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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
how do PCSK 9 inhibitors work?
by inhibiting the binding of PCSK9 to LDLR, PCSR9 inhibitor increases the number of LDLRs available to clear LDL, thereby lowering LDL-C levels.
26
what do diuretics do?
block Na reabsorption in kidneys
27
what type of diuretic is used in hypertension? what is an example of it?
thiazide diuretics | bendrofluazide
28
what are loop diuretics used to treat? what is an example of one?
used in heart failure or resistant hypertension | furosemide
29
what are diuretic side effects?
``` hypokalaemia - tired arrhythmias hyperglycaemia - diabetes increase in uric acid - gout impotence ```
30
what do beta blockers do?
block beta1 and/or beta2 adrenoceptors
31
what do cardioselective beta blockers do?
only block beta1 receptors
32
what are examples of cardioselective blockers?
atenolol, bisoprolol
33
what are cardioselective blockers used in?
``` angina acute coronary syndrome myocardial infarction hypertension heart failure ```
34
what do non-selective beta blockers do?
block beta1 and beta2 receptors
35
what are examples of non-selective beta blockers?
propranolol, carvedilol (alpha and beta blocker)
36
what are non-selective beta blockers used in?
thyrotoxicosis | migraine
37
what are side effects of beta blockers?
- asthma - contraindicated in brittle/severe asthma - tired - heart failure (can worsen in short term especially cardiogenic shock) - cold peripheries
38
what are the two types of calcium antagonists?
dihydropyridines | rate limiting calcium antagonists
39
what is an example of dihydropyridines?
amlodipine
40
what are dihydropyridines used in?
hypertension and angina
41
what are side effects of dihydropyridines?
ankle oedema
42
what are examples of rate limiting calcium antagonists?
verapamil, diltiazem
43
what are rate limiting calcium antagonists used in?
hypertension angina supraventricular arrhythmias (AF, SVT)
44
what should you avoid using rate limiting calcium antagonists with?
beta blockers.
45
what do angiotensin converting enzyme inhibitors do?
block angiotensin I becoming angiotensin II
46
what is an example of angiotensin converting enzyme inhibitor?
lisinopril
47
what are angiotensin converting enzyme inhibitor used in? what is it good for? what is it bad for?
- hypertension and heart failure - good for kidneys in diabetic nephropathy - bad for kidneys in renal artery stenosis
48
what are angiotensin converting enzyme inhibitors side effects?
cough renal dysfunction angioneurotic oedema
49
when should you never use angiotensin enzyme inhibitors?
in pregnancy induced hypertension
50
what do angiotensin receptor blockers do?
block angiotensin II receptors
51
what is an example of a angiotensin receptor blocker?
Losartan
52
what are angiotensin receptor blockers used in? what are they good for? what are they bad for?
- hypertension and heart failure - good for kidneys in diabetic nephropathy - bad for kidneys in renal stenosis
53
what are side effects of angiotensin receptor blockers?
renal dysfunction
54
when should angiotensin receptor blockers never be used?
pregnancy induced hypertension.
55
what do alpha blockers do?
block alpha adrenoceptors to cause vasodilatation
56
what are alpha blockers used in?
hypertension and prostatic hypertrophy
57
what is an example of an alpha blocker?
doxazosin
58
what are side effects of alpha blockers?
postural hypotension
59
what do mineralocorticoid antagonists do?
block aldosterone receptors
60
what are mineralocorticoid antagonists used in?
heart failure and resistant hypertension
61
what are examples of mineralocorticoid antagonists?
spironolactone, eplerenone
62
what are side effects of mineralocorticoid antagonists?
gynaecomastia hyperkalaemia renal impairment
63
what do nitrates do?
venodilators
64
what is an example of a nitrate?
isosorbide monoritrate
65
what are nitrates used in?
angina | acute heart failure
66
what are side effects of nitrates?
headache | hypotension/collapse
67
what is recommended with nitrates to avoid tolerance?
leave 8 hr/day nitrate-free
68
what does nicorandil do?
