Pharmacology Flashcards
1
Q
statins - action
A
reduce total and LDL cholesterol, decrease triglycerides and increase HDL
2
Q
statins - mechanism of action
A
inhibits rate limiting step in cholesterol synthesis in hepatocytes - competitive inhibitors of 3-hydroxy-3methylglutaryl enzyme CoA (HMG-CoA) reductase
3
Q
statins are ineffective in…
A
homozygous familial hypercholesterolaemia
4
Q
statines - other benefits
A
decreased inflammation, reversal of epithelial dysfunction, decreased thrombosis, stabilisation of atherosclerotic plaques
5
Q
statins - side effects
A
myositis, rhabdomyolysis
6
Q
fibrates - action
A
decrease in triglycerides, modest decrease in LDL and modest increase in HDL
7
Q
fibrates - prescribing
A
first line in patients with very high triglyceride levels
8
Q
fibrates - side effects
A
myositis, GI symptoms, pruritus, rash
9
Q
fibrates - mechanism of action
A
agonists of a nuclear receptor to enhance the transcription of several genes, including that encoding LPL
10
Q
bezafibrate and gemfibrozil are examples of…
A
fibrates
11
Q
atorvistatin and simvistatin are examples of…
A
statins
12
Q
colestyramine, colestipol and colsevelam are examples of…
A
bile acid binding resins
13
Q
bile acid binding resins - mechanism of action
A
cause excretion of bile salts resulting in more cholesterol to be converted to bile salts by interrupting enterohepatic recycling
14
Q
bile acid binding resins - action
A
cedreased absorption of triglycerides and increased expression of LDL receptor
15
Q
ezetimibe - mechanism of action
A
inhibits NPC1L1 transport protein in neterocytes of the duodenum, reducing the absorption of cholesterol
16
Q
ezetimibe - action
A
causes a decrease in LDL with little change in HDL
17
Q
ezetimibe - use
A
used in combination with statins after poor response to initial treatment
18
Q
ezetimibe - side effects
A
diarrhoea, abdominal pain, headaches
19
Q
ezetimibe - contraindications
A
breast feeding females
20
Q
ivabradine - mechanism of action
A
selective blocker of HCN channel (funny channel)
21
Q
ivabradine - action
A
slows heart rate
22
Q
adrenaline - action
A
increase force, rate, and cardiac output, increase O2 consumption,
23
Q
adrenaline mechanism of action
A
+ve inotropic and chronotropic actions, redistribution of blood flow to the heart (constricts blood vessels in skin, mucosa and abdomen, dilation of the coronary arteries
24
Q
adrenaline uses
A
cardiac arrest, anaphylactic shock
25
dobutamine uses
acute, potentially reversible heart failure
26
beta blocker mechanism of action
block beta-adrenoceptors selectively or non-selectively in a competitive manner
27
selective beta blockers
atenolol, bisoprolol
28
non-selective beta blockers
propranolol
29
beta blocker action
during exercise or stress, significantly reduce rate, force and CO, reduces myocardial O2 requirement
30
beta blocker uses
arrhythmias, angina, heart failure, hypertension
31
beta blocker side effects
bronchospasm, aggravtation of cardiac failure, bradycardia, hypoglycaemia, cold extremities, fatigue
32
atropine mechanism of action
competitive inhibitor of muscarinic acetylcholine receptors
33
atropine action
increase HR, no effect on arterial BP
34
atropine uses
first line in management of severe bradycardia, in anticholinesterase poisoning
35
digoxin mechanism of action
blocks the Na+/Ca2+ exchanger, causing an increase of Ca2+ in the sarcoplasmic recticulum, STIMULATES VAGAL ACTIVITY
36
digoxin action
increase contractility, makes heart srate stronger and more regular
37
digoxin uses
heart failure, particularly in heart failure with AF NOT FIRST LINE, LAST LINE!
