Intro to Pharmacology Flashcards
(126 cards)
1
Q
what is pharmacology
A
the study of the action of drugs on the function of living systems
2
Q
what are the different elements of pharmacology
A
pharmacokinetics and pharmacodynamics
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
4
Q
how can drugs be described as
A
bioactive
5
Q
when did pharmacology first emerge as a scientific discipline
A
in the mid 19th century
6
Q
what was used as medicine before drugs were discovered
A
herbal and other remedies
7
Q
what did the 1692 collection of choice remedies list
A
concoctions of worms, dung, urin and moss from a dead mans skull
8
Q
what makes drugs poisonous
A
their dosage
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
10
Q
what are examples of natural products of drugs
A
plants and animals
11
Q
what does serendipity mean
A
discovered by accident
12
Q
what are structure activity relationships
A
changing the structure of an existing molecule
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
14
Q
what drug is produced from willow trees and give the function
A
aspirin - painkiller
15
Q
what drug is produced from cocoa plants and give the function
A
cocaine - local anaesthetic
16
Q
what drug is produced from the cinchona tree and give the function
A
quinine - anti malarial
17
Q
what drug is produced from poppies and give the function
A
morphine - painkiller
18
Q
what drug is produced from foxgloves and give the function
A
digoxin- heart failure
19
Q
what drug is produced from guggul trees and give the function
A
statins - cholesterol lowering
20
Q
what drug is produced from leeches and what does it do
A
hirudin, an anticoagulent
21
Q
what drug is produced from cone snails and what does it do
A
ziconotide, powerful painkiller
22
Q
what drug is produced from bothrops jararaca
A
a peptide which lowers blood pressure, which is a forerunner for ACE inhibitors
23
Q
what is sildenafil
A
viagra
24
Q
when was viagra invested
A
1989 through accidental repurposing
25
what are the three types of drug names
chemical
generic
proprietary
26
what are chemical names for drugs
IUPAC name that describes the chemical structure of the drug
27
what are general names for drugs
international non proprietary name given to a molecule
28
what are proprietary names for drugs
trade names given to an approved drug by the manufacturer
29
when are drugs given code names
during their development as a way to disguise their identity
30
what is pharmacokinetics
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
31
what is pharmacodynamics
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
32
what is nitrous oxide
an inhaled gas with an analgesic effect which can help with the pain of labour or tooth extraction
33
what does amyl nitrate do
reduce anginal symptoms through inhalation
34
why canaspirin not be used in children
causes reyes syndrome, which leads to liver or brain damage
35
what are the drug effects on the level of the cell
effects on receptors, ion channels, enzymes, transporters and DNA
36
what are the impacts of drugs at the level of the organ and organ system
effects on heart, liver, kidney, CV, central nervous system etc
37
what is the impact of drugs at the level of the organism
therapeutic effects on disease state or process, as well as adverse effects or side effects
38
what is the impact of drugs on the level of society
cost, misuse and drug resistance (antimicrobial stewardship)
39
how many different cell types in the body
200
40
what are the primary tissues
- muscles
- nerves
- epithelium
- bone
- connective
41
how do many drugs work
by mimicing the action of endogenous molecules like neurotransmitters and hormones. can also block this activity
42
which sites do drugs commonly work at
receptors
ion channels
enzymes
transporters
43
how do drugs act
they are small chemical molecules that interact chemically with cellular constituents. they must bind to their targets in order to produce an effect
44
will a drug work if it is not bound
no
45
what can drugs target aside from receptors and ion channels
circulating proteins
DNA
bacterial cell wall
46
what is the primary use of receptors
cell to cell communication
47
what is cell cell comunication important in the context of
neurotransmission
effects of chemical mediators in the bloodstream
hormone and growth factor signalling
48
what is a receptor
recognition molecule for a chemical mediator through which a response is transduced
49
what is the common structure of receptors
protein or complex of proteins that is expressed on the surface of cells, although there are some exceptions to this
50
how do many drugs act in order to do
minimise effects or mimic them
51
what is the lock and key concept
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
what is the basic receptor structure (diagram included in answer)
1 - extracellular domain
2 - transmembrane domain
3 - intracellular domain
53
what is the extracellular domain of the basic receptor
this is where there are basic ligand binding sites that are comprised of hydrophilic amino acids
54
what is the transmembrane domain
anchors the protein in the membrane
comprised of hydrophobic amino acids
alpha helical structure
55
what is the intracellular domain of the basic receptor
interacts with effector mechanisms and is comprised of hydrophilic amino acids
56
what is the series of events of basic signal transduction
signal
reception
transduction
response
57
what is the signal step of signal transduction
this is when the ligand arrives at the receptor
58
what is the reception
this is when the ligand binds to the receptor
59
what is transduction
ligand bound receptor changes conformation
60
what is an example of a fast signal transduction
nictotinic acetylcholine receptor
61
describe type A receptors
very fast signal transduction
62
describe type B receptors
fast signal transduction
63
describe type C receptors
short signal transduction
64
describe type D receptors
very slow signal transduction
65
give an example of a type B receptor
muscarinic acetylcholine receptor
66
give an example of a type C receptor
