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Pharmacology B > Lecture 3 - Antianginals > Flashcards

Lecture 3 - Antianginals Flashcards

1
Q

List the drugs in this section

A
  • nitroglycerin, isosorbide dinitrate
  • sildenafil
  • nifedipine, amlodipine, felodipine
  • verapamil, diltazem
  • propranolol
  • metoprolol
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2
Q

What is nitroglycerin and isosorbide dinitrate metabolized to?

A

nitric oxide (NO)

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3
Q

What is sildenafil?

A

type 5 phosphodiesterase inhibitor

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4
Q

What are nifedipine, amlodipine, felodipine?

A

all calcium channel blockers (CCBs); dihydropyridines

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5
Q

What are verapamil and diltazem?

A

all CCBs (calcium channel blockers); non-dihydropyridines

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6
Q

What is propranolol?

A

B-blocker

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7
Q

What is metoprolol?

A

B1-blocker

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8
Q

List the 3 types of angina

A
  • Stable (angina of effort)
  • Unstable
  • Vasospastic (Variant; Prinzmetal’s)
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9
Q

What is angina defined as?

A

O2 demand > O2 supply

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10
Q

Describe a stable angina (angina of effort)

A
  • most common (atherosclerosis with cap)
  • a fixed narrowing of the coronary artery
  • onset associated with a given level of activity
  • PREDICTABLE
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11
Q

Describe an unstable angina

A
  • onset at rest or increased physical activity
  • NOT PREDICTABLE
  • related to coronary atherosclerotic plaque rupture (emboli)
  • dislodged clots lodge in coronary blood vessels
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12
Q

Describe vasospastic angina

A

occurs at anytime, spasms of the coronary artery

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13
Q

Angina pectoris treatment does one of two things - what are they?

A

increases oxygen supply
and/or
decreases oxygen demand

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14
Q

What can increase oxygen supply to treat angina pectoris?

A
  • pO2, Hgb concentration
  • coronary blood flow*
  • micro-circulation*
  • oxygen extraction

*sites for pharmacological intervention

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15
Q

What can decrease oxygen demand to treat angina pectoris?

A
  • heart rate*
  • ventricular wall stress*
    • intraventricular pressure
    • ventricular wall radius
    • wall thickness
  • contractile state*

*sites for pharmacological intervention

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16
Q

List the 3 types of treatment for angina pectoris

A

1) modify/treat risk factors
2) pharmacological treatment
3) surgical intervention

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17
Q

Describing modify/treat risk factors for angina pectoris

A
  • smoking, dyslipidemias, diabetes, hypertension, sedentary, obesity, stress
  • family history is important but unable to modify
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18
Q

Describe pharmacological treatment for angina pectoris

A
  • nitrates/nitrites
  • B-blockers
  • calcium channel blockers
  • Acetylsalicylic acid (ASA)
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19
Q

Describe surgical intervention

A
  • angioplasty

- revascularization

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20
Q

List the 2 nitrates

A
  • nitroglycerin

- isosorbide dinitrate

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21
Q

Describe nitroglycerin

A
  • acute and prophylactic use
  • acute (pain)
  • sublingual (popular)
  • lingual spray (less popular)
  • rapid onset 2-5 mins
  • duration 15-30 mins
  • prophylactically (prevent pain with exercise)
  • patch - onset 30 mins; duration 8-14 hours
  • oral - long acting; duration 6-8hrs
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22
Q

Describe isosorbide dinitrate

A
  • prophylactically (prevent pain with exercise)
  • sublingual - onset 2-5 mins; duration 1.5 to 2 hr
  • oral - onset 15 - 30 mins; duration 3 - 6 hrs
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23
Q

Mechanism of nitrates?

A
  • metabolized to nitric oxide (mainly in veins)
  • nitric oxide increases cGMP which mediates dilation
  • avoid giving with drugs that block cGMP breakdown (ex. sildenafil - a type 5 phosphodiesterase inhibitor)
  • relaxes veins at lower doses
  • relaxes larger arteries at higher doses
  • decrease preload (venous return)
  • decrease heart size (Law of LaPlace - decrease wall stress)
  • may redistribute blood to ischemic areas
  • decreases pulmonary artery resistance
  • useful in pulmonary hypertension seen in COPD
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24
Q

Describe how the veins are relaxed to decrease preload

A
  • vasodilation
  • decreases preload
  • decreases venous return
  • decreases filling pressure
  • decreases stretch
  • decreases myocardial oxygen demand
  • and less decrease in endocardial flow (inner wall) during systole
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25
Q

When does the endocardium get blood flow?

A

only during diastole

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26
Q

When does the pericardium get blood flow?

A

during diastole and systole

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27
Q

What do nitrates prevent?

A

coronary steal is prevented

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28
Q

Describe how nitrates prevent coronary steal?

A
  • smaller arterioles and pre capillary sphincters less affected by nitrates (good!)
  • prevents blood flow to only “healthy regions”
  • arterial vessels effected tend to be larger
  • increases blood flow to healthy and ischemic regions
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29
Q

Some vasodilators may worsen angina (ex. ________)

A

hydralazine

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30
Q

What is coronary steal?

A
  • part after the occlusion is maximally dilated due to metabolites (cannot be dilated further)
  • reflex dialtion on healthy tissue actually steals blood from ischemic area
  • do not want to dilate this area further - no need and would steal more flow
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31
Q 
Nitrates:
Tolerance develops (need \_\_\_\_ hr treatment intervals)
A

12

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32
Q

Adverse effects of nitrates?

A
  • orthostasis
  • throbbing headache
  • reflex activation of SNS
  • salt and water retention
  • high doses may decrease BP and increase sympathetic nerve activity - resultant increased oxygen demand and decreased perfusion pressure may be problematic
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33
Q

What is the formula for oxygen demand?

