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Pharmacology > EXAM #2: CV PHARM VI > Flashcards

EXAM #2: CV PHARM VI Flashcards

1
Q

What is the mechanism of action of the ACE inhibitors?

A

Block of Angiotensin Converting Enzyme (ACE) to reduce the amount of circulating Angiotensin II

Note that this also inhibits the breaksdown Bradykinin, which leads to vasodilation

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2
Q

What is the role of ACE inhibitors in antihypertensive therapy?

A
  • 1st line or add-on for uncomplicated HTN
  • 1st line therapy for comorbidities

Effects are enhanced by combining with diuretic*

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3
Q

How are ACE inhibitors cleared? What are the clinical implications?

A

Cleared by the kidney; thus, reduce dose in patients with kidney failure

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4
Q

What is the effect of elevated plasma renin activity in ACEI therapy?

A

Can cause hyper-responsiveness b/c:

  • Renin converts angiotensinogen to ANG I
  • Individuals are accostomed to having high ANG I levels that are NOT going to be converted to ANG II
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5
Q

What patients will have a high plasma renin activity?

A

Patients in heart failure and those with Na+ depletion

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6
Q

When are ACEIs contraindicated?

A

1) Pregnancy
2) Bilateral renal artery stenosis
3) Angioedema

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7
Q

What are the situations with potentially favorable effects of ACEIs?

A

1) Patients with low-normal K+ b/c these drugs INCREASE plasma K+
2) Prediabetes
3) Albuminuria

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8
Q

What are the situations with potentially unfavorable effects of ACEIs?

A

1) High-normal K+
2) Hyperkalemia
3) Volume depletion

ACEIs will cause vasodilation in patients with volume depletion and lead to HYPOTENSION*

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9
Q

What are the adverse effects of ACEIs?

A

1) Hypotension
2) Cough
3) Angioedema
4) Increased plasma K+
5) Acute renal failure
6) Fetopathic potential
7) Skin rash

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10
Q

What causes coughing in ACEI therapy? What can you consider as an alternative therapy?

A

Bradykinin

—> ARBs

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11
Q

What patient is a “good responder” to ACEI?

A

Young/ middle aged Caucasians

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12
Q

What patient population is labled as “bad responders” to ACEIs?

A

Elderly African Americans

Remember from the ED, increased angioedema in African Americans*

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13
Q

List the ACEIs. List the ARBs. How do you tell the difference?

A

Lisinopril
Captopril
Fosinopril

Losartan
Valsartan
Candesartan

Remember:

  • pril= ACEI
  • artan= ARB
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14
Q

What is the mechanism of action of the Angiotensin Receptor 1 Blockers?

A

Antagonize Angiotensin II Receptors, Type-I, which block ANG II from binding to the adrenal gland

Note that ANG II concentrations will either stay the same or increase with these drugs

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15
Q

What is the role of Angiotensin Receptor I blockers in antihypertensive therapy?

A

Alternative for patients with intolerance to ACE inhibitors

Think of as an alternative for elderly African American patients

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16
Q

When should you consider ARBs as first-line therapy?

A

1) DM
2) CKD
3) CAD
4) LV-Dysfunction

But NOT CVA

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17
Q

When is ARB use contraindicated?

A

1) Pregnancy

2) Bilateral renal artery stenosis

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18
Q

What patient populations have favorable and unfavorable responses to ARBs?

A

Same as ACEIs.

Favorable:

  • Low-normal K+
  • Pre-DM

Unfavorable:

  • Hyperkalemia
  • Volume depletion
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19
Q

What is the mechanism of action of the DHP Ca++ blockers for HTN?

A

Recall that these are the Ca++ channel blockers with a 10:1 vasodilatory effect compared to the NDPH

Note that this vasodiatory effect will induce reflex tachycardia, especially in the first week of use

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20
Q

What is the role of DHP Ca++ blockers for HTN?

A
  • First line or add-on therapy for uncomplicated HTN

- Add-on for DM and CAD

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21
Q

When should DHP Ca++ blockers be avoided?

