Drugs Flashcards

1
Q

What are the 4 basic factors that determine drug pharmacokinetics?

A

Absorption
Distribution
Metabolism
Elimination

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2
Q

What is absorption?

A

Absorption is defined as the process of movement of unchanged drug from the site of administration to the systemic circulation

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3
Q

To have a biological effect where does the drug have to enter?

A

The blood stream

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4
Q

What does taken orally mean?

A

In the mouth

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5
Q

What does administered intravenously mean?

A

Straight into the blood stream

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6
Q

What does subcutaneous mean?

A

Under the tongue

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7
Q

What does administered intramuscular mean?

A

Straight into the muscles

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8
Q

Give an example of a drug you inhale?

A

Asthma subutanol

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9
Q

Why is intravenous not absorbed?

A

As it just goes straight to the systemic circulation

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10
Q

What is Tmax?

A

The time for the drug to reach peak concentration

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11
Q

What is Cmax?

A

The peak concentration of the drug

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12
Q

Give a factor that can affect absorption of drugs?

A

How much food you have eaten

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13
Q

What is bioavailability?

A

The amount of drug that is available to achieve a certain effect

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14
Q

What is the therapeutic range?

A

The range of conc. at which a drug is active

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15
Q

If the drug is under the therapeutic range what happens?

A

There is no pharmalogical effect

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16
Q

If the drug is over the therapeutic range what happens?

A

Toxicity occurs

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17
Q

What is therapeutic index?

A

The range at which a drug is safe and active

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18
Q

How much bioavailability does a drug given intravenously have?

A

100%

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19
Q

What physical properties of a drug affect its absorption?

A

Particle size
Lipid solubility
pH and ionisation

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20
Q

What does the drug need to pass to get to the blood stream?

A

The cell membrane

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21
Q

Do ionised or un-ionised drugs cross the membrane?

A

Un-ionised

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22
Q

What can alter the ionisation of a drug?

A

Small pH changes

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23
Q

What happens to an ionised drug at the cell membrane?

A

Does not cross the membrane

May not be absorbed at all

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24
Q

What happens to an un-ionised drug at the cell membrane?

A

Should distribute across the membrane until equilibrium is reached - will rapidly diffuse across the membrane

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25
Q

Does food enhance or impair the rate of drug absorption?

A

Can do either

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26
Q

What is first pass metabolism?

A

Metabolism of the drug prior to reaching system circulation. There can be a limit on this on oral routes for some drugs

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27
Q

What is intramuscular administration most commonly used for now?

A

Vaccinations

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28
Q

How will sublingual be absorbed?

A

Under the tongue

Enters the circulation directly

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29
Q

Does sublingual bypass first past mechanism?

A

Yes - it is absorbed straight into the blood stream

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30
Q

What kind of agents is inhalation administration best for?

A

Better for volatile agents

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31
Q

Are substances well absorbed by transdermal route?

A

No - few substances are well absorbed this way

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32
Q

What does transdermal administration mean?

A

Absorbed through the skin

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33
Q

For a drug to be active where must it leave then enter?

A

Must leave the blood stream and enter the intercellular or intracellular spaces

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34
Q

What do many drugs bind to?

A

Plasma proteins

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35
Q

What drug is the active drug?

A

The drug that is not bound to plasma protein

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36
Q

Is the binding of a drug to a plasma protein reversible?

A

Yes

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37
Q

What is the clearance of a drug?

A

Defined as the theoretical volume of fluid from which a drug is completely removed over a period of time

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38
Q

What is clearance a measure of?

A

Elimination

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39
Q

What is the clearance of a drug dependent on?

A

How quickly the kidneys clear the drug

The rate of metabolism

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40
Q

What is the half life of a drug?

A

The half life is defined as the time taken for the drug concentration in the blood to decline to half of the current value

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41
Q

If it takes 4 hours for the conc. of a drug in the blood stream to drop from 10mg to 5mg then what is the half life?

A

4 hours

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42
Q

What does half life depend on?

A

The volume of distribution and the rate of clearance

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43
Q

If the half life is prolonged what is the effect?

A

There is a reduction in the drugs clearance

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44
Q

What does drug elimination mean?

A

This means the removal of the drug from the body

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45
Q

What is drug elimination dependent on?

