Drugs used in treating cardiovascular diseases Flashcards

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1
Q

Common CV conditions requiring drug therapy

A

Hypertension
Ischaemic heart disease and other atheromatous diseases
Heart failure
Arrhythmia

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2
Q

Hypertension

A

Most cases asymptomatic and 95% cases are ‘essential’ hypertension e.g. no secondary cause
CV morbidity and mortality can be < significantly by BP reduction

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3
Q

How can CV morbidity and mortality be reduced?

A

by BP reduction

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4
Q

Early detection of hypertension allows

A

Most effective risk management and treatment of hypertension

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5
Q

End organ damage in hypertension

A

Brain
Heart
Kidney: renal failure
Eyes: hypertensive retinopathy

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6
Q

End organ damage in hypertension: brain

A

Thrombotic, thromboembolic and haemorrhagic stroke, multi-infarct dementia, hypertensive encephalopathy

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7
Q

End organ damage in hypertension: heart

A

LVH, LV failure, coronary artery disease

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8
Q

Major risk factors for cerebrovascular atherosclerosis

A
Hypertension increases risk by x5-10
Smoking x2
Diabetes x2
Hyperlipidemia x1.5
Obesity x1.5
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9
Q

Prognosis of hypertension

A

Related to level of systolic and diastolic BPs
Related to age, sex and other risk factors such as hyperlipidaemia and diabetes
Worse if there is evidence of end-organ damage
Improved with antihypertensive therapy

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10
Q

Non-pharmalogical treatment of hypertension

A
Weight reduction
< salt intake
< fat intake
< alcohol intake
Exercise
Smoking cessation
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11
Q

Common antihypertensive drugs

A
Thiazide diuretics
ACE inhibitors 
Angiotensin II receptor antagonists
Beta blockers
Calcium channel blockers
Alpha blockers
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12
Q

Thiazide diuretics

A
Inhibit reabsorption of NaCl in proximal and early distal tubules of nephron
Cheap and recommended for first line use
Bendroflumethiazide 
Metolazone
Thiazide-related compounds
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13
Q

Renin-angiotensin system

A

Learn diagram

Regulates salts and fluid?

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14
Q

ACE inhibitors mechanism

-example

A

Inhibit conversion of angiotensin I to angiotensin II

e.g. ramipril < MI, stroke, CV death

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15
Q

Angiotensin receptor blocker

A

Acts on AT-1 receptor

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16
Q

Sprionolactone

A

Acts on aldosterone

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17
Q

Angiotensin II receptor antagonists (ARBs)

A

Similar effects to ACE inhibitors but do not influence bradykinin degradation so do not cause dry cough

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18
Q

Examples of ARBs

A

Losartan, valsartan, candesartan, irbesartan

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19
Q

Beta blockers (beta-adrenoreceptor antagonists)

A

< heart rate, BP and cardiac output

Variable selectivity for cardiac beta 1 receptors (which mediate sympathetic action)

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20
Q

Side effects of beta blockers

A
Fatigue
Hypotension
Cold peripheries
Bronchospasm
Impotence
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21
Q

Sympathetic and Parasympathetic action on heart and vessels

A

Symp > force and rate of heart contractions
-beta-1 receptors of heart mediate sympathetic action
-B-blockers can have adverse effects on vascular supply to the legs as sympathetic system increasing vasoconstriction in arterioles
Parasymp opposite

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22
Q

Calcium channel antagonists

A

Vasodilators - < systemic vascular tone

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23
Q

Main types of calcium channel antagonists

A
Two main types:
Verapamil and diltiazem
-cause bradycardia, inhibit AV node conduction, negative inotropes
Amlopidine, larcanipidine ... dipine
-may cause a reflex tachycardia
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24
Q

Side effects of calcium channel antagonists

A
Oedema
Flushing
Headache
Dizziness
Hypotension
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25
Q

Alpha blockers and others

A

A variety of other vasodilators are used to treat hypertension:

  • alpha blockers: doxazosin, indoramin
  • hydralazine
  • methyldopa (can be used in pregnancy)
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26
Q

Alpha blockers and others: side effects

A

Hypotension
Headache
Tachycardia
Oedema

27
Q

Thiazide diuretics side effects

A

Side effects include electrolyte disturbance, rash and postural hypotension

28
Q

Most commonly used thiazide diuretic

A

Bendroflumethiazide most commonly used thiazide

29
Q

Thiazide diuretic used for severe congestive heart failure

A

Metolazone used in combination with loop diuretics

30
Q

Thiazide related compounds

A

chlorthalidone, indapamide

31
Q

Side effects of ACE inhibitors

A

Relatively infrequent side effects except for dry cough

  • hypotension
  • rash
  • hyperkalaemia
  • renal failure (especially in presence of renal artery stenosis)
  • angioedema
  • ageusia
32
Q

Ischaemic heart disease

A

Atherosclerosis of coronary arteries may lead to stenosis and arterial thrombosis
Spectrum of presentations from stable angina to acute coronary syndromes – unstable angina and myocardial infarction – to heart failure and sudden death

33
Q

Progression of atherosclerosis to arterial thrombosis

A

Normal –> fatty streak –> (clinically silent) fibrous plaque –> athero-sclerotic plaque (can happen with age and can cause angina, transient ischemic attack and claudication/ PAD) –> plaque rupture/ fissure and thrombosis
This can lead to MI/ ischemic stroke / critical leg ischemia/ CV death