cytokine receptors
67
give an example of type D receptors
oestrogen receptors
68
what is an agonist
a drug that binds to a specific site on a receptor and mimics the effect of the endogenous ligand for that site
69
what is an antagonist
a drug that binds to a specific site on a receptor, and blocks the effect of the endogenous ligand
70
how do agonists work in lock and key
agonist fits into the lock, mimics the action of the key, and can be used to pick the lock and activate the receptor
71
describe how antagonists work in the lock and key concept
antagonist fits into the lock, gets stuck and prevents opening of the lock by either the endogenous ligand or the agonist
72
describe the affinity and efficacy of agonists
they have both
73
describe the affinity and efficacy of antagonists
they have affinity only
74
what is affinity
measure of the strength of association between the ligand and the receptor
75
what is efficacy
a measure of the ability of an agonist to evoke a cellular response
76
what is pharmacology
study of substances that mostly mimic or block the physiological actions of endogenous chemicals
77
what are the core concepts of pharmacology
pharmacokinetics
pharmacodynamics
78
what is pharmacokinetics
what the body does to the drug
79
what is pharmacodynamics
what the drug does to the body
80
how do drugs act
by binding to specific sites on target proteins, receptors, ion channels, enzymes and transporters
81
what are receptors
membrane bound recognition molecules that transduce chemical signals into cellular responses
82
what are the main causes of pharmacological variability
age
genetics
disease state
drug interactions
environment
83
describe general anaesthetic
- done through inhalation or injection
- dampens neural activity by blocking neurons in the brain
- reduces transmission by hyperpolarising the nerves
84
describe local anaesthetic
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
what does general anaesthetic sedate
the entire body
86
describe the synaptic blocking pathway of general anaesthetic
descreases presynaptic calcium ion entry and this reduces the release of transmitter.
increases the post synaptic hyperpolarisation to increase chlorine ion influx
87
describe the conduction blocking pathway of local anaesthetic
decreases axonal sodium entry to decrease action potential propagation
88
why are the local anaesthetic structures all sort of similar
they all need to act by blocking sodium channels
89
what is the pKa of most local anaesthetics
8-9 - weak bases
90
describe neuronal cell membranes at rest
mostly impermeable to sodium ions
resting negative membrane potential
91
what are the three states of sodium channels
resting
open
inactivated
92
describe the mechanism of action of local anaesthetics
- 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
is the block of nerve conduction by local anaesthetics irreversible
no
94
what must local anaesthetics do in order to be effective
- diffuse from the site of administration, across the nerve cell membrane to the intracellular side
- bind to the local anaesthetic target site
95
what is the half life of ester linked anaesthetics
less than three minutes
96
what is the half life of amide linked anaesthetics
1-3 hours
97
why is the half life of ester linked anaesthetics relatively short
it is taken up from the plasma quickly, so does not need as high of a half life
98
why are the half lives of amide linked anaesthetics relatively long
they have to travel in the blood to the liver to be metabolised, and so must live longer
99
describe the chemical structure of local anaesthetics
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
describe cocaine
medium onset
medium duration
half life of an hour
good tissue penetration
side effects on the CNS and the CV
101
describe procaine
medium onset
short duration
half life of less than an hour
poor tissue penetration
CV and CNS effects
102
describe lidocaine
rapid onset
medium duration
half life less around 2 hours
good tissue penetration
CV effects
103
describe tetracaine
very slow onset
long duration
half life of an hour
moderate tissue penetration
CV effects
104
describe bupivacaine
slow onset
long duration
half life of two hours
moderate tissue penetration
CV effects
105
describe prilocaine
medium onset
medium duration
half life of two hours
moderate tissue penetration
few side effects
106
describe articaine
rapid onset
short duration
half life of 30 minutes
good tissue penetration
CV effects
107
what are local anaesthetics often administered alongside
a vasoconstrictor
108
what causes side effects of local anaesthetics
escapism into systemic circulation
109
how can the side effects of local anaesthetics be managed
by being careful with dosage
110
describe the uses of topical anaesthesia
mucous membranes only, not effective on skin
111
examples of topical anaesthetics
lidocaine
tetracaine
benzocaine
112
describe subcutaneous anaesthetics
infiltration into tissue, combined with vasoconstrictor
113
examples of subcutaneous anaesthetics
most local anaesthetics
114
describe intravenous anaesthetics
used with pressure cuff to limit the spread
115
example of intravenous regional anaesthesia
lidocaine
prilocaine
116
describe nerve block anaesthesia
injected close to nerve plexus, for minor surgery and dentistry
117
example of nerve block anaesthesia
most local anaesthetics
118
describe spinal anaesthesia
surgery to the abdomen and pelvis when the general anaesthetic is not suitable
119
example of spinal anaesthesia
lidocaine
120
describe epidural anaesthesia
form of spinal anaesthesia, given mostly in childbirth
121
example of epidural anaesthesia
lidocaine
bupivacaine
122
what are the three most important things to know about drugs
what it does
its potency
its selectivity
123
describe potency
this is a measure of the dose or concentration of a drug at which it is effective
124
describe what a potent drug is
one that is effective at low doses
125
what does it mean if a drug is selective
if it works on one receptor but not on others
126
does a high potency mean a drug is good or bad
neither
