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pharmacology > Vasodilators for Angina Pectoris DRUGS > Flashcards

Vasodilators for Angina Pectoris DRUGS Flashcards

1
Q

what are the 3 drugs that reduce cardiac size, rate, force and reduce cardiac o2 demand are?

A

vasodilators
B-blockers
CCB

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2
Q

what is the MOA for Nitric Oxide

A

activates and increases cGMP

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3
Q

What 2 drug classes decrease intracellular Ca2+

A

Beta blockers
CCB

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4
Q

What drug class prevents the depolarization of vascular smooth muscle?

A

Potassium channel openers
ex. Minoxidil (K+ opener)

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5
Q

what is the MOA of Nitrates

A

releases and increases NO into the SM cells leading to vasodilation

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6
Q

what is rapid and short acting nitrates primarily used for?

A

Acute angina pectoris
Hypertensive urgency

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7
Q

What are the 3 main side effects of Nitrate

A
  1. headache
  2. GERD
  3. Hypotension with syncope
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8
Q

Is there a difference in MOA between organic nitrate vs nitrous acid esters of polyalcohols

A

Not a big difference in MOA

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9
Q

What is the required activation for organic nitrates?

A

by mitochondrial aldehyde reductase (so the action is not immediate)

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10
Q

what are 3 examples of organic nitrates?

A
  1. nitroglycerin
  2. isosorbide dinitrate
  3. isosorbide mononitrate
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11
Q

What is the onset of action of sodium nitroprusside?

A

immediate b/c it is activated non-enzymatically

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12
Q

What is the most favorable route of nitrates

A

sublingual b/c it avoids the first pass effect

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13
Q

What is the bioavailability level of nitrates/nitrites?

Why?

A

Low bioavailability due to the liver containing an organic nitrate reductase that in activates nitrates/nitrites

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14
Q

What is the best route to administer nitroglycerin and isosorbide dinitrate? How long does it take to reach therapeutic levels?

A

sublingual route
within a few minutes

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15
Q

what is the total duration of effect for nitroglycerin and isosorbide dinitrate?

A

15-30 minutes (brief)

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16
Q

what are the other routes for nitroglycerin

A

transdermal
buccal absorption (slow release)

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17
Q

what is the effect of Nitroglycerin in the body?

A

relaxes all types of smooth muscle regardlesss of preexisting muscle tone

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18
Q

What muscle does nitroglycerin not have a direct effect on?

A

cardiac or skeletal muscle

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19
Q

what is the primary direct result of an effective dose nitroglycerin?

4

A
  1. marked relaxation in the veins
  2. increase venous capacity and decreased ventricular period
  3. pulmonary vascular pressure decreased
  4. heart size is decrereased
  5. if absense of heart failure= output is reduced
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20
Q

what pulsations are associated with the headache from nitrates/ nitrites

A

temporal artery pulsations
meningeal artery pulsations

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21
Q

Why are nitrates/nitrites beneficial for heart failure

A

vasodilators reduce preload and have a benefit for cardiac output

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22
Q

what are indirect effects of nitroglycerin

A
  1. decreased arterial pressure
  2. ^ results in tachycardia and increased cardiac contractility
  3. retention of salt and water
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23
Q

what is the result of nitRITE ion and hemoglobin?

A

produces methemoglobin (by oxidation of ferrous to ferric iron)

“methemoglobinemia”- needs a lot to cause significant rx

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24
Q

what inotropic effect on the heart does nitroglycerin have?

A

weak negative inotropic effect

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25
Q
A
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26
Q

what ways can nitrate already be present in the human body in high levels?

A

processed meats
well water

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27
Q

how can nitrites be used to treat cyanide poisoning?

A

methemoglobin iron
administration of sodium nitrite after cyanide exposure regenerates cytochrome

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28
Q

what do you follow sodium nitrite with for treatment of cyanide exposure

A

IV sodium thiocyanate
methylen blue

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29
Q

What is the new treatment for cyanide exposure

A

hydrooxocobalamin

30
Q

the major acute toxicities of organic nitrates are ___

A

direct extensions of therapeutic vasodilation

31
Q

what is a major contraindication of nitrates

A

if intracranial pressure is elevated

32
Q

what nitrate does not experience tolerance

A

nitroprusside because it retains activity over long periods

33
Q

what is the onset of action of nitrates

A

1-3 minutes

34
Q

Why are nitrates not suitable for maintenance therapy

A

becuase duration of action is short (20-30 minutes)

35
Q

what is IV nitroglycerin used for?

