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MB1: Cardio > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

where would a fast response action potential be found

A

atrial and ventricular myocytes

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2
Q

where would a slow response action potential be found

A

SAN and AVN

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3
Q

Phase 0

A

rapid depolarisation by activation of Na channels

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4
Q

Phase 1

A

closure of sodium channels and activation of transient outward potassium current

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5
Q

Phase 2

A

plateau - L-type calcium channels open to balance potassium repolarisation
transient K channels close and delayed K channels open

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6
Q

Phase 3

A

outward potassium exceeds calcium influx so membrane repolarisation

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7
Q

Phase 4

A

resting potential
not fully resting due to small inward leak of sodium (funny current)
Na/KATPase keeps balance to prevent depolarisation

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8
Q

what is pacemaker potential

A

membrane potential sloping towards depolarisation
creates automaticity of nodal tissue
HCN triggers funny current at phase 3

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9
Q

noradrenaline and adrenaline bind to __ adrenoceptors in nodal and myocardial cells

A

B1

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10
Q

how is a positive chronotropic effect by noradrenaline and adrenaline achieved?

A

binds to B1, increase cAMP concn
enhances funny current so increase in calcium and depolarisaiton
reduction in threshold for action potential

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11
Q

besides a positive chronotropic effect, what other effects do noradrenaline and adrenaline have on the heart?

A

+ve inotropic - troponin more sensitive to calcium so more contraction
+ve dromotropic effect - velocity in AVN, enhanced funny current
+ve lusitropic
increased Na/KATPase activity

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12
Q

acetylcholine binds to __ muscarinic receptors largely in nodal cells

A

M2

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13
Q

how is a negative chronotropic effect by acetylcholine achieved?

A

binds to M2, alpha reduce cAMP. Beta/gamma cause outward K flow
decreased slope of funny current and increased threshold
hypolarisation in phase 4

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14
Q

besides a negative chronotropic effect what other effects do acetylcholine have

A
  • ve inotropic effect - decreased calcium entry

- ve dromotropic effect

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15
Q

true/false - the block of HCN increases funny current and pacemaker potential

A

false- it reduces it

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16
Q

what drug may block HCN in angina treatment?

A

Ivabridine

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17
Q

how does ivabridine prevent angina becoming unstable

A

reduces heart rate by lowering funny current so slows oxygen demand

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18
Q

describe excitation contraction coupling in cardiac muscle

A

calcium flows into cell (L-type) and binds to cause CICR from SR
Ca binds to troponin C and allows myosin cross bridge to form
in repolarisation L-type channels close and calcium pumped back into SR. muscles relax

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19
Q

how does cAMP increase cardiac contractility?

A

cAMP increases calcium sensitivity and so Troponin C becomes more sensitive to calcium causing increased CICR

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20
Q

3 examples of catecholamines

A

dobutamine, adrenaline, noradrenaline

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21
Q

cardiac efficiency with catecholamines is ___

A

decreased

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22
Q

adrenaline affects 3 different receptors significant in cardiac arrest. what are they?

A

B1- positive chronotropic/inotropic
B2 - coronary artery dilatation
A1 - redistricuting blood flow to heart and constricing blood supply to skin, gut

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23
Q

adrenaline is given IV/IM cor cardiac arrest and IV/IM for anaphylaxis

A

IV

IM

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24
Q

when is dobutamine given and why

A

acute heart failure (surgery, cardiogenic or septic shock)

causes less tachycardia

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25
Q

non selective beta blockers, what they block and some indications

A 
propanolol
carvedilol
metoprolol
alprenolol
migraines and thyrotoxicosis
block all beta adrenoceptors non-selectively
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26
Q

do beta blockers reduce rate, force, CO or MAP at rest?

A

no, only on exercise

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27
Q

beta blockers reduce the diameter of coronary arteries. is this bad?

A

no, as heart rate is lower and contraction is less intense there is better oxygenation

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28
Q

where are beta blockers indicated

A

cardiac arrythmia
Angina - after calcium entry blockers
heart failure - low dose carvedilol
hypertension if other comorbidities present

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29
Q

adverse effects of beta blockers

A 
bronchospasm in asthmatics 
aggrevation in cardiac failure - except low dose 
bradycardia 
hypoglycaemia 
fatigue 
cold extremities
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30
Q

atropine is a competitive antagonist of what

what does it do?

A

ACh

increase HR

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31
Q

where is atropine indicated?

A

severe or symptomatic bradycardia or MI
In MI give IV in incremental doses
anticolinesterase poisoning

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32
Q

why should atropine not be given in low doses

A

it may cause bradycardia

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33
Q

alternative to atropine

A

glycopyrronium

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34
Q

when is the use of digoxin indicated?

A

CO insufficient to provide adequate tissue perfusion

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35
Q

digoxin is an inotropic drug that enhances cardiac contractility. how does it do this?

A

reduces membrane potential by inhibiting Na/KATPase

increased intracellular Ca so greater CICR and contractility

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36
Q

digoxin has dangerously enhanced side effects in the presence of _____

A

hypokalaemia

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37
Q

what direct effect does digoxin have on the heart?

