Pharmacology Flashcards

1
Q

Selective HCN chanel blocker

Used in ____

A

Ivabradine

Angina - decreases HR and increases cardiac efficiency

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2
Q

β agonists eg.s

A

catecholamines - doputamine (β selective)
adrenaline
noradrenaline

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3
Q

In cardiac arrest adrenaline is given ____

Its effects are ___ (and give receptors)

A

IV

+ve chrono and iono (β1) peripheral vasoconstriction (α1) dilate coronary arteries (β2)

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4
Q

Dobutamine is given in ____ by ___ route

A

acute HF eg. post-op/shock

IV

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5
Q

β antagonists eg.s

A

propranolol (non-selective)

atenolol, bisoprolol, metoprolol (β1 selective)

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6
Q

Effect of β-blockers on HR, force, O2 requirement and exercise tolerance

A

decrease HR, force (therefore CO), O2 requirement (although non-selective cause coronary vessels to constrict) and exercise tolerance

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7
Q

Uses of β-blockers

A

AF and SVTs - delay at AVN
Angina - increase diastole = LV perfused
Post-MI
Compensated HF - low dose eg. carvedilol (also α1 antagonist)

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8
Q

adverse effects of β-blockers

A

bronchospasm
aggravate HF - if rely on sympathetic drive for CO
bradycardia/heart block
hypoglycaemia - glucose release in liver is β2 controlled
fatigue
cold extremities

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9
Q

non-selective competitive muscarinic ACh receptor antagonist eg. and effect

A

atropine
for bradycardia
increases HR

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10
Q

Drug that blocks NaKATPase on sarcolemma to increase influx of sodium and calcium => increased CICR and contractility

A

Digoxin

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11
Q

Use for HF with AF

A

digoxin

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12
Q

Indirectly increases vagal activity and slows SAN and AVN

A

digoxin

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13
Q

Digoxin toxicity may occur if ____

Unwanted effects=

A
hypokalaemic (competes w. K for space on NaKATPase)
self-repeating tachycardia
heart block
GI
yellow vision
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14
Q

Calcium sensitiser eg.
Mode of action
indication for use

A

levosimendan
sensitises troponin C for Ca2+ and vasodilation
IV for acute decompensated HF

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15
Q

Inodilator eg.s
Mode of action
Indication for use

A

milrinone amrinone
inhibit PDE => increase cAMP in cardiac and SM cells => increase contractility and decrease TPR
IV in acute HF

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16
Q

AT1 receptor blockers (ARBs) eg.

A

losartan, valsartan

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17
Q

ARB and ACEI indications for use

A

hbp, HF, post-MI, reduce oedema in HF

NOT IN PREGNANCY

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18
Q

Organic Nitrates benefits for angina __

A

decrease preload - mainly venodilators
decrease afterload (at high dose also = arteriodilators)
dilate coronary collaterals to supply ischaemic area

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19
Q

Organic Nitrates eg.s

Indications

A

isosorbide mononitrate - PO morning and lunch to stop tolerance
GTN spray / IV if ACS
stable angina, ACS and prinzmetal angina

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20
Q

antagonists of ETa receptor (for endothelin) eg.s

indicated for

A

bosentan, ambrisentan

pulmonary hypertension

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21
Q

renin inhibitors eg.

A

alsikiren

NOT WITH ACEI or ARB

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22
Q

ACEI eg.s
effects
side effects

A

lisinopril, ramipril
less vasoconstriction due to AT2 decrease
more vasodilation due to bradykinin increase
less blood vol due to aldosterone decrease
dry cough

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23
Q

CCB 3 eg.s

A

verapamil (mostly cardiac CaL channel selective)
amlodipine (mostly SM CaL channel selective)
diltiazem (intermediate selectivity)

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24
Q

effect and method of action of CCBs

A

block CaL channels => decreased rate and conduction through AVN and force of contraction

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25
Q

CCB preferred for hbp

A

amlodipine (less effects on heart)

causes arteriole and artery + coronary artery vasodilation

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26
Q

Side effects of CCBs

A

ankle swelling, hypotension, dizzy, flushing
DONT give verapamil with β-blockers.
DONT GIVE IN HF

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27
Q

K+ channel openers eg.s

mechanism of action

A

nicorandil - angina (also has NO activity)
minoxidil - last resort for severe hbp
open Katp channels in vascular SM by antagonising ATP that closes them => hyperpolarised + CaL inhibition => relaxation

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28
Q

α1 antagonists eg.
cause
indications for use

A

prazosin + doxazosin
vasodilation and decreased sympathetic transmission
for benign prostatic hyperplasia and if they also have hbp

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29
Q

Thiazide diuretic eg.
Inhibit ____ in ___
Indications

A

bendroflumethiazide
inhibit NaCl reabs by blocking NaCl co-transporter in distal tubule
mild HF, hbp, severe resistant oedema (along w. loop)