A

ONLY used for recurrent rest angina

36
Q

What are the CCB drugs

A

verapamil
Nifedipine
Diltiazem

37
Q

What calcium channel blockers are administered via IV

A

Verapamil and diltiazem

38
Q

what are the characteristics of the pharmacokinetics of CCB

A

High first pass effect
high plasma protein binding
extensive metabolism

39
Q

what is the MOA of CCB

A

reduces the frequency of opening in response to depolarization
-decreased transmembrane calcium current
-reduces contractility
-decreases sinus node pacemaker rate and AV node conduction

40
Q

How can CCB be partially reversed?

A

Elevating the concentration of Calcium
or
increase the transmembrane flux of calcium (sympathomimetics)

41
Q

do slide 20

A
42
Q
A
43
Q
A
44
Q
A
45
Q
A
46
Q
A
47
Q

Clinical effects of CCB

list 5

A
  1. decrease myocardial contractile force (reduces myocardial o2 req.)
  2. decreals arterial and intraventricular pressure
  3. relieve and prevent focal coronary artery spasm (contraction inhibited)
  4. SA and AV nodes are slowed
48
Q

Verapamil _____ affects slow response cells in SA and AV nodes

A

markedly

49
Q

Diltiazem _____ affects slow response cells in SA and AV nodes

A

moderately

50
Q

Dihydropyridines _____ affects slow response cells in SA and AV nodes

A

doesn’t (as much)

51
Q

What are calcium channel blockers used for prophylatically

A

angina pectoris

52
Q

Verapamil main effect? When is this possibly unwanted?

A

slows conduction through AV node
-unwanted in TX of HTN

53
Q

what is the effect of verapamil and b-blockers

A

AV block

54
Q

What are the peripheral vasodilator effects of verapamil?

A

reduce afterload and BP

55
Q

Toxic effects of verapamil

list 3 + 2 peripheral effects

A
  1. mild cardiodepression
  2. heart failure
  3. edema
  4. headache
  5. reflex tachycardia
56
Q

Nifedipine brand name

A

Procardia

57
Q

what class is Nifedipine

A

dihydropyridine CCB

58
Q

what is the predominant effect of nifedipine

A

-IN peripheral vasculature
-decreases afterload

59
Q

what vasodilator is recommended for pts already on a vasodilator? why

A

Nifedipine
they have less effect on the heart

60
Q

what drug class is diltiazem?

A

a benzodiazepine CCB

61
Q

what is the benefit of diltiazem

A

it has intermediate proprerties between verapamil and dihydropyridines

62
Q

what is diltiazem used to treat?

A

variant angina (prinzmetals)
stable angina

63
Q

what is the 1st line prophylactic treatment of chronic angina

A

beta-blockers

64
Q

what are the benefits of beta-blockers for angina pectoris

A

decreases HR, BP and contractility

this decreases myocardial O2 requirments at rest and during exertion

65
Q

For beta-blockers

what is a decreased heart rate also associated with (perfusion related)

A

increase diastolic perfusion time
increase coronary perfusion

66
Q

For maintenance therapy of chronic stable angina, what therapy regimes are options for your patient?

A
  1. Beta blockers
  2. CCB
  3. long acting nitrates
67
Q

for hypertensive pts, what therapy regimes may be used for angina pectoris?

A
  1. monotherapy with slow-release
  2. long acting CCB
  3. Beta blockers
68
Q

For normotensive patients, what vasodilator regime may be suitable?

A

long-acting nitrates

69
Q

what are the two combinations of drug classes that are more effective for angina together?

A
  1. B-blocker and CCB
  2. two different CCB
70
Q

In patients with unstable angina, NSTEMI, what is the recommended therapy regime?

4

A
  1. coronary stenting
  2. antilipid drugs
  3. heparin
  4. antiplatelet agents

pharmacology (20 decks)

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