Cardiac drugs Flashcards

1
Q

Loop diuretic

A

Furosemide

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2
Q

Indications of furosemide (3)

A

Relief of breathlessness in pulmonary oedema
Symptomatic treatment of fluid overload in CHF (1st line)
Symptomatic treatment of fluid over load in other oedematous stated (e.g. renal/kidney failure)

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3
Q

Main side effects of furosemide (4)

A

Ototoxicity - tinnitus and hearing loss at high doses due to blockage of transporter in the ear
Hyperuricaemia
Hyperglycaemia
Hypokalaemia

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4
Q

What part of the nephron does furosemide act on?

A

Loop of Henle

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5
Q

What transporter channel does Furosemide inhibit?

A

Na+/K+/2Cl- co-transporter
Ca
Inhibits ion transport from the lumen into epithelial cells, thus reducing the gradient for osmosis, having a diuretic effect

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6
Q

Other effects of furosemide (1)

A

Dilation of capitance veins, reducing preload and improving contractile function

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7
Q

Metabolism and excretion of furosemide

A

Hepatic metabolism
Renal glucuronidation
Renal and biliary excretion

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8
Q

Interactions of furosemide

A

Aspirin and salicylates - may potentiate effects
Synergistic effects with other antihypertensives and diuretics
Affects drugs excreted by the kidneys (e.g. lithium and digoxin, aminoglycosides), risking toxicity

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9
Q

Thiazide diuretic

A

Bendroflumethiazide

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10
Q

This drug is used when CCBs, ACEIs and ARBs are insufficient in the control of hypertension

A

Bendroflumethiazide

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11
Q

Side effects of bendroflumethiazide (2)

A

Hyponatraemia

Hypokalaemia -> arrhythmias

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12
Q

Bendroflumethiazide acts on what part of the nephron?

A

Distal convoluted tubule

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13
Q

Bendroflumethiazide takes its action through inhibition of which channel?

A

Na+/Cl- transporter

Increases sodium and chloride ion secretion, with water following

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14
Q

Contraindications of bendroflumethiazide

A

Hypoklaemia
Hyponatraeima
Gout (reduces uric acid secretion)

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15
Q

Interactions of bendroflumethiazide (3)

A

Alcohol - causes sudden drop in BP
NSAIDs - reduces effectiveness
Other thiazides that lower potassium (e.g. furosemide)

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16
Q

Potassium-sparing diuretic

A

Spironolatone

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17
Q

Indications of spironolactone (2)

A

Combination therapy for treatment of hypokalaemia

Hypertension

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18
Q

Side effects of spironolactone

A

Dizziness, hypotension and urinary symptoms

May lead to hyperkalaemia - potentially fatal

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19
Q

MoA of spironolactone

A

Antagonist of mineralocorticoid receptor
Competitive antagonist of aldosterone
Increases sodium excretion and reduces potassium loss

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20
Q

Site of action of spironolactone

A

DCT

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21
Q

Metabolism and excretion of spironolactone

A

Hepatic metabolism to active metabolites

Urinary and biliary excretion

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22
Q

Interactions of spironolactone (4)

A

Avoid using with potassium supplements (hyperkalaemia)
Increased likelihood of hyperkalaemia with trimethoprim/sulphamethoxazole
Induces CYP3A4
Increases serum digoxin concentration

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23
Q

Beta blocker

A

Atenolol

24
Q

Indications of atenolol (5)

A

Management of hypertension when other hypertensives are insufficient
1st line IHD to improve Sx and prognosis
CHF - first line
AF - reduced ventricular rate and maintains sinus rhythm
SVT - first line in patients with circulatory compromise to restore sinus rhythm

25
Q

Serious side effect of beta-blockers

A

Bronchospasm in patients with asthma - mediated by blockade of beta-2 adrenoceptors in the airways

26
Q

MoA of atenolol

A

Beta-1 adrenoceptor blocker (mainly in the heart)
Reduce speed of conduction and force of contraction, relieving myocardial ischaemia by reducing cardiac work and oxygen demand, increasing myocardial perfusion
Protect the heart from the effects of chronic sympathetic stimulation
Prolong refractory period of AVN (treatment of SVT)
Reduce renin secretion from the kidney (metabolised by beta-1 adrenoceptors) - Rx of hypertension

27
Q

Excretion and metabolism of atenolol

A

Excretion is renal and lactic in lactiferous females

Metabolism is hepatic

28
Q

Interactions of atenolol (1)

A

Non-dihydropyridine CCBs - verapamil, diltiazem

Can cause HF, bradycardia and asystole

29
Q

Thrombolytic

A

Tissue Plasminogen Activator (tPA)

