Pharmacology Flashcards

1
Q

what is the first-line treatment in younger patients with hypertension?

A

Angiotensin-converting enzyme (ACE) inhibitors.

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2
Q

What are ACE inhibitors used to treat apart from hypertension?

A

heart failure
diabetic nephropathy
secondary prevention of ischaemic heart disease

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3
Q

what types of patients are ACE inhibitors less effective on?

A

hypertensive afro-caribbean patients

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4
Q

how do ACE inhibiters work?

A

inhibit the conversion of angiotensin I to angiotensin II

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5
Q

what are the side effects of ACE inhibitors?

A

cough - occurs in around 15% of patients and may occur up to a year after starting treatment.
angioedema - may occur up to a year after starting treatment.
hyperkalaemia
first-dose hypotension - more common in patients taking diuretics

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6
Q

what are the cautions and contraindictions of ACE inhibitors?

A
  • avoid during pregnancy and breastfeeding
  • renovascular disease - significant renal impairment may occur in patients who have undiagnosed bilateral renal artery stenosis
  • aortic stenosis - may result in hypotension
  • patients receiving high-dose diuretic therapy - significantly increases the risk of hypotension
  • hereditary of idiopathic angioedema.
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7
Q

what should be checked before ACE Inhibitor treatment is initiated and after increasing the dose?

A

Urea and electrolytes

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8
Q

what would be expected to rise after starting ACE inhibitors? what are acceptable changes in those?

A

creatinine and potassium

increase in serum creatine - up to 30% from baseline
increase in potassium up to 5.5 mmol/l

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9
Q

what are the effects of adenosine enhanced by?

A

dipyridamole (anti-platelet agent)

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10
Q

what are the effects of adenosine blocked by?

A

theophyllines

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11
Q

what type of patients should adenosine be avoided in? and why?

A

asthmatics due to possible bronchospasm.

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12
Q

what does adenosine cause?

A

transient heart block in the AV node.

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13
Q

what does adenosine do?

A

agonist of the A1 receptor which inhibits adenylyl clyclase thus reducing cAMP and causing hyperpolarization by increasing outward potassium flux.

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14
Q

what is the half life of adenosine?

A

8-10 seconds

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15
Q

what are the side effects of adenosine?

A

chest pain
bronchospasm
can enhance conduction down accessory pathways, resulting in increased ventricular rate (e.g. WPW syndrome)

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16
Q

what are the three types of anti-cholesterol drugs?

A
  • statins
  • fibrates
  • PCSK 9 inhibitors
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17
Q

what is an example of a statin drug?

A

simvastatin, atrovastatin

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18
Q

what do statin drugs do?

A

block HMG coA reductase, anti-cholesterol drug

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19
Q

what conditions are statins used in?

A
  • hypercholesterolaemia
  • diabetes
  • angina/MI
  • CVA/TIA
  • high risk of MI and CVA
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20
Q

what are side effects of satins?

A

myopathy

rhabdomyolysis… renal failure

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21
Q

what is an example of fibrates?

A

bezafibrate

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22
Q

what are fibrates used in?

A

hypertriglyceridaemia
low HDL cholesterol
hyperlipidaemia

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23
Q

what are examples of PCSK 9 inhibitors?

A

evolocumab, alirocumab

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24
Q

what are PCSK 9 inhibitors used for?

A

familial hypercholesterolaemia

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25
Q

how do PCSK 9 inhibitors work?

A

by inhibiting the binding of PCSK9 to LDLR, PCSR9 inhibitor increases the number of LDLRs available to clear LDL, thereby lowering LDL-C levels.

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26
Q

what do diuretics do?

A

block Na reabsorption in kidneys

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27
Q

what type of diuretic is used in hypertension? what is an example of it?

A

thiazide diuretics

bendrofluazide

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28
Q

what are loop diuretics used to treat? what is an example of one?

A

used in heart failure or resistant hypertension

furosemide

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29
Q

what are diuretic side effects?

A
hypokalaemia - tired 
arrhythmias 
hyperglycaemia - diabetes
increase in uric acid - gout 
impotence
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30
Q

what do beta blockers do?

A

block beta1 and/or beta2 adrenoceptors

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31
Q

what do cardioselective beta blockers do?

A

only block beta1 receptors

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32
Q

what are examples of cardioselective blockers?

A

atenolol, bisoprolol

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33
Q

what are cardioselective blockers used in?

A
angina 
acute coronary syndrome 
myocardial infarction
hypertension 
heart failure
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34
Q

what do non-selective beta blockers do?