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30
Q

Loop diuretic eg.
Inhibit ___ in ___
indications

A

furosemide
NaCl reabs by NaKCl co-transporter blockage in thick ascending loop of Henle
acute pulmonary oedema (IV) chronic HF

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31
Q

Type I antiarrhythmics target-

A

Phase 0 - Na+ channels

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32
Q

Type I antiarr. classes

A

a-moderate ass/dis rate = longer refractory period disopyramide
b - rapid ass/dis = prevent prem beats lignocaine
c - slow dis/ass = depress conduction flecainide

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33
Q

Type 2 antiarrhythics

A

β-blockers - act on depol in SAN and AVN eg. metoprolol

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34
Q

Type 3 antiarrhythmics

A

K+ channel blockers -prolong AP and increase refractory period eg. amiodarone, sotalol

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35
Q

Type 4 antiarrhythmics

A

CCBs - slow SAN and AVN conduction and decrease force

eg. verapamil

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36
Q

Drugs that work on atria (rate control of SVT) =

A

Ic and III eg. flecainide and amiodarone

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37
Q

rate control antiarrhythmics =

A

β blockers and CCBs

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38
Q

rhythm control antiarrhythmics =

A

K+ and Na+ blockers

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39
Q

Drugs that work on AVN (rhythm control of SVT) =

A

adenosine, digoxin, II and IV ie. β-blockers and verapamil

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40
Q

Drugs that work on atria (rate control of SVT) =

A

Ic and III = flecainide, sotalol/amiodarone

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41
Q

Antiarrhythmics that work on the ventricles =

A

Ia+b + II

disopyramide, lignocaine, β-blockers

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42
Q

antiarrhythmics that work on atria and ventricles + AV accessory pathways

A

amiodarone, sotalol (III) and disopyramide (Ia) and flecainide (Ic)

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43
Q

Adenosine (IV) acts on ____ receptors in the ___

Used in ____

A
A-1 adenosine receptors in the AVN
paroxysmal SVTs (atria=140-250bpm) caused by re-entry involving the SA/AVN/atrial tissue
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44
Q

Drug for termination of paroxysmal SVTs (atria=140-250bpm)

A

Adenosine IV

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45
Q

A-1 adenosine receptors are coupled to ___ > activates ____ > _____ AVN

A

Gi/o
GIRK
hyperpolarises AVN and so suppresses impulse transduction

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46
Q

Adenosine is used in acute/chronic SVT

A

acute - is quickly removed

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47
Q

Drug that stimulates vagal activity = slows conduction and increases refractory period in AVN and bundle of His
+ve ionotropic effect

A

digoxin (IV/PO)

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48
Q

Inhibits the NaKATPase

Treats acute/chronic AF

A

digoxin

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49
Q

Used for prophylaxis of AF and atrial flutter =

A

verapamil (PO)

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50
Q

adenosine/verapamil is better for acute AF/ atrial flutter

A

adenosine

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51
Q

don’t prescribe verapamil with ___

A

β-blockers (other -ve ionotropic drugs)

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52
Q

Used in ventricular arrythmias post-MI

A

Ib - lignocaine IV

Ia - procainamide IV

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53
Q

Used to prevent recurrent Ventricular arrhythmias

A

Ia - disopyramide PO

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54
Q

Prophylaxis for AF (a Na blocker)

A

Ic - Flecainide

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55
Q

Depress conduction in AVN (control SVT)

Suppress excessive symp drive (prevent VT)

A

propranolol and atenolol β-blockers

56
Q

Drug with Ia, II and IV properties used for SVT and VT

A

amiodarone

57
Q

Antiarrhythmic used when others have failed and reduces mortality post-MI and in CCF

A

amiodarone

58
Q

pulmonary fibrosis, thyroid disorders, photosensitivity and peripheral neuropathy are side effects of

A

amiodarone

59
Q

Side effects of diuretics =

A

hypokalaemia may => arrhythmias
hyperglycaemia
^uric acid => gout
impotence

60
Q

Thiazides are given in ___
Loops are given in ____
NEITHER IN ____

A

hbp
CCF
GOUT

61
Q

cardioselective β-blockers for ___
non-selective for ____
neither in ___ or ___

A

angina, hbp, CCF
thyrotoxicosis
asthma; short term in HF - fine if start low and increase for medium to long term HF

62
Q

dihyropyridine CCB used in hbp and angina

may cause ankle swelling

A

amlodipine

63
Q

rate limiting CCBs for hbp and angina, AF and SVT

reduce HR and vasodilate

A

verapamil and (diltiazem - not as much for AF and SVT)

