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316 Pharmacology > Exam 1: Pharmacokinetics & Pharmacodynamics > Flashcards

Exam 1: Pharmacokinetics & Pharmacodynamics Flashcards

1
Q

Pharmacokinetics

A

what happens to a drug from the time it enters the body until the parent drug and all metabolites have left the body

-“What the body does to the drug”

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2
Q

Pharmacodynamics

A

Drug actions on target cells, with resulting alterations in cellular biochemical reactions and functions

  • “What the drug does to the body”
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3
Q

Four processes involved in pharmacokinetics

A

Absorption
Distribution
Metabolism (Biotransformation)
Excretion (Elimination)

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4
Q

Absorption is…

A

the movement of the drug from its site of administration into the bloodstream

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5
Q

What determines how soon effects will begin?

A

The route the drug takes

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6
Q

What mode of administration is rapid?

A

Drugs that are administered IM or SQ are absorbed by small capillaries fairly rapidly

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7
Q

What mode of administration take the longest to be absorbed

A

Orally (PO)

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8
Q

Drugs administered intravenously do not _____

A

Need to be absorbed and/or are instantly absorbed

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9
Q

If a drug is administered in solid form, what must first happen?

A

Disintegration and dissolution of the medication, needs to become liquid!

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10
Q

What must happen to the medication before it can cross the cellular membranes

A

Medication must become a liquid before it can cross cellular membranes

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11
Q

What promotes disintegration and dissolution of most drugs?

A

Gastric acidity

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12
Q

What slows disintegration

A

Food in the GI tract

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13
Q

Hydrolysis and medication

A

Taking medication with water promotes disintegration

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14
Q

What helps protect against gastric acid

A

Enteric coatings resist disintegration

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15
Q

Once dissolved, PO medications must

A

Pass THROUGH the cell membranes of the GI tract

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16
Q

How can drugs pass through the cell

A
  1. directly penetrate via diffusion, most drugs use this route
  2. transport system (may or may not use ATP)
  3. channels and pores (very small compounds such as ions)
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17
Q

What type of cell is able to diffuse

A

lipophilic

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18
Q

After crossing GI epithelial cells, medications

A

Cross capillary wall (endothelial cells) and into circulation

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19
Q

order of drug passing through body

A 
Absorbed from GI tract 
To hepatic portal circulation 
Liver 
superior vena cava 
Heart 
lungs 
heart 
general circulation (distribution)
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20
Q

After entering the bloodstream from the GI system, the drug is carried

A

to the liver by the portal system before it reaches systemic circulation

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21
Q

What system protects the body from systemic effects of ingested toxins?

A

hepatic portal circulation serves to protect the body

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22
Q

How does the portal circulation protect the body

A

Delivering these substances to the liver for detoxification

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23
Q

First pass effect

A

Drugs that are extensively metabolized in the liver with only part of the dose reaching the systemic circulation

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24
Q

Drug distribution is

A

the movement throughout the body to its site of action

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25
Q

After absorption, the drug

A

Must reach the target organ at therapeutic level in order to have desired response

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26
Q

Distribution is determined by three major factors

A

Blood flow to tissues
Ability of drug to exit vascular system
Ability of drug to enter cells

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27
Q

What can effect the ability of drug to exit vascular system

A

Protein binding
BBB
Fetal-placental barrier

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28
Q

What can effect the ability for a drug to enter cells

A

Liquid solubility

carrier or receptor

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29
Q

Enteral absorption

A

Via gastrointestinal tract

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30
Q

Parenteral absorption

A

Outside GI tract (injection)

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31
Q

Ability of a drug to exit the vasculature to be available for action depends on

A

the extent of protein binding

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32
Q

When a drug is in the plasma,

A

it may form a reversible bond with plasma proteins

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33
Q

What is the most significant (&Abundant) plasma protein

A

Albumin

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34
Q

What determines the % of drug bound to albumin

A

The strength of attraction between them

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35
Q

What drug can leave the vascular space and reach target tissues?
-Bound or unbound?

A

Unbound!!

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36
Q

what is the portion of the drug that is protein bound?

A

Inactive

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37
Q

What counts as an active drug?

A

Only unbound drugs are active drugs that can exert a pharmacological effect

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38
Q

Drugs bind to plasma proteins to varying degrees, what affects it?

A

their affinity

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39
Q

warfarin is ____ protein bound

A

99%

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40
Q

Gentamicin is a ___ protein bound

A

10%

41
Q

As the free drug leaves the vascular space,

A

more of the drug is released from the protein and becomes free

42
Q

What impacts the distribution of a drug to the CNS?

