Pharm Anti-Anginal Agents Linger Flashcards Preview

Cardiovascular II Exam 3 > Pharm Anti-Anginal Agents Linger > Flashcards

Flashcards in Pharm Anti-Anginal Agents Linger Deck (55):
1

4 common β-Adrenergic Antagonists (β-Blockers) from the list

Atenolol Metoprolol Propranolol Timolol

2

Name the 3 Organic Nitrates

Nitroglycerin Isosorbide dinitrate Isosorbide mononitrate

3

Name the 2 sub-classes of Calcium Channel Blockers (CCBs)

Dihydropyridines (DHPs) Non-dihydropyridines

4

Name the Dihydropyridines (DHPs)

Amlodipine Felodipine Nicardipine

5

Name the Non-dihydropyridines

Diltiazem Verapamil

6

What is the primary symptom of ischemic heart disease?

Angina Pectoris

7

What are the types of Angina?

Effort angina Variant angina Unstable angina

8

What is effort angina?

Increased myocardial O2 demand (exercise) exceeds coronary flow abilities

9

What is variant angina?

Pain due to coronary artery vaso spasm (Prinzmetal's angina)

10

What is unstable angina?

Chest pain at rest, typically a progression from effort angina.

11

Agents that decrease O2 demand

ß adrenergic antagonist, Ca entry blockers, organic nitrates,

12

Agents that increase O2 supply

Vasodilators, statins, anti-thrombotics

13

Nitrates and nitrites MOA

metabolized to NO which Increase cGMP

 

14

Which Ca blockers are cardio specific

Non-DHPs (Verapamil > diltiazem > DHPs)

15

Non-DHPs physiologic effect

decrease rate and contractility in cardiac myocytes

16

Organic nitrates prototype?

nitroglycerin (NTG)

17

NTG formulation?

  1. Sublingual tablet
  2. spray
  3. Sustained release oral capsules
  4. Buccal tablets
  5. gel Ointment
  6. Transdermal patch

18

NTG preferentially dilates which vessels?

Large veins

19

How does NTG relieve angina?

Primary antiischemic effect is to decrease myocardial O2 demand by producing systemic vasodilation (more so than coronary vasodilation)

20

First-line therapy for an acute anginal attack?

NTG typically sublingual administration, spray equally effective

21

NTG formulations that improve exercise tolerance and time to onset of angina?

Long-acting oral and transdermal formulations

22

NTG improves antianginal and antiischemic effects of?

beta blockers and calcium channels blockers

23

NTG Long-term utility is limited by?

tolerance

24

NTG tolerance is not a problem with which formulation? 

Generally not a problem with sublingual nitroglycerin

25

How to prevent nitrate tolerance?

Intermittent therapy with a nitrate-free interval of at least 8 hours may prevent tolerance

26

Nitrates: Adverse Effects

Common: orthostatic hypotension, syncope, throbbing headache, flushing

27

NTG Drug-drug interaction?

synergistic hypotension with phosphodiesterase type 5 (PDE5) inhibitors (e.g., sildenafil, tadalafil, vardenafil) Think viagra.

Can lead to myocardial infarction and death

28

ß blockers list the non-selective

Propranolol

Carteolol

Nadolol

Penbutolol

Timolol

Pindolol

29

Cardioselective ß blocker

Metoprolol

Acebutolol

Atenolol

Nebivolol

Esmolol

Bisoprolol

Betaxolol

 

30

Combined alpha beta blockers

Labetalol

Carvedilol

31

Beta Blockers: Pharmacodynamics

Reduce cardiac work (i.e., O2 consumption) by decreasing heart rate and contractility

Most are not vasodilators; no effect on O2 supply

32

Beta Blocker Use in Angina prototype

Propranolol

33

First-line therapy to reduce frequency of angina (i.e., prophylaxis) and improve exercise tolerance

Propranolol

34

Propranolol Reduce O2 requirement by?

reducing heart rate and contractility

35

ß blocker NOT effective in_____ angina.

variant

36

All types of ß blockers are equally effective in _______ angina; _______ often preferred

exertional

cardioselective (β1-selective)

37

Beta Blockers that Prolong Survival After MI

Timolol, propranolol, and metoprolol have been specifically studied in large-scale clinical trials

Use of other beta-blockers for this indication is less compelling

38

Why are ß blockers used in conjunction with ACE inhibitors for Tx of CHF

Combined effect on mortality is increased over using either alone

39

Beta Blockers Adverse Effects?

