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D&T3 Cardiology > Vasodilators > Flashcards

Vasodilators Flashcards

1
Q

Describe the general mechanism of vasodilators (in regards to arterial and venous)?

A

Arteriodilation –> Decreased TPR –> Decreased BP

Venodilation –> Decreased CO –> Decreased BP

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2
Q

What is the normal physiological response to decreased BP?

A
  1. Increase Sympathetic Activity –> Increased CO and PR –> Increased BP
  2. Increase Renin –> AII –> Increased Aldo –> Increased Na+ and H2O –> Increased Blood Volume –> Increased BP
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3
Q

Angiotensin II stimulated what?

A

Aldosterone and NE

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4
Q

What are the classes of Vasodilators?

A
  1. Ca Channel Blockers
  2. K Channel Openers
  3. Guanyly Cyclase Activators
  4. Phosphodiesterase Inhibitors
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5
Q

What are the Ca Channel Blocker drugs?

A
  1. Dihydropyridines
    • Amlodipine
    • Other drugs ending in pine
  2. Non-Dihydropyridines
    • Verapamil
    • Diltiazem
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6
Q

What is the MOA of Ca Channel Blockers?

A

Decrease Ca++ Influx through L-Type Ca++ Channels

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7
Q

What are the vascular and cardiac effects of Ca Channel Blockers?

A
  1. Arteriodilation –> Decreased TPR –> Decreased BP
  2. Inhibition of Phase 2 of AP in Cardiac Muscle Cells (Decreased Ca++ available for contraction in the heart musculature)
  3. Inhibition of Phase 0 of AP in SA and AV nodes (results in slower HR due to SA and decreased conduction due to AV block)
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8
Q

What is the order of effectiveness of the Ca Channel Blockers in terms of CARDIAC effects?

A

Verapamil > Diltiazem > DHPs (Amlodipine)

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9
Q

Which Ca Channel Blocker has the most potent vascular effect?

A

Amlodipines (And other DHPs)

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10
Q

Describe the metabolism of Ca Channel Blockers?

A

Hepatic Metabolism

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11
Q

Describe the pharmacokinetics of Ca Channel Blockers

A
  1. Effective orally

2. qd (1/day) or bid dosing

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12
Q

What are the therapeutic uses of Ca Channel Blockers?

A
  1. Angina
  2. Supraventricular Tachyarrhythmias
  3. HTN
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13
Q

How do Ca Channels work to treat Angina?

A
  1. Increase Coronary Blood Flow
  2. Decrease Myocardial Oxygen Consumption
    - Decrease Afterload
    - Decrease CO (Verapamil and Diltiazem)
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14
Q

How do Ca Channels work to treat Supraventricular Tachyarrhythmias?

A
  1. Decrease AV Nodal Conduction (Verapamil) and control rate in A flutter and fib
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15
Q

How do Ca Channel Blockers work to treat HTN?

A
  1. Decrease TPR
  2. Decrease CO (Verapamil and Diltiazem)
    * *The decrease in BP only results in mild increase in HR b/c these drugs have effects on the heart
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16
Q

What are common adverse effects of Ca Channel Blockers?

A
  1. Hypotension (worse with DHPs)
  2. CHF
  3. AV Block (Not with DHPs)
  4. Edema (Worse with DHPs)
  5. Headaches
  6. Constipation (Verapamil only)
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17
Q

What are the contraindications and precautions of Ca Channel Blockers?

A
  1. Avoid Short Acting Agents
  2. Severe Hepatic Dysfxn
  3. LV Dysfxn (Verapamil and Diltiazem)
  4. Hypotension
  5. AV Block (Verapamil and Diltiazem)
  6. Sick Sinus Syndrome (Verapamil and Diltiazem)
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18
Q

With which drugs do Ca Channel Blockers have interactions?

A
  1. CYP3A4 Inhibitors
  2. B Blockers (Verapamil and Diltiazem)
  3. Digoxin (Verapamil)
  4. Antiarrhythmic Drugs
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19
Q

Which drug is a K Channel opener?

A

Minoxidil

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20
Q

What is the MOA of Minoxidil?