38
digoxin side effects
excessive depression of AV node, propensity to cause arrhythmias, nausea, vomiting, diarrhoea, disturbances of colur vision (yellow vision)
39
calcium sensitzers mechanism of action
bind to troponin C in cardiac muscle sensitizing it to the action of Ca2+
40
calcium sensitizers action
cause vasodilation
41
calcium sensitizers uses
acute heart failure
42
levosimendan is a...
calcium sensitizer
43
inodilator mechanism of action
inhibit phosphodiesterase in cardiac and smooth muscle so increase cAMP
44
inodilator action
increase myocardial contractility, decrease peripheral resistance, worsen survival
45
inodilators uses
acute heart failure (IV)
46
amrinone and milrinone are...
inodilators
47
nitrates mechanism of action
converted to NO which reacts with cGMP
48
nitrates action (low dose)
dilates large veins, increases venous pressure, decreases preload, decreases SV, but CO maintained by reflex increase in HR
49
nitrates action (high dose)
arteriolar dilation - decreases arterial pressure, reducing the afterload, large muscular arteries more sensitive
50
nitrates action (in angina)
dilation of collateral vessels allowing increased blood supply to the ischaemic zone
51
nitrates uses
stable angina and acute coronary syndrome
52
GTN and isosorbide mononitrate are...
nitrates
53
nitrate tolerance
repeated administration may be associated with a diminished effect - nitrates free periods at night
54
nitrates side effect
postural hypotension, headaches, formation of methaemoglobin
55
ACEI mechanism of action
block conversion of angiotensin I to angiotensin II
56
ACEI action
causes venous dilation (decreased preload) and arteriolar dilatation (decreased fterload and decreased TPR) decreasing arterial blood pressure and cardiac load
57
lisinpril and ramipril are...
ACEI
58
ACEI side effects
initial hypotension and dry cough
59
ARB mechanism of action
block the action of angiotensin II at AT1 receptors in a competitive manner
60
ARB uses
hypertension, cardiac failure, following MI
61
ACEI uses
hypertension, cardiac failure, following MI
62
calcium channel blockers mechanism of action
prevent the opening of L-type channels in excitable tissues in response to depolarisation and hence limit increase of Ca2+ concentration
63
verapamil selectivity
selective for cardiac L-type channels
64
amplodipine selectivity
relatively selective for smooth muscle L-type channels
65
diltiazem selectivity
intermediate selectivity
66
calcium channel blockers uses
hypertension, angina, dysrhythmias
67
potassium channel openers mechanism
open ATP-modulated K+ channels in vasculaar smooth muscle which cause hyperpolarisation which switches off L-type Ca2+ channels
68
potassium channel openers action
act upon aarterial smooth muscle
69
minoxidil uses
last resort in severe hypertension but causes reflex tachycardia and salt and water retention (need beta-blocker and diuretic)
70
nicorandil uses
angina
71
class IA antiarrhythmic drugs - mechanism of action
Na+ channel blocker, associate and dissociate at a MODERATE rate
72
class IB antiarrhythmic drugs - mechanism of action
Na+ channel blocker, associate and disassociate at a RAPID rate
73
class IC antiarrhythmic drugs - mechanism of action
Na+ channel blocker, associate and disassociate at a SLOW rate
74
class II antiarrhythmic drugs - mechanism of action
B-adrenoceptor blocker
75
class III antiarrhythmic drugs - mechanism of action
K+ channel blocker
76
class IV antiarrhythmic drugs - mechanism of action
Ca2+ channel blocker
77
class IA antiarrhythmic drugs action
slow rate of rise of AP and prolong refractory period
78
class IB antiarrhythmic drugs action
prevents premature beats
79
class IC antiarrhythmic drugs action
depress conduction
80
class II antiarryhtmic drugs action
decrease rate of depolarisation in SA and AV nodes
81
class III antiarrhythmic drugs action
prolong AP duration by increasing refractory period
82
