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Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Define pharmacokinetics

A

The process by which a drug is absorbed, distributed, metabolized, and eliminated by the body

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2
Q

Define absorption

A

It is the transfer of a drug from its site of administration to the systemic blood stream

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3
Q

What are the factors affecting the drug absorption related to the drug ?

A

Water and lipid solubility
Ionization
Concentration
Nature
Pharmaceutical preparation

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4
Q

What is meant by pharmaceutical preparations

A
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5
Q

What are the factors affecting drug absorption related to the patient

A

Route of administration
Absorbing surface
Systemic circulation
Gut contents

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6
Q

Explain the route administration factor

A
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7
Q

Explain the absorbing surface factor

A
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8
Q

Explain the gut contents factor

A
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9
Q

Define first pass effect

A

Means metabolism of drug in gut wall or liver before reaching the systemic circulation

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10
Q

Explain the gut first pass effect

A
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11
Q

Explain the hepatic first pass effect

A
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12
Q

Define bioavailability

A

The fraction of unchanged drugs reaching systemic circulation after any route of administration

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13
Q

Bioavailability is less in oral administration why

A

The drug may be incompletely absorbed
The absorbed drug may undergo first pass metabolism in the intestinal wall/liver pr be excreted in bile

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14
Q

What is distribution

A

Once in the bloodstream the drug is distributed to the tissues throughout the body

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15
Q

The delivery of a drug from the plasma to the interstitial and intracellular fluids depends on what

A
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16
Q

Define volume of distribution

A
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17
Q

What is the equation for volume of distribution

A
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18
Q

What is the percentage of water in one’s body

A

60% of body weight

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19
Q

The water is partitioned into what 2 main compartments

A
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20
Q

What does it mean if a chemical distributes only to the plasma compartment

A

It has high plasma concentration and low volume of distribution

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21
Q

What does it mean if a chemical distributes throughout the body

A

It has low plasma concentration and high volume of distribution

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22
Q

What is the clinical significance of the volume of distribution

A
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23
Q

Once a drug enters the body, from whatever route of administration, it has the potential to distribute into what

A

Plasma compartment
Extracellular fluid
Total body water

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24
Q

When does the drug stay in the plasma compartment

A
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25
Q

When is the drug in extracellular fluid

A
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26
Q

When is the drug in total body water

A
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27
Q

What are the factors affecting distribution

A

Blood flow
Binding of drugs to plasma proteins and tissues
Hydrophobicity
Capillary permeability

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28
Q

Explain how blood flow affects distribution

A
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29
Q

What does binding to plasma protein cause ?

A

Slow transfer of drugs out of the vascular compartment

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30
Q

How do many drugs circulate in the bloodstream

A
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31
Q

What is the clinical significance of binding of drugs to plasma proteins and tissues

A
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32
Q

What is the clinical significance of the bound fraction ?

A
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33
Q

Plasma protein binding is also what

A

A temporary storage of drug

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34
Q

What is the result of high degree of protein binding

A

Generally makes the drug long acting, because bound fraction is not available for metabolism or excretion

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35
Q

Describe the displacement interaction among drugs

A
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36
Q

What are some important displacement reactions

A
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37
Q

What is meant by fat as a reservoir

A
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38
Q

What is meant by bone as a reservoir

A
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39
Q

Explain the penetration into the brain and CNS

A
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40
Q

Why is the transfer of drugs across the placenta is of critical importance ?

A

Because drugs may cause anomalies in the developing fetus

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41
Q

Why does the ion trapping of basic drugs occur in case of fetal plasma ?

A

The fetal plasma is slightly more acidic than that of the mother

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42
Q

Why is the placenta considered an incomplete barrier ?

A

The fetus is to some extent exposed to all drugs taken by the mother

43
Q

Termination of the drug effect after withdrawal of a drug is usually done by what

A

By metabolism and excretion
It may also happen by redistribution of the drug from its site of action into other tissues or sites

44
Q

When does redistribution occur ?