A

Increase K+ efflux from vascular smooth muscle –> hyper polarization –> relaxation –> Decreased TPR

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21
Q

What are the effects of K Channel Openers?

A
  1. Potent Arterial Vasodilation –> Decreased TPR

* *Severe compensatory responses (Increases HR, CO and Fluid Retention)

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22
Q

What is Minoxidil used for?

A

Treatment of refractory/malignant HTN

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23
Q

What are the side effects of Minoxidil?

A
  1. Fluid Retention (treat w/ loop)
  2. Tachy (give B-blocker)
  3. Hypertrichosis
  4. Pericardial Effusion/ Cardiac Tamponade
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24
Q

What is the MOA of Guanylyl Cyclase Activators?

A

Activation of Guanylyl Cyclase –> Increased cGMP –> Vasodilation

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25
What are the 3 Classes of Guanylyl Cyclase Activators?
1. Nitroprusside 2. Organic Nitrates 3. Hydralazine
26
What are the effects of Nitroprusside?
1. Arteriodilation (decreased TPR) 2. Venodilation (decreased CO) 3. Increase HR (due to reflex from decreasing BP)
27
Describe the kinetics of Nitroprusside
Unstable, with a t1/2 of minutes; IV only
28
What are the Therapeutic Uses of Nitroprusside?
1. Hypertensive Emergencies 2. Acute CHF 3. MI
29
What is the side effect of chronic Nitroprusside?
Thiocyanate/Cyanide Toxicity
30
How is Cyanide from the breakdown of Nitroprusside converted to the less toxic Thiocyanate?
Rhodanase enzyme couples the cyanide with Thiosulfate
31
What are the symptoms of Thiocyanate Toxicity?
1. Weakness 2. Nausea 3. Disorientation 4. Delerium
32
What are the symptoms of Cyanide toxicity?
1. Anoxia 2. Hypoxia 3. Convulsions 4. Respiratory Arrest
33
Which Guanylyl Cyclase inhibiting drugs are classified as Organic Nitrates?
1. Nitroglycerin | 2. Isosorbide Dinitrate (longer acting)
34
What are the effects of Organic Nitrates?
Venodilation >>> Arteriodilation
35
What effect is seen with low doses of Organic Nitrates?
1. Venodilation (decreased LVEDV --> decreased SV --> decreased CO) 2. Reflex causes increased HR and TPR 3. Mild effect on BP
36
What effects are seen with high doses of Organic Nitrates?
1. Venodilation 2. Arteriodilation 3. Increased HR (reflex) * *Decreased CO, TPR and BP; Increased HR
37
Where are Organic Nitrates metabolized?
Liver; via glutathione-organic nitrate reductase
38
Which drugs have extensive first pass elimination and must be given sublingually, transdermally or via IV?
Organic Nitrates
39
What are the therapeutic uses of Organic Nitrates?
1. Angina 2. CHF ** (use with Hydralizine) 3. Acute MI
40
What are the adverse effects of Organic Nitrates?
1. Excessive Hypotension (HA, tachy, orthostatic hypotension and angina) 2. Tolerance
41
Poorly perfused coronary vessels result in what condition?
Angina
42
What is the therapeutic use of NO?
Hypoxic respiratory failure in neonates with pulmonary hypertension
43
What are the adverse effects of NO?
1. Pulmonary Edema (due to NO2 formation) | 2. Hypoxemia upon sudden withdrawal
44
What is the effect of Hydralazine?
1. Arterial Dilation --> decreased TPR and BP; Increased HR
45
How is Hydralazine administered?
Orally
46
What is the therapeutic use of Hydralazine?
1. CHF **(good if used with ISDN) | 2. Hypertension
47
What are the side effects of Hyrdralazine?
1. Fluid Retention 2. Tachy 3. +ANA --> Lupus like syndrome
48
Describe the features of the Lupus Like Syndrome caused by Hydralazine
1. Seen in slow acetylators 2. No renal involvement 3. Reversible 4. Occurs at HIGH doses
