Phamacology Flashcards

1
Q

Define pharmacology

A

Study of the actions and effects of chemicals on body and body on chemicals

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2
Q

What are the main 2 components of pharmacology

A

Pharmacokinetics

Pharmacodynamics

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3
Q

Define pharmacodynamics

A

Drugs effect on body

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4
Q

Define pharmacokinetics

A

Bodys effect on drugs

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5
Q

3 considerations of drugs in terms of pharmacodynamics

interaction with …, what about drug, modifies?

A

Interaction with cells
Effect of drug concentration on body
Drug modifying disease

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6
Q

3 properties of drugs

A

Affinity
Efficacy
Potency

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7
Q

Define affinity

A

Ability of drug to bind to receptor

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8
Q

Define efficacy

A

Ability of drug to induce an response

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9
Q

Define potency

A

Amount of drug required to illicit desired response

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10
Q

What is the equation for potency

A

Affinity + efficacy

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11
Q

List 4 families of receptors for drugs

A

Ligand gated ion channels
G coupled protein receptors
Enzyme linked receptors
Intracellular receptors

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12
Q

List 4 drug action sites

A

Enzymes
Receptors
Carriers
Ion channels

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13
Q

What are 2 ways things a drug can act as?

A

As an agonist or an antagonist

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14
Q

List 3 types of agonists

A

Full agonist
Partial agonist
Inverse agonist

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15
Q

List 3 types of antagonists

A

Antagonists
Competitive antagonists
Non-competitive antagonists

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16
Q

Define a full agonist drug

A

Drug that binds to receptor to initiate a response

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17
Q

What do agonist drugs mimic?

A

Body’s function

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18
Q

What are 2 features of a full agonist

A

High affinity and efficacy

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19
Q

Define a partial agonist drug

A

Drug that binds to a receptor to initiate a response but without the efficacy of a full agonist

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20
Q

Partial agonists can act as what when given with a full agonist?

A

Competitive agonist

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21
Q

Define a inverse agonist drug

A

Drug that binds to a receptor to initiate the opposite response e.g. naloxone on opioid receptors

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22
Q

Define a antagonist drug

A

Drug that binds to a receptor to initiate no response/prevent response from occurring

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23
Q

Define a competitive antagonist drug

A

Drug that binds to same receptor as another drug/ligand thus competes for receptor site

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24
Q

Define a non-competitive antagonist

A

Drug that binds to a different site on receptor leaving the receptor ineffective

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25
Q

What do dose response curves show?

A

Body’s response to drug against logarithmic dose

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26
Q

On a dose response curve graph what does the X axis demonstrate about which feature of a drug (i.e. efficacy, potency, affinity)?
(which direction is highest to lowest)

A

X axis demonstrates a drugs potency from highest to lowest (left to right)

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27
Q

On a dose response curve graph what does the Y axis demonstrate about which feature of a drug (i.e. efficacy, potency, affinity)
(which direction is highest to lowest)

A

Y axis demonstrates a drugs efficacy and affinity from lowest to highest (bottom to top)

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28
Q

True or false, modified forms/doses of drugs should never be crushed or chewed?

A

True

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29
Q

3 considerations of drugs in regards to pharmacokinetics

route, time, exit

A

Process of absorption from administered route
Period between administration and effect
Process of elimination from body

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30
Q

What are the 4 stages of pharmacokinetics?

A
ADME 
Absorption 
Distribution 
Metabolism 
Excretion
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31
Q

Define absorption

from where to where

A

Transfer of drug from administered site into systemic circulation

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32
Q

What % of drug is absorbed in how many hours given via oral route?

A

75%

1-3 hours

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33
Q

What 3 cause the loss of 25% of a drug administered orally?

A

GIT acid
Enzymes
1st pass metabolism

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34
Q

First pass metabolism only occurs when drugs are taken orally?

A

True

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35
Q

List 6 factors that effect oral absorption of a drug

A
Particle size 
Formulation 
Enzymes and pH of GIT 
GIT motility 
Physiochemical factors e.g. salt form 
Food eaten
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36
Q

What would inactivate a drug to mean that it couldn’t be given orally?

A

Drugs left inactive due to first pass metabolism

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37
Q

Define a depot and what does it mean for speed of absorption?

A

Drug given in a suspension

Allows for slow sustained absorption

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38
Q

What type of substance does a specialised depot come in and what does does this mean for absorption?

A

Oily substance

Slow absorption

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39
Q

Drugs given IM in an aqueous solution have fast or slow absorption?

A

Fast

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40
Q

Which 2 routes can suspensions be given into?

A

IM or subcut

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41
Q

What is the bioavailability of a drug given IV?

A

100%

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42
Q

Define distribution

A

Process where drug is reversibly transferred

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43
Q

Name 2 methods of distribution

clue: transfer, distance

A

Bulk flow transfer - in blood

Diffusion transfer - molecule by molecule through phospholipid bilayer

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44
Q

How are drugs reversibly transferred?

