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Drug Action I > Block 3 - Ischemic Heart Disease Med Chem > Flashcards

Block 3 - Ischemic Heart Disease Med Chem Flashcards

1
Q

What are the symptoms of Ischemic Heart disease?

A
  1. Angina pectoris
  2. Silent myocardial ischemia
  3. Acute coronary insufficiency
  4. Myocardial infarction
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2
Q

What is angina pectoris?

A

Imbalance between oxygen requirement of heart and oxygen supplied to it via coronary vessels

Primary symptom of ischemic heart disease

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3
Q

What is the most common cause of angina pectoris?

A

Atheromatous obstruction of large coronary vessels (coronary artery disease, CAD)

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4
Q

What is classic angina? Cause?

A

inadequate blood flow in the presence of CAD caused when myocardial oxygen requirement increases but coronary blood flow does not i.e. exercise

  1. Ischemia with acidic metabolites → pain
  2. May not have pain = silent or ambulatory ischemia
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5
Q

What is coronary miscovascular dysfunction?

A

typical symptoms but normal epicardial coronary vessels

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6
Q

What is vasospastic (variant Prinmzmetals) angina?

A

transient spasm of localized portions of vessels→ myocardial ischemia and pain

O2 delivery decreases

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7
Q

What is unstable angina? Cause?

A

episodes occur at rest; increase in severity, frequency and duration of chest pain

Caused by episodes of increased epicardial coronary artery resistance or small platelet clots in area of an atherosclerotic plaque

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8
Q

Nitatrates are _____ absorbed due to ____ nature therefore it is highly effective in _____ situations

A

Rapidly; lipophilic; emergency

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9
Q

Describe structure of nitrates?

A

esters of simple organic alcohols or polyols with nitric acid

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10
Q

What are the function of nitrates?

A
  1. Vasodilation of veins → pooling of blood in veins and decreased return to heart (decrease preload)
  2. Vasodilation of coronary arterioles → decrease resistance of peripheral tissues (decreased after load)

Decrease in myocardial workload → reduced O2 demand by heart

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11
Q

What cells produce NO?

A

produced by vascular endothelial cells, causes relaxation of vascular smooth muscle (VSM)

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12
Q

Describe the nitrates MOA?

A
  1. Organic nitrates mimic the actions of endogenous NO by releasing NO radicals
  2. Prodrug
  3. Increases in cGMP
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13
Q

Why are nitrates hard to formulate?

A
  1. Small esters → very volatile
  2. Moisture can easily hydrolyze the ester bond
  3. Explosive when pure → must dilute
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14
Q

Does increase nitrogen groups mean increased activity of NO?

A

No, activity will be the same

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15
Q

What are nitrate formulations used for? What properties are important its use?

A
  1. Treatment of acute anginal attacks (Fast onset)
  2. Prevention of anginal attacks (Longer DOA)
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16
Q

What is acute NO for? Dosage forms?

A

rapid onset, can have short duration of action

SL/Inhalation

17
Q

What is something to be aware of we use SL Nitrates?

A
  1. SL can avoid some hepatic metabolism (buccal and transdermal)
  2. Onset is 2 min, DOA: 30 min
18
Q

What is something to be aware of we use inhalation Nitrates?

A

Inhalable amyl nitrate onset = 15 – 30 sec, duration 1 min

19
Q

What is prevention NO for? Dosage forms?

A

Longer DOA, Longer onset

Active metabolites help isosorbide denigrate

Oral/ointment/transdermal patch

20
Q

Common ADRs of nitrates?

A

HA, Tachycardia, and postural hypotension

Tolerance can develop → Shortened DOA

21
Q

DDIS for nitrates?

A

Agents that cause hypotension (vasodilators, alcohol, tricyclic antidepressants)

22
Q

MOA of ranolazine?

A
  1. Lowers intracellular Ca2+ → Reduces Na+ current (Ina) allowing Ca2+ entry through sodium-calcium exchanger
  2. Reduces diastolic tension, cardiac contractility and work
  3. Doesn’t change BP and HR
23
Q

ADRs of ranolazine? Indication?

A

Prolongs QT intervals in patients with CAD

No torsades de pointes

Ind: PO prophylactic

24
Q

DDI of ranolazine?

A

Metabolized by CYP3A4 – affected by inhibitors

Inhibits P-gp

25
Q

What is MOA of pentoxifylline?

A

Reduces viscosity of blood and increases deformability of red blood cells → Blood flows more easily through partially obstructed areas

25
Q

What is MOA of pentoxifylline?

A

Reduces viscosity of blood and increases deformability of red blood cells → Blood flows more easily through partially obstructed areas

Drug Action I (32 decks)

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