Pharmacology - Antihypertensives and Inotropes Flashcards Preview

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Flashcards in Pharmacology - Antihypertensives and Inotropes Deck (93)
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1
Q

Class: Clonidine

A

alpha-2 agonist

Anti-hypertensive

2
Q

Class: Methyldopa

A

alpha-2 agonist

Anti-hypertensive

3
Q

What is the effect of alpha-2 stimulation, as caused by drugs like clonidine and methyldopa?

A

Decrease in sympathetic outflow;

Decrease in TPR and HR (because lowers NE, therefore indirect effects to lower alpha 1 and beta 1 effects)

4
Q

Use:
Clonidine
Methyldopa

A

Mild to moderate HTN

*use methyldopa for HTN in pregnancy

5
Q

Unique application: Clonidine

A

Opiate withdrawal

6
Q

Side effects:
Clonidine
Methyldopa

A

Rebound HTN is stopped abruptly;
edema
CNS depression

7
Q

Class: Reserpine

A

Ganglion-blocking agent

Anti-hypertensive

8
Q

MOA: Reserpine

A

Destroys vesicles for NE, dopamine, serotinin

9
Q

Use: Reserpine

A

Not used anymore bc of SE (suicide);

Decreases CO and systemic vascular resistance

10
Q

What is a common side effect of antihypertensives and why?

A

Edema

Bc lower BP –> activate renin-angiotensin system

11
Q

Class: Doxazosin (Prazosin and Terazosin also…)

A

alpha-1 blockers

12
Q

Use: Doxazosin (Prazosin and Terazosin also…)

A

Decreases arteriolar and venous resistance –> causes reflex tachycardia;
BPH (decrease tone or urinary sphincter);
Second-tier medication for HTN, use when other conditions exits

13
Q

What re the only class of anti-hypertensives associated with reflex tachycardia?

A

Alpha-1 blockers (causes worsening of angina)

14
Q

Side effects: Doxazosin (Prazosin and Terazosin also…)

A

Orthostatic hypotension (bc venous resistance down), “first-dose syncope”;
edema;
worsening angina due to reflex tachycardia

15
Q

Class: Esmolol

A

Beta-1 selective blocker

16
Q

Use: Esmolol

A

AV nodal blockade in unstable pts

17
Q

Esmolol is know for having what characteristic?

A

Beta-1 selective blocker;

Short half-life

18
Q

Class: Hydralazine

A

Direct-acting vasodilator

Anti-hypertensive

19
Q

Class: Minoxidil

A

Direct-acting vasodilator

Anti-hypertensive

20
Q

MOA:
Hydralazine
Minoxidil

A

Decreases TPR via arteriolar dilation
Hydralazine - acts through NO
Minozidil - opens K channels

21
Q

Use: Hydralazine

A

Moderate to severe HTN;

patients with both advanced CHF and hypertension

22
Q

What is a unique side effect of hydralazine?

A

Can cause drug-induced SLE

23
Q

Use: Minoxidil

A

Hair loss;

Refractory HTN

24
Q

Side Effects: Hydralazine

A

Reflex tachycardia;
Edema;
Drug-induced SLE (high protein binding)

25
Q

Can hydralazine be used in pregnancy to treat HTN?

A

Yes

26
Q

Class: Verapimil and Diltiazem

A

Anti-arrhythmics AND

Anti-hypertensives

27
Q

MOA: Verapimil and Diltiazem

A

Block L-type Ca channels

**good tropism for the heart

28
Q

Use: Verapimil and Diltiazem

A

HTN;
Anti-anginal effect (decrease myocardial O2 demand);
SVT (because class IV anti-arrhythmic)

29
Q

Side effects: Verapimil and Diltiazem

A
Edema in legs;
Bradycardia;
AV nodal blockade (bc reduced chronotropy);
Hypotention;
Worsening HF;
Constipation (Ca channels in gut)
30
Q

In what conditions are Verapimil and Diltiazem contraindicated?

A

Decompensated HF;
Bradycardia;
SA dysfunction;
High-degree AV block

**Same contraindications for amlodipine, nifedipine

31
Q

How are verapimil, diltiazem and amlodipine/nifedipine similar?

A

They are all Ca channel blockers. They exist on a spectrum based on their tropism. Verapimil has the most cardioselectivity (non-dihydropyridine) –> Diltiazem –> Amlodipine and Nifedipine (dihydropyridine). The latter two have tropism for blood vessels

32
Q

Class: amlodipine, nifedipine

A

Ca channel blockers

Anti-hypertensives (dihydropyridine)

33
Q

Use: amlodipine, nifedipine

A

Hypertension;
Raynaud’s;
3rd choice drug for angina (bc they work better in the vasculature than the heart)

34
Q

Side effects: amlodipine, nifedipine

A
leg edema,
HF
AV nodal blockade,
***reflex tachycardia;
constipation;
gingival hyperplasia (like phenytoin)
35
Q

What is the role of renin (kidney)?

