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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
After absorption, the drug
Must reach the target organ at therapeutic level in order to have desired response
26
Distribution is determined by three major factors
Blood flow to tissues Ability of drug to exit vascular system Ability of drug to enter cells
27
What can effect the ability of drug to exit vascular system
Protein binding BBB Fetal-placental barrier
28
What can effect the ability for a drug to enter cells
Liquid solubility | carrier or receptor
29
Enteral absorption
Via gastrointestinal tract
30
Parenteral absorption
Outside GI tract (injection)
31
Ability of a drug to exit the vasculature to be available for action depends on
the extent of protein binding
32
When a drug is in the plasma,
it may form a reversible bond with plasma proteins
33
What is the most significant (&Abundant) plasma protein
Albumin
34
What determines the % of drug bound to albumin
The strength of attraction between them
35
What drug can leave the vascular space and reach target tissues? -Bound or unbound?
Unbound!!
36
what is the portion of the drug that is protein bound?
Inactive
37
What counts as an active drug?
Only unbound drugs are active drugs that can exert a pharmacological effect
38
Drugs bind to plasma proteins to varying degrees, what affects it?
their affinity
39
warfarin is ____ protein bound
99%
40
Gentamicin is a ___ protein bound
10%
41
As the free drug leaves the vascular space,
more of the drug is released from the protein and becomes free
42
What impacts the distribution of a drug to the CNS?
the blood brain barrier
43
The blood brain barrier prevents
Large, hydrophilic or highly charged molecules from passing into brain
44
What passes easily through the BBB
Lipid soluble molecules (nicotine, alcohol,heorin)
45
What can alter the BBB
Trauma and infection can alter the BBB and make it more permeable
46
Metabolism involves
The enzymatic alteration of the drug structure
47
what does metabolism do to drug
inactivates or biotransforms them
48
Where does most drug metabolism take place
in the liver
49
Drugs bound to plasma proteins are
pharmacologically inactive
50
P-450 system
Hepatic microsomal enzyme system
51
When does the P-450 system occur for PO drugs
During the first pass effect
52
Metabolism occurs, for all drugs...
during subsequent times while it circulates to the liver
53
Pro drugs
Drugs that are inactive until they are metabolized
54
What should be assessed before administering a pro drug
if the liver is functional
55
Cytochrome P450 enzymes are a group of enzymes
Expressed as membrane bound proteins found in the hepatic endoplasmic reticule,
56
Cytochrome P450 enzyme maximum absorbance
450 nm
57
What activates pro drugs
Cytochrome P450 enzyme
58
Cytochrome p450 enzymes exihbit
Genetic variability (polymorphisms) among individuals and racial groups
59
Possible consequences of P-450 system and drug interaction
- Inactivitation of drug - Activation of prodrugs - Increase toxicity of drug - induction of P-450 enzymes - Inhibition of P-450 enzymes
60
Bioavailability of a dug
Describes the amount of drug that reaches the systemic circulation AFTER metabolism (or biotransformation)
61
What route has the highest % of bioavailability
IV
62
Excretion is
the movement of drugs and their metabolites of the body
63
What organ accounts for majority of drug excretion
Kidneys
64
What other ways are drugs eliminated?
Bile, Feces, Lungs, sweat, Saliva, and breast milk
65
only ___, ____, and ____ drugs can be eliminated by kidneys
Only free, unbound, and hydrophilic drugs can be eliminated
66
Drug excretion is accomplished by
Glomerular filtration Tubular reabsorption Tubular Secretion
67
Drug excretion is influenced by
Bound or unbound to proteins Lipid soluble or water soluble GFR Urine pH
68
drugs may require dosage adjustments based on
Patients renal function
69
Half life
Time required for the serum concentration of the drug to decrease by 50%
70
Factors that affect half-life
Rate of metabolism and excretion | Function of 2 organs: Liver and kidneys
71
How does renal failure affect biological half life
Increases half life (takes more time to have 50%)
72
Peak
Highest plasma drug level
73
What indicate the rate of absorption
Peak
74
Trough
Lowest plasma drug level
75
What indicates the rat at which the drug is eliminated
Trough
76
What are measured when drugs have a narrow therapeutic index
Peak & trough
77
Loading dose (bolus)
Large initial dose given first
78
Therapeutic index
Measure of drugs safety
79
LD50:
average lethal dose
80
ED50
Average effective dose
81
Therapeutic index=
LD50 + ED50
82
A drug that is relatively safe has a
Wide therapeutic index
83
A drug that is relatively unsafe has a
Narrow therapeutic index
84
Pharmacodynamics is concerned
with the effects of drugs on target cells; their mechanism of action
85
How do most drugs exert their effects
By interacting with cellular receptors
86
Receptor
A macromolecule in a cell to which a drug binds to produce its effects
87
Most receptors are
Proteins
88
Where can receptors be found
either on the inside or outside
89
Agonist
drugs that binds to a receptor & produces a response that activates a receptor
90
Antagonist
drug that blocks a response! has no effect by itself, but prevents other drugs
91
Pharmacotherapeutics
Clinical pharmacology; study of therapeutic uses and effects of drugs
92
Pharmacodynamics are impacted by
Drug-related and patient related variables
93
Variables of Pharmacotherapeutics
``` Age gender body weight baseline physiological functioning & laboratory data co-morbidities other medications diet Known drug allergies functional abilities ```
94
Critically important role for RN are
assessment and monitoring
95
Efficacy
ABILITY of drug to achieve the desired effect
96
Potency
AMOUNT of drug necessary to produce the desired effect
97
Pharmacogenetics
Study of genetic variations in drug response & Focuses on single-gene variations
98
what can lead to drug responses that are qualitatively & quantitatively different from those of the population at large
A patients unique genetic make up
99
High alert medications HIPPO
``` Heparin Insulin Potassium, Magnesium, other concentrated electrolytes Paralyzing agents Opiates ```

316 Pharmacology (19 decks)

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