49
What is Fenoldopam?
A rapid acting IV D1-Receptor Agonist that causes peripheral vasodilation
50
What is the therapeutic use of Fenoldopam?
Hypertensive Emergencies
51
What are the adverse effects of Fenoldopam?
1. Hypersensitivity 2. Tachy 3. Hypotension
52
What are the PDE Inhibitor Drugs?
1. Sildenafil 2. Tadalafil 3. Vardenafil
53
What is the MOA of Sildenafil, Tadalafil and Vardenafil?
Inhibit PDE Type 5 --> increased effect of NO --> Increased cGMP --> relaxed muscle in corpus cavernous --> erection and --> relaxed muscle in the lower UT --> urination
54
What is the therapeutic use of the PDE inhibitors?
1. Tx of ED | 2. Tx of BPH (Tadalafil)
55
Describe the kinetics of the PDE Inhibitors
1. Given orally | 2. Hepatic Metabolism
56
What are the side effects of PDE Inhibitors?
1. Hypotension - Contraindications: 1. Use of Organic Nitrates 2. Use of alpha-blockers 3. CYP3A4 interacting drugs
57
What are the effects of Angiotensin II?
1. Vasoconstriction 2. Increased Aldosterone Secretion --> Na retention 3. Vascular remodeling
58
The net effect of the RAA system is what?
Increasing TPR and BP
59
In addition to converting Angiotensin I --> II, what is the converting enzyme involved in?
The breakdown of Bradykinin into inactive products | **More Bradykinin --> Increased PG synthesis --> Cough
60
Dry Cough is associated with what medication?
ACE Inhibitors
61
What is the MOA of ACE Inhibitors?
Inhibit ACE --> decreased Angiotensin II formation --> decreased Aldo, vasoconstriction, NE, and cardiac remodeling; Increased Bradykinin and PGs
62
What is the net effect of ACE Inhibitors?
1. Decreased TPR 2. Decreased Na+ and Fluid Retention 3. Decreased BP 4. Slightly elevated HR
63
What are the ACE Inhibitor Drugs?
1. Enalapril 2. Lisinopril 3. "pril" drugs
64
Which class of drugs are predominantly prodrugs? What are the exceptions?
ACE Inhibitors | -Exception- Lisinopril and Captopril
65
Which ACE Inhibitor is metabolized in the liver prior to renal excretion?
Fosinopril
66
What are the Therapeutic Uses of ACE Inhibitors?
1. HTN 2. CHF 3. Post MI 4. Diabetic Nephropathy
67
What are the side effects of ACE Inhibitors?
1. Fetopathic Potential 2. Cough 3. Hyperkalemia 4. Renal Failure 5. Hypotension 6. Hypersensitivity
68
What are the contraindications and precautions of using ACE Inhibitors?
1. Pregnancy 2. Bilateraly Renal Artery Stenosis 3. Hyperkalemia 4. Hypersensitivity
69
ACE Inhibitors are contraindicated in hyperkalemia, so which conditions would not permit ACE Inhibitor use?
1. Renal Disease 2. Use of K+ Sparing Diuretics 3. K+ Supplementation
70
What are the Angiotensin II "AT" Receptor Antagonists?
1. Losartan 2. Valsartan 3. "Sartan Drugs"
71
What is the MOA of AT Receptor Antagonists?
MOA- competitive antagonism at AT1 Receptors | --> decreased Aldo, vasoconstriction, NE and remodeling
72
What are the net effects of AT Receptor Antagonists?
1. Decreased TPR 2. Decreased Na+ and Fluid Retention 3. Decreased BP
73
What are the therapeutic uses of AT Receptor Antagonists?
1. HTN 2. CHF 3. Post MI 4. Diabetes
74
What are the adverse effects of AT receptor Antagonists?
1. Fetopathic Potential 2. Hyperkalemia 3. Hypotension 4. Hypersensitivity
75
What are the contraindications to use of AT Receptor Antagonists?
1. Pregnancy 2. Renal Artery Stenosis 3. K+ Diuretics 4. K+ Supplements 5. Hypersensitivity
76
What drug is an inhibitor of Renin?
Aliskiren
77
What is the use of Aliskiren?
HTN
78
What are the general uses of vasodilators and RAA System Inhibitors?
1. HTN 2. Angina and Ischemia 3. CHF

D&T3 Cardiology (7 decks)

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