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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
non selective beta blockers, what they block and some indications
``` propanolol carvedilol metoprolol alprenolol migraines and thyrotoxicosis block all beta adrenoceptors non-selectively ```
26
do beta blockers reduce rate, force, CO or MAP at rest?
no, only on exercise
27
beta blockers reduce the diameter of coronary arteries. is this bad?
no, as heart rate is lower and contraction is less intense there is better oxygenation
28
where are beta blockers indicated
cardiac arrythmia Angina - after calcium entry blockers heart failure - low dose carvedilol hypertension if other comorbidities present
29
adverse effects of beta blockers
``` bronchospasm in asthmatics aggrevation in cardiac failure - except low dose bradycardia hypoglycaemia fatigue cold extremities ```
30
atropine is a competitive antagonist of what | what does it do?
ACh | increase HR
31
where is atropine indicated?
severe or symptomatic bradycardia or MI In MI give IV in incremental doses anticolinesterase poisoning
32
why should atropine not be given in low doses
it may cause bradycardia
33
alternative to atropine
glycopyrronium
34
when is the use of digoxin indicated?
CO insufficient to provide adequate tissue perfusion
35
digoxin is an inotropic drug that enhances cardiac contractility. how does it do this?
reduces membrane potential by inhibiting Na/KATPase | increased intracellular Ca so greater CICR and contractility
36
digoxin has dangerously enhanced side effects in the presence of _____
hypokalaemia
37
what direct effect does digoxin have on the heart?
shortens action potential and refractory period
38
what does digoxin do to vagal activity
it increases it, to slow SAN discharge and AVN conduction
39
where is digoxins use indicated in disease?
IV acute heart failure oral chronic heart failure AF - sometimes
40
side effects of digoxin
``` heart block oscillatory afterpotentials due to Ca overload Nausea and vomiting diarrhoea vision disturbance ```
41
name a calcium sensitiser and where it is used
levosimendan | IV treatment of acute decompensated heart failure
42
what do calcium sensitisers do?
bind to troponin C to sensitise it to calcium to enhance contractility vasodilate smooth muscle to reduce afterload
43
name 2 inodilators and where used
amrinone and milrinone | IV acute heart failure
44
what do inodilators do?
increase myocardial contractility and decrease SVR | worsens survival
45
what are the common uses of statins and 2 common ones
hypercholesterolaemia, diabetes, angina/MI, TIA or high risk of MI/CVA Simvastatin/atorvastatin
46
contraindications of statins
muscle pain | Rhabdomyolysis
47
name a fibrate and its indication
benzfibrate | hypertriglyceraemia or low HDL
48
where is a PCSK9 inhibitor indicated and what does it do
FH | inhibits binding of PCSK9 to LDLR, so more LDLR free to clear cholesterol
49
names of PCSK9 inhibitors
evolucumab, alirocumab
50
name a 2 thiazide diuretics and where they would be used
bendroflurothiazide - hypertension | furesemide - heart failure
51
contraindications of thiazides
hypokalaemia increased uric acid and gout impotence hyperglycaemia
52
name 2 cardioselective beta blockers and their indication
atenolol, bisoprolol | angina, MI, hypertension, heart failure
53
beta blocker contraindication
asthma, especially non selective beta blocker tiredness cold peripheries heart failure in short term
54
name a dihydropyridine (CCB) and indication/contraindication
amlodipine angina, hypertension heart failure
55
name 2 rate limiting calcium antagonists (CCB) and their indications/contraindication
verapamil, diltiazem hypertension, angina, SVT, AF contraindicated with beta blockers and heart failure
56
name an ACEI and how it works
lisinopril | blocks ACE converting Angiotensin I to angiotensin II
57
contraindications of, or issuing, ACEI/ARB
bad for renal artery stenosis | can cause cough, angioneurotic oedema or renal dysfunction
58
true/false - the only drug you should use in pregnancy for hypertension is an ACEI/ARB
False - never use it
59
name an ARB and its use
losartan | heart failure or hypertension
60
name an alpha blocker, why it would be used and contraindication
doxazosin hypertension, prostatic hypertrophy causes postural hypotension
61
how does an alpha inhibitor work?
blocks alpha receptors to prevent vasoconstriction
62
name a mineralocorticoid antagonist and its use/contraindication
spironolactone resistant hypertension, heart failure hyperkalaemia, renal impairment, gynaecomastia
63
how does spironolactone work
blocks aldosterone receptors
64
use of isosorbide mononitrate and contraindiation
acute heart failure and angina headache, hypotension/collapse drug tolerance
65
what is nicorandil and how often is it used
K ATP channel activator | it shouldnt be use where possible as it can cause mouth ulcers and GI bleeds
66
use of ranolazine
refractory angina
67
4 antiplatelet drugs
aspirin, clopidogrel, ticagrelor, prasugrel
68
where are antiplatelet drugs used
angina, acute MI, CVA, TIA
69
what clotting factors does warfarin block
2, 7, 9, 10
70
rivaroxaban inhibits factor X/IIa and dabigatran inhibits factor X/IIa
X | IIa
71
2 fibrinolytic drugs, indications and contraindication
TPA, streptokinase STEMI, CVA, PE avoided in haemorrage, trauma, peptic ulcer, severe diabetic retinopathy
72
pharmacologic treatment of AF
BB, digoxin, CCB, chemical cardioversion with amiodarone
73
what drugs can be used in heart failure?
