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Cardiovascular and haemotology > Biochemicals principles of pharmacology > Flashcards

Biochemicals principles of pharmacology Flashcards

1
Q

what does ACE inhibitors stand for

A

angiotensin converting enzyme inhibitors

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2
Q

what are ACE inhibitors

A

enzyme inhibitors, drugs that target enzymes, protease

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3
Q

targets of enzyme inhibitors include…

A

enzymes, ion channels, transport proteins, receptors

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4
Q

examples of enzyme inhibitors used as an antibiotic

A

amoxicillin

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5
Q

examples of enzyme inhibitors used for cardiovascular problems

A

ACE inhibitors, statins, aspirin

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6
Q

examples of enzyme inhibitors used as an analgesic/pain

A

paracetamol, ibuprofen, rivaroxaban

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7
Q

examples of enzyme inhibitors used as an anticoagulant/blood thinner

A

warfarin

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8
Q

what are ACE inhibitors derived from

A

snake venom

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9
Q

what do ACE inhibitors do

A

reduced blood pressure

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10
Q

adverse effects of ACE inhibitors

A

coughs and dizziness

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11
Q

what do the name of ACE inhibitors end in

A

-pril
captopril, lisinopril, ramipril

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12
Q

what 2 things does ACE inhibitors reduce and what are the effects of it

A
  1. reduce formation of angiotensin II- reduces vasoconstriction and salt/water retention
  2. reduces breakdown of bradykinin (signalling peptides) into inactive peptides- increased bradykinin causes persistent coughing
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13
Q

what causes a persistent cough

A

increased amount of bradykinin

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14
Q

mechanism of action of a reversible inhibitor

A

non-covalent

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15
Q

mechanism of action of a irreversible inhibitor

A

covalent

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16
Q

example of a reversible inhibitor

A

captopril binding to ACE with hydrogen bonds

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17
Q

example of a irreversible inhibitor

A

aspirin binding to cox enzymes

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18
Q

what is enzyme kinetics

A

action of enzyme inhibitors can be determined using experiments that determine the rate of enzymatic reactions in response to changes like changing substrate concentration

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19
Q

name the two types of plot/graphs used in enzyme kinetics

A

michaelis-menten
lineweaver-burk

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20
Q

what does the michaelis-menten plot show

A

how rate changes as substrate concentration changes

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21
Q

what is the michaelis-menten constant

A

Km, concentration of substrate at which the initial velocity of catalysis is half maximal

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22
Q

what does the Km tell us

A

how well the enzyme binds to the substrate

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23
Q

how to determine Km

A

doing experiments that vary substrate conc, enzyme conc constant, determine initial velocity (product formation over time)

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24
Q

what is the problem with michaelis-menten plot and what is the solution

A

the hyperbola is difficult to fit accurately without a computer, solution is to us a double reciprocal plot (1/s and 1/v) which is the lineweaver-burk plot

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25
Q

what is the michaelis-menten equation

A

v=vmax[s]/Km+[s]

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26
Q

what is the lineweaver-burk equation

A

1/v=(Km/vmax)(1/[s]
)+1/vmax

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27
Q

how to transform a michaelis-menten graph into lineweaver-burk graph

A

do double reciprocals of the values in michaelis-menten (put the values 1/x)

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28
Q

why is lineweaver-burk plot better

A

allows more accurate estimation of Km and vmax

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29
Q

example of a calcium channel blocker

A

amlodipine

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30
Q

what do calcium ions do

A

trigger muscle contraction

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31
Q

calcium channel blockers such as amlodipine prevent the uptake of Ca2+ by what two structures

A

vascular smooth muscle and cardiomyocytes

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32
Q

what are the vascular effects of amlodipine

A

vasodilation (smooth muscle relaxation)

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33
Q

what are the cardiac effects of amlodipine

A

decreased contractility and decreased heart rate

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34
Q

what is amlodipine

A

calcium channel blocker

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35
Q

adverse effects of calcium channel blockers

A

arterial dilation, veins unaffected, excess fluid goes into surrounding tissue causing tissue to swell

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36
Q

what are ion channels

A

proteins that facilitate transport of molecules across the cell membrane

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37
Q

two types of ion channels and how they are controlled

A
  1. voltage gated- controlled by potential differences
  2. ligand gated- binding of a ligand will cause it to open
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38
Q

ion channels are multimeric proteins, what does multimeric mean

A

its a protein composed of several subunits

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39
Q

how does the calcium channel blocker amlodipine work

A

calcium channel has 4 aspartate residues, amlodipine binds and causes asymmetry in the selectivity filter which prevents calcium ions from passing through