A

Catalyzes angiotensinogen –> angiotensin I

36
Q

What is the role of ACE (plasma)?

A

Catalyzes angiotensin I –> angiotensin II

37
Q

What is the effect of angiotensin II on the adrenal cortex?

A

Increased aldosterone secretion

38
Q

What is the effect of angiotensin II in the blood vessels?

A

Vasoconstriction

39
Q

Class: Aliskiren

A

Renin inhibitor (not very effectve as an antihypertensive)

40
Q

Class: Losartan (and Valsartan, Irbesartan)

A

Angiotensin II receptor blockers “ARBs”

41
Q

MOA: Losartan (and Valsartan, Irbesartan)

A

ARBs

Competitive inhibition of angiotensin II in vascular endothelium

42
Q

Use: Losartan (and Valsartan, Irbesartan)

A

Drop in peripheral resistance w/o change in HR, CO

Use in CHF, LV hypertrophy, post-MI

43
Q

Side effects: Losartan (and Valsartan, Irbesartan)

A

Angioedema
Decreased renal fx;
Hypotension

44
Q

In what conditions are Losartan (and Valsartan, Irbesartan) contraindicated?

A

Pregnancy;
Renal artery stenosis;
Hyperkalemia;
Prior angioedema

SAME contraindications as ACE inhibitors ie lisinopril, captopril

45
Q

Class: Captopril

A

ACE-I inhibitor

short-acting

46
Q

MOA: Captopril

Lisinopril (Benzapril, Quinapril, Ramipril)

A

blocks formation of angiotensin II
lowers aldosterone levels
vasodilates
prevents bradykinin degradation

47
Q

Use: Captopril;

Lisinopril (Benzapril, Quinapril, Ramipril)

A

CHF;
LV hypertrophy;
post-MI
**prevents remodeling of LV

48
Q

Side effects: Captopril;

Lisinopril (Benzapril, Quinapril, Ramipril)

A

dry cough;
***angioedema;
decreased renal fx;
hypotension

49
Q

Class: Lisinopril (Benzapril, Quinapril, Ramipril)

A

ACE-I inhibitor

long-acting

50
Q

What is the antihypertensive of choice in a patient with HTN and angina?

A
Beta blockers (ie metoprolol);
Calcium channel blockers (ie diltiazem, amlodipine)
51
Q

What is the antihypertensive of choice in a patient with HTN and diabetes?

A

ACEIs (ie lisinopril)

ARBs (ie losartan)

52
Q

What is the antihypertensive of choice in a patient with HTN and HF?

A

ACEIs (ie lisinopril);
ARBs (ie losartan);
Beta blockers (ie metoprolol);

53
Q

What is the antihypertensive of choice in a patient with HTN and is post-MI?

A

Beta blockers (ie metoprolol);

54
Q

What is the antihypertensive of choice in a patient with HTN and BPH?

A

Alpha blockers (ie terazosin, doxazosin)

55
Q

What is the antihypertensive of choice in a patient with HTN and dyslipidemias?

A

Alpha blockers (ie terazosin, doxazosin);
Calcium channel blockers (ie diltiazem, amlodipine);
ACEIs (ie lisinopril);
ARBs (ie losartan)

DO NOT USE beta blockers

56
Q

Captopril is an ACE inhibitor that is first-line therapy for:

A

CHF
**inhibits LV remodeling

All ACE inhibitors: Captopril, Enalapril, Lisinopril, Ramipril, Quinapril, Fosinopril
are 1st line for CHF tx.

57
Q

Class: Dobutamine

A

beta 1 agonist
inotrope/chronotrope

**use in acutely decompensated patients only

58
Q

Why is dobutamine indicated for short-term use only?

A

The effect of a beta-1 agonist such as dobutamine is beta-1 receptor insensitivity over time. Need a longer-term solution for CHF patients.

59
Q

Digoxin is an anti-arrhythmic that is effective therapy for:

A

CHF; good for SVTs
increases vagal activity (indirect effect) to the heart;
inhibits Na/K ATPase;
reduces SA firing rate and conduction through AV node;
increases contractility
improves LV fx

60
Q

Why does digoxin have a long half life?

A

High protein binding

Large volume of distribution

61
Q

How is digoxin cleared?

A

Renally

62
Q

An arrhythmia of the conduction accessory pathways defines what syndrome?

A

Wolff-Parkinson-White Syndrome

SA node –> direct to ventricles (AV node might not be depolarized yet)

Treat either with surgery–lasar ablation or drugs (class IA such as quinidine or class III)

63
Q

In the management of Wolff-Parkinson-White Syndrome, NEVER do what?