Most common: bradycardia and fatigue

40

ß blocker Relative contraindications

Asthma/COPD

Diabetes

Variant angina

Acute decompensated heart failure

41

ß blocker Can cause heart block, especially if combined with

other negative inotropes (e.g., verapamil, diltiazem)

42

Calcium Channel Blockers (CCBs) bind to?

L-type Ca++ channels

But the two classes bind to different sites, resulting in different effects on vascular versus cardiac tissue.

Non-dihydropyridines:

Prominent cardiac effects, but also act at vascular tissues

Verapamil > Diltiazem

Dihydropyridines (DHPs):

Predominantly arteriolar vasodilation effects

Amlodipine, Clevidipine, Felodipine, Isradipine, Nicardipine, Nifedipine, Nisoldipine

43

Pharmacokinetic Properties of CCBs

Good oral absorption but high 1st pass effect

Amlodipine, felodipine, isradipine slowly absorbed, long t1/2 is advantage

DHPs with long plasma half-lives preferred to minimize reflex cardiac effects; extended release preparations available

Nifedipine, clevidipine, verapamil, and diltiazem sometimes used IV

44

CCBs: Pharmacodynamics

Relaxation of vascular smooth muscle causes peripheral vasodilation

Arterioles are more sensitive than veins

Reduce afterload and decrease O2 demand

Little effect on preload

Also increase O2 supply due to dilation of coronaries

45

vasodilator that is most effective on 

1. large veins

2. arterioles 

1. organic nitrates

2. Ca channel blockers

46

Calcium Channel Blocker Use in Angina

Preferred agents: diltiazem, verapamil, amlodopine, or felodipine

Added to or substituted for beta blockers in chronic stable angina

Also effective in vasospastic angina

Reduce O2 requirement by reducing heart rate and contractility

Increase O2 delivery by vasodilation and reversal of vasospasm

47

CCBs: Adverse Effects & Toxicity

Generally very well tolerated

Excessive vasodilation – dizziness, hypotension, headache, flushing, nausea; diminished by long-acting formulations and long half-life agents

Constipation (esp., verapamil), peripheral edema, coughing, wheezing, pulmonary edema

Use of verapamil/diltiazem with  a β-blocker is contraindicated because of the potential for AV block

Verapamil/diltiazem should not be used in patients with ventricular dysfunction, SA or AV nodal conduction defects and systolic BP< 90 mmHg

Short-acting dihydropyridines can cause reflex tachycardia

48

According to board exams constipation is always caused by?  

verapamil

49

Relatively newer antianginal drug with a MOA: late sodium channel blocker

Ranolazine

Typically reserved for angina that is refractory to treatment with beta blockers, calcium channel blockers, and nitrates

Used either in combination with beta blocker or as a substitute in patients who cannot receive beta blockers

50

Angina  Preventative Therapies

Regular aerobic exercise

Stress reduction

Smoking cessation

Weight control

Blood pressure control

Diabetes management

Pharmacotherapies to prevent cardiovascular events:

Aspirin (or clopidogrel)

HMG-CoA reductase inhibitors (the –statins) 

ACE inhibitors (the –prils) and ARBs (the –sartans)

51

Three primary drug classes that are utilized in angina

beta blockers, calcium channel blockers, & nitrates

52

Nitrates are the mainstay of treatment for ____ symptoms

acute

53

Cardioselective beta blockers are often recommended as?

initial first-line therapy for long-term prophylaxis

54

Anti-anginal Combinations may be

more effective than monotherapy 

55

Only CCBs or nitrates can be used to relieve

vasospastic angina by preventing coronary artery spasm