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Pharmacology > Vasodilators & Anti-anginal Medications > Flashcards

Vasodilators & Anti-anginal Medications Flashcards

1
Q

What is “sudden, severe, and strangling chest discomfort that can radiate to the left shoulder and along the left arm”?

A

Angina Pectoris

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2
Q

Angina Pectoris

  • Arises when there is a _______ in myocardial blood flow and ____________ in myocardial oxygen demand
  • May be accompanied by ______ changes
A
  • Arises when there is a DECREASE in myocardial blood flow and INCREASE in myocardial oxygen demand
  • May be accompanied by EKG changes
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3
Q

Stable/Classical Angina

  • “angina of ______;” “________ angina”
  • Typically caused by advanced __________
  • Plaque containing cholesterol and lipids obstruct the large ________ vessels
  • Occurs when factors __________ myocardial oxygen demand, such as emotion, exercise, environmental factors such as cold temperatures
A
  • “angina of EFFORT;” “EXERTIONAL angina”
  • Typically caused by advanced ARTHEROSCLEROSIS
  • Plaque containing cholesterol and lipids obstruct the large CORONARY vessels
  • Occurs when factors INCREASE myocardial oxygen demand, such as emotion, exercise, environmental factors such as cold temperatures
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4
Q

Unstable Angina

  • Usually caused by formation and release of __________ from a damaged atherosclerotic plaque
  • Highest risk of _________ and ________
A
  • Usually caused by formation and release of THROMBUS from a damaged atherosclerotic plaque
  • Highest risk of INFARCTION and DEATH
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5
Q 
VASODILATORS - DRUG TARGETS
A) Remember: muscle contraction occurs when \_\_\_\_\_\_\_\_ dependent calcium channels open and calcium enters the cell
B) Inhibition of voltage-dependent calcium channels --> decreased intracellular calcium leads to \_\_\_\_\_\_\_\_\_\_\_\_\_. Drugs like \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ and \_\_\_\_\_\_\_\_\_\_\_ do this.
C) Inhibition of calcium release from endoplasmic reticulum into intracellular space. What 4 drugs do this?
D) Inhibit breakdown of cyclic GMP. What drug class does this?
A

A) Remember: muscle contraction occurs when VOLTAGE dependent calcium channels open and calcium enters the cell
B) Inhibition of voltage-dependent calcium channels –> decreased intracellular calcium leads to VASODILATION. Drugs like CALCIUM CHANNEL BLOCKERS (CCB) and BETA-1 BLOCKERS do this.
C) Inhibition of calcium release from endoplasmic reticulum into intracellular space. 1) ALPHA BLOCKERS, 2) ORGANIC NITRATES, 3) NITRATES, 4) ANGIOTENSIN RECEPTOR BLOCKERS
D) PHOSPHODIESTERASE INHIBITORS

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6
Q

NITRATES

  • Nitric oxide (NO) does exist ____________. ACH (via muscarinic receptors) and bradykinins (via beta receptors) cause endothelial cells on arteries and veins to release nitric oxide
  • Released Nitric Oxide travels through the wall of the blood vessel to reach the _______ muscle cells to initiate response
  • Nitric Oxide binds and activates cytosolic guanylate cyclase, which converts ______ to _________
  • The overall effect of cGMP is to cause smooth muscle ___________ by decreasing intracellular calcium levels. cGMP is degraded by phosphodiesterase inhibitors (PDE) type V
A
  • Nitric oxide (NO) does exist ENDOGENOUSLY. ACH (via muscarinic receptors) and bradykinins (via beta receptors) cause endothelial cells on arteries and veins to release nitric oxide
  • Released Nitric Oxide travels through the wall of the blood vessel to reach the SMOOTH muscle cells to initiate response
  • Nitric Oxide binds and activates cytosolic guanylate cyclase, which converts GTP to cGMP
  • The overall effect of cGMP is to cause smooth muscle RELAXATION by decreasing intracellular calcium levels. cGMP is degraded by phosphodiesterase inhibitors (PDE) type V
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7
Q

What is the mechanism of action (MOA) of Nitroglycerin?

