Pharmacology - Antihypertensives and Inotropes Flashcards
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
Can hydralazine be used in pregnancy to treat HTN?
Yes
26
Class: Verapimil and Diltiazem
Anti-arrhythmics AND
| Anti-hypertensives
27
MOA: Verapimil and Diltiazem
Block L-type Ca channels
| **good tropism for the heart
28
Use: Verapimil and Diltiazem
HTN;
Anti-anginal effect (decrease myocardial O2 demand);
SVT (because class IV anti-arrhythmic)
29
Side effects: Verapimil and Diltiazem
```
Edema in legs;
Bradycardia;
AV nodal blockade (bc reduced chronotropy);
Hypotention;
Worsening HF;
Constipation (Ca channels in gut)
```
30
In what conditions are Verapimil and Diltiazem contraindicated?
Decompensated HF;
Bradycardia;
SA dysfunction;
High-degree AV block
**Same contraindications for amlodipine, nifedipine
31
How are verapimil, diltiazem and amlodipine/nifedipine similar?
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
Class: amlodipine, nifedipine
Ca channel blockers
| Anti-hypertensives (dihydropyridine)
33
Use: amlodipine, nifedipine
Hypertension;
Raynaud's;
3rd choice drug for angina (bc they work better in the vasculature than the heart)
34
Side effects: amlodipine, nifedipine
```
leg edema,
HF
AV nodal blockade,
***reflex tachycardia;
constipation;
gingival hyperplasia (like phenytoin)
```
35
What is the role of renin (kidney)?
Catalyzes angiotensinogen --> angiotensin I
36
What is the role of ACE (plasma)?
Catalyzes angiotensin I --> angiotensin II
37
What is the effect of angiotensin II on the adrenal cortex?
Increased aldosterone secretion
38
What is the effect of angiotensin II in the blood vessels?
Vasoconstriction
39
Class: Aliskiren
Renin inhibitor (not very effectve as an antihypertensive)
40
Class: Losartan (and Valsartan, Irbesartan)
Angiotensin II receptor blockers "ARBs"
41
MOA: Losartan (and Valsartan, Irbesartan)
ARBs
| Competitive inhibition of angiotensin II in vascular endothelium
42
Use: Losartan (and Valsartan, Irbesartan)
Drop in peripheral resistance w/o change in HR, CO
| Use in CHF, LV hypertrophy, post-MI
43
Side effects: Losartan (and Valsartan, Irbesartan)
Angioedema
Decreased renal fx;
Hypotension
44
In what conditions are Losartan (and Valsartan, Irbesartan) contraindicated?
Pregnancy;
Renal artery stenosis;
Hyperkalemia;
Prior angioedema
SAME contraindications as ACE inhibitors ie lisinopril, captopril
45
Class: Captopril
ACE-I inhibitor
| short-acting
46
MOA: Captopril
| Lisinopril (Benzapril, Quinapril, Ramipril)
blocks formation of angiotensin II
lowers aldosterone levels
vasodilates
prevents bradykinin degradation
47
Use: Captopril;
| Lisinopril (Benzapril, Quinapril, Ramipril)
CHF;
LV hypertrophy;
post-MI
**prevents remodeling of LV
48
Side effects: Captopril;
| Lisinopril (Benzapril, Quinapril, Ramipril)
dry cough;
***angioedema;
decreased renal fx;
hypotension
49
Class: Lisinopril (Benzapril, Quinapril, Ramipril)
ACE-I inhibitor
| long-acting
50
What is the antihypertensive of choice in a patient with HTN and angina?
```
Beta blockers (ie metoprolol);
Calcium channel blockers (ie diltiazem, amlodipine)
```
51
What is the antihypertensive of choice in a patient with HTN and diabetes?
ACEIs (ie lisinopril)
| ARBs (ie losartan)
52
What is the antihypertensive of choice in a patient with HTN and HF?
ACEIs (ie lisinopril);
ARBs (ie losartan);
Beta blockers (ie metoprolol);
53
What is the antihypertensive of choice in a patient with HTN and is post-MI?
Beta blockers (ie metoprolol);
54
What is the antihypertensive of choice in a patient with HTN and BPH?
Alpha blockers (ie terazosin, doxazosin)
55
What is the antihypertensive of choice in a patient with HTN and dyslipidemias?
Alpha blockers (ie terazosin, doxazosin);
Calcium channel blockers (ie diltiazem, amlodipine);
ACEIs (ie lisinopril);
ARBs (ie losartan)
DO NOT USE beta blockers
56
Captopril is an ACE inhibitor that is first-line therapy for:
CHF
**inhibits LV remodeling
All ACE inhibitors: Captopril, Enalapril, Lisinopril, Ramipril, Quinapril, Fosinopril
are 1st line for CHF tx.
