Tx of Angina Flashcards

1
Q

Name the 5 Dihydropyridines CCBs

A

“Dipines”

  1. Amlodipine
  2. Nifedipine
  3. Felodipine
  4. Nicardipine
  5. Isradipine
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2
Q

Name the 2 non-dihydropyridines CCBs

A
  1. Verapamil

2. Diltiazem

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3
Q

Uses of CCBs:

A
  1. Angina
  2. HTN
  3. Arrhythmias
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4
Q

What type of calcium channels do CCBs act on, and why do they not have significant side effects?

A

L-type calcium channels

  • other types of Ca2+ channels are insensitive to CCBs
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5
Q

MOA of all CCBs

A

Increase the time that Ca2+ channels are closed which:

  1. reduces the magnitude of Ca2+ current (and therefore less contraction)
  • Induce relaxation of Arterial smooth muscle only
  • Effect AFTERLOAD (not preload)
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6
Q

Addition MOA of non-dihydropyridine CCBs

A

Increase the time that Ca2+ channels are closed which:

  1. reduces the magnitude of Ca2+ current (and therefore less contraction)
  2. Slow recovery of the channel

*reduce inotropy, slow AV conduction, and slow SA firing

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7
Q

Selectivity of Dyhydropyridine CCBs in the CV system?

A
  1. Peripheral vasodilation

2. Coronary vasodilation

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8
Q

Selectivity of non-Dyhydropyridine CCBs in the CV system?

A
  1. Peripheral and Coronary vasodilation

2. Cardiac tissue (Myocytes)!

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9
Q

Potential side effect of Dyhydropyridine CCBs?

A
  1. Reflex tachycardia (Increase HR)
  2. Reflex increase in myocardial contractility
  3. Increase O2 demand

*should only use in combo with B-Blocker to modulate these effects

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10
Q

Pharm effect of non-Dyhydropyridine CCBs

A
  1. Decrease inotropy (Contractility)
  2. Decrease HR
  3. Slow conduction
  4. Vasodilate
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11
Q

What type of binding to L-type Ca2+ channels do non-Dihydropyridines (Diltiazem/Verapamil) demonstrate?

A

Use-dependent binding
- bind to channels with higher activity because it is more likely that they will encounter an open channel to inhibit

(i.e. channels in Cardiac cells)

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12
Q

What type of binding to L-type Ca2+ channels do Dihydropyridines CCBs demonstrate?

A

Voltage-dependent binding
- bind to channels that have very slow changing voltages

(i.e. Channels in Smooth muscle cells)

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13
Q

Absorption of CCBs?

A

Absorbed in the GI tract

*extensive 1st-pass hepatic metabolism reduces bioavailabilty

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14
Q

Metabolism of CCBs

A

Hepatic metabolism

  • reduce dose in hepatic disease
  • CYP3A4 interactions (verapamil > Diltiazem)
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15
Q

Adverse effects of Dihydropyridine CCBs?

A
  1. excessive vasodilation (dizziness, hypotension, headache)
  2. GI irritation (nausea)
  3. Peripheral Edema
  4. Paradoxical exacerbation of Angina (Coronary steal- less common in slow-release form)
  5. Fetotoxicity
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16
Q

Adverse effects of non-Dihydropyridine CCBs?

A
  1. Bradycardia, Asystole, AV Block
  2. Constipation
  3. Fetotoxicity

**Do not use w/ B-Blocker (slows conduction) or in CHF (neg-iontropic effects)

17
Q

Drug interactions with Verapamil and Diltiazem?

A
  1. CYP3A4 drugs (Macrolides, Azoles, Statins, Grapefruit juice)
  2. B-Blockers
18
Q

Pharmalogical effects of Nitrates?

A
  1. Venodilation (Reduced Preload)

2. Coronary Vasodilation

19
Q

Overall effect of Nitrates on hemodynamics?

A

BP: Unchanged or slight decrease
HR: Unchanged or slight increase
Pulm Vascular Resistance: Decreased
CO: Slight reduction

20
Q

Adverse effects of Nitrates

A
  1. Hypotension
    - may trigger reflex tachycardia, increased contractility and decrease coronary (paradoxically worsen angina)
    - Dizziness, orthostatic hypotension, syncope in PTs who are sensitive to reduced preload
  2. Headache *most commonly
  3. Rash - seen w/ longer acting nitrates and w/ cutaneous administration
21
Q

Contraindications for Nitrates

A

Boner Pills (Sildenidil- Viagra)

22
Q

Biggest problem with nitrate therapy? And how to deal with it?

A

Loss of efficacy due to repeated exposure (Tolerance)

*Cycle its use with 8-12 hour “nitrate free” intervals

23
Q

What happens if you abruptly stop IV nitroglycerin in unstable angina? How do you prevent this?

A

Anginal Rebound - coronary vasospasms

*bridge with transdermal or oral form

24
Q

Drugs that Tx Angina

A
  1. Nitrates
  2. B-Blockers
  3. CCBs
  4. Ranazoline
25
Q

Approaches for treating Angina?

A
  1. increase coronary blood flow (increase supply)
  2. Reduce myocardial demand for 02
    - decrease HR and contractility and workload
  3. Prevent platelet adhesion/aggregation

*most therapies involve many of these factors

26
Q

What is the first drug of choice for tx of Angina? For all types of angina?

A

B-blockers
- Unstable and exertional angina

*ineffective for vasospastic (prinzmetal) angina

27
Q

What should be used in conjunction with Dihydropyridine CCBs when treating Angina? Why?

A

B-Blockers

-To reduce the reflex sympathetic activity caused by DHPs
Increase HR and contractility

28
Q

What should be used in conjunction with Non-DHP CCBs? Why?

A

NOTHING
- Verapamil and Diltiazem reduce heart work and cause coronary vasodilation.

*NEVER COMBINE WITH B-BLOCKER (due to slowing of the AV conduction)

29
Q

DHP or non-DHP CCB to tx Angina?

A
  • DHP w/ beta-blocker

- unless PT is in-tolerant to B-blocker (Asthma or COPD), then use non-DHP CCB

30
Q

What type of angina(s) are CCBs highly effective in relieves symptoms?

A
  1. Exertional angina

2. Vasospastic angina

31
Q

When should beta-blockers be used?

A
  1. Unstable Angina
  2. Exertional Angina
  3. MI (if no CHF, Hypotension, or sinus bradycardia/heart block)
32
Q

What is Renolazine? When is it indicated?

A

Metabolic modulator

Indication: Chronic stable angina that is refractory to amlodapine, beta-blocker or Nitrate

*adjuntive agent used in combo with drugs above

33
Q

Contraindications of Renolazine?

A
  1. Concurrent use of CYP3A4 inhibitors
  2. Existing QT-prolongation
  3. w/ Class Ia and III antiarrthythmics
  4. w/ tricyclic antidepressants

*increase DIGOXIN concentrations 40-60% via p-gp inhibition. Very toxic!!!

34
Q

T or F: B-Blocker and Nitrates reduce CHD events

A

FALSE

Only Beta-Blockers reduce CHD events, NOT Nitrates

35
Q

T or F: all patients with CHD should recieve asprin therapy unless contraindicated

A

T