A

By binding to plasma proteins

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45
Q

Name 2 proteins that help transfer drugs

A

Albumin

Glycoproteins

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46
Q

True or false, drugs are chemically inert when bound to plasma proteins

A

True

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47
Q

List 4 methods by which drugs cross cell membrane

A

Passive diffusion
Facilitated diffusion
Active transport
Pinocytosis

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48
Q

During passive diffusion what concentration do drugs move from to?

A

High to low concentration

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49
Q

What drug action site facilitates passive diffusion?

A

Ion channels

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50
Q

What drug action site facilitates facilitated diffusion

A

Protein carriers

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51
Q

Which is quicker facilitated or passive diffusion?

A

Facilitated

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52
Q

What does active transport allow for in terms of drug concentration?

A

Movement of drug against concentration gradient

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53
Q

What does a drug need to be soluble in to be able to cross the blood brain barrier?

A

Lipid soluble

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54
Q

List 5 factors that effect drug distribution

A
Plasma protein binding 
Location of receptor site 
Regional blood flow 
Lipid solubility 
Disease
55
Q

How do pregnancy and liver conditions effect distribution of drugs?

A

Reduce albumin concentration

56
Q

What would you do to the dose of a drug if a patient had low albumin levels and why?

A

Reduce dose

As drug is bioactive when unbound increasing likelihood of ADRs and toxicity occurring

57
Q

What does the % of protein binding of a drug have to be for displacement of another protein bound drug to be clinically significant?

A

90%

58
Q

Define narrow therapeutic index

A

Drug with a small difference between therapeutic and toxic concentrations

59
Q

What do you need to do when a pt is prescribed a drug with a narrow therapeutic index

A

Monitor blood plasma concentrations of drug

60
Q

What tissue is responsible for the difference in drug distribution in children and the elderly?

A

Adipose tissue

61
Q

List 6 factors effecting metabolism

A
1st pass effect 
Perfusion of liver 
Liver disease 
Generic factors 
Other drugs 
Age
62
Q

Define bioavailability

A

% of drug that makes it into systemic circulation

63
Q

Define bioequivalence

A

Drug that has no difference in its rate of uptake/action at receptor site when given at same dose via same route

64
Q

List 4 outcomes of metabolism

A

Activation of inactive drug
Increased activity of already activated drug
Inactivation of active drug
Change in activity of drug

65
Q

List 4 metabolic barriers

A

GIT mucosa
Lung
Liver
GIT wall

66
Q

What is the main site of local hormone metabolism?

A

Lungs

67
Q

Define clearance

A

Measure of the time it takes for a volume of blood plasma to be completely clear of a drug

68
Q

Clearance a measure of the time it takes for a drug to be removed from blood plasma OR a measure of the amount of drug removed from blood plasma?

A

Measure of TIME of drug removal not amount

69
Q

Define half life

A

Time taken for plasma concentration of a drug to halve

70
Q

True or false, half life is effected by the dose of drug taken?

A

False

71
Q

What does an enzyme inducing drug do to the bioavailability of another?

A

Reduces bioavailability

72
Q

When given an enzyme inducing drug, what might you have to do to the dose of the original drug?

A

Increase dose

73
Q

What does an enzyme inhibiting drug do to the bioavailability of another?

A

Increases bioavailability

74
Q

When giving an enzyme inhibiting drug, what might you have to do to the dose of the original drug?

A

Decrease dose

75
Q

What does the liver do to help with the elimination of drugs from the kidneys?

A

Metabolises/breaks down drugs so that they are more water soluble to help with excretion from the kidneys.

76
Q

List 4 stages of excretion of drugs from the kidneys

A

Filtration
Re-absorption
Secretion
Excretion

77
Q

What 2 types of drugs are reabsorbed by the kidneys during excretion?

A

Lipid soluble

Unionised

78
Q

What type of membrane transport occurs during secretion in excretion of drugs from the kidneys?

A

Active transport by membrane carriers

79
Q

Where in the kidneys does secretion of drugs during excretion occur?

A

Transporters in the PCT membrane

80
Q

Define rate of absorption

A

Speed at which drug is transferred from administered route into systemic circulation

81
Q

Define extent of absorption

A

Amount of total drug transferred from administered route into systemic circulation

82
Q

What does increased GIT motility do to the rate of absorption?

A

Increases rate of absorption

83
Q

What does hyper GIT motility do to the extent of absorption?

A

Decreases the extent of absorption

84
Q

Name 4 routes that require absorption into systemic circulation first before they are able to take effect

A

Inhalation
Oral
Vaginal
Ocular

85
Q

What 2 factors determine receptor effect?

A

Rate and extent of absorption

86
Q

What about a drug determines it’s rate and extent of absorption?

A

Size of drug particles

87
Q

During decreased GIT motility is there a change in the extent of absorption?

A

No

88
Q

List 5 barriers between oral route and drug receptor site

A

GIT mucosa
Vascular endothelium
Renal tubule cells
Blood brain barrier

89
Q

Lipid soluble drugs cross the cell membrane by what form of transport?

