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Antianginals Flashcards

1
Q

Angina

A

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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2
Q

Class 0 Angina

A

Asymptomatic

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3
Q

Class 4 Angina

A

Occurs at any level of exertion

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4
Q

Treatment rationale

A

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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5
Q

Isosorbide mononitrate class

A

Organic Nitrates

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6
Q

Isosorbide dinitrate class

A

Organic nitrates

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7
Q

Nitroglyceran class

A

Organic nitrate

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8
Q

Sodium Nitroprusside class

A

Organic nitrate

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9
Q

Organic nitrate description

A

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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10
Q

Functions of NO

A

Vasodilation
Anti-thrombotic
Anti inflammatory

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11
Q

Organic nitrate mechanism

A

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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12
Q

Isosorbide mononitrate indication

A

Oral prophylaxis

Longer onset and duration than nitroglyceran

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13
Q

Isosorbide mononitrate PK

A

Metabolites are active

Onset > 1 hr

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14
Q

Isosorbide mononitrate adverse effect

A

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

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

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15
Q

Organic nitrates contraindications

A

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

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16
Q

Isosorbide dinitrate indication

A

ongoing attack

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17
Q

Isosorbide dinitrate PK

A

similar to nitroglyceran but longer action

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18
Q

Isosorbide dinitrate adverse

A

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

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

19
Q

Nitroglycerin adverse

A

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

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

20
Q

Nitroglyceran indication

A

IV -> unstable angina and acute HF

Sublingual -> 1st line treatment of acute symptoms

21
Q

Nitroglyceran PK

A

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

22
Q

Sodium nitroprusside indication

A

Direct NO donor -> immediate vasodilation used in EMERGENCY settings

23
Q

Sodium nitroprusside PK

A

Continuous IV infusion

Protect from light due to conversion to cyanide

24
Q

Sodium nitroprusside adverse

A

Headache -> cerebral vasodilation

Postural hypotension
Flushing
Reflex tachycardia

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

**Cyanide poisoning*

25
Anti-anginal beta blockers
Acebutolol Atenolol -cardio selective Metoprolol - cardio selective Propranolol - not cardioselective
26
Beta blcokers mechanism
Decrease heart rate and contractility ***Decrease oxygen demand *** Decrease frequency and severity of **stable/unstable angina** attacks
27
Beta blockers indication
Recommended in all patients with stable angina who have LV dysfunction
28
Beta blockers adverse
Rebound HTN or angina if drug is discontinued abruptly (upregulate receptors)
29
Beta blocker contraindications
Asthma, COPD Diabetes, PVD Severe bradycardia **Prinzmetal angina**
30
Calcium channel blocker drugs for angina
Amlodipine, Felodipine Verapamil Diltiazem
31
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
33
Calcium channel blockers adverse
``` Flushing Headache Hypotension Peripheral edema **Constipation for verapamil** ```
34
Verapamil mechanism for angina
Slows AV conduction directly -> decreases HR, contractility, BP, O2 demand
35
Diltiazem mechanism for angina
slows AV conduction similar to Verapamil, but decreases HR to a lesser extent
36
Verapamil and Diltiazem contraindications
Pre-existing depressed cardiac function or AV conduction abnormalities Use with caution in patients on digoxin
37
Sodium channel blocker for angina
Ranolazine
38
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
41
Ranolazine Adverse
QT prolongation*** | Nausea, constipation, Dizziness
42
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.
43
Treatment strategy for Prinzmetal (variant) angina
Symptoms respond to *nitroglycerin and calcium channel blockers (all types)*

Pharmacology (24 decks)

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