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Pharmacology - Winter > 3 - Anti-anginals > Flashcards

3 - Anti-anginals Flashcards

1
Q

What is a myocardial infarction?

A

Damage to the muscular layer of the heart, so pumping action is compromised, leading to heart failure

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2
Q

What causes a myocardial infarction?

A

Severe obstruction of the blood supply causing nutrient and oxygen deficiency, leading to ischemia

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3
Q

What is anginal pain a symptom of?

A

Ischemic heart disease

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4
Q

When does angina pectoris occur?

A

When there is insufficient oxygen to meet the requirement of the heart

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5
Q

What are some risk factors for angina pectoris?

A
  • Male
  • Older age
  • Post-eating (normally fatty meal)
  • Physical exertion
  • Smoker
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6
Q

What is stable angina?

A

When the px knows when it will occur and can take steps to prevent it

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7
Q

What are the 3 types of angina?

A

1) Stable
2) Unstable
3) Vasospastic or prinzmetal

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8
Q

What are some inducing factors of stable angina?

A

Atherosclerosis and exercise, emotions

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9
Q

What are some inducing factors of unstable angina?

A
  • Atherosclerosis w/ unstable plaque (Plaque ruptures)

- Can occur at rest

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10
Q

What is an inducing factor of vasospastic or prinzmetal angina?

A
  • Vasospasm

- Can occur at rest or in the morning when high epinephrine release or high serotonin levels

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11
Q

What is the test for prinzmetal angina?

A

Vasoconstrictor is given during cardiac catheterization, after no atherosclerosis is visualized

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12
Q

What are the 2 factors of angina pectoris that drugs may affect?

A
  • Oxygen demand of tissues

- Oxygen supply to tissues

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13
Q

How can you increase oxygen supply?

A
  • Nasal oxygen
  • Increase coronary flow and distribution through vasodilation of certain blood vessels (increasing flow isn’t enough, need to increase distribution to make sure it reaches ischemic areas)
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14
Q

If arteries are constricted, afterload will ______

A

Increase

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15
Q

How can oxygen demand be decreased?

A
  • Less work by the heart (rest)
  • Lessen preload or venous return (venodilate w/ drugs like nitrate)
  • Decrease work by the heart by decreasing afterload/BP
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16
Q

What determines contraction of smooth muscle cells?

A

Calcium that initiates actin-myosin interaction

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17
Q

Which substances inhibit contraction of smooth muscle? How?

A
  • Cyclic AMP and cyclic GMP

- Lower smooth muscle cell calcium

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18
Q

What will be the result if a drug increases cyclic GMP or cyclic AMP?

A

Relax smooth muscle and vasodilate

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19
Q

Do cyclic GMP and cyclic AMP relax cardiac muscle?

A

Cyclic GMP does, cyclic AMP does not

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20
Q

Which types of drugs can be used to treat or prevent angina?

A
  • Vasodilators
  • Agents that decrease cardiac work
  • Agents that decrease calcium load
  • Agents that prevent thrombus formation
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21
Q

What are the types of nitrates? Which has the shortest duration of action?

A
  • Amyl nitrate (shortest duration)
  • Nitroglycerin
  • Isosorbide dinitrate (longest duration)
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22
Q

How do nitrates help w/ angina?

A
  • Nitrates increase nitrites, which increase nitric oxide, which increases cyclic GMP, and causes smooth muscle relaxation
  • Primarily affects venous system, so preload is decreased, and so is oxygen demand
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23
Q

_____ route of nitrates is preferred

A

Sublingual

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24
Q

How are nitrates excreted?

A

By kidneys as glucouronide

25
Q

What is required to release nitric oxide from nitrates?

A

Esterases

26
Q

Esterases are more abundant in ____ than _____

A

Veins than arteries

27
Q

Do nitrates have a direct affect on cardiac muscle?

A

No, affects smooth muscle and possibly platelets

28
Q

How does nitric oxide increase cGMP?

A

NO reacts w/ -SH containing receptor of guanyl cyclase

29
Q

What affect do nitrates have on angina that is different from someone w/o angina?

A
  • In normal px, there is an increase in coronary flow

- In angina, there is redistribution of flow to ischemic region by opening of collateral vessels w/ nitrates

30
Q

What are the problems w/ nitrate use?