A

Drug metabolism

Drug excretion

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46
Q

What is the primary organ for drug excretion?

A

The kidneys

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47
Q

What damage is important in causing drug toxicity?

A

Renal damage

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48
Q

Are most medicines taken once off or chronically?

A

Chronically

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49
Q

In theory what should the Vd be?

A

42L

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50
Q

What determines the drug delivery system we use?

A

The dose of drug to be given
The frequency of administration
The timing of administration

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51
Q

What do we refer to for finding out the recommended dose of a drug in adults?

A

BNF

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52
Q

What do we refer to for finding out the recommended dose of a drug in children?

A

BNFc

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53
Q

What two organs do we consider the function o in drug prescription?

A

Kidneys (renal function)

Liver (hepatic function)

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54
Q

What is the most common form or drug administration?

A

Orally

Oral medication

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55
Q

In what state are suspended drugs?

A

Liquid

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56
Q

Who are solutions and suspensions useful for?

A

The young and elderly with swallowing difficulties

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57
Q

How quickly are drugs in solution absorbed?

A

Extremely rapidly

58
Q

What is a suspension of a drug?

A

Dispersions of coarse drug particle in a liquid phase

59
Q

What is the rate limiting step in absorption in tablets and capsules?

A

The dissolution or tablet breakdown

60
Q

Where are enteric coated tablet disintegrated?

A

The small intestine

61
Q

Why are some tablets enteric coated?

A

To protect the dug from the stomach acid

To protect the stomach from the drug

62
Q

Give an example of a drug that if not enteric coated can harm the stomach?

A

Aspirin

63
Q

What does prolonged release reduce the need for?

A

Frequent dosing

64
Q

What does prolonged drug release maintain?

A

Drug levels within a therapeutic range

65
Q

Why can’t after stabilisation on one drug can you switch the patient straight over to another drug?

A

Because the interaction of the previous drug still in the system and the new introduced drug can produce acute severe toxicity

66
Q

What is a pro drug?

A

A drug that requires to be metabolically activated after administration

67
Q

What are the advantages of pro-drugs?

A

The prolonged duration of action of the drug

The avoidance of the degradation of the drug in the gut

68
Q

Where do sublingual drugs dissolve?

A

Under the tongue or in the buccal cavity

69
Q

What sublingual drug treats angina?

A

GTN

70
Q

Who might the rectal route be used for administration for?

A

For patients who cannot swallow tablets

71
Q

Does rectal route bypass pre-systemic metabolism?

A

Yes

72
Q

How is the rectal route administered?

A

As a suppository

73
Q

How quickly do IV drugs work?

A

Immediately

74
Q

How quickly can IV drugs produce toxicity?

A

Immediately

75
Q

Does IV administration bypass first-pass metabolism?

A

Yes

76
Q

How might drugs with a short half-life be administered?

A

Through IV administration

77
Q

Why might a drug be given IV?

A

When a rapid onset of action is required
When careful control of plasma levels is required
When a drug has a short half-life

78
Q

Where is an intramuscular injection given into?

A

Muscle mass

79
Q

What is a disadvantage of IM injection?

A

They may be painful

80
Q

What does subcutaneous injection bypass?

A

The need for venous access

81
Q

Name a drug that is given by subcutaneous injection?

A

Insulin

82
Q

Where are transdermal drugs delivered to?

A

The skin

83
Q

With transdermal administration how does the drug cross the skin?

A

By diffusion

84
Q

Do transdermal drugs achieve a local effect or a systemic effect?

A

Both

85
Q

What do skin patches allow?

A

The release of a drug from a reservoir into the skin and systemic circulation

86
Q

What drug is inhaled for systemic effect?

A

Anaesthetic

87
Q

Where are inhaled drugs usually targeting?

A

Lung

88
Q

What disease is treated through an inhaler?

A

Asthma

89
Q

Is inhaled administration effect rapid?

A

Yes

90
Q

Are large or small doses used for inhaled administration?

A

Small

91
Q

What does a monoclonal antibodies deliver?

A

Toxins, cytokines or other active drug

92
Q

How does a monoclonal Ab work?

A

It delivers straight to the site you want it to be active
They then release
Means the toxicity just affects the site directly

93
Q

What does liposomal drug delivery exhibit a reduction of?