A

Left ventricular dysfunction

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22
Q

List the DHP Ca++ blockers that are used as anti-hypertensive drugs.

A

Nifedipine
Amlodipine
Felodipine

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23
Q

What are the situations that are favorable for DHP Ca++ blockers?

A

1) Reynaud Syndrome
2) Elderly patients with isolated systolic HTN
3) Cyclosporine-induced HTN

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24
Q

What are the situations that are unfavorable for DHP Ca++ blockers?

A

1) Peripheral edema b/c one of the side effects is peripheral edema
2) High normal rate–>Tachycardia

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25
Q

What is the mechanism of action of the Non-DHP Ca++ blockers?

A

These are the Ca++ blockers that have a 1:1 vasodilatory to cardiac effect

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26
Q

What is the role of Non-DHP Ca++ blockers in anti-HTN therapy?

A

1) First-line or add-on for uncomplicated HTN
2) Add-on for DM
3) Alternative to B-blockers in CAD**

These drugs will decrease myocardial contractility and thus reduce myocardial oxygen consumption

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27
Q

When should Non-DHP Ca++ blockers be avoided?

A

1) 2nd or 3rd degree heart block

2) LV dysfunction b/c of decreased contracility

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28
Q

What are the situations with potentially favorable effects for NDPH Ca++ blockers?

A

1) Reynaud Syndrome
2) Migraine headache
3) Arrhythmias
4) Tachycardia/ high-normal rate

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29
Q

What are the situations with potentially unfavorable effects for NDPH Ca++ blockers?

A
  • Peripheral edema
  • Low-normal heart rate
  • AV block
30
Q

What is the mechanism of action of the Thiazide diuretics for HTN?

A
  • Block the NaCl Cotransporter in the DCT

- Na+ in the lumen increases water excretion

31
Q

What is the role of Thiazide diuretics in anti-HTN therapy?

A

1) First line or add on therapy for uncomplicated HTN
2) First line therapy for:
- LV-Dysfunction
- Prior ischemic stroke

32
Q

When should the use of Thiazide diuretics be avoided?

A

1) Allergy to sulfa
2) Gout
3) Hyponatremia
4) Hypokalemia (drugs cause further loss of K+)

Note that patients with CHF will already have depleted Na+*

33
Q

What are the favorable situations for Thiazide diuretic use?

A

HTN with

  • Osteoporosis b/c drug will INCREASE Ca++ reuptake
  • High- normal K+
34
Q

What are the unfavorable situations for Thiazide diuretic use?

A
  • Gout
  • Pre-DM
  • Low-normal K+
  • Elevated fasting glucose
35
Q

List the Beta-adrenergic receptor antagonists that are used for HTN. What are their receptor specificities?

A

1) Propanolol–non-selective
2) Metoprolol- cardio-selective
3) Pindolol–ISA
4) Labetalol–mixed alpha and beta

36
Q

What is the role of Beta-antagonists in antihypertensive therapy?

A

1) 1st line for HTN w/
- CAD
- LV dysfunction
2) Add on therapy for DM

37
Q

What are the favorable situations for Beta-blocker use?

A
  • Migraine
  • Tachycardia
  • Hyperthyroidism
  • Tremor
  • Preoperative tremor
38
Q

List the two aldosterone antagonists. What is their role in antihypertensive therapy?

A

Spironolactone
Eplerenone

Add on therapy for

  • Resistant HTN
  • CAD
  • LV dysfunction
39
Q

When is aldosterone antagonists use favorable for HTN?

A
  • Low K+

- CKD

40
Q

When is aldosterone antagonists use unfavorable for HTN?

A

High K+ e.g. late stage kidney disease/ rhabdomyolsis

41
Q

What is the definition of the “other agents” for HTN?

A

These are agents that are:

  • Effective in lowering BP
  • Approved for treatment of HTN
  • Have NOT been shown in clinical trials to reduce the risks of CV events
42
Q

List the classes of “other” agents for use in HTN?

A

1) Alpha blockers
2) Arterial vasodilators
3) Central alpha 2 agonists
4) Direct rennin inhibitors
5) Rauwolfia alkaloids

43
Q

List the alpha 1 adrenergic receptor blockers.

