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Flashcards in Antianginals Deck (43):
1

Angina

Transient episodes of pressure like discomfort resulting from myocardial ischemia that do not cause cell death (MI) and last for fifteen seconds to fifteen minutes

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Class 0 Angina

Asymptomatic

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Class 4 Angina

Occurs at any level of exertion

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Treatment rationale

Increasing oxygen delivery through coronary vasodilators or antithrombotic agents, or decreasing oxygen demand via vasodilators and cardiac depressants; decreasing the oxygen demand is the only therapy that can be used in Prinzmetal angina

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Isosorbide mononitrate class

Organic Nitrates

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Isosorbide dinitrate class

Organic nitrates

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Nitroglyceran class

Organic nitrate

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Sodium Nitroprusside class

Organic nitrate

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Organic nitrate description

Indicated for ALL anginas

Mimic the action of endogenous NO

**Rapid reduction in myocardial oxygen demand** via systemic vasodilation and relief of symptoms

Functions of NO:
Vasodilation
Anti-thrombotic
Antiinflammatory

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Functions of NO

Vasodilation
Anti-thrombotic
Anti inflammatory

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Organic nitrate mechanism

*Nitrates activate guanylyl cyclase* which converts GTP into cGMP; elevated cGMP aids in the de phosphorylation of myosin light chains -> *smooth muscle relaxation*

Decreased coronary vasoconstriciton -> increased myocardial perfusion

Large venous dilation -> decreased preload and work of the heart

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Isosorbide mononitrate indication

*Oral prophylaxis*
Longer onset and duration than nitroglyceran

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Isosorbide mononitrate PK

Metabolites are active
Onset > 1 hr

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Isosorbide mononitrate adverse effect

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

*Desensitization-> nitrate free interval of 10-12 hours needed*

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Organic nitrates contraindications

Sildenafil inhibits PDE5 which breaks down cGMP leading to an even greater increase in cGMP

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Isosorbide dinitrate indication

ongoing attack

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Isosorbide dinitrate PK

similar to nitroglyceran but longer action

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Isosorbide dinitrate adverse

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

*Desensitization-> nitrate free interval of 10-12 hours needed*

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Nitroglycerin adverse

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

*Desensitization-> nitrate free interval of 10-12 hours needed*

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Nitroglyceran indication

IV -> unstable angina and acute HF

*Sublingual -> 1st line treatment of acute symptoms*

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Nitroglyceran PK

High 1st pass metabolism ->parental admin
Onset in 2-5 mins
Lasts 30 mins

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Sodium nitroprusside indication

Direct NO donor -> immediate vasodilation used in EMERGENCY settings

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Sodium nitroprusside PK

Continuous IV infusion
Protect from light due to conversion to cyanide

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Sodium nitroprusside adverse

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

*Desensitization-> nitrate free interval of 10-12 hours needed*

*****Cyanide poisoning****

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Anti-anginal beta blockers

Acebutolol
Atenolol -cardio selective
Metoprolol - cardio selective
Propranolol - not cardioselective

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Beta blcokers mechanism

Decrease heart rate and contractility
***Decrease oxygen demand ***
Decrease frequency and severity of **stable/unstable angina** attacks

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Beta blockers indication

Recommended in all patients with stable angina who have LV dysfunction

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Beta blockers adverse

Rebound HTN or angina if drug is discontinued abruptly (upregulate receptors)

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Beta blocker contraindications

Asthma, COPD
Diabetes, PVD
Severe bradycardia
**Prinzmetal angina**

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Calcium channel blocker drugs for angina

Amlodipine, Felodipine
Verapamil
Diltiazem

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Calcium channel blockers for angina description

Calcium is increased in ischemia due to hypoxia induced membrane depolarization

Angina is improved by coronary and peripheral vasodilation and reducing contractility

**DOC for variant angina**
Use with beta blockers when they aren't successful or replace them when contraindicated

32

Amlodipine and Felodipine mechanism

Minimal effect on conduction or heart rate

Entry of calcium blocked -> decrease smooth muscle tone and PVR -> arteriolar vasodilation -> decrease BP

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Calcium channel blockers adverse

Flushing
Headache
Hypotension
Peripheral edema
**Constipation for verapamil**

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Verapamil mechanism for angina

Slows AV conduction directly -> decreases HR, contractility, BP, O2 demand

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Diltiazem mechanism for angina

slows AV conduction similar to Verapamil, but decreases HR to a lesser extent

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Verapamil and Diltiazem contraindications

Pre-existing depressed cardiac function or AV conduction abnormalities

Use with caution in patients on digoxin

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Sodium channel blocker for angina

Ranolazine

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Ranolazine description

Sodium/calcium exchanger reverses direction in sichemia

Indirectly decreases calcium levels by blocking this exchanger
May also produce myocardial relaxation

39

Ranolazine mechanism

decreases contractility
decreases O2 demand
May modify fatty acid oxidation

40

Ranolazine PK

metabolized by CYP3A4

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Ranolazine Adverse

QT prolongation***
Nausea, constipation, Dizziness

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Treatment strategy for Stable/unstable angina

Acute attacks are promptly relieved by rest or nitroglycerin; maintenance therapy is best with long acting nitrates and beta blockers; Calcium channel blockers are used when beta blockers are not successful or contraindicated; Ranolazine is a last ditch effort when all else fails. Patients should also take aspirin and modify their lifestyle.

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Treatment strategy for Prinzmetal (variant) angina

Symptoms respond to *nitroglycerin and calcium channel blockers (all types)*