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Cardiovascular Pharmacology > Cardiovascular Pharmacology Summary Part 3 > Flashcards

Cardiovascular Pharmacology Summary Part 3 Flashcards

1
Q

Which drugs are thiazide diuretics?

A
  1. Hydrochlorothiazide (HCTZ)

2. Indapamide

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2
Q

What is the mechanism of action of the thiazide diuretics (cellular)?

A

Blocks Na/Cl reabsorption in the distal convoluted tubule. Also reabsorbs calcium and increases potassium excretion leading to hypokalaemia. Increases serum uric acid by competing with uric acid for secretion in the proximal convoluted tubule.

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3
Q

What is the mechanism of action of the thiazide diuretics (physiological)?

A

It is a low ceiling diuretic with a shallow dose response. In hypertension causes a mild volume depletion which often reverts back to normal. The persistent drop in BP, implies TPR decrease after 2-3 weeks.

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4
Q

What are the therapeutic uses of the thiazide diuretics?

A
  1. Could be used in mild heart failure to mobilize oedema and prevent congestion. Relatively weak diuretic = constrains its use in heart failure.
  2. Has a paradoxical effect in diabetes insipidus
  3. MAIN USE = HYPERTENSION
  4. Used with loop diuretics in heart failure.
  5. Often added to ACE and beta-blockers to augment anti-hypertensive effect.
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5
Q

What are the adverse effects / contraindications of the thiazide diuretics?

A
  1. Hypokalaemia
  2. Hyperuricaemia
  3. Decreased release of insulin and increases blood glucose
  4. Sulphur drug
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6
Q

Which drug is an aldosterone antagonist?

A

Spironolactone

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7
Q

What is the mechanism of action of spironolactone (cellular)?

A

Structurally similar to aldosterone. Blocks the aldosterone binding site, induces Na / K exchange in the collecting duct. Leads to potassium retention as well as retention of hydrogen ions.

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8
Q

What is the mechanism of action of spironolactone (physiological)?

A

Is a very weak diuretic. Is seldom used as a diuretic alone. Only used in hypertension as an add-on to existing therapy.

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9
Q

What are the therapeutic uses of spironolactone?

A
  1. Used with hydrochlorothiazide n hypertension.
  2. Also used in heart failure with ACE inhibitors to prevent aldosterone escape.
    - Major impact on mortality in heart failure
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10
Q

What are the adverse effects and contraindications of spironolactone?

A
  1. Hyperkalaemia
  2. Gynecomastia, inhibits testosterone synthesis
  3. Caution use with ACE-I
  4. ARB check for severe hyperkalaemia
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11
Q

Which drugs are potassium sparing diuretics?

A

Amiloride

Triamterene

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12
Q

What is the mechanism of action of the potassium sparing diuretics (cellular)?

A

Block Na/K exchange in the collecting duct independent of aldosterone. Also causes loss of H ions.

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13
Q

What is the mechanism of action of the potassium sparing diuretics (physiological)?

A

Is a very low ceiling diuretic and is seldom used as a diuretic alone. Only used in combination with HCTZ to prevent K loss in hypertension.

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14
Q

What is the therapeutic use of the potassium sparing diuretics?

A

Used with HCTZ in hypertension.

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15
Q

What are the adverse effects / contraindications of the potassium sparing diuretics?

A
  1. Hyperkalaemia
  2. Not to be given with ACE inhibitors.
  3. Acidosis also possible
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16
Q

Which drugs are fibrates?

A

Benzafibrate

Gemfibrozil

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17
Q

What is the mechanism of action of the fibrate drugs (cellular)?

A

Reduces the synthesis of VLDL and increases synthesis of HDL. Also stimulates the activity of lipoprotein lipase which increase adipose tissue deposition of FFA and lipids, this serum triglycerides drop.

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18
Q

What is the mechanism of action of the fibrate drugs (physiological)?

A

Primarily reduces triglycerides but also reduces LDL. HDL increases by 10-15%. More effective than statins in increasing HDL. Little effect on LDL.

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19
Q

What are the therapeutic uses of the fibrate drugs?

A

Used only as add on or if there is very high triglycerides and low HDL.

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20
Q

What are the adverse effects / contraindications of the Fibrate drugs?

A
  1. Well tolerated, but myalgia can occur
  2. Life threatening rhabdomyolysis
    - Can cause renal failure and death if combined with statin.
  3. Also sometimes causes an increase in liver enzymes
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21
Q

Which drugs are HMG Co A Reductase Inhibitors?

A

Simvastatin
Atorbastatin
Rosuvastatin

22
Q

What is the mechanism of action of the HMG Co A Reductase Inhibitors (cellular)?