34
Q

Anti-anginal drugs

A

Beta blockers
Nitrates
Calcium channel blockers
Potassium channel activators

35
Q

Relative contraindications of beta-blockers

A

asthma, uncontrolled heart failure, bradycardia

36
Q

Anti-anginal drugs: beta blockers

A

Lower myocardial oxygen demand by < HR, BP and myocardial contractility
May exacerbate cardiac failure (need to be introduced slowly) and peripheral vascular disease (claudication), and cause bronchospasm

37
Q

Abrupt withdrawal from beta blockers as anti-anginal drugs

A

may lead to arrhythmia, worsening angina or myocardial infarction

38
Q

Anti-anginal drugs: nitrates

-how do you take them

A

Oral, sublingual (GTN tabs/spray), buccal, transdermal and intravenous forms used commonly

39
Q

Anti-anginal drugs: nitrates

-action

A

Symptomatic relief of angina
Produce nitric oxide at endothelial surface leading to vascular smooth muscle relaxation and arteriolar and venous dilatation
< myocardial oxygen demand (lower preload and afterload) and increase myocardial oxygen supply (coronary vasodilatation)

40
Q

Side effects of anti-anginal drugs: nitrates

A

Headache
Flushing
Postural hypotension

41
Q

Anti-anginal drugs: calcium antagonists

A

Lower myocardial oxygen demand by < BP and myocardial contractility and < myocardial oxygen supply by dilating coronary arteries

42
Q

Anti-anginal drugs: calcium antagonists

-when to avoid

A

Verapamil and diltiazem should be avoided in heart failure

43
Q

Anti-anginal drugs: Potassium channel activators

A

Nicorandil
Arterial and venous dilating properties
No problems with tolerance as seen with nitrates

44
Q

Anti-anginal drugs: Potassium channel activators

-side effects

A

Can cause mucocutaneous ulceration

-relegated to second-line therapy

45
Q

Anti-platelet drugs: action

A

Inhibit platelet aggregation and arterial thrombus formation, thus preventing heart attack, stroke and CV death

46
Q

Anti-platelet drugs: aspirin

A

blocks platelet cyclo-oxygenase (COX1) and the production of thromboxane A2, a platelet activating substance

47
Q

Anti-platelet drugs: clopidogrel, prasugrel and ticagrelor

A

platelet ADP (P2Y12) receptor inhibitors; used alone or, more often, in combination with aspirin

48
Q

Anti-platelet drugs: dipyridamole

A

Mainly used in combination with aspirin to prevent stroke

49
Q

Bleeding time in healthy volunteers treated with ticagrelor +/- aspirin
-in Lancet bleeding time (s)

A

Non antiplalet treatment: 150 +/- 54
Ticagrelor 250 +/- 77
Ticagrelor + aspirin: 541 +/- aspirin

50
Q

Statins

A

Hydroxymethyl-glutaryl (HMG) CoA reductase inhibitors
Lower LDL cholesterol and may increase HDL cholesterol
< risks of MI stroke and CV death

51
Q

Examples of statins

A

Simvastatin, pravastatin, atorvastatin, rosuvastatin, …statin

52
Q

Heart failure

A

imprecise term describing state that develops when heart cannot maintain adequate cardiac output or can do so only at the expense of an elevated filling pressure
Associated with activation of RAS axis and sympathetic nervous system

53
Q

How do pulmonary and/ or peripheral oedema develop?

A

due to high atrial pressures and salt/water retention caused by impaired renal perfusion and secondary aldosteronism

54
Q

Drug treatment for chronic heart failure

A

Diuretics
ACE inhibitors
Beta Blockers
Aldosterone antagonists

55
Q

Diuretics for treatment of heart failure

A

Thiazides
K-sparing
Loop diuretics
-strongest
more powerful than those used for hypertension
synergistic effects of combining all diuretics

56
Q

Thiazides for treatment of heart failure

A

Inhibit active exchange of Cl-Na in the cortical diluting segment of the ascending loop of Henle
Acts on cortex

57
Q

K-sparing diuretics for treatment of heart failure

A

Acts on cortex
Inhibit reabsorption of Na in the
distal convoluted and collecting tubule

58
Q

Loop diuretics for treatment of heart failure

A

Inhibit exchange of Cl-Na-K in
the thick segment of the ascending
loop of Henle
Acts on medulla

59
Q

Aldosterone inhibitors

A

Spironolactone
Eplerenone
-competitive antagonist of the aldosterone receptor
-acts on myocardium, arterial walls, kidney
-tackle salt and water retention
-prevent potassium level from going too low
-may reduce fibrosis in the myocardium

60
Q

Tacharryhthmias

A

Abnormal rapid heart rhythms
Different types depending on origin in heart of abnormal electrical activity including:
-atrial fibrillation (AF) or atrial flutter with rapid ventricular rate response
-supraventricular tachycardia (SVT)
-ventricular tachycardia (VT)

61
Q

Digoxin (digitalis)

A

Most often used to treat AF and heart failure
Glycoside drug
Blocks Na+/ K+ ATPase –> Ca++
> vagal tone - slows conduction in atrial fibrillation

62
Q

Oral antiarrhythmics

A

Drugs for controlling tachyarrhythmia
Class Ia,b,c – disopyramide, flecainide, procainamide
Class II – beta blockers
Class III – amiodarone, dronedarone, sotalol
Class IV – calcium antagonists (verapamil, diltiazem)

63
Q

What can low potassium lead to?

A

Heart rhythm disturbance (arrhythmia)

64
Q

Interaction between anticoagulants and antiplatelets

A

Both interact (antithrombotics)
Both coagulation and platelet formation are driven by thrombin
-if you block thrombin by one drug, will affect other pathway
Higher bleeding risk if on both