K ATP channel activator | vasodilator
69
what kind of drug is nicroandil?
anti-anginal
70
what are side effects of nicroandil?
headache | mouth/GI ulcers
71
what does ivabradine do?
Lf channel modulator in sinus node | slows HR in sinus rhythm
72
when does ivabradine not work?
atrial fibrillation
73
what does ranolazine do?
late sodium channel modulator decrease calcium load on heart is is a metabolic modulator
74
when is ranolazine effective?
in refractory angina
75
what are examples of antiplatelet drugs?
aspirin clopidogrel prasugrel ticagrelor
76
what are examples of anticoafulant drugs?
- heparin - fondaparinux (subcuntaneously) - warfarin - riveroxaban - dabigatran - edoxaban
77
what are examples of fibrinolytic?
streptokinase | tPA (tissue plasminogen activator)
78
what do antiplatelet agents do?
prevent new thrombosis
79
what are antiplatelet agents used in?
angina acute MI CVA/TIA patients at high risk of MI and CVA
80
what are side effects of antiplatelet agents?
haemorrhage anywhere peptic ulcer -> haemorrhage aspirin sensitivity -> asthma
81
what do anticoagulants do?
prevent new thrombosis
82
how can heparin only be given? how can warfarin only be given?
IV | oral
83
what are anticoagulants used in?
deep vein thrombosis pulmonary embolism NSTEMI Atrial fibrillation
84
what are side effects of anticoagulants?
haemorrhage anywhere
85
what are anticoagulants reversed by?
vitamin K
86
what do fibrinolytic drugs do?
dissolve formed clots
87
what are fibrinolytic drugs used in?
``` STEMI pulmonary embolism (selected cases only) CVA (selected cases only) ```
88
what is the side effect of fibrinolytic drugs?
serious risk of haemorrhage
89
when should fibrinolytic drugs be avoided?
``` recent haemorrhage (some CVAs) trauma bleeding tendencies severe diabetic retinopathy peptic ulcer ```
90
what does digoxin do?
1) blocks atrial-ventricular (AV) conduction | 2) increases ventricular irritability which produces ventricular arrhythmias
91
when is digoxin good?
in atrial fibrillation
92
what happens if too much digoxin is given?
bradycardia and heart block
93
what does digoxin toxicity cause?
``` nausea vomiting yellow vision bradycardia, heart block ventricular arrhythmias ```
94
what are side effects of neprilysin inhibitor side effects?
hypotension renal impairment hyperkalaemia angioneurotic oedema
95
what is hydralazine?
an 'older' antihypertensive not commonly used anymore
96
when is hydralazine still used sometimes?
hypertension in pregnancy and severe hypertension
97
how does hydralazine work?
increases cGMP leading to smooth muscle relaxation
98
what are the contradictions of hydralazine?
systemic lupus erythematous | ischaemic heart disease
99
what are the adverse effects of hydralazine?
``` tachycardia palpitations flushing fluid retention headache drug-induced lupus ```
100
what compounds the antihypertensive effect of ACE inhibitors?
alcohol
101
what do vagal manoeuvres do?
increase parasympathetic output
102
when can vagal manoeuvres be used?
atrial tachycardia, atrial flutter or atrial fibrillation
103
what are examples of vagal manoeuvres?
valsalva manoeuvre - activates aortic baroreceptors | massage of the bifucation of the carotid artery - stimulates baroreceptors in the carotid sinus
104
when is adenosine most commonly used?
to terminate supraventricular tachycardias
105
what is aminodarone used in?
atrial, nodal and ventricular tachycardia
106
what class of drug is aminodarone?
class III antiarrhythmic agent
107
what is the mechanism of action of aminodarone?
blocks potassium channels which inhibits repolarisation and hence prelongs action potential. also blocks sodium channels
108
why is the use of aminodarone limited?