A
  • Postural hypotension
  • Reflex symp activation (tachycardia, venoconstriction)
  • Hypoxia and death due to methemoglobin formation (rare from therapeutic doses)
  • Tolerance w/ long acting preparations
31
Q

What can be done to prevent nitrate tolerance?

A

8 hour nitrate free period

32
Q

What is an important drug interaction w/ nitrates?

A
  • Sildenafil (viagra)

- Selective inhibitor of cGMP-specific phosphodiesterase type 5, which is required for smooth muscle relaxation

33
Q

What are side effects of sildenafil?

A
  • Mild headache and flushing

- Dyspepsia

34
Q

What are the 3 types of calcium channel blockers?

A

1) Dihydro-pyridines
2) Phenyl-alkylamines
3) Benzothiazepines

35
Q

What do calcium channel blockers do?

A

Convert the channel into a closed state, and thus block calcium influx and induce relaxation

36
Q

Which smooth muscle do calcium channel blockers mostly affect?

A

Arterioles more sensitive, little effect on veins

37
Q

Do calcium channel blockers cause postural hypotension?

A

Not normally

38
Q

What affect do calcium channel blockers have on cardiac muscle?

A
  • Impulse generation in SA node and AV nodal conduction may be blocked by all types
  • Direct effect on myocardial cell calcium influx and reduces oxygen demand
  • Protects from excessive loading of ischemic cell w/ calcium, reducing incidence of arrhythmias and infarct size
39
Q

What are the uses of calcium channel blockers?

A
  • Angina (esp. prinzmetal), hypertension
  • Migraines, Raynaud’s syndrome
  • Hypertrophic cardiomyopathy and cardiac arrhythmias
40
Q

Which calcium channel blocker is preferred for unstable angina?

A

Verapamil

41
Q

What are some minor side effects of calcium channel blockers?

A

Constipation, edema, flushing

42
Q

What can happen if calcium channel blockers are used w/ propranolol?

A

Could be a cardiac depressant at lower concentration than usual

43
Q

Which calcium channel blocker is preferred for atrial fibrillation in the presence of hypotension?

A

Verapamil

44
Q

What is the concern of verapamil with digoxin?

A

Verapamil can elevate concentration of digoxin in blood

45
Q

What are the affects of beta-adrenergic blockers in angina?

A
  • Reduce work of the heart and oxygen demand
  • Reduce BP
  • Reduce frequency and severity of angina
  • Reduce mortality
46
Q

For angina, beta blockers are used with _____

A

Nitrates

47
Q

What are beta blockers contraindicated w/?

A
  • Asthma
  • Diabetes
  • Peripheral vascular diseases (Raynaud’s syndrome)
48
Q

Why are beta blockers contraindicated in diabetes?

A

Px won’t be able to tell when they are hypoglycemic

49
Q

Are all vasodilators useful for angina? Why?

A
  • No, many are arteriolar dilators which can cause rebound symp stimulation and are harmful
  • “Coronary steal” - by dilating arteries to normal tissues, some vasodilators can steal blood which could otherwise perfuse ischemic areas
50
Q

What are the drugs used for coronary vascular disease?

A
  • Nitrates
  • Calcium channel blockers
  • Beta adrenergic blockers
51
Q

What can be used for revascularization in coronary vascular disease?

A
  • Clot busters (thrombolytics)
  • Coronary stents
  • Ballon angioplasty
  • CABG (coronary artery bypass grafting)
52
Q

Which enzyme converts NADPH + L-arginine to NO?

A

Nitric oxide synthetase

53
Q

What are the 3 types of nitric oxide synthetase? Where is each form found?

A

1) Isoform 1 (nNOS) - neurons, epithelia
2) Isoform 2 (iNOS) - macrophages, inducible by LPS
3) Isoform 3 (eNOS) - endothelium

54
Q

What is the action of nitric oxide at low concentrations?

A

Vasodilation

55
Q

What is the action of nitric oxide at high concentrations?

A

Kill bacteria, inhibit Cyt P450, inflammation

56
Q

What are some inhibitors of nitric oxide?

A
  • Aminoguanidines

- Arginine analogues

57
Q

What are the uses of nitric oxide donors?

A
  • Angina
  • Pre-eclampsia
  • Pulmonary hypertension
  • Hypertensive emergencies
  • Respiratory distress
58
Q

What are the uses of nitric oxide inhibitors?

A
  • Arthritis
  • Inflammatory liver diseases
  • Septic shock

Pharmacology - Winter (18 decks)

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