution phase is prolonged

- drug half-life increases

64
Q

Protein binding can also be a source for what?

A

Drug interactions

65
Q

Because each albumin only have a few binding sites, this can be a source for what?

A

Drug interaction of unbound drugs?

66
Q

Drugs competing for binding sites can be a source for what?

A

Drug interactions

67
Q

Why can competition of protein binding cause potential for drug interactions?

A

When competing drugs may displace each other and cause serum drug levels to rise

68
Q

Can competition for binding sites increase intensity f drug responses?

A

Yes

69
Q

The rise of plasma drug levels can cause what?

A

Drug toxicity

70
Q

What decreased bioavailability, resulting in less ADRs and drug toxicity risk?

A

Increased protein binding?

71
Q

What increases bioavailability, resulting in more risk of ADRs and drug toxicity?

A

Decreased protein binding

72
Q

How does the BBB protect the body?

A

It has tight junction between cells and CNS (making hard to easily pass through)

73
Q

How can drug get around the BBB?

A
  • Be lipid soluble to pass through cell wall

- or be able to use existing transport system

74
Q

Receptors are special chemical sites in the body that most drugs do what with?

A

Interact to produce effect

75
Q

Can many cellular components be considered drug receptors?

A

Yes

76
Q

Is binding to a receptor usually reversible?

A

Yes

77
Q

When a drug binds to a receptor it will do what?

A

Mimic or block body’s regulatory molecules

78
Q

Do drugs help the body help itself?

A

Yes

79
Q

Because drugs can only mimic or block its own regulatory molecules, this means what?

A

Drugs can’t give cells new function

80
Q

The enzymatic alteration of drug structure is called what?

A

Drug metabolism

81
Q

Drug metabolism most often takes place where?

A

Liver

82
Q

Hepatic Drug-Metabolizing Enzyme works through what?

A

Hepatic microsomal enzyme system/ P450 system

83
Q

The hepatic microsomal enzyme system/P450 system is capable of what?

A

Catalyzing a wide variety of drug reactions

84
Q

What does P450 refer to?

A

Cytochrome

85
Q

Cytochrome P450 is a key component of what?

A

The hepatic microsomal enzyme system/P450 system

86
Q

Drug metabolism does not always result in breakdown of a drug, it can also result in what?

A

Formation of a large parent drug

87
Q

The time required for the amount of drug in the body to decrease by 50% is called what?

A

Serum half-life

88
Q

What does the serum half-life determine?

A

Dosing intervals

89
Q

A short-half life means what?

A

Drug leaves quickly

90
Q

A long half-life means what?

A

Drug leaves slowly

91
Q

Explain Morphine if it has a half-life of 3 hours:

A
  • body stores morphine will decrease by 50% in 3 hours regardless of how much in body
  • 50mg would equal 25mg in 3 hours
92
Q

When the liver metabolizes drugs to such an extent that only a small amount of active drug emerges is called what?

A

First pass effect

93
Q

Does the first pass effect decrease therapeutic effect?

A

Yes

94
Q

What may need to be changed in relation to the first pass effect on a drugs therapeutic effect?

A

Dose may need to be increased

95
Q

The “first pass” through the liver can cause rapid inactivation of some oral drugs which does what?

A

Greatly reduces the availability of the drug

ex: drug may be need to be 1-2mg IV, 4mg IM, and 10mg Oral

96
Q

Does the first pass effect have an impact in drug bioavailability?

A

Yes

97
Q

The first pass effect may cause a too low of drug dose to not produce therapeutic effects why?

A

Not enough drug made it ti bloodstream to produce desired response

98
Q

What labs are we concerned about related to drug metabolism?

A
  • AST
  • ALT (very liver specific)
  • Alkaline phospatase
  • Bilirubin
  • GGT
99
Q

Is cytochrome p450 system a single molecular entity?

A

No

100
Q

Is the cytochrome P450 system a group of 12 closely related enzyme families?

A

Yes

101
Q

3 of the cytochrome p450 enzyme families do what?

A

Metabolize drugs (CYP1, CYP2, CYP3)

102
Q

CYP1, CYP2, and CYP3 are each composed of multiple form that only do what?

A

Metabolize certain drugs

103
Q

What do the other 9 enzyme families of the cytochrome p450 family do?

A

metabolize endogenous compounds (steroids, fattty acids, etc)

104
Q

Taking multiple drugs with the same metabolizing enzyme a decrease dose or what will happen?

A

bioavailability will increase and possibly cause drug toxicity

105
Q

Drugs that act on the liver to increase rates of drug metabolism are called what?

A

inducers (enzyme induction)

106
Q

What consequences of inducers?