A

Toxicities

94
Q

What does liposomal drug delivery exhibit and enhanced of?

A

Efficiency

95
Q

What are nanoerythrosomes?

A

RBC that are transformed into drug delivery systems

96
Q

What is an adverse drug reaction?

A

Any reaction to a drug which is harmful or unpleasant resulting from an intervention related to the use of a medicinal product

97
Q

How many inpatients suffer form an ADR?

A

10-20%

98
Q

How many hospital deaths occur as a result of ADR?

A

0.25-3%

99
Q

How long is acute ADR onset?

A

Within 60 minutes

100
Q

How long is sub-acute ADR onset?

A

1 to 24 hours

101
Q

How long is latent ADR onset?

A

> 2 days

102
Q

Describe mild ADR?

A

Bothersome but no change to therapy

103
Q

Describe moderate ADR

A

Requires change to therapy

Requires additional treatment

104
Q

Describe severe ADR

A

Disabling or life threatening

Kidney Failure

105
Q

What is the name given to Type A ADR?

A

Augmented

106
Q

What is the name given to Type B ADR?

A

Bizarre

107
Q

What is the name given to Type C ADR?

A

Chronic

108
Q

What is the name given to type D ADR?

A

Delayed

109
Q

What is the name given to Type E ADR?

A

End of treatment

110
Q

What is the name given to type F ADR?

A

Failure of treatment

111
Q

What gender is ADR more common in?

A

Women

112
Q

What ages are ADR more common for?

A

Elderly and neonates

113
Q

Problems with which 2 organs can affect drug metabolism and therefore their functioning has to be considered before drug administration?

A

Kidneys and liver

114
Q

What are type A ADR?

A

Normal but augments response to a drug

115
Q

Are type A ADR predictable?

A

Yes

116
Q

What are type A ADR reactions due to?

A

Excess pharmacological action

117
Q

How do type A ADR resolve?

A

By reducing or stopping the drug treatment

118
Q

What factors affect absorption of a drug in pharmacokinetic variation?

A

Dose
Formulation
GI motility
First pass metabolism

119
Q

What factors affect drug metabolism in pharmacokinetic variation?

A

Hepatic - enhanced/impaired

120
Q

What factors affect drug elimination in pharmacokinetic variation?

A

Renal function

121
Q

What type of drug metabolism is under genetic control?

A

Acetylation

122
Q

What % of the population are slow metabolisers?

A

10%

123
Q

What are slow metabolisers prone to?

A

Drug toxicity

124
Q

Are most type A ADRS pharmacokinetic or pharmacodynamic in nature?

A

Pharmacokinetic

125
Q

What are the characteristics of type B ADRs?

A

Bizarre
Unpredictable
Rare

126
Q

What do type B ADRS cause?

A

Serious illness or death

127
Q

Are type B ADRs related to the dose of the drug?

A

No

128
Q

What causes the differences in response to drugs?

A

Genetics

Immunological system

129
Q

What is type C ADR related to?

A

The duration of the treatment

130
Q

How predictable are Type C ADRs?

A

Semi-predictable

131
Q

How quickly do Type D ADRs occur?

A

They occur some time after the treatment

132
Q

Who do ADR type D occur in?

A

The children of the treated patients

The patients themselves years after the treatment has stopped

133
Q

What is Type E ADR?

A

Adverse effects which occur when a drug treatment is stopped especially suddenly

134
Q

What commonly used substance can cause Type E ADR when stopped?

A

Alcohol - withdrawal symptoms

135
Q

When does rebound phenomena occur?

A

When a drug is suddenly withdrawn

136
Q

What does Type F ADR cause?

A

Failure of therapy

137
Q

Are type F ADRs common?

A

Yes

138
Q

What are type F ADRs related to?

A

Dose

139
Q

Give examples of drugs that are commonly involved in ADRs?

A

Antibiotics
Cardiovascular drugs
Anticoagulants
Antineoplastics

140
Q

Who are particularly at risk from ADR?

A
Young and old 
Those on multiple medications 
Those with altered physiology 
Those with prior history of ADRs
Those with genetic predispositions
141
Q

How do you report ADRs?

A

Using the yellow card scheme