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Molecules and Cells > Intro to Pharmacology > Flashcards

Intro to Pharmacology Flashcards

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1
Q

what is pharmacology

A

the study of the action of drugs on the function of living systems

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2
Q

what are the different elements of pharmacology

A

pharmacokinetics and pharmacodynamics

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3
Q

what is a drug

A

a chemical substance or natural product that affects the function of cells, organs, systems or the whole body

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4
Q

how can drugs be described as

A

bioactive

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5
Q

when did pharmacology first emerge as a scientific discipline

A

in the mid 19th century

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6
Q

what was used as medicine before drugs were discovered

A

herbal and other remedies

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7
Q

what did the 1692 collection of choice remedies list

A

concoctions of worms, dung, urin and moss from a dead mans skull

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8
Q

what makes drugs poisonous

A

their dosage

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9
Q

what are some different sources of the drugs

A

natural products
serendipity
changing the structure of an existing molecule
using an existing drug in a new disease
computer aided design
studying disease processes

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10
Q

what are examples of natural products of drugs

A

plants and animals

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11
Q

what does serendipity mean

A

discovered by accident

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12
Q

what are structure activity relationships

A

changing the structure of an existing molecule

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13
Q

describe the discovery of pencillium

A

1928 - alexnader fleming first noted the antibacterial properties of it
1938 - howard florey and ernst chain isolated penicllin from the mould and tested it in human volunteers

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14
Q

what drug is produced from willow trees and give the function

A

aspirin - painkiller

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15
Q

what drug is produced from cocoa plants and give the function

A

cocaine - local anaesthetic

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16
Q

what drug is produced from the cinchona tree and give the function

A

quinine - anti malarial

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17
Q

what drug is produced from poppies and give the function

A

morphine - painkiller

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18
Q

what drug is produced from foxgloves and give the function

A

digoxin- heart failure

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19
Q

what drug is produced from guggul trees and give the function

A

statins - cholesterol lowering

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20
Q

what drug is produced from leeches and what does it do

A

hirudin, an anticoagulent

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21
Q

what drug is produced from cone snails and what does it do

A

ziconotide, powerful painkiller

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22
Q

what drug is produced from bothrops jararaca

A

a peptide which lowers blood pressure, which is a forerunner for ACE inhibitors

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23
Q

what is sildenafil

A

viagra

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24
Q

when was viagra invested

A

1989 through accidental repurposing

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25
Q

what are the three types of drug names

A

chemical
generic
proprietary

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26
Q

what are chemical names for drugs

A

IUPAC name that describes the chemical structure of the drug

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27
Q

what are general names for drugs

A

international non proprietary name given to a molecule

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28
Q

what are proprietary names for drugs

A

trade names given to an approved drug by the manufacturer

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29
Q

when are drugs given code names

A

during their development as a way to disguise their identity

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30
Q

what is pharmacokinetics

A

looking at what the body does to the drug, ie the fate of the drug molecule following administration to a living organism or how a drug molecule is affected by exposure to living cells

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31
Q

what is pharmacodynamics

A

what the drug does to the body, the mechanism of drug action or what happens to cell, organs, systems as a result of drug exposure

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32
Q

what is nitrous oxide

A

an inhaled gas with an analgesic effect which can help with the pain of labour or tooth extraction

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33
Q

what does amyl nitrate do

A

reduce anginal symptoms through inhalation

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34
Q

why canaspirin not be used in children

A

causes reyes syndrome, which leads to liver or brain damage

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35
Q

what are the drug effects on the level of the cell

A

effects on receptors, ion channels, enzymes, transporters and DNA

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36
Q

what are the impacts of drugs at the level of the organ and organ system

A

effects on heart, liver, kidney, CV, central nervous system etc

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37
Q

what is the impact of drugs at the level of the organism

A

therapeutic effects on disease state or process, as well as adverse effects or side effects

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38
Q

what is the impact of drugs on the level of society

A

cost, misuse and drug resistance (antimicrobial stewardship)

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39
Q

how many different cell types in the body

A

200

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40
Q

what are the primary tissues

A
  • muscles
  • nerves
  • epithelium
  • bone
  • connective
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41
Q

how do many drugs work

A

by mimicing the action of endogenous molecules like neurotransmitters and hormones. can also block this activity

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42
Q

which sites do drugs commonly work at

A

receptors
ion channels
enzymes
transporters

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43
Q

how do drugs act

A

they are small chemical molecules that interact chemically with cellular constituents. they must bind to their targets in order to produce an effect