- 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
what investigations should be done to patients prior to taking aminodarone?
thyroid function test liver function test urea and electrolyte chest x-ray
110
what investigations should be done to patients after taking aminodarone?
thyroid function test and liver function test every 6 months
111
what are the adverse effects of aminodarone?
- thyroid dysfunction - corneal deposits - pulmonary fibrosis/hepatitis - peripheral neuropathy/myopathy - photosensitivity - 'slate grey' appearance - thrombophlebitis and injection site reactions - bradycardia - lengths QT interval
112
when are angiotensin II receptor blockers used?
situations where patients have not tolerated an ACE inhibitor, usually due to a development of a cough
113
what are examples of angiotensin II receptor blockers?
candesartan losartan irbesartan
114
what are the adverse effects of angiotensin II receptor blockers?
hypotension and hyperkalaemia
115
what is the mechanism of action of angiotensin II receptor blocker?
block effects of angiotensin II at the AT1 receptor
116
what is the mechanism of action of atropine?
antagonist of the muscarinic acetycholine receptor
117
what are the uses of atropine? what does it do?
treatment of organophasophate poisoning | speeds up heart rate
118
what are the physiological effects of atropine?
tachycardia | mydriasis
119
what are beta blockers used for?
``` angina post MI heart failure arrhythmias hypertension thyrotoxicosis migraine prophylaxis anxiety ```
120
what are side effects of beta blockers?
``` bronchospasm cold peripheries fatigue sleep disturbances including nightmares erectile dysfunction ```
121
when should beta blockers not be used?
uncontrolled heart failure asthma sick sinus syndrome concurrent verapamil
122
what is bivalirudin?
a reversible direct thrombin inhibitor used as an anticoagulant in the management of acute coronary syndrome.
123
what artery is mostly used for CABG?
internal mammary artery
124
what does CABG stand for?
coronary artery bypass graft
125
how is suitability for CABG determined?
by angiography or cardiac catheterisation
126
what are the complications of CABG?
AF (30-40%) | stroke (2%)
127
what is the prognosis of CABG?
90% operations successful but further revascularisation needed in 5-10% after 5 years , mortality = 1-2% at 30 days
128
what type of drug is clopidogrel?
antiplatelet
129
when is clopidogrel a first-line drug?
in patients following an ischaemic stroke and in patients with peripheral arterial disease
130
what class of drugs does clopidogrel belong to? what are other examples?
thienopyridines prasugrel ticagrelor ticlopidine
131
what is the mechanism of action of clopidogrel?
antagonist of the P2Y12 adenosine diphosphate (ADP) receptor, inhibiting the activation of platelets
132
what drug may make clopidogrel less effective?
proton pump inhibitor (PPIs)
133
what is dabigatran?
an oral anticoagulant that works by being a direct thrombin inhibitor
134
what is dabigatran used for?
- 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
what are the side effects of dabigatran?
haemorrhage
136
what kind of drug is dipyridamole?
antiplatelet
137
when is dipyridamole used?
in combination with aspirin after an ischaemic stroke or transient ischaemic attack
138
what is the mechanism of action of dipyridamole?
inhibits phosphodiesterase, elavating cAMP levels which in turn reduce intracellular calcium levels reduces uptake of adenosine and inhibition of thromboxane synthase
139
what type of drug is hydralazine?
antihypertensive
140
when is hydralazine it still used?
not often but sometimes for hypertension in pregnancy or severe hypertension
141
how does hydralazine work?
increases cGMP leading to smooth muscle relaxation
142
when should hydralazine not be used?
systemic lupus erythematous | ischaemic heart disease
143
what are the adverse effects of hydralazine?
``` tachycardia palpitations flushing fluid retention headache drug-induced lupus ```
144
what are examples of loop diuretics?
furosemide and bumetanide
145
how do loop diuretics work?
inhibit the Na-K-Cl cotransporter (NKCC) in the thick ascending limb of the loop of henle, reducing the absorption of NaCl
146
what are loop diuretics used for?
heart failure: acute (IV) and chronic (oral) | resistant hypertension, particularly patients with renal impairment
147
what are adverse effects of loop diuretics?
