Pharmacokinetics Flashcards

0
Q

What are the four stages of pharmacokinetics?

A

Absorption
Distribution
Metabolism
Excretion

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1
Q

What is pharmacokinetics?

A

It involves the movement through the body to it’s site of action (what the body does to the drug)

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2
Q

Where does metabolism mostly occur?

A

In the liver

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3
Q

What must drugs pass in get into a cell?

A

Cell membrane

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4
Q

What are the three mechanisms a drug can cross the cell membrane?

A

Passing through pores
Undergoing transport
Penetrating the membrane directly

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5
Q

What are usually the only types of drugs that can directly pass through a cell membrane?

A

Lipid soluble drugs

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6
Q

What are the only two elements that pass a cell membrane directly?

A

Potassium and sodium.

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7
Q

Where is P-glycoprotein found and what does it do?

A

Found in liver, placenta, intestine, and brain capillaries. It can transport a variety of drugs OUT of cells.

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8
Q

What will happen to a drug if it binds to P-glycoprotein?

A

Absorption of drug will decrease. It is a large protein and will not be able to pass through cell membrane.

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9
Q

What does ionize mean?

A

The change of a drug becoming water soluble.

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10
Q

Is a drug harder or easier to absorb once it’s been ionized?

A

Harder.

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11
Q

Acidic drugs ionize in _________ media

A

Basic alkaline

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12
Q

Basic drugs ionize in __________ media

A

Acidic.

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13
Q

When drugs can not be absorb in the liver, where are they excreted?

A

Bile.

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14
Q

When drugs can not be absorbed in the kidney, where are they excreted?

A

Urine

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15
Q

When a drug can not be absorbed into the placenta, where does it go?

A

Maternal blood

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16
Q

Is the stomach level acidic or basic?

A

Acidic

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17
Q

Is the intestine level acidic it basic?

A

Baisic

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18
Q

What type of soluble can penetrate a cell membrane?

A

Lipid soluble

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19
Q

What type of soluble can NOT pass the cell membrane?

A

Water soluble.

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20
Q

What is the definition of absorption?

A

The movement of a drug from it’s site of administration into the blood.

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21
Q

Where is alkaline drugs absorb?

A

Liver.

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22
Q

Where does acidic drugs absorb?

A

Stomach

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23
Q

What are different routes to administer drugs?

A

Intravenous
Intramuscular
Oral

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24
What are the factors that affect drug absorption?
``` Rare of dissolution Surface area (small intestine- large surface area) Blood flow Lipid solubility pH partitioning ```
25
The better the blood follow the better the __________?
Absorption.
26
The more lipid soluble the drug the grater the _________.
Absorption
27
What is pH partitioning?
When a drug accumulates in an area because a media levels pH is very different from drug.
28
What can you do for a patient if pH partitioning is a concern?
You can give the patient something to make the urine more acidic.
29
What are the characteristic/advantage of intravenous drug administration?
Very quick. Directly into blood stream. 100% absorbed.
30
What are the disadvantages of IV administration?
Expensive, increase risk for infection, irreversible.
31
What are the characteristics of oral administration?
Slow absorption rate. Everyone will have different absorption rate. Extreme variations.
32
What two drugs can not be administered orally?
Insulin and penicillin G.
33
What does depot preparation mean?
Drug is high potency. Only needs to be administered once or twice a month.
34
What is the definition of distribution?
Movement of drugs throughout body to site of action.
35
What tie systems work to distribute drugs?
Vascular and lympathic
36
Drug distribution is determined by what three factors?
Blood flow Exciting vascular system Entering cells
37
Drugs are carried by the blood to ____________ and organs of the body.
Tissues.
38
What is the major factor for distribution?
Blood flow.
39
When drugs exit the vascular system what do they typically pass through?
Capillary beds.
40
Drugs pass through or between capillary cells?
Between
41
Capillary pores are extremely close together in which two structures. Making it difficult for drugs to pass through?
Brain and placenta
42
Junctions between the tight cells that compose the walls of most capillaries in the CNS.
Blood brain barrier.
43
Drugs can for reversible bonds with various proteins. Which protein is the most abundant and important?
Plasma albumin.
44
Large molecule that always remains in the bloodstream. Impacts drug distribution.
Albumin.
45
If a drug binds to albumin does the drug come out of the cell?
No. It has to unbound to come out.
46
Most drugs must enter cells to undergo which to phases of pharmacokinetics?
Metabolism and excretion.
47
When do most drugs produce their effects?
By binding with receptors on external surface of cell membrane. Does not need to cross cell membrane to act.
48
When do most drugs become active?
In disruption.
49
Metabolism is also known as.
Bio transformation
50
The enzymatic alteration of drug structure (changes structure of drug).
Metabolism.
51
Metabolism often takes place where?
Liver
52
Drug metabolism in liver is performed by what enzyme system?
Hepatic microsomal enzyme system. (P450)
53
If P450 system is increased or decreased the structure of the drug will?
Alter more.
54
Therapeutic consequences of drug metabolism are:
``` Accelerated renal drug excretion Drug inactivation Activation of prodrugs Increased therapeutic action Increased or decreased toxicity ```
55
To eliminate drug through kidney need to change to water soluble drug.
Accelerated renal drug excretion.
56
What does Activation of prodrugs mean?
Drugs need to go through metabolism to become active.
57
What happens in increased therapeutic action?
A drug (codeine) will need to go through change to become morphine
58
A special consideration in drug metabolism is induction of drug metabolism enzymes (P450). What would occur?
P450 will change a drug to be effective to not effective. Most important when patient is taking more than 1 drug. Increase dose of other drugs because other drug is being metabolized faster.
59
First to pass drugs can not be administered how?
Orally.
60
Removal of drugs from the body
Excretion
61
Drugs and their metabolites can exit the body through?
``` Urine Sweat Saliva Breast milk Expired air ```
62
What are the three steps in renal drug excretion?
Glomerular filtration Passive tubular re absorption Active tubular secretion.
63
What are three factors that modify renal drug excretion by lowering excretion?
pH dependent ionization Competition for active tubular transport Age
64
What gets re absorbed in glomerular filtration?
Large molecules
65
What gets reabsorbed in passive reabsorption?
Lipid soluble drugs
66
What happens in active transport?
Organic acids and bases move drugs from blood to urine.
67
Non renal routs of excretion are
Breast milk Bile Lungs Sweat salvia
68
Plasma drug levels are drug levels in what?
Blood
69
Two plasma drug levels defined:
``` Minimum effective concentration (MEC) Toxic concentration (TC) ```
70
When MEC is increased and TC is decreased this is a good or bad drug level?
Good
71
The objective of drug dosing is to maintain drug levels within what range?
Therapeutic range
72
A toxic drugs had what two characteristics?
Narrow therapeutic range | Low therapeutic index
73
Time required for the amount of drug in body to decrease by 50%
Half life
74
What is a plateau?
Drug becomes stabilized in the body. Takes about 4 to 5 to stabilize and another 4 to 5 to eliminate.
75
The longer the half life the less or more frequently you need to take drug?
Less
76
Peak concentration and trough concentration?
Peak is increase and trough is decreased
77
A loading dose is ?
A very large amount of a drug
78
Maintain dose is?
A dose to maintain effects of drug.
79
Enteric coated preparation protects | What?
Absorption in stomach goes into the liver for absorption
80
Sustained release preparation
Longtime to take drug absorption.