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44
Q

will a drug work if it is not bound

A

no

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45
Q

what can drugs target aside from receptors and ion channels

A

circulating proteins
DNA
bacterial cell wall

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46
Q

what is the primary use of receptors

A

cell to cell communication

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47
Q

what is cell cell comunication important in the context of

A

neurotransmission
effects of chemical mediators in the bloodstream
hormone and growth factor signalling

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48
Q

what is a receptor

A

recognition molecule for a chemical mediator through which a response is transduced

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49
Q

what is the common structure of receptors

A

protein or complex of proteins that is expressed on the surface of cells, although there are some exceptions to this

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50
Q

how do many drugs act in order to do

A

minimise effects or mimic them

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51
Q

what is the lock and key concept

A

receptor is the lock, drug is the key
this concept depends on the drug structure
most locks have a master key called an endogenous ligand

52
Q

what is the basic receptor structure (diagram included in answer)

A

1 - extracellular domain
2 - transmembrane domain
3 - intracellular domain

53
Q

what is the extracellular domain of the basic receptor

A

this is where there are basic ligand binding sites that are comprised of hydrophilic amino acids

54
Q

what is the transmembrane domain

A

anchors the protein in the membrane
comprised of hydrophobic amino acids
alpha helical structure

55
Q

what is the intracellular domain of the basic receptor

A

interacts with effector mechanisms and is comprised of hydrophilic amino acids

56
Q

what is the series of events of basic signal transduction

A

signal
reception
transduction
response

57
Q

what is the signal step of signal transduction

A

this is when the ligand arrives at the receptor

58
Q

what is the reception

A

this is when the ligand binds to the receptor

59
Q

what is transduction

A

ligand bound receptor changes conformation

60
Q

what is an example of a fast signal transduction

A

nictotinic acetylcholine receptor

61
Q

describe type A receptors

A

very fast signal transduction

62
Q

describe type B receptors

A

fast signal transduction

63
Q

describe type C receptors

A

short signal transduction

64
Q

describe type D receptors

A

very slow signal transduction

65
Q

give an example of a type B receptor

A

muscarinic acetylcholine receptor

66
Q

give an example of a type C receptor

A

cytokine receptors

67
Q

give an example of type D receptors

A

oestrogen receptors

68
Q

what is an agonist

A

a drug that binds to a specific site on a receptor and mimics the effect of the endogenous ligand for that site

69
Q

what is an antagonist

A

a drug that binds to a specific site on a receptor, and blocks the effect of the endogenous ligand

70
Q

how do agonists work in lock and key

A

agonist fits into the lock, mimics the action of the key, and can be used to pick the lock and activate the receptor

71
Q

describe how antagonists work in the lock and key concept

A

antagonist fits into the lock, gets stuck and prevents opening of the lock by either the endogenous ligand or the agonist

72
Q

describe the affinity and efficacy of agonists

A

they have both

73
Q

describe the affinity and efficacy of antagonists

A

they have affinity only

74
Q

what is affinity

A

measure of the strength of association between the ligand and the receptor

75
Q

what is efficacy

A

a measure of the ability of an agonist to evoke a cellular response

76
Q

what is pharmacology

A

study of substances that mostly mimic or block the physiological actions of endogenous chemicals

77
Q

what are the core concepts of pharmacology

A

pharmacokinetics
pharmacodynamics

78
Q

what is pharmacokinetics

A

what the body does to the drug

79
Q

what is pharmacodynamics

A

what the drug does to the body

80
Q

how do drugs act

A

by binding to specific sites on target proteins, receptors, ion channels, enzymes and transporters

81
Q

what are receptors

A

membrane bound recognition molecules that transduce chemical signals into cellular responses

82
Q

what are the main causes of pharmacological variability

A

age
genetics
disease state
drug interactions
environment

83
Q

describe general anaesthetic

A
  • done through inhalation or injection
  • dampens neural activity by blocking neurons in the brain
  • reduces transmission by hyperpolarising the nerves
84
Q

describe local anaesthetic

A

blocks sodium channels to block nerve transduction so when teeth are being extracted, the nerves are blocked and the person is unaware of the pain

85
Q

what does general anaesthetic sedate

A

the entire body

86
Q

describe the synaptic blocking pathway of general anaesthetic

A

descreases presynaptic calcium ion entry and this reduces the release of transmitter.
increases the post synaptic hyperpolarisation to increase chlorine ion influx

