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Cardiovascular Pharmacology > Cardiovascular Pharmacology Summary Part 2 > Flashcards

Cardiovascular Pharmacology Summary Part 2 Flashcards

1
Q

Which drug is a long acting vasodilator?

A

Hydralazine

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2
Q

What are the pharmacokinetics of Hydralazine?

A

Taken orally
Direct vasodilator
Long acting

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3
Q

What is the mechanism of action of Hydralazine (chemical)?

A

Nitric oxide donor increases cGMP through guanylate cyclase. Mainly acts to decrease blood pressure and reduce TPR. Some effect on venous return but not like nitrates.

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4
Q

What is the mechanism of action of Hydralazine (chemical)?

A

Causes vasodilation and venodilation. Drop in TPR, increases HR and fluid retention.

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5
Q

What are the therapeutic uses of Hydralazine?

A
  1. Decreasing preload and afterload (less of an effect)
  2. Used in combination with nitrates in heart failure patients with a contraindication to ACE/ARBs always with diuretics and beta blockers
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6
Q

What are some of the adverse effects and contraindications of Hydralazine?

A
  1. Headache
  2. Tachycardia
  3. Do not use with Sildenafil = decreases venous return and blooc pressure which can be fatal.
  4. Also causes a lupus like syndrome
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7
Q

Which drug is a short acting vasodilator?

A

Sodium Nitroprusside

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8
Q

What are the pharmacokinetics of Sodium Nitroprusside?

A

Direct vasodilator
Short acting
Taken IV

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9
Q

What is the mechanism of action of Sodium Nitroprusside (cellular)?

A

Nitric oxide donor increases cGMP through guanylate cyclase. Mainly acts to decrease blood pressure and reduce TPR. Some effect on venous return but not like nitrates.
Very short half life allows for titration of dose.

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10
Q

What is the mechanism of action of Sodium Nitroprusside (physiological)?

A

Causes vasodilation and venodilation. Drop in TPR, increases HR and fluid retention.
Used only for hypertensive emergency.

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11
Q

What are the therapeutic uses of Sodium Nitroprusside?

A

Decreasing preload and afterload in hypertensive emergency!

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12
Q

What are the adverse effects and contraindications of Sodium Nitroprusside?

A
  1. Headache
  2. Tachycardia
  3. Do not use with Sildenafil = decreases venous return and blooc pressure which can be fatal.
  4. Causes acidosis and liver problems.
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13
Q

Which drugs are ACE-inhibitors?

A

Catopril
Enalapril
Ramipril

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14
Q

What are the pharmacokinetics of the ACE-inhibitors?

A
  1. Catopril: short half life, needs to be taken 2-3 times / day
  2. Enalapril / Ramipril: long acting, only needs to be used once daily
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15
Q

What is the mechanism of action of the ACE-inhibitors (cellular)?

A

Blocks the conversion of AI to active AII. AII normally is a vasoconstrictor and releases aldosterone.

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16
Q

What is the mechanism of action of the ACE-inhibitors (physiological)?

A

Decreases total peripheral resistance and reduces the amount of sodium and water reabsorbed in the kidney. Increases bradykinin which is a vasodilator and irritant. Decreases aldosterone levels and reduces preload.

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17
Q

What are the therapeutic uses of the ACE-inhibitors?

A
  1. Hypertension (primarily on TPR)
  2. Heart failure by decreasing afterload and preload
  3. Reduces sodium and water retention
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18
Q

What are the adverse effects and contraindications of the ACE-inhibitors?

A
  1. Dry cough (due to bradykinin)
  2. Angioedema
  3. Rash
  4. Hyperkalaemia especially with K sparing diuretics (spironolactone)
    C/I in severe renal failure and pregnancy
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19
Q

Which drugs are angiotensin receptor blockers (ARBs)?

A

Valsartan

Losartan

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20
Q

What are the pharmacokinetics of the ARBs?

A

Long acting only needs to be used once daily

21
Q

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

A

Blocks the binding of AII to its AT1 receptor, competitive antagonist.
AII normally is a vasoconstrictor and releases aldosterone.

22
Q

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

A

Decreases total peripheral resistance and reduce the amount of sodium and water reabsorbed by the kidney. Reduces aldosterone. Does not produce bradykinin.

23
Q

What are the therapeutic uses of the ARBs?

A
  1. Hypertension (primarily on TPR)
  2. Heart failure by decreasing afterload and preload
  3. Reduces sodium and water retention
24
Q

What are the adverse effects and contraindications of the ARBs?