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40
Q

what does potency mean

A

the amount of drug needed to produce an effect

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41
Q

how is the potency of a drug determined

A

by comparing the concentration at which 50% inhibition is achieved (IC50)

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42
Q

how is IC50 represented on a graph

A

10log

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43
Q

IC50 units of low, medium and high potency

A

low- mM
medium- μM
high- nM

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44
Q

two things that IC50 is used to measure for

A

ion channels and enzyme inhibitors

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45
Q

what characteristic of a drug is the most desired (potency and IC50)

A

high potency and low IC50

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46
Q

what are solute transporters

A

diverse proteins involved in transport of ions and organic compounds

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47
Q

what do thiazide diuretics do

A

inhibits action of specific transporters

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48
Q

effects of thiazide diuretics

A

reduce cardiac output, reduce blood volume, lowers blood pressure, increases water and salt excretion

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49
Q

where does energy for active transport come from

A

hydrolysis of ATP

50
Q

what inhibits sodium potassium pump

A

cardiac glycosides

51
Q

what do cardiac glycosides do

A

inhibit sodium potassium pump

51
Q

what are the effects of inhibiting sodium potassium pump

A

reduces heart rate, increases the force of contraction of the heart muscle

51
Q

what is used to treat heart failure

A

cardiac glycosides

51
Q

example of a cardiac glycoside

A

digoxin

51
Q

name 2 inhibitors used to treat hypotension

A

calcium channel blockers and thiazide diuretics

51
Q

what are cardiac glycosides used for

A

treating heart failure

52
Q

what is used to treat the stomach

A

proton pump inhibitor

52
Q

what does the inhibition of sodium potassium ATPase lead to

A

increased intracellular sodium ion concentration which leads to increase of intracellular calcium ion concentration via the sodium calcium exchange system

53
Q

name two parts of the nervous system

A

central and peripheral

54
Q

name two parts of the peripheral nervous system

A

somatic and autonomic

55
Q

difference between somatic and autonomic nervous system

A

somatic- voluntary control of skeletal muscles, sensory/motor control
autonomic- subconscious, organ function

56
Q

types of autonomic nervous system

A

sympathetic and parasympathetic

57
Q

difference between sympathetic and parasympathetic nervous system

A

sympathetic- prepares body, flight of fight, increases heart rate, vasoconstriction

parasympathetic- promotes restorative functions, rest or digest, slows heart rate

58
Q

what is the anatomic difference between somatic and autonomic nervous system

A

somatic has a single axon extending from neurone in CNS to effector and autonomic is a two neurone system

59
Q

what are the normal conditions in the heart in terms of signalling from the peripheral nervous system

A

balanced signals from sympathetic and parasympathetic

60
Q

what does efferent mean

A

CNS to organ/muscle

61
Q

what does afferent mean

A

organ to CNS

62
Q

what is ganglion

A

cluster of peripheral autonomic neurones

63
Q

anatomy of autonomic nervous system

A

-preganglionic neurone and post ganglionic neurone
sympathetic- short, long
parasympathetic- long, short
-two neurone chain
-CNS to ganglion to effector tissue

64
Q

what is a synapse

A

structure/gap between 2 neurones that allow one neurone to transmit a signal to the second neurone

65
Q

what does SNAP stand for

A

sympathetic noradrenaline, acetylcholine parasympathetic

66
Q

what are beta blockers

A

competes with binding of noradrenaline/adrenaline to beta 1 adrenergic receptors to block sympathetic signalling to the heart

67
Q

adverse effects of beta blockers

A

affinity for beta 2 adrenergic receptors so it can exacerbate asthma

68
Q

short definition of beta blockers

A

antagonist of beta 1 adrenergic receptors

69
Q

what are beta blockers used to treat

A

angina- chest pain from narrowing arteries supplying the heart
heart failure- not enough blood pumped to body
atrial fibrillation- irregular heartbeat
heart attack- blocked blood supply to heart