A

block beta1 and beta2 receptors

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35
Q

what are examples of non-selective beta blockers?

A

propranolol, carvedilol (alpha and beta blocker)

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36
Q

what are non-selective beta blockers used in?

A

thyrotoxicosis

migraine

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37
Q

what are side effects of beta blockers?

A
  • asthma - contraindicated in brittle/severe asthma
  • tired
  • heart failure (can worsen in short term especially cardiogenic shock)
  • cold peripheries
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38
Q

what are the two types of calcium antagonists?

A

dihydropyridines

rate limiting calcium antagonists

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39
Q

what is an example of dihydropyridines?

A

amlodipine

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40
Q

what are dihydropyridines used in?

A

hypertension and angina

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41
Q

what are side effects of dihydropyridines?

A

ankle oedema

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42
Q

what are examples of rate limiting calcium antagonists?

A

verapamil, diltiazem

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43
Q

what are rate limiting calcium antagonists used in?

A

hypertension
angina
supraventricular arrhythmias (AF, SVT)

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44
Q

what should you avoid using rate limiting calcium antagonists with?

A

beta blockers.

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45
Q

what do angiotensin converting enzyme inhibitors do?

A

block angiotensin I becoming angiotensin II

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46
Q

what is an example of angiotensin converting enzyme inhibitor?

A

lisinopril

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47
Q

what are angiotensin converting enzyme inhibitor used in? what is it good for? what is it bad for?

A
  • hypertension and heart failure
  • good for kidneys in diabetic nephropathy
  • bad for kidneys in renal artery stenosis
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48
Q

what are angiotensin converting enzyme inhibitors side effects?

A

cough
renal dysfunction
angioneurotic oedema

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49
Q

when should you never use angiotensin enzyme inhibitors?

A

in pregnancy induced hypertension

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50
Q

what do angiotensin receptor blockers do?

A

block angiotensin II receptors

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51
Q

what is an example of a angiotensin receptor blocker?

A

Losartan

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52
Q

what are angiotensin receptor blockers used in? what are they good for? what are they bad for?

A
  • hypertension and heart failure
  • good for kidneys in diabetic nephropathy
  • bad for kidneys in renal stenosis
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53
Q

what are side effects of angiotensin receptor blockers?

A

renal dysfunction

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54
Q

when should angiotensin receptor blockers never be used?

A

pregnancy induced hypertension.

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55
Q

what do alpha blockers do?

A

block alpha adrenoceptors to cause vasodilatation

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56
Q

what are alpha blockers used in?

A

hypertension and prostatic hypertrophy

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57
Q

what is an example of an alpha blocker?

A

doxazosin

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58
Q

what are side effects of alpha blockers?

A

postural hypotension

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59
Q

what do mineralocorticoid antagonists do?

A

block aldosterone receptors

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60
Q

what are mineralocorticoid antagonists used in?

A

heart failure and resistant hypertension

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61
Q

what are examples of mineralocorticoid antagonists?

A

spironolactone, eplerenone

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62
Q

what are side effects of mineralocorticoid antagonists?

A

gynaecomastia
hyperkalaemia
renal impairment

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63
Q

what do nitrates do?

A

venodilators

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64
Q

what is an example of a nitrate?

A

isosorbide monoritrate

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65
Q

what are nitrates used in?

A

angina

acute heart failure

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66
Q

what are side effects of nitrates?

A

headache

hypotension/collapse

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67
Q

what is recommended with nitrates to avoid tolerance?

A

leave 8 hr/day nitrate-free

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68
Q

what does nicorandil do?

A

K ATP channel activator

vasodilator

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69
Q

what kind of drug is nicroandil?

A

anti-anginal

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70
Q

what are side effects of nicroandil?

A

headache

mouth/GI ulcers

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71
Q

what does ivabradine do?

A

Lf channel modulator in sinus node

slows HR in sinus rhythm

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72
Q

when does ivabradine not work?

A

atrial fibrillation

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73
Q

what does ranolazine do?

A

late sodium channel modulator
decrease calcium load on heart
is is a metabolic modulator

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74
Q

when is ranolazine effective?

A

in refractory angina

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75
Q

what are examples of antiplatelet drugs?

A

aspirin
clopidogrel
prasugrel
ticagrelor

76
Q

what are examples of anticoafulant drugs?

A
  • heparin
  • fondaparinux (subcuntaneously)
  • warfarin
  • riveroxaban
  • dabigatran
  • edoxaban
77
Q

what are examples of fibrinolytic?