A
  1. Rash
  2. Side effect profile similar to placebo.
  3. ACE without the cough.
  4. Hyperkalaemia with K sparing diuretics (spironolactone)
    C/I: In severe renal failure, renal stenosis and pregnancy
25
Q

Which drug is an alpha-1 receptor blocker?

A

Doxazosin

26
Q

What are the pharmacokinetics of Doxazosin?

A

Only needs to be used once daily.

27
Q

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

A

Blocks the action of noradrenaline to the arteriolar VSM alpha 1 adrenergic receptor, competitive antagonist. Blocks the increase in intracellular IP3 and Ca.

28
Q

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

A

Decreases total peripheral resistance, but also causes first dose first dose hypotension and orthostatic hypotension (blocks SNS reflex increase in SNS after postural changes).

29
Q

What are the therapeutic uses of Doxazosin?

A
  1. Hypertension (primarily on TPR).
    - Only used as a third line drug.
  2. Also used in patients with benign prostatic hypertrophy to improve urine outflow
30
Q

What are the adverse effects / contraindications of Doxazosin?

A
  1. Depression
  2. Tiredness (blockade of the alpha 1 receptors in the brain)
  3. Orthostatic hypotension can be serious
31
Q

Which drug is an alpha-2 receptor agonist?

A

Alpha Methyldopa

32
Q

What are the pharmacokinetics of Alpha Methyldopa?

A

Needs to be taken twice daily.

Metabolized in the liver.

33
Q

What is the mechanism of action of Alpha Methyldopa (cellular)?

A

An alpha 2 presynaptic agonist, blocks the release of Noradrenaline in the vasomotor center, SNS activity falls. Decreases release of noradrenaline in the vasomotor center, SNS activity decreases.

34
Q

What is the mechanism of action of Alpha Methyldopa (physiological)?

A

Decreases total peripheral resistance, but also causes first dose first dose hypotension and orthostatic hypotension (blocks SNS reflex increase in SNS after postural changes).

35
Q

What are the therapeutic uses of Alpha Methyldopa?

A
  1. Hypertension (primarily on TPR via reduction of central SNS)
  2. Used for hypertension associated with pregnancy
36
Q

What are the adverse effects / contraindications of Alpha Methyldopa?

A
  1. Depression
  2. Tiredness (reduction of noradrenaline in the brain)
  3. Orthostatic hypotension
37
Q

Which drug is a cardiac glycoside?

A

Digoxin

38
Q

What are the pharmacokinetics of Digoxin?

A

Taken once daily.

Excreted in the kidney and metabolized in the liver.

39
Q

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

A

Increases the entry of calcium into the myocardium by inhibiting the membrane Na/K ATPase pump. The increase in intracellular Na = less Ca being expelled from the cell. Increases the activity of the vagal nerve to SA/AV node and increases sensitivity of SA and AV node to acetylcholine.

40
Q

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

A

Blocks conduction through the AV node and decreases SA node firing, heart rate decreases. Contractility and SV increase marginally. O2 demand by heart increases.

41
Q

What are the therapeutic uses of Digoxin?

A
  1. Heart failure (primarily with atrial fibrillation)
  2. Supraventricular arrhythmia, slow AV conduction. Used with verapamil or diltiazem. Caution in hypokalaemia, effects potentiated.
42
Q

What are the adverse effects / contraindications of Digoxin?

A
  1. SA / AV nodal problems
  2. Headache
  3. Confusion
  4. Visual disturbances
    * NARROW THERAPEUTIC INDEX!
43
Q

Which drug is a loop diuretic?

A

Furosemide

44
Q

How is Furosemide administered?

A

Given oral / IV

45
Q

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

A

Blocks the Na/K/Cl co-transporter in the ascending limb of the loop of Henle. Also causes calsium loss and magnesium excretion.

46
Q

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

A

It is a high ceiling diuretic with a large dose response, given IV or oral. Causes significant potassium loss and hydrogen ion loss, leading to alkalosis.

47
Q

What are the therapeutic uses of furosemide?

A
  1. Used in right ventricular heart failure to mobilize peripheral oedema.
  2. Also used in left sided heart failure to reduce pulmonary congestion.
  3. Also used for hypercalcaemia caused by cancer
  4. Very seldom used in hypertension because of severe volume depletion compromising cardiac output.
    * Used with potassium supplements to prevent hypokalaemia.
48
Q

What are the adverse effects / contraindications of furosemide?

A
  1. Hypokalaemia
  2. Hyperuricemia
  3. Volume depletion
  4. Hyponatremia
  5. Hypotension

Cardiovascular Pharmacology (5 decks)

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