70
Q

4 types of receptors

A

-ligand gated ion channels
-GPCR
-kinase linked receptors
-nuclear receptors

71
Q

example of GPCR

A

adrenergic and cholinergic

72
Q

example of ligand gated ion channel receptors

A

nicotinic acetylcholine

73
Q

what does GPCR stand for

A

G protein coupled receptors

74
Q

what do drugs do to receptors

A

drugs can stimulate or inhibit receptors, stimulators are agonists and drugs that inhibit are called antagonists

75
Q

what are agonists

A

drugs that stimulate receptors

76
Q

example of an agonist

A

adrenaline

77
Q

what are antagonist

A

drugs that inhibit/block receptors

78
Q

example of an antagonist

A

beta blockers

79
Q

at effector organs what is the receptor for acetylcholine

A

muscarinic receptors

80
Q

name the receptor adrenaline and noradrenaline binds to

A

adrenergic receptors

81
Q

name of receptor acetylcholine binds to

A

cholinergic receptors

82
Q

what is a ligand

A

chemical that can form a complex with a receptor

83
Q

what is a receptor

A

protein that recognises a specific chemical signal from outside the cell

84
Q

principles of signalling

A

specificity, amplification, modularity, desensitisation/adaptation, integration of signalling

85
Q

what is specificity

A

receptor recognises a specific signal leading to a response

86
Q

what is amplification

A

signal of a single ligand gives rise to many second messengers and modified molecules in the cell

87
Q

describe the process of amplification

A

-ligand L binds to receptor R
-receptor R binds to intracellular G protein
-G protei activates enzyme (AC=adenylyl cyclase) that produces a second messenger cAMP
-signalling cascade

88
Q

membrane proteins involved in gpcr signalling

A

integral, lipid modified, accessory

89
Q

what is modularity

A

receptor signalling uses interchangeable parts
-both receptors use the same chemical to stimulate but different outcomes

90
Q

what is desensitisation/adaptation

A

activation of a receptor triggers a feedback loop that inactivates the receptor

91
Q

what is integration of signalling

A

activation of two or more receptors lead to a receptor that integrates both signals

92
Q

describe scatchard analysis

A
93
Q

what is B max in the scatchard analysis

A

total number of binding sites

94
Q

what is the dissociation constnat in the scatchard analysis

A

1/2Bmax

95
Q

autonomic nervous system anatomy

A

sympathetic- short, long
autonomic- long, short

96
Q

what is potency

A

measure of drug activity expressed in terms of amount required to produce an effect

97
Q

what is EC50

A

effective concentration at 50% of max response

98
Q

what is receptor occypancy

A

fraction of receptors bound by ligand/drug

99
Q

what is efficacy

A

ability of a drug to produce an effect

100
Q

equation for response of drug

A

R=Rmax x conc of drug/(conc of drug+EC50)

101
Q

what is a partial agonist

A

agonist that is unable to produce a full response even when all receptors are occupied

102
Q

what is an agonist

A

stimulator

103
Q

what is an antagonist

A

inhibitor

104
Q

what does affinity of a ligand mean

A

ability of ligand to bind to a receptor

105
Q

what is potency

A

concentration of an agonist required to reach half maximum effect

106
Q

reversible antagonist and an example

A

non covalent ligand receptor interaction, competitive and uncompetitive

eg. propanolol to beta1 adrenergic receptors

107
Q

irreversible antagonist and an example

A

covalent ligand and receptor interaction

eg. phenoxybenzamine binding to a1 and a2 adrenergic receptors

108
Q

what is a pure antagonist

A

no effect on receptor activity

109
Q

what is an inverse angonsist

A

inhibits constitutive activity

110
Q

what are spare receptors

A

fraction of receptors not occupied at max response

111
Q

what does unsurmountable mean

A

non competitive, irreversible, no amount of concentration can increase the response

112
Q

what does parasympatholytic mean and example

A

substance that reduces the activity of the parasympathetic nervous system like atropine (antagonist)

113
Q

what does sympathomimetic mean and example

A

substance increases sympathetic signals like adrenaline (agonist)

114
Q

what is -mimetic and -olytic

A

sympathomimetic/parasympathomimetic= increases signals/activity

sympatholytic/parasympatholytic= reduces activity

115
Q

what is therapeutic index and its equation

A

ratio of dose of drug that causes adverse effects to the dose that leads to desired pharmacological effect

Ti=TD50/ED50

TD50=toxic dose for 50% population
ED50=effective dose

116
Q
A

Cardiovascular and haemotology (11 decks)

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