A

streptokinase

tPA (tissue plasminogen activator)

78
Q

what do antiplatelet agents do?

A

prevent new thrombosis

79
Q

what are antiplatelet agents used in?

A

angina
acute MI
CVA/TIA
patients at high risk of MI and CVA

80
Q

what are side effects of antiplatelet agents?

A

haemorrhage anywhere
peptic ulcer -> haemorrhage
aspirin sensitivity -> asthma

81
Q

what do anticoagulants do?

A

prevent new thrombosis

82
Q

how can heparin only be given? how can warfarin only be given?

A

IV

oral

83
Q

what are anticoagulants used in?

A

deep vein thrombosis
pulmonary embolism
NSTEMI
Atrial fibrillation

84
Q

what are side effects of anticoagulants?

A

haemorrhage anywhere

85
Q

what are anticoagulants reversed by?

A

vitamin K

86
Q

what do fibrinolytic drugs do?

A

dissolve formed clots

87
Q

what are fibrinolytic drugs used in?

A
STEMI
pulmonary embolism (selected cases only)
CVA (selected cases only)
88
Q

what is the side effect of fibrinolytic drugs?

A

serious risk of haemorrhage

89
Q

when should fibrinolytic drugs be avoided?

A
recent haemorrhage (some CVAs)
trauma 
bleeding tendencies
severe diabetic retinopathy
peptic ulcer
90
Q

what does digoxin do?

A

1) blocks atrial-ventricular (AV) conduction

2) increases ventricular irritability which produces ventricular arrhythmias

91
Q

when is digoxin good?

A

in atrial fibrillation

92
Q

what happens if too much digoxin is given?

A

bradycardia and heart block

93
Q

what does digoxin toxicity cause?

A
nausea
vomiting 
yellow vision 
bradycardia, heart block
ventricular arrhythmias
94
Q

what are side effects of neprilysin inhibitor side effects?

A

hypotension
renal impairment
hyperkalaemia
angioneurotic oedema

95
Q

what is hydralazine?

A

an ‘older’ antihypertensive not commonly used anymore

96
Q

when is hydralazine still used sometimes?

A

hypertension in pregnancy and severe hypertension

97
Q

how does hydralazine work?

A

increases cGMP leading to smooth muscle relaxation

98
Q

what are the contradictions of hydralazine?

A

systemic lupus erythematous

ischaemic heart disease

99
Q

what are the adverse effects of hydralazine?

A
tachycardia
palpitations
flushing
fluid retention 
headache 
drug-induced lupus
100
Q

what compounds the antihypertensive effect of ACE inhibitors?

A

alcohol

101
Q

what do vagal manoeuvres do?

A

increase parasympathetic output

102
Q

when can vagal manoeuvres be used?

A

atrial tachycardia, atrial flutter or atrial fibrillation

103
Q

what are examples of vagal manoeuvres?

A

valsalva manoeuvre - activates aortic baroreceptors

massage of the bifucation of the carotid artery - stimulates baroreceptors in the carotid sinus

104
Q

when is adenosine most commonly used?

A

to terminate supraventricular tachycardias

105
Q

what is aminodarone used in?

A

atrial, nodal and ventricular tachycardia

106
Q

what class of drug is aminodarone?

A

class III antiarrhythmic agent

107
Q

what is the mechanism of action of aminodarone?

A

blocks potassium channels which inhibits repolarisation and hence prelongs action potential. also blocks sodium channels

108
Q

why is the use of aminodarone limited?

A
  • very long half life (20-100 days)
  • should be given into central veins which causes thrombophlebitis
  • has proarrthymic effects due to lengthening of the QT interval
  • interacts with drugs used concurrently
  • numerous long term adverse effects
109
Q

what investigations should be done to patients prior to taking aminodarone?

A

thyroid function test
liver function test
urea and electrolyte
chest x-ray

110
Q

what investigations should be done to patients after taking aminodarone?

A

thyroid function test and liver function test every 6 months

111
Q

what are the adverse effects of aminodarone?

A
  • thyroid dysfunction
  • corneal deposits
  • pulmonary fibrosis/hepatitis
  • peripheral neuropathy/myopathy
  • photosensitivity
  • ‘slate grey’ appearance
  • thrombophlebitis and injection site reactions
  • bradycardia
  • lengths QT interval
112
Q

when are angiotensin II receptor blockers used?