A

Forms nitric oxide which activates guanylate cyclase, which increases cGMP, ultimately causing vascular smooth muscle relaxation

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8
Q

NITROGLYCERIN

  • produces both _______ vasodilation and ______, but the degree of ________ vasodilation is thought to be much more significant. Reduces myocardial demand by decreasing _________
  • Mostly used for ______ (prevention or treatment) and ___________ disease b/c of vasodilation to coronary arteries
A
  • produces both VENOUS vasodilation and ARTERIAL, but the degree of VENOUS vasodilation is thought to be much more significant. Reduces myocardial demand by decreasing PRELOAD
  • Mostly used for ANGINA (prevention or treatment) and CORONARY ARTERY disease b/c of vasodilation to coronary arteries
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9
Q

What are 8 adverse drug reactions of nitroglycerin?

A
  1. Headache
  2. Hypotension
  3. Facial flushing
  4. Bradycardia
  5. Dizziness
  6. Lightheadedness
  7. Syncope
  8. Reflex tachycardia
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10
Q

Nitroglycerin

  • Tolerance can develop within __________ hours of continuous administration, resulting in reduced efficacy and the need for higher doses
  • Always consider a “_______________ period” (10-12 hours) when using chronic management
  • ___________ drug
A
  • Tolerance can develop within 24 - 48 hours of continuous administration, resulting in reduced efficacy and the need for higher doses
  • Always consider a “NITRATE FREE period” (10-12 hours) when using chronic management
  • SYMPTOMATIC drug
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11
Q

What are 5 beneficial effects of vasodilators?

A
  1. Decrease ventricular volume
  2. Decrease arterial pressure
  3. Decrease ejection time
  4. Vasodilation of coronary arteries
  5. Increase blood flow to collateral arteries
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12
Q

What are 3 negative effects of vasodilators?

A
  1. Reflex tachycardia
  2. Reflex increase in cardiac contractility
  3. Decrease in cardiac perfusion related to tachycardia
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13
Q

Vasodilators

  • decreased ventricular volume, arterial pressure, and ejection time all result in decreased _______________ requirements (demand)
A
  • decreased ventricular volume, arterial pressure, and ejection time all result in decreased MYOCARDIAL OXYGEN requirements (demand)
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14
Q

Vasodilators

  • Vasodilation of coronary arteries leads to relief of coronary artery _______
A
  • Vasodilation of coronary arteries leads to relief of coronary artery SPASMS
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15
Q

Vasodilation

- increase in blood flow to collateral arteries leads to improved myocardial ___________ (supply)

A
  • increase in blood flow to collateral arteries leads to improved myocardial PERFUSION (supply)
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16
Q

Vasodilation
- Reflex tachycardia and reflexive increase in cardiac contractility results in increased myocardial _________ requirements

A
  • Reflex tachycardia and reflexive increase in cardiac contractility results in increased myocardial OXYGEN requirements
17
Q

Vasodilation

- Decrease in cardiac perfusion related to tachycardia results in decreased coronary __________

A
  • Decrease in cardiac perfusion related to tachycardia results in decreased coronary PERFUSION
18
Q

Patient Education on Proper use of Sublingual Nitro
When chest pain begins:
1) _____ down
2) Place 1 nitro __________ tab under tongue (or spray x2)
3) Wait _______ minutes –> if no relief, activate EMS
4) Can then take _____ dose
5) If 2nd dose does not provide results, can take _____ dose 5 minutes later. Do NOT exceed three doses total.
*Patients should avoid, at all cost, driving themselves to hospital

A

When chest pain begins:

1) SIT down
2) Place 1 nitro SUBLINGUAL tab under tongue (or spray x2)
3) Wait 2 minutes –> if no relief, activate EMS
4) Can then take SECOND dose
5) If 2nd dose does not provide results, can take THIRD dose 5 minutes later. Do NOT exceed three doses total.
* Patients should avoid, at all cost, driving themselves to hospital

19
Q

Isosorbide Mononitrate (Imdur)

  • A ______ acting nitrate that ultimately results in release of nitric oxide
  • NOT for _____ angina
  • Given __________ for prevention of chest pain
  • Always a concern of nitrate __________
  • Avoid use in patients taking _________________ d/t risk of severe hypotension or MI
A
  • A LONG acting nitrate that ultimately results in release of nitric oxide
  • NOT for ACUTE angina
  • Given CHRONICALLY for prevention of chest pain
  • Always a concern of nitrate TOLERANCE
  • Avoid use in patients taking PHOSPHODIESTERASE INHIBITORS d/t risk of severe hypotension or MI
20
Q

Isosorbide Mononitrate (Imdur)

Adverse Drug Reactions (ADR): similar to nitroglycerin, though maybe not as significant and tolerance to the side effects can develop /c time, except _________

A

Adverse Drug Reactions (ADR): similar to nitroglycerin, though maybe not as significant and tolerance to the side effects can develop /c time, except HYPOTENSION

21
Q

What is the mechanism of action (MOA) for Hydralazine (Apresoline)?