A

shortens action potential and refractory period

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38
Q

what does digoxin do to vagal activity

A

it increases it, to slow SAN discharge and AVN conduction

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39
Q

where is digoxins use indicated in disease?

A

IV acute heart failure
oral chronic heart failure
AF - sometimes

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40
Q

side effects of digoxin

A 
heart block
oscillatory afterpotentials due to Ca overload 
Nausea and vomiting 
diarrhoea 
vision disturbance
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41
Q

name a calcium sensitiser and where it is used

A

levosimendan

IV treatment of acute decompensated heart failure

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42
Q

what do calcium sensitisers do?

A

bind to troponin C to sensitise it to calcium to enhance contractility
vasodilate smooth muscle to reduce afterload

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43
Q

name 2 inodilators and where used

A

amrinone and milrinone

IV acute heart failure

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44
Q

what do inodilators do?

A

increase myocardial contractility and decrease SVR

worsens survival

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45
Q

what are the common uses of statins and 2 common ones

A

hypercholesterolaemia, diabetes, angina/MI, TIA or high risk of MI/CVA
Simvastatin/atorvastatin

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46
Q

contraindications of statins

A

muscle pain

Rhabdomyolysis

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47
Q

name a fibrate and its indication

A

benzfibrate

hypertriglyceraemia or low HDL

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48
Q

where is a PCSK9 inhibitor indicated and what does it do

A

FH

inhibits binding of PCSK9 to LDLR, so more LDLR free to clear cholesterol

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49
Q

names of PCSK9 inhibitors

A

evolucumab, alirocumab

50
Q

name a 2 thiazide diuretics and where they would be used

A

bendroflurothiazide - hypertension

furesemide - heart failure

51
Q

contraindications of thiazides

A

hypokalaemia
increased uric acid and gout
impotence
hyperglycaemia

52
Q

name 2 cardioselective beta blockers and their indication

A

atenolol, bisoprolol

angina, MI, hypertension, heart failure

53
Q

beta blocker contraindication

A

asthma, especially non selective beta blocker
tiredness
cold peripheries
heart failure in short term

54
Q

name a dihydropyridine (CCB) and indication/contraindication

A

amlodipine
angina, hypertension
heart failure

55
Q

name 2 rate limiting calcium antagonists (CCB) and their indications/contraindication

A

verapamil, diltiazem
hypertension, angina, SVT, AF
contraindicated with beta blockers and heart failure

56
Q

name an ACEI and how it works

A

lisinopril

blocks ACE converting Angiotensin I to angiotensin II

57
Q

contraindications of, or issuing, ACEI/ARB

A

bad for renal artery stenosis

can cause cough, angioneurotic oedema or renal dysfunction

58
Q

true/false - the only drug you should use in pregnancy for hypertension is an ACEI/ARB

A

False - never use it

59
Q

name an ARB and its use

A

losartan

heart failure or hypertension

60
Q

name an alpha blocker, why it would be used and contraindication

A

doxazosin
hypertension, prostatic hypertrophy
causes postural hypotension

61
Q

how does an alpha inhibitor work?

A

blocks alpha receptors to prevent vasoconstriction

62
Q

name a mineralocorticoid antagonist and its use/contraindication

A

spironolactone
resistant hypertension, heart failure
hyperkalaemia, renal impairment, gynaecomastia

63
Q

how does spironolactone work

A

blocks aldosterone receptors

64
Q

use of isosorbide mononitrate and contraindiation

A

acute heart failure and angina
headache, hypotension/collapse
drug tolerance

65
Q

what is nicorandil and how often is it used

A

K ATP channel activator

it shouldnt be use where possible as it can cause mouth ulcers and GI bleeds

66
Q

use of ranolazine

A

refractory angina

67
Q

4 antiplatelet drugs

A

aspirin, clopidogrel, ticagrelor, prasugrel

68
Q

where are antiplatelet drugs used

A

angina, acute MI, CVA, TIA

69
Q

what clotting factors does warfarin block

A

2, 7, 9, 10

70
Q

rivaroxaban inhibits factor X/IIa and dabigatran inhibits factor X/IIa

A

X

IIa

71
Q

2 fibrinolytic drugs, indications and contraindication

A

TPA, streptokinase
STEMI, CVA, PE
avoided in haemorrage, trauma, peptic ulcer, severe diabetic retinopathy

72
Q

pharmacologic treatment of AF

A

BB, digoxin, CCB, chemical cardioversion with amiodarone

73
Q

what drugs can be used in heart failure?

A 
ACEI/ARB
Beta blockers 
spironolactone 
neprilisin inhibitors
diuretics 
digoxin
74
Q

side effects of salcubitril valsartin

A

hypotension, renal impairment, hyperkalaemia, angioneurotic oedema

75
Q

side effects digoxin

A

nausea, vomiting, yellow vision, bradycardia or heart block, ventricular arrythmia

76
Q

atherosclerosis is associated with high/low LDL and high/low HDL

A

low

high

77
Q

lipoproteins have a hydrophobic core containing what?