57
Class: Dobutamine
beta 1 agonist
inotrope/chronotrope
**use in acutely decompensated patients only
58
Why is dobutamine indicated for short-term use only?
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
Digoxin is an anti-arrhythmic that is effective therapy for:
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
Why does digoxin have a long half life?
High protein binding
| Large volume of distribution
61
How is digoxin cleared?
Renally
62
An arrhythmia of the conduction accessory pathways defines what syndrome?
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
In the management of Wolff-Parkinson-White Syndrome, NEVER do what?
In the management of Wolff-Parkinson-White Syndrome, NEVER:
Slow AV conduction;
Give digoxin, beta-blockers, Ca channel blockers, or adenosine
64
When are diuretics indicated in the treatment of CHF?
Add-ons for Class III and IV CHF
65
Class: Sprinonolactone (and Epleranone)
Aldosterone antagonist AND K+ sparing diuretic
66
Sprinonolactone (and Epleranone) are diuretics also indicated for what?
Add-ons for Class III and IV CHF
67
Beta blockers, such as:
Bisoprolol, Carvedilol, Metoprolol, are indicated for CHF and dramatically reduce mortality. What is a pearl to remember about their administration?
Do not stop beta-blocker use suddenly.
Titrate slowly, start with a very low dose
68
Patients with HF have increased levels of:
```
NE;
Endothelin;
Cytokines;
Angiotensin II;
Aldosterone;
Vasopression
--all due to lower perfusion of the periphery --> all adversely affect the heart further
```
69
What is the first-line pharmacological choice for treating HF patients
```
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
What is responsible for the side effects of cough in ACE inhibitors?
The prevention of breakdown of bradykinin;
| NOT seen in ARBs
71
What is a significant shared effect of ACE inhibitors and ARBs on the heart?
Both inhibit cardiac and vascular remodeling (ie LV)
72
When should you consider an ARB in a HF patient?
If cough or other side effects of ACE inhibitors are an issue
73
When is it ok to add an ARB to an ACE-I?
If the patient has healthy kidneys and is maxed out on other anti-hypertensives
74
```
Losartan
Irbesartan
Valsartan
Candesartan
Olmesartan
Telmisartan
--all belong to what drug family?
```
ARBs!!
Anti-hypertensives use in HF
Same uses as ACE-I
75
Once you have had angioedema as a side effect of taking an ACE-I, what drug class must you also avoid?
ARBs
| There is some cross-over with this SE, not well understood
76
When using diuretics to reduce volume in CHF patients, what is a dangerous side effect if the diuresis is unmonitored?
Hypovolemia --> ventricular fibrillation
77
Spironolactone carries what unsightly side effect for men?
Gynecomastia
Also, peptic ulcer disease is an issue...but not unsightly
78
What are the only beta blockers indicated for HF?
Carvedilol
Bisoprolol
Sustained-release metoprolol
must start very low and titrate up and down
79
What are the two drugs of choice (IV) indicated for patients who present to the hospital in decompensated HF?
Dobutamine;
| Milrinone
80
MOA: Dobutamine
```
Beta-1 agonist in myocardium;
increases contractility;
increases HR;
--> increases CO
**arrhythmia threshold**
```
81
Would you use dobutamine in a patient who presents with acute MI and is chronically ischemic?
No, bc it's a positive inotrope, and the dobutamine would only increase the demands on the heart.
82
Class: Milrinone
Phosphodiesterase IIIa inhibitor;
| positive inotrope
83
Why are thiazides better than loop diuretics for HTN?
Longer half life;
| Less intense depletion of volume
84
When GFR
Loop diuretics ie furosemide
85
Hypokalemia carries what major risk?
Cardiac arrythmia
86
What diuretics RAISE K+?
Spironolactone
Amilioride
Triamterene
87
T/F: Thiazide diuretics may promote insulin resistance.
True (so can beta blockers in raising serum glucose)
Also promotes gout (uric acid up)
88
To prevent kidney stones, what kind of diuretic would be recommended?
Thiazides
| reduce Ca excreted
89
What is hypoglycemic unawareness?
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
Lower extremity edema is a major side effect of what drugs?
CCBs
ie verapamil
diltiazem
nifedipine
amlodipine
felodipine
isradipine
91
Name the NON-dihydropyridine CCBs.
Verapmil;
Diltiazem
Different from other CCBs because they lower HR
92
Are alpha-blockers indicated for patients with CAD?
NO NO NO
| Alpha blockers worsen CAD and increase mortality.
93
What is the effect of bradykinin in the body?
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.