30
Q

Indications of tPA (3)

A

Management of MI, acute ischaemic stroke, and lysis for acute pulmonary emboli

31
Q

Side effect of tPA

A

Haemorrhage, IC bleeding (high dose)

32
Q

Contraindication

A

Haemorrhagic stroke

33
Q

MoA of tPA

A

Bind fibrin in thrombi and convert pladminogen to plasmin which degrades the fibrin matrix of the thrombus

Also produces conversion of plasminogen in the absence of fibrin

34
Q

Metabolism of tPA

A

Hepatic

35
Q

Interactions of tPA

A

Coumarin derivatives, oral anti-coagulants, platelet aggregation inhibitors, unfractioned heparin, LMWH or active substances interfering with coagulation - risk of haemorrhage
Use of GPiib/iiia antagonists - increased risk of bleeding

36
Q

Statin

A

Simvastatin

37
Q

Indications of simvastatin (3)

A
  1. Primary prevention of CVD
  2. Secondary prevention of CVD
  3. Primary hyperlipidaemia (1st line in hypercholesterolaemia)
38
Q

Side effects of statins

A

Muscle ache, myopathy and rarely, rhabdomyolysis

39
Q

Contraindications of statins

A

Renal impairment and pregnancy and breastfeeding (cholesterol is essential for foetal growth)

40
Q

MoA of simvastatin

A

Inhibition of HMG coenzyme A reductase - decrease cholesterol production by the liver and increased clearance of LDL from the blood
Directly reduce triglycerides and increase HDL level
Slow and reverse the atherosclerotic process

41
Q

Metabolism and excretion of simvastatin

A

Hepatic metabolism by CYP3A4

Renal and faecal excretion

42
Q

Interactions of simvastatin

A

Metabolism reduced by CYP450 inhibitors - amiodarone, diltiazem, itraconazole, macrolides, protease inhibitors - reduces risk of adverse effects due to accumulation

43
Q

Novel anticoagulant

A

Rivaroxaban

44
Q

Indications of rivaroxaban (4)

A
  1. Prevention of VTE in pts undergoing joint replacement
  2. Prevention of stroke and ischaemic embolism in pts with non-valvular AF
  3. Treatment of DVT and PE
  4. Reduce risk of recurrent DVT and PE
45
Q

Side effects of rivaroxaban

A

Bleeding (but lower rate than warfarin)
Renal toxicity
Liver impairment

46
Q

MoA of rivaroxaban

A

Inhibition of free and clot-bound factor Xa, which activates prothrombin (ii) to thrombin (iia)
One molecule of factor Xa can generate > 1000 molecules of thrombin
Action is irreversible

47
Q

Metabolism and excretion of rivaroxaban

A

Metabolism: CYP3A4 and CYP2J2
Excretion: renal

48
Q

Interactions of rivaroxaban

A

CYP3A4 and P-gp inhibitors e.g. ketoconazole and ritonavir - increased risk of bleeding
Othe anticoagulants - increased risk of bleeding
NSAIDs/platelet aggregation inhibitors e.g. clopidogrel - increased risk of bleeding
CYP3A4 inducers - reduced plasma concentrations - thrombosis

49
Q

Nitrate

A

Isosorbide mononitrate

50
Q

Indications of isosorbide mononitrate (2)

A

1) Prophylaxis of angina

2) Treatment of pulmonary oedema, usually with furosemide and oxygen

51
Q

Side effects of isosorbide mononitrate

A

Headache, hypotension

Can lead to tolerance - minimise dose to avoid unnecessary administration

52
Q

MoA of isosorbide mononitrate

A

Converted to nitric acid which increases CMP synthesis and reduces IC calcium in vascular SMCs, causing relaxation and vasodilation

53
Q

Effects on isosorbide mononitrate

A

Relaxation of venous capacitance vessels, reducing cardiac preload and LV filling - these effects reduce cardiac work and oxygen demand, relieving angina and cardiac failure

54
Q

Metabolism and excretion of isosorbide mononitrate

A

Hepatic metabolism

Renal excretion

55
Q

Interactions of isosorbide mononitrate (4)

A

Phosphodiesterase inhibitors (viagra, slidenafil) - enhance and prolong hypotensive effects
Antihypertensives - hypotension
Propranolol - causes fall in portal pressure, reduction in hepatic flow and CO, and mean arterial BP
Calcium antagonists - orthostatic hypotension when used in combination

56
Q

Anti-dysrrhythmic

A

Amiodarone

57
Q

Indications of amiodarone

A

Management of tacchycardias - AF, atrial flutter, SVT, VT, refractory VF