``` hypotension hyponatreamia hypokalaemia hypomagnesaemia hypochloraemic alkalosis ototoxicity hypocalcaemia renal impairement hyperglycaemia gout ```
148
what is minoxidil?
originally an antihypertensive. now used for treatment of androgenic alopecia
149
what is the mechanism of action of minoxidil?
potassium channel opener, causing hyperpolarisation of the cell membranes
150
what are the adverse effects of minoxidil?
hypertrichosis tachycardia fluid retention
151
what is nicotinic acid used in?
treatment of hyperlipidaemia
152
what does nicotinic acid do?
lower cholesterol and triglyceride concentrations and raises HDL levels
153
what are the adverse effects of nicotinic acid?
flushing impaired glucose tolerance myositis
154
what effects do nitrates have?
vasodilating
155
what are nitrates used for?
angina | acute treatment of heart failure
156
how do nitrates work?
- 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
what are the side effects of nitrates?
hypotension tachycardia headache flushing
158
how do statins work?
inhibit the action of HMF-CoA reductase, the rate limiting enzyme in hepatic cholesterol synthesis
159
what are adverse effects of statins?
myopathy liver impairment increased risk of intracerebral haemorrhage in patients who have had a previous stroke
160
how do thiazide diuretics work?
by inhibiting sodium reabsorption at the beginning of the distal convoluted tubule (DCT) by blocking thiazide-sensitive Na+-Cl- symporter.
161
what are thiazide diuretics used to treat?
mild heart failure
162
what are common adverse effects of thiazide diuretics?
``` dehydration postural hypotension hypoantraemia, hypokalaemia, hypercalcaemia gout impaired glucose tolerance impotence ```
163
what are rare adverse effects of thiazide diuretics?
thrombocytopaenia agranulocytosis photosensitivity rash pancreatitis
164
what type of drug is warfarin?
anticoagulant
165
how does warfarin work?
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
what is warfarin used in?
venous thromboembolism atrial fibrillation mechanical heart valves
167
what factors may potentiate warfarin?
liver disease p450 enzyme inhibitors cranberry juice drugs which displace warfarin from plasma albumin drugs which inhibit platelet function (NSAIDs)
168
what are the side effects of warfarin?
``` haemorrhage teratogenic skin necrosis thrombosis purple toes ```
169
what are the two types of heparin?
standard and low molecular weight heparin
170
how does heparin work?
by activating antithrombin III
171
how does standard heparin work?
forms a complex which inhibits thrombin, factors Xa, IXa, XIa and XIIa.
172
how does LMWH work?
increases action of antithrombin III on factor Xa
173
what are the adverse effects of heparin?
bleeding thrombocytopenia osteoporosis and increased risk of fractures hyperkalaemia
174
what is spironolactone?
an aldosterone antagonist which acts in the cortical collecting duct
175
what is spironolactone used to treat?
``` ascites hypertension nephrotic syndrome heart failure conn's syndrome ```
176
what are the the adverse effects of spironolactone?
hyperkalaemia | gynaecomastia
177
what are examples of calcium channel blockers?
verapamil diltiazem nifedipine, amlodipine, felodipine
178
what is verapamil used in?
angina hypertension arrhythmias
179
what are side effects of verapamil?
heart failure, constipation, hypotension, bradycardia, flushing
180
when should verapamil not be given?
with beta blockers as it could cause heart block
181
what is diltiazem used for?
angina, hypertension
182
what are the side effects of diltiazem?
hypotension bradycardia heart failure ankle swelling
183
what is nifedipine, amlodipine, felodipine used in?
hypertension, angina and raynaud's
184
what are the side effects of nifedipine, amlodipine, felodipine?
flushing headache ankle swelling
185
what are the side effects of atropine?
- tachycardia - mydriasis - dry mouth - hypohidrosis - constipation - urinary retention

Cardiovascular (16 decks)

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