64
Q

α-blockers for prostatic hypertrophy and hbp

may cause hypotension

A

doxazosin

65
Q

for hbp and CCF
good in diabetic neuropathy
bad in renal artery stenosis and gestational hbp

A

ACEIs

66
Q

Side effects = dry cough, angioedema, renal dysfunction,

A

ACEI

67
Q

Venodilators for acute HF and angina

side effects = tolerance, headaches, hypotension

A

organic nitrates

68
Q

Prevent new thrombus in angina, acute MI, CVA/TIA and those at risk of MI/CVA/TIA

A

antiplatelts eg. aspirin

69
Q

aspirin sensitivity may induce ___

A

asthma

70
Q

Blocks clotting factors 2, 7, 9 and 10

A

Warfarin PO

71
Q

Given in DVT, PE, NSTEMI and AF

A

warfarin PO

72
Q

Anticoagulant eg.s

A

warfarin PO
heparin IV
rivaroxaban and dabigatran

73
Q

fibrinolytic drugs eg.s

A

alteplase, duteplase, streptokinase, tPA

74
Q

Contra-ind.s for fibrinolytics

A
recent haem
trauma
bleeding tendency (haemophilia)
peptic ulcer
sever diabetic neuropathy
75
Q

Used in hypertriglyceridaemia and low HDL

A

fibrates eg. bezafibrate

76
Q

Statins block ____
Used in ____
side effects (rare)

A

HMG CoA reductase
hypercholesteraemia, diabetes, MI, TIA, angina
myopathy, rhabdomyolysis, renal failure

77
Q

Used to cardiovert SVT and VT if can’t DC cardiovert

A

amiodarone, flecainide, β-blockers

78
Q

Used in acute phase of SVT

A

adenosine

79
Q

Digoxin toxicity =

A

nausea, vomiting, yellow vision, bradycardia, heart block, ventricular arrhythmias

80
Q

gestational hbp sometimes w. fluid retention and proteinurea =

A

pre-eclampsia

81
Q

Inhibition of ___ by ___ increases LDL receptor expression and clearance of LDL

A

HMG CoA-reductase

statins

82
Q

decreases total chol+LDL by up to 60% + tri. 40%
+HDL increases by 10%
reduce inlam
stabilise atheromatous plaques

A

statins

83
Q

Homozygous familial hypercholesterolaemia means you have no ____
and dont respond to ___

A

LDL receptors

statins

84
Q

Statins are given ___ at ___ (route and time)

A

PO night

85
Q

decrease tri.s 50% + LDL 15%

increase HDL 20%

A

fibrates

eg. bezafibrate and gemfibrozil

86
Q

agonise nuclear receptor PPARα + increase transcription of genes including that for LPL

A

fibrates mechanism of action

87
Q

fibrates are not to be used in ____

A

alcoholics

88
Q

Bile binding resins eg.s

A

colestyramine, colestipol, colesevelam PO

89
Q

bile binding resins prevent ___
results in ___
side effects=

A

enterohepatic (in ileum) recycling of bile
decreased abs of tris and increased LDL expression
GI irritation

90
Q

Ezetimibe mechanism of action:
Causes a ____ in LDL and ___ in HDL
Not for ___

A

inhibits NPC1L1 transport protein in duodenal enterocytes decreasing chol. abs.
18% less LDL no change in HDL
NOT in pregnancy

91
Q

2ndry causes of hyperlipidaemia =

A

TIID
hypothyroidism
alcoholism
liver disease

92
Q

If chylomicron levels are elevated then the treatment is ___

A

none - no elevation in atherosclerotic risk

93
Q

If LDL levels are high then the treatment is ___

A

statins w/wo ezetimibe - high atherosclerotic risk

94
Q

If LDL and VLDL are high the treatment is ___

A

fibrates, statin (nicotinic acid) high atherosclerotic risk

95
Q

If βVLDL or VLDL is raised the treatment is ____

A

fibrates - moderate atherosclerotic risk

96
Q

If VLDL and chylomicron levels are raised treatment is ___

A

fibrate, niacin, fish oil and statin - atherosclerotic risk not elevated

97
Q

Pleiotropic effects of statins

A
improve endothelial dysfunction
increase NO bioavailability
anti-oxidant
inhibit inflam response
stabilise atheromatous plaques
98
Q

Warfarin blocks ____

stops the formation of the precursors of Factors ___

A

Vitamin K reductase

2, 7, 9 + 10

99
Q

Anticoagulants are used to prevent ____ thrombi and emboli

eg. in

A

venous

DVT, post-op, artificial heart valves, AF

100
Q

Warfarin is a ____ derivative and has a similar shape to ___

A

coumarin

Vitamin K

101
Q

Warfarin has a ____ onset of action within ____

A

slow

2-3 days

102
Q

If warfarin is taken factors that increase the risk of haemorrhage =

A
liver disease (less clotting factors)
high metabolism (clotting factors cleared)
drugs - NSAIDS, antiplatelets, inhibit liver, inhibit reduction/availability of vit. K
103
Q