A

situations where patients have not tolerated an ACE inhibitor, usually due to a development of a cough

113
Q

what are examples of angiotensin II receptor blockers?

A

candesartan
losartan
irbesartan

114
Q

what are the adverse effects of angiotensin II receptor blockers?

A

hypotension and hyperkalaemia

115
Q

what is the mechanism of action of angiotensin II receptor blocker?

A

block effects of angiotensin II at the AT1 receptor

116
Q

what is the mechanism of action of atropine?

A

antagonist of the muscarinic acetycholine receptor

117
Q

what are the uses of atropine? what does it do?

A

treatment of organophasophate poisoning

speeds up heart rate

118
Q

what are the physiological effects of atropine?

A

tachycardia

mydriasis

119
Q

what are beta blockers used for?

A
angina 
post MI
heart failure
arrhythmias
hypertension 
thyrotoxicosis
migraine prophylaxis 
anxiety
120
Q

what are side effects of beta blockers?

A
bronchospasm
cold peripheries
fatigue 
sleep disturbances including nightmares
erectile dysfunction
121
Q

when should beta blockers not be used?

A

uncontrolled heart failure
asthma
sick sinus syndrome
concurrent verapamil

122
Q

what is bivalirudin?

A

a reversible direct thrombin inhibitor used as an anticoagulant in the management of acute coronary syndrome.

123
Q

what artery is mostly used for CABG?

A

internal mammary artery

124
Q

what does CABG stand for?

A

coronary artery bypass graft

125
Q

how is suitability for CABG determined?

A

by angiography or cardiac catheterisation

126
Q

what are the complications of CABG?

A

AF (30-40%)

stroke (2%)

127
Q

what is the prognosis of CABG?

A

90% operations successful but further revascularisation needed in 5-10% after 5 years , mortality = 1-2% at 30 days

128
Q

what type of drug is clopidogrel?

A

antiplatelet

129
Q

when is clopidogrel a first-line drug?

A

in patients following an ischaemic stroke and in patients with peripheral arterial disease

130
Q

what class of drugs does clopidogrel belong to? what are other examples?

A

thienopyridines

prasugrel
ticagrelor
ticlopidine

131
Q

what is the mechanism of action of clopidogrel?

A

antagonist of the P2Y12 adenosine diphosphate (ADP) receptor, inhibiting the activation of platelets

132
Q

what drug may make clopidogrel less effective?

A

proton pump inhibitor (PPIs)

133
Q

what is dabigatran?

A

an oral anticoagulant that works by being a direct thrombin inhibitor

134
Q

what is dabigatran used for?

A
  • prophylaxis of venous thromboembolism following hip or knee replacement surgery
  • prevention of stroke in patients with non-valvular atrial fibrillation who have one or more risk factors.
135
Q

what are the side effects of dabigatran?

A

haemorrhage

136
Q

what kind of drug is dipyridamole?

A

antiplatelet

137
Q

when is dipyridamole used?

A

in combination with aspirin after an ischaemic stroke or transient ischaemic attack

138
Q

what is the mechanism of action of dipyridamole?

A

inhibits phosphodiesterase, elavating cAMP levels which in turn reduce intracellular calcium levels
reduces uptake of adenosine and inhibition of thromboxane synthase

139
Q

what type of drug is hydralazine?

A

antihypertensive

140
Q

when is hydralazine it still used?

A

not often but sometimes for hypertension in pregnancy or severe hypertension

141
Q

how does hydralazine work?

A

increases cGMP leading to smooth muscle relaxation

142
Q

when should hydralazine not be used?

A

systemic lupus erythematous

ischaemic heart disease

143
Q

what are the adverse effects of hydralazine?

A
tachycardia
palpitations
flushing
fluid retention
headache
drug-induced lupus
144
Q

what are examples of loop diuretics?

A

furosemide and bumetanide

145
Q

how do loop diuretics work?

A

inhibit the Na-K-Cl cotransporter (NKCC) in the thick ascending limb of the loop of henle, reducing the absorption of NaCl

146
Q

what are loop diuretics used for?

A

heart failure: acute (IV) and chronic (oral)

resistant hypertension, particularly patients with renal impairment

147
Q

what are adverse effects of loop diuretics?

A
hypotension
hyponatreamia
hypokalaemia
hypomagnesaemia
hypochloraemic alkalosis
ototoxicity
hypocalcaemia
renal impairement 
hyperglycaemia
gout
148
Q

what is minoxidil?

A

originally an antihypertensive. now used for treatment of androgenic alopecia

149
Q

what is the mechanism of action of minoxidil?