A

not entirely clear, but we do know it is a potent dilator of arteries

22
Q

HYDRALAZINE (PRESOLINE)

- ______ acting, given 3 - 4x/day

A
  • SHORT acting, given 3 - 4x/day
23
Q

What are 4 uses for Hydralazine (Apresoline)?

A
  1. Hypertension (as adjunct therapy)
  2. Acute Hypertension
  3. Pre-elampsia in pregnant women for BP control
  4. Heart Failure (reduced mortality in African Americans when combined /c nitrate)
24
Q

What are 4 adverse drug reactions of Hydralazine (Apresoline)?

A
  1. Hypotension
  2. Peripheral Edema
  3. Tachycardia
  4. Lupus-like condition
25
Q

RANOLZINE (RANEXA)

- What is the mechanism of action?

A

Inhibits sodium channel during cardiac repolarization. End result is a reduction in calcium concentrations

26
Q

RANOLZINE (RANEXA)

  • Used for ______ management (prevention) of chest pain
  • Contraindicated /c any degrees of _______ impairment. Extensively metabolized in the gut and liver
  • Also contraindicated /c strong _________ inhibitors (metabolized by CYP3A4
  • Benefit is thought to be /c its lack of effect on _______ and ________ (no tachycardia, no hypotension)
  • Expensive
A
  • Used for CHRONIC management (prevention) of chest pain
  • Contraindicated /c any degrees of HEPATIC impairment. Extensively metabolized in the gut and liver
  • Also contraindicated /c strong CYP3A4 inhibitors (metabolized by CYP3A4
  • Benefit is thought to be /c its lack of effect on BP and HR (no tachycardia, no hypotension)
  • Expensive
27
Q

RANOLZINE (RANEXA)

- What are 4 adverse drug reactions?

A
  1. headache (minimal)
  2. Dizziness (minimal)
  3. Constipation
  4. Increases QT interval
28
Q

When do you use Ranolazine (Ranexa)?

A

After first trying calcium-channel blockers, beta-blockers, and nitrates

29
Q

SILDENAFIL (VIAGRA, REVATIO)

  • Phosphodiesterase (PDE) inhibitors (increase ______ availability)
  • Takes 60 minutes for onset, 2 -4 hour duration of action
  • Used for ______ dysfunction and ______________ hypertension
  • Always caution /c patients taking any other ________
A
  • Phosphodiesterase (PDE) inhibitors (increase cGMP availability)
  • Takes 60 minutes for onset, 2 -4 hour duration of action
  • Used for ERECTILE dysfunction and PULMONARY ARTERY hypertension
  • Always caution /c patients taking any other VASODILATOR
30
Q

SILDENAFIL (VIAGRA, REVATIO)

- What are 5 adverse drug reactions?

A
  1. Headache
  2. Flushing
  3. Hypotension (high doses)
  4. Priapism (A prolonged erection of the penis, usually without sexual arousal)
  5. Visual Disturbances (i.e. blue vision @ high doses)
31
Q

Where is PDE -5 located?

A

penis and pulmonary vasculature

32
Q

Where is PDE - 6 located?

A

retina

33
Q

Where is PDE-3 located?

A

smooth muscle vasculature

34
Q

TADALAFIL (CIALIS, ADCIRCA)

  • Used for ______ dysfunction, _____________ hypertension, and ________________ hyperplasia
  • Must adjust dose for ________ and ______ impairment
  • Onset of action = _______ minutes
  • Duration of action = ________ (the “weekender”)
A
  • Used for ERECTILE dysfunction, PULMONARY ARTERY hypertension, and BENIGN PROSTATE hyperplasia
  • Must adjust dose for RENAL and HEPATIC impairment
  • Onset of action = 60 minutes
  • Duration of action = 36 (the “weekender”)
35
Q

VARDENAFIL (LEVITRA)

  • only indicated for ________ dysfunction
  • onset of activity is _______ minutes
A
  • only indicated for ERECTILE dysfunction

- onset of activity is 30 - 60 minutes

36
Q

AVANAFIL (STENDRA)

- advantage _____ min onset

A
  • advantage 30 min onset

Pharmacology (10 decks)

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