A

Prazosin
Doxazosin
Terazosin

44
Q

What is the role of alpha 1 blockers in antihypertensive therapy?

A
  • Enhanced efficacy when used in conjunction with a diuretic
  • Lowers: LDL, TG, and total cholesterol
45
Q

What are the adverse effects of alpha-1 blockers?

A
  • Tolerance
  • Reflex tachycardia
  • Sexual dysfunction
46
Q

List the central alpha-2 agonists.

A

Clonidine

Methyldopa

47
Q

What limits the use of Clonidine?

A

Anticholinergic effects e.g.

  • Constipation
  • Dry mouth
  • Drowsiness

**Note that a relatively high degree of rebound HTN is seen

48
Q

What is the role of a-methyldopa in antihypertensive therapy?

A

Gestational HTN

Also used in patients with chronic HTN that get pregnant*

49
Q

What are the adverse effects seen with alpha-methyldopa?

A

1) Hepatotoxicity
2) Positive direct coombs’ test

Note that methyldopa has fewer anticholinergic effects than Clonidine

50
Q

What is the mechanism of action of Hydralazine?

A

Arterial vasodilator

  • Decreases IP3 induced Ca++ release
  • Opens K+ channels to hyperpolarize smooth muscle and cause vasodilation
51
Q

What is the role of hydralazine in the management of HTN?

A

1) Add-on therapy for resistant HTN, esp w/ chronic kidney disease
2) Safe in pregnancy

52
Q

What are the adverse effects of Hydralazine?

A
  • Drug induced Lupus
  • Tachycardia and Na+ retention

Thus, it should be combined with a diuretic and Beta-blocker

53
Q

What is the mechanism of action of Minoxidil?

A

Open K+ channels to relax arteriolar vascular smooth muscle cells

54
Q

What are the cardiac effect of Minoxidil?

A
  • Decrease BP
  • Increases blood flow to skin, muscles, GI tract, and CNS
  • Increased CO
  • Increased RBF
55
Q

What is the role of Minoxidil as an antihypertensive?

A

Severe refractory HTN in conjunction with a beta blocker

56
Q

What are the adverse effects of Minoxidil?

A
  • Fluid and salt retention

- Reflex increase in contractility

57
Q

What is the mechanism of action of Sodium Nitrporusside?

A

IV agent that is a potent arterial vasodilator

  • Donates NO for cGMP mediated Ca++ sequestration
  • Decreases both afterload and preload (cardiac workload)
58
Q

What are the adverse effects of Sodium Nitroprusside?

A
  • Methemoglobinemia
  • Cyanide poisoning
  • Cell death via inhibition of cellular respiration (CN)
59
Q

What is the clinical indication for Sodium Nitroprusside?

A

Hypertensive emergency

60
Q

What is the mechanism of action of Aliskiren?

A

Direct renin inhibitor

61
Q

What is the clinical use of Aliskrein?

A

Monotherapy or combination therapy for HTN

62
Q

What are the precautions associated with Aliskrein?

A
  • Hyperkalemia

- NEVER use in pregnancy

63
Q

What is the mechanism of action of Reserpine?

A

Blocks transport of NE into storage granules

64
Q

What is the role of Reserpine in antihypertensive therapy?

A

Used for resistant HTN

65
Q

What is the most effective use of reserpine?

A

In conjunction with a thiazide diuretic

66
Q

What are the side effects of Reserpine?

A

Sympatholytic i.e. increases PNS activity

67
Q

What is one of the major contributing factors to Resistant HTN? What are the implications?

A

Excessive dietary Na+

Thus, Na+ reduction should ALWAYS be integrated into the management of resistant HTN

68
Q

What diuretic is preferred to treat resistant HTN?

A

Chlorthalidone

69
Q

What should be added to Clorthalidone treatment for Resistant HTN?

A

Spironolactone

70
Q

What is the surgical procedure that can be used for resistant HTN?

A

Renal sympathetic denervation

Pharmacology (64 decks)

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