87
Q

describe the conduction blocking pathway of local anaesthetic

A

decreases axonal sodium entry to decrease action potential propagation

88
Q

why are the local anaesthetic structures all sort of similar

A

they all need to act by blocking sodium channels

89
Q

what is the pKa of most local anaesthetics

A

8-9 - weak bases

90
Q

describe neuronal cell membranes at rest

A

mostly impermeable to sodium ions
resting negative membrane potential

91
Q

what are the three states of sodium channels

A

resting
open
inactivated

92
Q

describe the mechanism of action of local anaesthetics

A
  • LA binds to target site on the intracellular side of the sodium channel
  • LA prevents sodium ion influx, preventing depolarisation
  • prevents action potential propagation to pervent perception of pain
  • prevents sodium influx in two ways - blocks channel and stabilises it
93
Q

is the block of nerve conduction by local anaesthetics irreversible

A

no

94
Q

what must local anaesthetics do in order to be effective

A
  • diffuse from the site of administration, across the nerve cell membrane to the intracellular side
  • bind to the local anaesthetic target site
95
Q

what is the half life of ester linked anaesthetics

A

less than three minutes

96
Q

what is the half life of amide linked anaesthetics

A

1-3 hours

97
Q

why is the half life of ester linked anaesthetics relatively short

A

it is taken up from the plasma quickly, so does not need as high of a half life

98
Q

why are the half lives of amide linked anaesthetics relatively long

A

they have to travel in the blood to the liver to be metabolised, and so must live longer

99
Q

describe the chemical structure of local anaesthetics

A

weak bases
has an amine group, which is ionised or unionised
pKa ranges from 7.6 - 9
at pH 7.4, both ionised and neutral forms of the local anaesthetic exists, although there is more of the ionised form

100
Q

describe cocaine

A

medium onset
medium duration
half life of an hour
good tissue penetration
side effects on the CNS and the CV

101
Q

describe procaine

A

medium onset
short duration
half life of less than an hour
poor tissue penetration
CV and CNS effects

102
Q

describe lidocaine

A

rapid onset
medium duration
half life less around 2 hours
good tissue penetration
CV effects

103
Q

describe tetracaine

A

very slow onset
long duration
half life of an hour
moderate tissue penetration
CV effects

104
Q

describe bupivacaine

A

slow onset
long duration
half life of two hours
moderate tissue penetration
CV effects

105
Q

describe prilocaine

A

medium onset
medium duration
half life of two hours
moderate tissue penetration
few side effects

106
Q

describe articaine

A

rapid onset
short duration
half life of 30 minutes
good tissue penetration
CV effects

107
Q

what are local anaesthetics often administered alongside

A

a vasoconstrictor

108
Q

what causes side effects of local anaesthetics

A

escapism into systemic circulation

109
Q

how can the side effects of local anaesthetics be managed

A

by being careful with dosage

110
Q

describe the uses of topical anaesthesia

A

mucous membranes only, not effective on skin

111
Q

examples of topical anaesthetics

A

lidocaine
tetracaine
benzocaine

112
Q

describe subcutaneous anaesthetics

A

infiltration into tissue, combined with vasoconstrictor

113
Q

examples of subcutaneous anaesthetics

A

most local anaesthetics

114
Q

describe intravenous anaesthetics

A

used with pressure cuff to limit the spread

115
Q

example of intravenous regional anaesthesia

A

lidocaine
prilocaine

116
Q

describe nerve block anaesthesia

A

injected close to nerve plexus, for minor surgery and dentistry

117
Q

example of nerve block anaesthesia

A

most local anaesthetics

118
Q

describe spinal anaesthesia

A

surgery to the abdomen and pelvis when the general anaesthetic is not suitable

119
Q

example of spinal anaesthesia

A

lidocaine

120
Q

describe epidural anaesthesia

A

form of spinal anaesthesia, given mostly in childbirth

121
Q

example of epidural anaesthesia

A

lidocaine
bupivacaine

122
Q

what are the three most important things to know about drugs

A

what it does
its potency
its selectivity

123
Q

describe potency

A

this is a measure of the dose or concentration of a drug at which it is effective

124
Q

describe what a potent drug is

A

one that is effective at low doses

125
Q

what does it mean if a drug is selective

A

if it works on one receptor but not on others

126
Q

does a high potency mean a drug is good or bad

A

neither

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