A

the blood brain barrier

43
Q

The blood brain barrier prevents

A

Large, hydrophilic or highly charged molecules from passing into brain

44
Q

What passes easily through the BBB

A

Lipid soluble molecules (nicotine, alcohol,heorin)

45
Q

What can alter the BBB

A

Trauma and infection can alter the BBB and make it more permeable

46
Q

Metabolism involves

A

The enzymatic alteration of the drug structure

47
Q

what does metabolism do to drug

A

inactivates or biotransforms them

48
Q

Where does most drug metabolism take place

A

in the liver

49
Q

Drugs bound to plasma proteins are

A

pharmacologically inactive

50
Q

P-450 system

A

Hepatic microsomal enzyme system

51
Q

When does the P-450 system occur for PO drugs

A

During the first pass effect

52
Q

Metabolism occurs, for all drugs…

A

during subsequent times while it circulates to the liver

53
Q

Pro drugs

A

Drugs that are inactive until they are metabolized

54
Q

What should be assessed before administering a pro drug

A

if the liver is functional

55
Q

Cytochrome P450 enzymes are a group of enzymes

A

Expressed as membrane bound proteins found in the hepatic endoplasmic reticule,

56
Q

Cytochrome P450 enzyme maximum absorbance

A

450 nm

57
Q

What activates pro drugs

A

Cytochrome P450 enzyme

58
Q

Cytochrome p450 enzymes exihbit

A

Genetic variability (polymorphisms) among individuals and racial groups

59
Q

Possible consequences of P-450 system and drug interaction

A
  • Inactivitation of drug
  • Activation of prodrugs
  • Increase toxicity of drug
  • induction of P-450 enzymes
  • Inhibition of P-450 enzymes
60
Q

Bioavailability of a dug

A

Describes the amount of drug that reaches the systemic circulation AFTER metabolism (or biotransformation)

61
Q

What route has the highest % of bioavailability

A

IV

62
Q

Excretion is

A

the movement of drugs and their metabolites of the body

63
Q

What organ accounts for majority of drug excretion

A

Kidneys

64
Q

What other ways are drugs eliminated?

A

Bile, Feces, Lungs, sweat, Saliva, and breast milk

65
Q

only ___, ____, and ____ drugs can be eliminated by kidneys

A

Only free, unbound, and hydrophilic drugs can be eliminated

66
Q

Drug excretion is accomplished by

A

Glomerular filtration
Tubular reabsorption
Tubular Secretion

67
Q

Drug excretion is influenced by

A

Bound or unbound to proteins
Lipid soluble or water soluble
GFR
Urine pH

68
Q

drugs may require dosage adjustments based on

A

Patients renal function

69
Q

Half life

A

Time required for the serum concentration of the drug to decrease by 50%

70
Q

Factors that affect half-life

A

Rate of metabolism and excretion

Function of 2 organs: Liver and kidneys

71
Q

How does renal failure affect biological half life

A

Increases half life (takes more time to have 50%)

72
Q

Peak

A

Highest plasma drug level

73
Q

What indicate the rate of absorption

A

Peak

74
Q

Trough

A

Lowest plasma drug level

75
Q

What indicates the rat at which the drug is eliminated

A

Trough

76
Q

What are measured when drugs have a narrow therapeutic index

A

Peak & trough

77
Q

Loading dose (bolus)

A

Large initial dose given first

78
Q

Therapeutic index

A

Measure of drugs safety

79
Q

LD50:

A

average lethal dose

80
Q

ED50

A

Average effective dose

81
Q

Therapeutic index=

A

LD50 + ED50

82
Q

A drug that is relatively safe has a

A

Wide therapeutic index

83
Q

A drug that is relatively unsafe has a

A

Narrow therapeutic index

84
Q

Pharmacodynamics is concerned

A

with the effects of drugs on target cells; their mechanism of action

85
Q

How do most drugs exert their effects

A

By interacting with cellular receptors

86
Q

Receptor

A

A macromolecule in a cell to which a drug binds to produce its effects

87
Q

Most receptors are

A

Proteins

88
Q

Where can receptors be found

A

either on the inside or outside

89
Q

Agonist

A

drugs that binds to a receptor & produces a response that activates a receptor

90
Q

Antagonist

A

drug that blocks a response! has no effect by itself, but prevents other drugs

91
Q

Pharmacotherapeutics

A

Clinical pharmacology; study of therapeutic uses and effects of drugs

92
Q

Pharmacodynamics are impacted by

A

Drug-related and patient related variables

93
Q

Variables of Pharmacotherapeutics

A 
Age 
gender 
body weight 
baseline 
physiological functioning & laboratory data
co-morbidities 
other medications 
diet 
Known drug allergies 
functional abilities
94
Q

Critically important role for RN are

A

assessment and monitoring

95
Q

Efficacy

A

ABILITY of drug to achieve the desired effect

96
Q

Potency

A

AMOUNT of drug necessary to produce the desired effect

97
Q

Pharmacogenetics

A

Study of genetic variations in drug response & Focuses on single-gene variations

98
Q

what can lead to drug responses that are qualitatively & quantitatively different from those of the population at large

A

A patients unique genetic make up

99
Q

High alert medications HIPPO

A 
Heparin
Insulin
Potassium, Magnesium, other concentrated electrolytes 
Paralyzing agents 
Opiates

316 Pharmacology (19 decks)

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