A

In the management of Wolff-Parkinson-White Syndrome, NEVER:
Slow AV conduction;
Give digoxin, beta-blockers, Ca channel blockers, or adenosine

64
Q

When are diuretics indicated in the treatment of CHF?

A

Add-ons for Class III and IV CHF

65
Q

Class: Sprinonolactone (and Epleranone)

A

Aldosterone antagonist AND K+ sparing diuretic

66
Q

Sprinonolactone (and Epleranone) are diuretics also indicated for what?

A

Add-ons for Class III and IV CHF

67
Q

Beta blockers, such as:
Bisoprolol, Carvedilol, Metoprolol, are indicated for CHF and dramatically reduce mortality. What is a pearl to remember about their administration?

A

Do not stop beta-blocker use suddenly.

Titrate slowly, start with a very low dose

68
Q

Patients with HF have increased levels of:

A
NE;
Endothelin;
Cytokines;
Angiotensin II;
Aldosterone;
Vasopression
--all due to lower perfusion of the periphery --> all adversely affect the heart further
69
Q

What is the first-line pharmacological choice for treating HF patients

A
ACE-I
ie lisinopril
benazepril
quinapril
ramipril
captopril (shorter acting)
enalapril

can increase CO without increases in HR or contractility;
benefits seen in patients with mild, moderate and severe HF

70
Q

What is responsible for the side effects of cough in ACE inhibitors?

A

The prevention of breakdown of bradykinin;

NOT seen in ARBs

71
Q

What is a significant shared effect of ACE inhibitors and ARBs on the heart?

A

Both inhibit cardiac and vascular remodeling (ie LV)

72
Q

When should you consider an ARB in a HF patient?

A

If cough or other side effects of ACE inhibitors are an issue

73
Q

When is it ok to add an ARB to an ACE-I?

A

If the patient has healthy kidneys and is maxed out on other anti-hypertensives

74
Q
Losartan
Irbesartan
Valsartan
Candesartan
Olmesartan
Telmisartan
--all belong to what drug family?
A

ARBs!!
Anti-hypertensives use in HF
Same uses as ACE-I

75
Q

Once you have had angioedema as a side effect of taking an ACE-I, what drug class must you also avoid?

A

ARBs

There is some cross-over with this SE, not well understood

76
Q

When using diuretics to reduce volume in CHF patients, what is a dangerous side effect if the diuresis is unmonitored?

A

Hypovolemia –> ventricular fibrillation

77
Q

Spironolactone carries what unsightly side effect for men?

A

Gynecomastia

Also, peptic ulcer disease is an issue…but not unsightly

78
Q

What are the only beta blockers indicated for HF?

A

Carvedilol
Bisoprolol
Sustained-release metoprolol

must start very low and titrate up and down

79
Q

What are the two drugs of choice (IV) indicated for patients who present to the hospital in decompensated HF?

A

Dobutamine;

Milrinone

80
Q

MOA: Dobutamine

A
Beta-1 agonist in myocardium;
increases contractility;
increases HR;
--> increases CO
**arrhythmia threshold**
81
Q

Would you use dobutamine in a patient who presents with acute MI and is chronically ischemic?

A

No, bc it’s a positive inotrope, and the dobutamine would only increase the demands on the heart.

82
Q

Class: Milrinone

A

Phosphodiesterase IIIa inhibitor;

positive inotrope

83
Q

Why are thiazides better than loop diuretics for HTN?

A

Longer half life;

Less intense depletion of volume

84
Q

When GFR

A

Loop diuretics ie furosemide

85
Q

Hypokalemia carries what major risk?

A

Cardiac arrythmia

86
Q

What diuretics RAISE K+?

A

Spironolactone
Amilioride
Triamterene

87
Q

T/F: Thiazide diuretics may promote insulin resistance.

A

True (so can beta blockers in raising serum glucose)

Also promotes gout (uric acid up)

88
Q

To prevent kidney stones, what kind of diuretic would be recommended?

A

Thiazides

reduce Ca excreted

89
Q

What is hypoglycemic unawareness?

A

Beta blocker use in diabetics can blunt the catecholamine response, when patients “sense” their blood sugar is low - cause for caution when using beta blockers in diabetics

90
Q

Lower extremity edema is a major side effect of what drugs?

A

CCBs
ie verapamil
diltiazem

nifedipine
amlodipine
felodipine
isradipine

91
Q

Name the NON-dihydropyridine CCBs.

A

Verapmil;
Diltiazem
Different from other CCBs because they lower HR

92
Q

Are alpha-blockers indicated for patients with CAD?

A

NO NO NO

Alpha blockers worsen CAD and increase mortality.

93
Q

What is the effect of bradykinin in the body?

A

It is a vasodilator. ACE inhibitors, by preserving extra bradykinin, are thought to have added value as antihypertensives, in addition to their inhibition of angiotensin I conversion to angiotensin II.