A

potassium channel opener, causing hyperpolarisation of the cell membranes

150
Q

what are the adverse effects of minoxidil?

A

hypertrichosis
tachycardia
fluid retention

151
Q

what is nicotinic acid used in?

A

treatment of hyperlipidaemia

152
Q

what does nicotinic acid do?

A

lower cholesterol and triglyceride concentrations and raises HDL levels

153
Q

what are the adverse effects of nicotinic acid?

A

flushing
impaired glucose tolerance
myositis

154
Q

what effects do nitrates have?

A

vasodilating

155
Q

what are nitrates used for?

A

angina

acute treatment of heart failure

156
Q

how do nitrates work?

A
  • cause release of nitric oxide in smooth muscle, increasing cGMP which leads to a fall in intracellular calcium levels
  • in angina they dilate the coronary arteries and reduce venous return which in turn reduces ventricular work, reducing myocardial oxygen demand
157
Q

what are the side effects of nitrates?

A

hypotension
tachycardia
headache
flushing

158
Q

how do statins work?

A

inhibit the action of HMF-CoA reductase, the rate limiting enzyme in hepatic cholesterol synthesis

159
Q

what are adverse effects of statins?

A

myopathy
liver impairment
increased risk of intracerebral haemorrhage in patients who have had a previous stroke

160
Q

how do thiazide diuretics work?

A

by inhibiting sodium reabsorption at the beginning of the distal convoluted tubule (DCT) by blocking thiazide-sensitive Na+-Cl- symporter.

161
Q

what are thiazide diuretics used to treat?

A

mild heart failure

162
Q

what are common adverse effects of thiazide diuretics?

A
dehydration
postural hypotension 
hypoantraemia, hypokalaemia, hypercalcaemia
gout
impaired glucose tolerance
impotence
163
Q

what are rare adverse effects of thiazide diuretics?

A

thrombocytopaenia
agranulocytosis
photosensitivity rash
pancreatitis

164
Q

what type of drug is warfarin?

A

anticoagulant

165
Q

how does warfarin work?

A

inhibits reduction of vitamin K to its active hydroquinone form, which in turn acts as a cofactor in the carboxylation of clotting factors II,VII, IX and X and protein C

166
Q

what is warfarin used in?

A

venous thromboembolism
atrial fibrillation
mechanical heart valves

167
Q

what factors may potentiate warfarin?

A

liver disease
p450 enzyme inhibitors
cranberry juice
drugs which displace warfarin from plasma albumin
drugs which inhibit platelet function (NSAIDs)

168
Q

what are the side effects of warfarin?

A
haemorrhage 
teratogenic
skin necrosis
thrombosis
purple toes
169
Q

what are the two types of heparin?

A

standard and low molecular weight heparin

170
Q

how does heparin work?

A

by activating antithrombin III

171
Q

how does standard heparin work?

A

forms a complex which inhibits thrombin, factors Xa, IXa, XIa and XIIa.

172
Q

how does LMWH work?

A

increases action of antithrombin III on factor Xa

173
Q

what are the adverse effects of heparin?

A

bleeding
thrombocytopenia
osteoporosis and increased risk of fractures
hyperkalaemia

174
Q

what is spironolactone?

A

an aldosterone antagonist which acts in the cortical collecting duct

175
Q

what is spironolactone used to treat?

A
ascites
hypertension
nephrotic syndrome
heart failure
conn's syndrome
176
Q

what are the the adverse effects of spironolactone?

A

hyperkalaemia

gynaecomastia

177
Q

what are examples of calcium channel blockers?

A

verapamil
diltiazem
nifedipine, amlodipine, felodipine

178
Q

what is verapamil used in?

A

angina
hypertension
arrhythmias

179
Q

what are side effects of verapamil?

A

heart failure, constipation, hypotension, bradycardia, flushing

180
Q

when should verapamil not be given?

A

with beta blockers as it could cause heart block

181
Q

what is diltiazem used for?

A

angina, hypertension

182
Q

what are the side effects of diltiazem?

A

hypotension
bradycardia
heart failure
ankle swelling

183
Q

what is nifedipine, amlodipine, felodipine used in?

A

hypertension, angina and raynaud’s

184
Q

what are the side effects of nifedipine, amlodipine, felodipine?

A

flushing
headache
ankle swelling

185
Q

what are the side effects of atropine?

A
  • tachycardia
  • mydriasis
  • dry mouth
  • hypohidrosis
  • constipation
  • urinary retention