A

Inhibits HMG Co A reductase in the liver, the rate limiting enzyme for the production of cholesterol. The reduction in cholesterol induces an increase in synthesis of liver LDL receptors and cholesterol levels drop.

23
Q

What is the mechanism of action of the HMG Co A Reductase Inhibitors (physiological)?

A

Primarily lowers total cholesterol and LDL. Triglycerides also reduced but not as much as LDL. HDL remains unchanged.

24
Q

What are the therapeutic uses of the HMG Co A Reductase Inhibitors?

A

The most effective drugs in the lowering of LDL. The percentage decrease in LDL is roughly associated with a similar drop in CVD events (stroke, CAD, MI and mortality)

25
Q

What percentage drop in LDL is seen with Simvastatin?

A

20%

26
Q

What percentage drop in LDL is seen with Atorvastatin?

A

10%

27
Q

What percentage drop in LDL is seen with Rosuvastatin?

A

31%

28
Q

What are the adverse effects / contraindications of the HMG Co A Reductase Inhibitors?

A
  1. Well tolerated, but myalgia can occur
  2. Life threatening rhabdomyolysis
    - Can cause renal failure and death (rare)
  3. Also sometimes causes a transient increase in liver enzymes
29
Q

Which drug is a GIT cholesterol inhibitor?

A

Ezetemibe

30
Q

What is the mechanism of action of Ezetemibe (cellular)?

A

Blocks cholesterol in the gut (high proportion of cholesterol). The reduction in liver cholesterol induces an increase in the synthesis of liver LDL receptors and LDL cholesterol levels drop.

31
Q

What is the mechanism of action of Ezetemibe (physiological)?

A

Primarily lowers total cholesterol and LDL. Triglycerides also reduced but not as much as LDL. HDL remains unchanged.

32
Q

What are the therapeutic uses of Ezetemibe?

A

Only used as add on to reduce LDL in familial hypercholesterolaemia.

33
Q

What is the percentage decrease in LDL seen with Ezetemibe?

A

20%

34
Q

What are the adverse effects / contraindications of Ezetemibe?

A

Well tolerated

35
Q

Which drug is a COX I Platelet Inhibitor?

A

Aspirin

36
Q

How is aspirin given (as a platelet inhibitor)?

A

Used in a low dose as a once a day dose

37
Q

What is the mechanism of action of aspirin (cellular)?

A

Blocks the activity of cyclo-oxygenase in all tissues, but because platelets only produce TXA2, this effects platelets most. Aspirin in the only COX inhibitor to irreversibly bind to and inhibit platelet COX.

38
Q

What is the mechanism of action of aspirin (cellular)?

A

Because platelets cannot regenerate new COX, the production of TXA2 is inhibited at at these doses. Prostacyclin is not affected.

39
Q

What are the therapeutic uses of aspirin (in CVD)?

A

Used to prevent platelet aggregation in TIA, MI, stroke, PVD, colon cancer.

40
Q

What are the adverse effects / contraindications of aspirin?

A
  1. GIT most common: reflux, perforation of ulcers and GIT bleeds = rare but fatal
  2. Asthma
41
Q

Which drug is an ADP inhibitor?

A

Clopidogrel

42
Q

What is the mechanism of action of Clopidogrel?

A

Blocks the action of ADP on ADP receptors and therefore inhibits platelet aggregation.

43
Q

What are the therapeutic uses of Clopidogrel?

A

Used in addition to aspirin to prevent stroke, CVD and PVD.

44
Q

What is the primary adverse effect of Clopidogrel?

A

Bleeding

45
Q

Which drugs are heparins?

A

Heparin

Enoxaparin

46
Q

What is the mechanism of action of heparin (cellular)?

A

Accelerates the action of antithrombin III by a thousand fold. Blocks the active factors IIa (thrombin - that converts soluble fibrinogen to fibrin) and Xa. Also blocks XII, XI, IX.

47
Q

What is the difference between the high and low molecular weight heparins?

A

Difference between HMW and LMW is that LMW has less activity on thrombin, and more selective on Xa.

48
Q

What is the onset of action of heparin?

A

Immediate onset of action

49
Q

What is an antagonist to heparin?

A

Protamine

50
Q

What are the therapeutic uses of heparin?

A

Used before the action of oral anticoagulants. Used for DVT prophylaxis, for hip surgery and in high risk patients.

51
Q

What are the adverse effects of heparin?

A
  1. Bleeding is the major problem.

2. Can cause osteoporosis

Cardiovascular Pharmacology (5 decks)

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