``` ACEI/ARB Beta blockers spironolactone neprilisin inhibitors diuretics digoxin ```
74
side effects of salcubitril valsartin
hypotension, renal impairment, hyperkalaemia, angioneurotic oedema
75
side effects digoxin
nausea, vomiting, yellow vision, bradycardia or heart block, ventricular arrythmia
76
atherosclerosis is associated with high/low LDL and high/low HDL
low | high
77
lipoproteins have a hydrophobic core containing what?
esterified choleserol and TAGs
78
apoA-1, apoA-II is found in ____
HDL
79
apoB-100 is found in ____
LDL and VLDL
80
apoB-48 is found in ____
chylomicrons
81
where are chylomicrons formed?
intestinal cells
82
What protein allows cholesterol into the cell?
niemann pick C1 like protein (NPC1L1)
83
how are chylomicrons transported into central circulation
via thoracic duct
84
chylomicrons and VLDL must undergo activation by
apoC-II
85
what protein breaks down TAGs into fatty acids and glycerol to enter the cell
lipoprotein lipase
86
what are chylomicrons and VLDL termed after depositing TAGs into cell
remnants
87
clearance of LDL is dependent on?
LDL receptor
88
cholesterol is a rate limiting step in cholesterol synthesis. how does it do this?
inhibits HMG-CoA reductase
89
why is LDL bad
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
Why is HDL good
accepts cholesterol from plasma membrane of cells and returns to liver for elimination
91
how does ezitimibe work
inhibits NPC1L1 to reduce cholesterol absorption as add on drug
92
how do fibrates reduce TGA levels
enhance transcription of certain genes such as that of LPL
93
where are fibrates contraindicated
in use with statins or alcoholics as can cause rhabdomyolysis
94
when are statins ineffective
homozygous FH as no LDLR to target to increase
95
when should lipid levels be measured?
MI, CVA, acute pancreatitis or any vascular disease, FHx or clinical signs
96
What level should total cholesterol be below
5mmol/L
97
how does hypertriglyceridaemia cause acute pancreatitis
chylomicrons obstruct capillaries to cause ischaemia and acidosis. this causes cytotoxic injury and inflammation
98
describe smooth muscle contraction in blood vessels
influx of calcium causes CICR from SR which activates MLCK and contracts smooth muscle
99
describe smooth muscle relaxation in blood vessels
calcium is pumped back into SR, inhibits calcium influx and promotes efflux. MLC phosphatase depohophorylates MLCK and promotes relaxation
100
how does nitric oxide cause muscle relaxation
stimulates guanyate cyclase to promote muscle relaxation
101
how do organic nitrates used as medicines cause muscle relaxation and vasodialtion
directly stimulate guanylate cyclase to promote muscle relaxation
102
how do nitrates relieve symptoms of angina
venodilation reduces preload and vasodilation reduces afterload so less work required for the heart = less ischaemia
103
Adverse effects of nitrates
headache hypotension and fainting reflex tachycardia methaemoglobin formation
104
true/false- patients can have a tolerance to nitrates
true - nitrate free times should be kept to
105
what do calcium antagonists block
opening of L-type calcium channels
106
what do L-type Ca channels mediate and therefore how do CCB act
upstroke of AP in SAN and AVN - reduce rate and conduction | Phase 2 of ventricular AP - reduce force of contraction
107
what CCB preferred for hypertension
amlodipine, targets vascular smooth muscle
108
what CCB preferred for angina
verapamil and diltiazem as reduce contractile force and conduction. amlodipine can be used to reduce afterload
109
what CCB used for arrythmia and why
verapamil and suppresses AVN conduction
110
Adverse effects amlodipine
hypotension, ankle oedema, dizziness, flushing
111
contraindication of verapamil
do not use in heart failure or in conjunction with beta blockers
112
how does lisonopril reduce hypertension
reduced aldosterone release so greater water loss | arterial and venous dilation due to reduced AT1 stimulation
113
adverse effects of ACEI
hypotension dry cough hyperkalaemia angioedema
114
how does losartan work
blocks angiotensin II from binding to AT1 receptors competitively
115
where are ACEI and ARB contraindicated
pregnancy and bilateral renal stenosis
116
how are beta blockers effective in angina
reduce HR and SV so decrease workload on the heart
117
true/false - beta blockers only work in patients with hypertension for a limited time
true - CO is reduced but returns over time
118
how do potassium channel openers work
open potassium channels to cause closure of calcium channels to relax smooth muscle
119
minoxidil has what side effects
reflex tachycardia and salt and water retention
120
name 2 alpha blockers and a side effect
doxazosin and prazosin | postural hypotension

MB1: Cardio (17 decks)

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