Pharm Anti-Anginal Agents Linger Flashcards

1
Q

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

A

Atenolol Metoprolol Propranolol Timolol

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2
Q

Name the 3 Organic Nitrates

A

Nitroglycerin Isosorbide dinitrate Isosorbide mononitrate

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3
Q

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

A

Dihydropyridines (DHPs) Non-dihydropyridines

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4
Q

Name the Dihydropyridines (DHPs)

A

Amlodipine Felodipine Nicardipine

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5
Q

Name the Non-dihydropyridines

A

Diltiazem Verapamil

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6
Q

What is the primary symptom of ischemic heart disease?

A

Angina Pectoris

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7
Q

What are the types of Angina?

A

Effort angina Variant angina Unstable angina

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8
Q

What is effort angina?

A

Increased myocardial O2 demand (exercise) exceeds coronary flow abilities

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9
Q

What is variant angina?

A

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

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10
Q

What is unstable angina?

A

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

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11
Q

Agents that decrease O2 demand

A

ß adrenergic antagonist, Ca entry blockers, organic nitrates,

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12
Q

Agents that increase O2 supply

A

Vasodilators, statins, anti-thrombotics

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13
Q

Nitrates and nitrites MOA

A

metabolized to NO which Increase cGMP

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14
Q

Which Ca blockers are cardio specific

A

Non-DHPs (Verapamil > diltiazem > DHPs)

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15
Q

Non-DHPs physiologic effect

A

decrease rate and contractility in cardiac myocytes

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16
Q

Organic nitrates prototype?

A

nitroglycerin (NTG)

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17
Q

NTG formulation?

A
  1. Sublingual tablet
  2. spray
  3. Sustained release oral capsules
  4. Buccal tablets
  5. gel Ointment
  6. Transdermal patch
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18
Q

NTG preferentially dilates which vessels?

A

Large veins

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19
Q

How does NTG relieve angina?

A

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

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20
Q

First-line therapy for an acute anginal attack?

A

NTG typically sublingual administration, spray equally effective

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21
Q

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

A

Long-acting oral and transdermal formulations

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22
Q

NTG improves antianginal and antiischemic effects of?

A

beta blockers and calcium channels blockers

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23
Q

NTG Long-term utility is limited by?

A

tolerance

24
Q

NTG tolerance is not a problem with which formulation?

A

Generally not a problem with sublingual nitroglycerin

25
Q

How to prevent nitrate tolerance?

A

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

26
Q

Nitrates: Adverse Effects

A

Common: orthostatic hypotension, syncope, throbbing headache, flushing

27
Q

NTG Drug-drug interaction?

A

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

Can lead to myocardial infarction and death

28
Q

ß blockers list the non-selective

A

Propranolol

Carteolol

Nadolol

Penbutolol

Timolol

Pindolol

29
Q

Cardioselective ß blocker

A

Metoprolol

Acebutolol

Atenolol

Nebivolol

Esmolol

Bisoprolol

Betaxolol

30
Q

Combined alpha beta blockers

A

Labetalol

Carvedilol

31
Q

Beta Blockers: Pharmacodynamics

A

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

Most are not vasodilators; no effect on O2 supply

32
Q

Beta Blocker Use in Angina prototype

A

Propranolol

33
Q

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

A

Propranolol

34
Q

Propranolol Reduce O2 requirement by?

A

reducing heart rate and contractility

35
Q

ß blocker NOT effective in_____ angina.

A

variant

36
Q

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

A

exertional

cardioselective (β1-selective)

37
Q

Beta Blockers that Prolong Survival After MI

A

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
Q

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

A

Combined effect on mortality is increased over using either alone

39
Q

Beta Blockers Adverse Effects?

A

Most common: bradycardia and fatigue

40
Q

ß blocker Relative contraindications

A

Asthma/COPD

Diabetes

Variant angina

Acute decompensated heart failure

41
Q

ß blocker Can cause heart block, especially if combined with

A

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

42
Q

Calcium Channel Blockers (CCBs) bind to?

A

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
Q

Pharmacokinetic Properties of CCBs

A

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
Q

CCBs: Pharmacodynamics

A

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
Q

vasodilator that is most effective on

  1. large veins
  2. arterioles
A
  1. organic nitrates
  2. Ca channel blockers
46
Q

Calcium Channel Blocker Use in Angina

A

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
Q

CCBs: Adverse Effects & Toxicity

A

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
Q

According to board exams constipation is always caused by?

A

verapamil

49
Q

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

A

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
Q

Angina Preventative Therapies

A

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
Q

Three primary drug classes that are utilized in angina

A

beta blockers, calcium channel blockers, & nitrates

52
Q

Nitrates are the mainstay of treatment for ____ symptoms

A

acute

53
Q

Cardioselective beta blockers are often recommended as?

A

initial first-line therapy for long-term prophylaxis

54
Q

Anti-anginal Combinations may be

A

more effective than monotherapy

55
Q

Only CCBs or nitrates can be used to relieve

A

vasospastic angina by preventing coronary artery spasm