A

Passive diffusion

90
Q

What happens to the blood brain barrier during inflammation and what does this allow in terms of drug solubility?

A

Becomes leaky

Allows for water soluble drugs to cross from blood plasma into CSF

91
Q

What type macromolecule is present in a drug meaning that it is unsuitable to be given via the oral route?

A

Proteins e.g. insulin

92
Q

What route should protein containing drugs be given via?

A

Injection

93
Q

What is the name given to drugs that are inactive until activated by being metabolised?

A

Prodrugs

94
Q

Which 2 groups of drugs are important to substitute for one that is bioequivalent?

A

Mood enhancing drugs

Anti-epileptics

95
Q

What 3 compartments is water and thus drugs distributed into?

A

Intracellular
Extracellular
Adipose tissue

96
Q

What is volume of distribution used to work out?

A

Dose of drug needed to reach certain plasma concentration

97
Q

Does a highly protein bound drug have a high or low volume of distribution?

A

Low

98
Q

Does a highly lipid soluble drug have a high or low volume of distribution?

A

High

99
Q

Do water soluble drugs need to be metabolised to be excreted into the urine?

A

No

100
Q

What does a phase I reaction do to a drug?

A

Makes it more chemically reactive

101
Q

What does a phase II reaction do to a drug?

A

Adds water via a process called conjugation to make drug inactive and able to be renally excreted

102
Q

Drugs excreted into the bile end up being excreted via what?

A

The faeces

103
Q

What stage of renal excretion removes large protein bound drugs?

A

Secretion

104
Q

What % of small water soluble drugs are removed by filtration?

A

20%

105
Q

Define teratogenic

A

Drugs able to cross the placenta during 1st trimester leading to congenital malformations

106
Q

List 7 factors that effect transfer of drug from mother to foetus via placenta

A
Concentration of drug 
Blood flow via placenta 
Anion or cation 
pH of maternal blood 
Protein affinity 
Lipophilicity 
Molecular weight
107
Q

What does pharmacodynamics allow for the prediction of?

A

A drugs effect and ADRs

108
Q

Name 3 target molecules for drugs

A

Enzymes
Transport mechanisms
Receptors

109
Q

What is a ligand?

A

Molecule that binds to receptors initiating a response/preventing a response thus regulating bodily functions.

110
Q

Name 2 locations of receptors

A

Intracellular

Plasma membrane bound

111
Q

List 5 classes of plasma membrane receptor

A
Adrenoreceptors 
Dopamine 
Opioid 
5HT 
Acetylcholine
112
Q

What ligand binds to a 5HT receptor?

A

Seritonin

113
Q

What ligand binds to adrenoreceptors?

A

Adrenaline and noradrenaline

114
Q

How many types of andrenoreceptors are there?

A

4

115
Q

What are the 4 types of andrenoreceptors called?

A

alpha 1
alpha 2
beta 1
beta 2

116
Q

Name the 4 locations of beta 1 andrenoreceptors?

A

Heart
GIT smooth muscle
Glandular tissue
Nerve terminals

117
Q

Stimulation of beta 1 andrenoreceptors in the heart causes what?

A

Increase in heart rate and force of contraction

118
Q

Stimulation of beta 1 andrenoreceptors on smooth muscle stimulates what?

A

Relaxation

119
Q

Stimulation of beta 1 andrenoreceptors on glandular tissue stimulates what?

A

Increased secretion

120
Q

Stimulation of beta 1 andrenoreceptors on nerve terminals stimulates what?

A

Increased neurotransmitter release

121
Q

Name the 4 locations of beta 2 andrenoreceptors

A

Liver
Vascular, uterine, bronchial, bladder smooth muscle
Skeletal muscles
Mast cells

122
Q

Stimulation of beta 2 andrenoreceptors in the liver stimulates what?

A

Glycogenolysis

123
Q

Stimulation of beta 2 andrenoreceptors on skeletal muscle causes what?

A

Tremour

124
Q

Stimulation of beta 2 andrenoreceptors on mast cells stimulates what?

A

Decreased histamine release

125
Q

Stimulation of beta 2 andrenoreceptors on smooth muscle stimulates what?

A

Relaxation

126
Q

Where are beta 2 smooth muscle receptors located?

A

Uterine, bladder, bronchial and vascular

127
Q

Where are beta 1 smooth muscle receptors located?

A

GIT

128
Q

How many types of 5HT receptors are there?

A

3

129
Q

How many types of acetylcholine receptors are there and what are their names?

A

2
Muscanic
Nicotinic

130
Q

How many types of dopamine receptors are there?

A

4

131
Q

What endogenous ligand to intracellular receptors usually bind to?

A

Steroids

132
Q

Explain the mechanism of drugs that bind to intracellular receptors
(which part of the cell do they go to to change what, causing what change to cell metabolism)

A

Drug receptor complex moves to nucleus where it changes gene transcription
Change in gene transcription changes protein synthesis.

133
Q

Steroids bind to which type of receptor?

located where

A

Intracellular