Factors that increase the risk of a thrombus

A

pregnancy, hypothyroidism, Vit. K consumption, drugs that increase liver metabolism

104
Q

To reverse warfarin overdose give ___/____

A

vitamin K/plasma clotting factors

105
Q

Heparin binds to ____ an endogenous inhibitor of clotting factors and increases its affinity especially for __+___

A

ATIII (antithrombin3)

Xa and IIa

106
Q

Heparin must bind to both ATIII and ___ to speed up its degradation.
But only needs to bind to ATIII to speed up breakdown of ___

A

both = IIa

only ATIII = Xa

107
Q

Eg.s of LMWHs

Inhibit ___

A

dalteparin, enoxaparin

Xa

108
Q

Heparin is given ___/__ (route)
Need a ____ for optimum dosage
Eliminated by ___ order kinetics
Preferred over LMWHs in ____

A

IV (immediate onset) or S/C (onset after 1hr)
in vitro test
0 order (saturation) kinetics
renal failure

109
Q

LMWH are given __ (route)
No optimum dosage test needed
eliminated by __

A

S/C

1st order kinetics ie. only by the kidneys

110
Q

adverse effects of heparin and LMWHs:

A

haemorrhage

rare = osteoporosis, hypoaldosteronism, hypersensitivity

111
Q

If haemorrhage when on heparin give ____ to inactivate it

A

protamine sulfate

112
Q

Oral direct inhibitor anticoagulants eg.s

used in ___

A

dabigatran (IIa)
rivaroxaban (Xa)
hip and knee replacement prophylaxis

113
Q

INR is monitored in administration of ____

A

warfarin

114
Q

Antiplatelet eg.s

A

Aspirin
Clopidogrel
Tirofiban

115
Q

Aspirin blocks ___
1) in platelets = _____
2) in endothelial cells = ___
Balances toward antithrombotic as ___ can’t synthesis new COX - take 7-10 days to ____

A

COX-1
no TXA2
no antithrombotic PGI
platelets - turnover

116
Q

Drug that blocks P2Y12 receptor on platelets and stops it binding to ADP
Inhibits ___

A

Clopidogrel

Inhibits conversion of fibrinogen to fibrin

117
Q
Drug that blocks fibrinogen from binding to GPIIb/IIIa receptor on platelets
Given \_\_\_ (route) short term to prevent MI in \_\_\_\_\_
A

tirofiban IV

unstable angina

118
Q

Fibrinolytic drugs activate ___ by stimulating ___

A

plasminogen by stimulating tPA to convert it to plasmin

119
Q

Effect of plasmin

A

lyses fibrin to fibrinogen

120
Q

Fibrinolytics are used in ____

A
acute MI (if no PCI in 90mins) or stroke 
rarely: venous thrombosis/PE
121
Q

recombinant tPA eg.s
route =
more effective against ____ bound plasminogen over ___plasminogen

A

alteplase duteplase IV (no allergic reaction unlike streptokinase)
fibrin bound>plasma

122
Q

Sort of antidote to fibrinolytic drugs

A

tranexamic acid

123
Q

GTN can come in __/__/___ forms

A

sublingual pills, spray or patch

124
Q

If take 1 GTN and doesn’t relieve pain then ____

A

Phone an ambulance - don’t take another

125
Q

Gingival hypertrophy, ankle oedema and tachycardia are potential side effects of ___

A

amlodipine

126
Q

Side effects of ivabradine =

A

blurred vision, headaches

127
Q

Late Na+ channel inhibitor in cardiac myocytes
Used to treat chronic angina
side effects = drug interactions

A

ranolazine

128
Q

_____ may mask angina symptoms due to neuropathy

A

diabetes mellitus

129
Q

If have claudication do not give _____ as makes it worse

A

β-blockers

130
Q

K+ sparing diuretic - aldosterone antagonist for HF

A

spironolactone

131
Q

mnemonic for treatment of cardiogenic shock with acute HF

A
LMNOP
Loop diuretic (ferusemide IV)
Morphine
Nitrate
O2
Position - sit up
132
Q

IABP =

A

intra-aortic balloon pump

inflates in diastole so coronary arteries fill up

133
Q

Digoxin is less effective when ____

don’t give with ____ as causes heart block

A

active (sympathetic activity increases)

amiodarone

134
Q

Treatment for chronic HF:

A

oral ferusemide, anti-coag to prevent DVT, stockings, β-blocker, ACEI, spironolactone

135
Q

DONT give thiazide with warfarin because ___

A

become HYPERHAEMORRHAGIC

136
Q

K+ sparing diuretics work on the ___

A

collecting duct in the kidney