class IV antiarrhythmic drugs action
slow conduction in SA and AV nodes, decrease force of cardiac contraction
83
antiarrhythmic drugs affecting the atria (rate control of SVT)
classes IC, III
84
antiarrhythmic drugs affecting the ventricles
classes IA, IB, II
85
antiarrhythmic drugs affecting AV node (rhythm control of SVT)
adenosine, digoxin, xlasses II, IV
86
antiarrhythmic drugs affecting the atria and ventricles, AV accessory pathways
amiodarone, sotalol, classes IA, IC
87
adenosine mechanism of action
activates A1 adenosine receptors which opens Ach-sensitive K+channels
88
adenosine action
hyperpolarises the AV node, suppressing impulse conduction
89
adenosine uses
terminating paroxysmal SVT
90
verapamil mechanism of action
blocks L-type Ca2+ channel
91
verapamil action
slows conduction and prolongs refractory period in AV node and bundle of His
92
verapamil uses
atrial fibrillation and atrial flutter
93
verapamil side effects
in high doses may cause heart block
94
lignocaine mechanism of action
blocks Na+ channels (class IB)
95
lignocaine action
mainly affects areas of ischaemic muscle
96
lignocaine uses
ventricular arrhythmia following MI (IV)
97
disopyramide mechanism of action
moderately blocks Na+ channels
98
disopyramide uses
orally to prevent recurrent ventricular arrhythmias
99
procainamide mechanism of action
IV to treat ventricular arrhythmias following MI
100
propranolol mechanism of action
blocker B-adrenoceptors
101
propranolol uses
control SVT, suppress excessive sympathetic drive that may trigger VT
102
amiodarone mechanism of action
block K+ cannel, increase AP and refractory period duration
103
amiodarone action
control SVT and VT
104
amiodarone side effects
pulmonary fibrosis, thyroid disorders, photosensitivity, peripheral neuropathy
105
warfarin mechanism of action
inactivates factors II, VII, IX and X
106
warfarin action
blocks coagulation, after slow onset (2-3 days)
107
factors that increase warfarin action
liver disease (decreased clotting factors), high metabolic rate (increased clearance of clotting factors), drug interactions
108
factors that lessen warfarin action
pregnancy (increase clotting factor systhesis), hyperthyroidism (decreased degradation of clotting factors), vitamin K consumption, drug interactions
109
reversal of warfarin
vitamin K
110
warfarin side effects
increase risk of haemorrhage
111
heparin and LMWH mechanism of action
bind to anti-thrombin III which increases its affinity for serine protease factors which inactivate clotting factors
112
warfarin uses
prophylaxis in rheumatic heart disease, AF, valve replacement, DVT and PE
113
heparin uses
treatmtent of PE, unstable angina and acute peripheral arterial occlusion, treatment of DVT, thromboprophylaxis, preferred in renal damage
114
LMWH uses
prevention of venous thromboembolism - DVT and PE, also in treatment of MI and unstable coronary artery disease
115
heparin side effects
thrombocytopenia - platelet deficiency
116
dabigatran mechanism of action
thrombin inhibitor
117
rivaroxaban mechanism of action
factor Xa inhibitor
118
NOAC advantages over warfarin and heparin
convenience, predictable degree of anticoagulation
119
NOAC uses
prevent venous thrombosis in patients undergoing hip and knee replacements
120
aspirin mechanism of action
irreversibly blocks cyclooxegenase (COX) in platelets, preventing TXA2 sysnthesis
121
aspirin use
thromboprophylaxis in patients at high cardiovascular risk
122
aspirin side effects
GI bleeding and ulceration
123
copidogrel mechanism of action
links to P2Y12 by a disulphide bond producing irreversible inhibition
124
clopidogrel use
most commonly used in patients intolerant to asprin or synergistically with aspirin
125
fibrinolytic drugs mechanism of action
stimulate the fibrinolytic cascade which opposes the coagulation cascade
126
fibrinolyitc drugs use
unblocking occluded arteries in acute MI
127
streptokinase is an example of a...
fibrolytic drug