A

esterified choleserol and TAGs

78
Q

apoA-1, apoA-II is found in ____

A

HDL

79
Q

apoB-100 is found in ____

A

LDL and VLDL

80
Q

apoB-48 is found in ____

A

chylomicrons

81
Q

where are chylomicrons formed?

A

intestinal cells

82
Q

What protein allows cholesterol into the cell?

A

niemann pick C1 like protein (NPC1L1)

83
Q

how are chylomicrons transported into central circulation

A

via thoracic duct

84
Q

chylomicrons and VLDL must undergo activation by

A

apoC-II

85
Q

what protein breaks down TAGs into fatty acids and glycerol to enter the cell

A

lipoprotein lipase

86
Q

what are chylomicrons and VLDL termed after depositing TAGs into cell

A

remnants

87
Q

clearance of LDL is dependent on?

A

LDL receptor

88
Q

cholesterol is a rate limiting step in cholesterol synthesis. how does it do this?

A

inhibits HMG-CoA reductase

89
Q

why is LDL bad

A

oxidation of LDL, taken up by macrophages to form fatty foam cells that cause fatty streaks, the first step to synthesising atheromas.
collagen depositon and smooth muscle proloferation to form fibrous cap of plaque

90
Q

Why is HDL good

A

accepts cholesterol from plasma membrane of cells and returns to liver for elimination

91
Q

how does ezitimibe work

A

inhibits NPC1L1 to reduce cholesterol absorption as add on drug

92
Q

how do fibrates reduce TGA levels

A

enhance transcription of certain genes such as that of LPL

93
Q

where are fibrates contraindicated

A

in use with statins or alcoholics as can cause rhabdomyolysis

94
Q

when are statins ineffective

A

homozygous FH as no LDLR to target to increase

95
Q

when should lipid levels be measured?

A

MI, CVA, acute pancreatitis or any vascular disease, FHx or clinical signs

96
Q

What level should total cholesterol be below

A

5mmol/L

97
Q

how does hypertriglyceridaemia cause acute pancreatitis

A

chylomicrons obstruct capillaries to cause ischaemia and acidosis. this causes cytotoxic injury and inflammation

98
Q

describe smooth muscle contraction in blood vessels

A

influx of calcium causes CICR from SR which activates MLCK and contracts smooth muscle

99
Q

describe smooth muscle relaxation in blood vessels

A

calcium is pumped back into SR, inhibits calcium influx and promotes efflux. MLC phosphatase depohophorylates MLCK and promotes relaxation

100
Q

how does nitric oxide cause muscle relaxation

A

stimulates guanyate cyclase to promote muscle relaxation

101
Q

how do organic nitrates used as medicines cause muscle relaxation and vasodialtion

A

directly stimulate guanylate cyclase to promote muscle relaxation

102
Q

how do nitrates relieve symptoms of angina

A

venodilation reduces preload and vasodilation reduces afterload so less work required for the heart = less ischaemia

103
Q

Adverse effects of nitrates

A

headache
hypotension and fainting
reflex tachycardia
methaemoglobin formation

104
Q

true/false- patients can have a tolerance to nitrates

A

true - nitrate free times should be kept to

105
Q

what do calcium antagonists block

A

opening of L-type calcium channels

106
Q

what do L-type Ca channels mediate and therefore how do CCB act

A

upstroke of AP in SAN and AVN - reduce rate and conduction

Phase 2 of ventricular AP - reduce force of contraction

107
Q

what CCB preferred for hypertension

A

amlodipine, targets vascular smooth muscle

108
Q

what CCB preferred for angina

A

verapamil and diltiazem as reduce contractile force and conduction. amlodipine can be used to reduce afterload

109
Q

what CCB used for arrythmia and why

A

verapamil and suppresses AVN conduction

110
Q

Adverse effects amlodipine

A

hypotension, ankle oedema, dizziness, flushing

111
Q

contraindication of verapamil

A

do not use in heart failure or in conjunction with beta blockers

112
Q

how does lisonopril reduce hypertension

A

reduced aldosterone release so greater water loss

arterial and venous dilation due to reduced AT1 stimulation

113
Q

adverse effects of ACEI

A

hypotension
dry cough
hyperkalaemia
angioedema

114
Q

how does losartan work

A

blocks angiotensin II from binding to AT1 receptors competitively

115
Q

where are ACEI and ARB contraindicated

A

pregnancy and bilateral renal stenosis

116
Q

how are beta blockers effective in angina

A

reduce HR and SV so decrease workload on the heart

117
Q

true/false - beta blockers only work in patients with hypertension for a limited time

A

true - CO is reduced but returns over time

118
Q

how do potassium channel openers work

A

open potassium channels to cause closure of calcium channels to relax smooth muscle

119
Q

minoxidil has what side effects

A

reflex tachycardia and salt and water retention

120
Q

name 2 alpha blockers and a side effect

A

doxazosin and prazosin

postural hypotension

MB1: Cardio (17 decks)

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