A
  • they can also increase their own rate of metabolism

- can accelerate metabolism of other drugs

107
Q

Drugs that act on liver to decrease rates of drug metabolism are called what?

A

Inhibitors (enzyme inhibition)

108
Q

What are consequences of inhibitors?

A

-Slower metabolism= increase active drug accumulation; and can lead to increase risk of ADRs and toxicity

109
Q

What is excretion of a drug?

A

Removal of drug from the body

110
Q

What is excretion of a drug carried out through?

A
  • Urine
  • Sweat, saliva (small amount)
  • Breast milk
  • Bile
  • Expired Air (anesthetics)
111
Q

Are most drugs excreted through the kidneys?

A

Yes

112
Q

What facilitates the removal of a drug through the kidneys?

A
  • Glomerular filtration
  • Passive tubular transport
  • Active tubular secretion
113
Q

What labs are we concerned about in relation to excretion (renal function)?

A
  • GFR
  • BUN
  • Creatinine
  • I & O’s
114
Q

Drug receptors change in response to what?

A

Inhibition and activation

115
Q

Continuous exposure of a receptor to a drug causes what with time?

A

Desensitized or refractory “down regulation”

116
Q

What does a receptor being desensitized or refractory “down regulation” mean?

A

Receptor becomes less responsive

117
Q

Continuous exposure of a receptor to an antagonist causes what?

A

hypersensitivity

118
Q

Does an “empty stomach” require fasting?

A

No

119
Q

What does take a drug on a empty stomach mean?

A

-1 hour before meal
or
-2 hours after a meal

120
Q

May a drug need to be taken on an empty stomach due to acidity needs?

A

Yes

121
Q

Do some drugs need to be taken on a empty stomach due to possible drug/food interactions?

A

Yes

122
Q

What does the range of plasma drug levels which fall between the MEC and the toxic concentration signify?

A

The therapeutic index of that drug

123
Q

What does MEC mean?

A

minimum effective concentration

124
Q

When there is enough drug present to produce therapeutic responses but not so many as to cause toxicity, what is this achieving?

A

Plasma drug level in a therapeutic range

125
Q

How is therapeutic range calculated?

A

By ratio of drugs LD50 to its ED50

126
Q

The average lethal dose in 50% of the animals treated is called the what?

A

LD50

127
Q

The median effective dose that produces a specific effect in 505 of population is called what?

A

ED50

128
Q

TD divided by Ed equals what?

A

Therapeutic dose

129
Q

The smaller the therapeutic dose number the more what?

A

Dangerous the drug is

130
Q

A drug with a wider/larger therapeutic index means what?

A

Safer the drug is

131
Q

A drug with a smaller/more narrow therapeutic index means what?

A

Less safe the drug is

132
Q

A nurse who is aware of drugs with narrow therapeutic range which are most likely to require intervention for drug related complications, can focus on what?

A

Additional attention need to monitor these patients for S/S of toxicity

133
Q

What a drug-drug risk of interaction directly proportionate to?

A

number of drugs and individual is taking

134
Q

For safety how should you monitor drugs with a narrow therapeutic range?

A

check labs for serum drug levels

135
Q

The more drugs a person is taking puts them at more risk for what?

A
  • drug toxicity

- drugs that decrease effectiveness of each other

136
Q

When the combined effect of two drugs exceeds the expected additive effect of each the drugs administered independently , then one drug is said to be what over the other?

A

Potentiative

137
Q

When a drug decreased the metabolism of other drugs what are they called?

A

Inhibitory drugs (sometimes desired)

138
Q

A medication that mimics the action of the signal ligand by binding to and activating a receptor is called a what?

A

Agonist

139
Q

A medication that typically binds to a receptor without activating them, which instead decreased the receptors ability to be activated by other agonists is called a what?

A

Antagonist

140
Q

What are 3 ideal drug properties?

A
  • Effectiveness (most important)
  • Safety
  • Selectivity
141
Q

When a drug produces a response for which it was given means the drug has what?

A

Effectiveness

142
Q

When a drug can’t produce harm even at high doses and for prolonged periods, means the drug is what?

A

Safe

143
Q

In regards to safety do all drugs have benefits and risks?

A

Yes

144
Q

When a drug produces only the response for which it was given means the drug is what?

A

Selective

145
Q

Is complete drug selectivity possible?

A

No all drugs have side effects

146
Q

What are other ideal properties of a drug?

A
  • Reversible action
  • Predictability
  • Ease of administration
  • Freedom of drug interactions
  • Low cost
  • Chemical stability
  • Simple generic name

Pharmacology Exam 1 (4 decks)

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