A

When a highly lipid-soluble drug that acts on the brain or cardiovascular system is administered rapidly by intravenous injections or inhalation

45
Q

What is metabolism

A
46
Q

Do hydrophilic drugs undergo metabolism

A
47
Q

What is the primary site for drug metabolism

A

Liver

48
Q

What are other site for drug metabolism

A

Kidney, intestine, lungs, plasma

49
Q

Biotransformation may lead to what

A
50
Q

What is the phase 1 of biotransformation

A
51
Q

What does phase 1 include

A
52
Q

Non-microsomal enzymes are present where

A
53
Q

Give examples of non-microsomal enzymes

A
54
Q

What is microsomal oxidation

A
55
Q

Explain cytochrome p450 inducers

A
56
Q

What is the effect of cytochrome p450 inducers

A
57
Q

How many days does induction take to reach its peak and is maintained til the inducing agent is being given

A

4-14 days

58
Q

After the induction how long does it take for the enzymes to return to their original value ?

A

1-3 weeks

59
Q

What are the consequences of microsomal enzyme induction

A
60
Q

Explain cytochrome p450 inhibitors

A
61
Q

What are the examples of inhibitors of drug metabolism

A
62
Q

What is faster enzyme inhibition or induction

A
63
Q

Explain phase 2 of metabolism

A
64
Q

What is the most common and the most important conjugation reaction

A

Glucuronidation

65
Q

Glucuronidation is carried out by what

A
66
Q

What is the route of the Glucuronidation

A
67
Q

Who are deficient in conjugating system

A

Neonates

68
Q

Glutathione conjugation is carried out by what

A
69
Q

Glutathione conjugation serves to do what

A
70
Q

Explain acetylation

A
71
Q

Rate of acetylation shows what

A
72
Q

What is first pass metabolism

A
73
Q

What is elimination

A

It is the passage out of systemically absorbed drugs

74
Q

Drugs and their metabolites are excreted in what

A
75
Q

Explain the excretion through faeces

A
76
Q

What are examples of drugs that are excreted through faeces

A
77
Q

Explain the secretion of drug by saliva and sweat

A
78
Q

Explain the excretion of drugs by exhaled air

A
79
Q

Explain the excretion of drug by milk

A
80
Q

What is renal excretion

A
81
Q

What are the 3 processes of renal excretion

A

Glomerular filtration
Active tubular secretion
Passive tubular reabsorption

82
Q

How are drugs excreted by glomerular filtration

A
83
Q

Glomerular filtration of a drug depends on what

A

It’s plasma protein binding
Renal blood flow

84
Q

What is the glomerular filtration rate

A
85
Q

When does the glomerular filtration rate decline

A

After the age of 50
Renal failure

86
Q

What is proximal tubular secretion

A
87
Q

What does the organic acid transport operate for

A
88
Q

What does organic base transporter operates for

A
89
Q

Both OATP and OCT transport processes are what

A
90
Q

What is predominantly secreted into the tubular lumen

A

Exogenous substances

91
Q

What is predominantly reabsorbed

A

Endogenous substrate

92
Q

Give an example when the drugs utilizing the same active transport compete with each other

A
93
Q

Distal tubular reabsorption occurs by what

A

Passive diffusion

94
Q

What does distal tubular reabsorption depend on

A

Lipid solubility
Ionization of the drug at the existing urinary pH

95
Q

When would the drug go back into the systemic circulation

A
96
Q

What is ion trapping

A
97
Q

Ion trapping is utilized for what

A

Utilized for facilitating elimination of the drug in poisoning

98
Q

Give example of overdose with weak acid

A
99
Q

Give example of overdose with weak base

A
100
Q

What is the effect of tubular transport mechanism not being well developed at birth

A
101
Q

What is plasma half life

A
102
Q

The half life of a drug may be decreased by what

A
103
Q

The half life of a drug is increased by what

A
104
Q

Therapeutic drug monitoring is particularly useful in what situations

A

Pharmacology (25 decks)

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