A

oxygen demand = HR * SBP

34
Q

What does double product allow?

A

allows you to exercise longer before pain and hypoxia occur

35
Q

What do nitrates do?

A

decrease oxygen demand, but do not increase delivery

36
Q

With treatment for angina - may have a ______ in blood pressure

A

decrease

  • reflex response to a decrease in BP may be a problem
  • RAAS - slide 15
37
Q

Nitrates:

If _____, a slight tingling sensation should be felt under the tongue

A

potent

38
Q

Nitrates:

crumbly tablets = ____

A

bad

39
Q

Nitrates:

_____ and _____ sensitive

A

heat

light

40
Q

Nitrates:

Better absorption if sublingual mucosa ____

A

MOIST

41
Q

List some general points about the use of nitrates

A
  • contact physician if pain persists or worsens 5 mins after one tablet (some say wait til after 3 tablets - may be wasting valuable time?)
  • use for acute episodes
  • under used for when increased activity is anticipated (mowing lawn, walking, etc.)
42
Q

Nitrates:

30-50% of ____ may be poor responders

A

Asians

43
Q

Nitrates:

Why are a proportion of Asians poor responders?

A
  • due to decreased mitochondrial aldehyde dehydrogenase (ALDH2)
  • which is needed to convert nitrate to nitric oxide
  • therefore they will make less nitric oxide and have a lower therapeutic effect
44
Q

What is ALDH2 also needed for?

A
  • to breakdown aldehyde associated with alcohol metabolism

- a flush response to alcohol suggests lack of ALDH2

45
Q

Propranolol and metoprolol are _______

A

B-blockers

46
Q

Propranolol and metoprolol are ____ line treatment in chronic stable angina, but not for acute angina attacks

A

first

47
Q

What type of B-blockers do you want to avoid?

A

want to avoid beta-blockers with ISA (intrinsic sympathetic activity)

48
Q

Mechanism of action of B-blockers in treating angina

A
  • decreased oxygen demand (decreased heart rate, blood pressure and contractility)
  • reverse steal? Increase flow to ischemic region
49
Q

Is coronary steal prevented by beta blockers?

A

Yes

50
Q

Benefit of beta-blockers?

A
  • improved survival (important)
  • following an MI, only abtianginal proven to decrease incidence of reinfarction and improve patient survival
  • if a patient has no previous MI, B-blockers are as good as CCBs and nitrates as antianginal
  • prophylactic use of antianginals to prevent the first MI appears to be ineffective
  • benefit in systolic heart failure
51
Q

Adverse effects of beta-blockers?

A

slowing of the heart increases EDV and increases oxygen demand
*may use with nitrates to decrease preload and EDV

52
Q

What type of angina is B-blockers not intended for?

A

vasospastic angina

**may worsen if B2 is blocked?

53
Q

List the 2 classes of calcium channel blockers (CCB’s)

A

Dihydropyridines

Non-dihydropyridines

54
Q

List 2 points about the classes of CCB’s

A
  • both block calcium channels (arteries, heart)

- both effective in treating stable angina pectoris

55
Q

List 2 Dihydropyridines (CCB’s)

A

amlodipine

felodipine

56
Q

How do Dihydropyridines (CCB’s) work?

A
  • arterial vessels more sensitive than veins
  • decrease after load (peripheral resistance)
  • DECREASE AFTERLOAD NOT PRELOAD
  • may also decrease coronary vascular tone
  • little cardiac suppression
  • may cause reflex increase (SNS) in cardiac B-receptor activity
  • decreases coronary artery spasm - good for Prinzmetal angina (vasospastic angina)
  • do not change “double product” value where angina is felt
  • WORK BY DECREASING OXYGEN DEMAND
57
Q

List 2 Non-Dihydropyridines (CCB’s)

A

verapamil

diltiazem

58
Q

What kind of effects does verapamil produce?

A

mainly cardiac effects

59
Q

What kind of effects does diltiazem produce?

A

cardiac and vascular effects

60
Q

How does verapamil work?

A
  • decreases oxygen demand
  • negative inotrope, chronotrope, lowers blood pressure
  • *poor vascular dilator
  • *that’s why it has mainly only cardiac effects
61
Q

How does diltiazem work?

A
  • decreases oxygen demand
  • negative inotrope, chronotrope, lowers blood pressure
  • effective coronary arterial dilator (less peripheral)
62
Q

Benefits of CCB’s?

A
  • decrease symptoms, increase exercise tolerance/time
  • if beta-blocker alone is ineffective or CI
    • substitue with a CCB or combine with a CCB
  • effective for vasospastic angina - dihydropyridines (preferred)
63
Q

Adverse effects of CCB’s?

A
  • serious cardiac suppression
  • verapamil and B-blocker - possible heart block
  • constipation, ankle edema
  • sympathetic reflexes (nifedipine vs. verapamil)
  • dizziness, hypotension, headache, flushing
64
Q

Where does amlodipine work?

A

vasodilates really well

65
Q

Where does verapamil work?

A
  • decreases AV and SA node activity
  • decreases contractility
  • vasodilates
66
Q

Where does nicardipine work?

A

selective for coronary arteries?

67
Q

Where does amlodipine work?

A
  • peripheral and coronary vasodilation

- less tachycardia

68
Q

List 2 combination treatments that make sense

A

B blocker + amlodipine

B blocker + nitrate

*slide 25

69
Q

How do we want to treat angina of effort?

A
  • ASA or clopidogrel if ASA CI (to block platelet aggregation)
  • nitrates or B-blockers as initial treatment
  • CCB if there’s a problem with the first 2
    • increase time of onset of angina and ST depression during exercise treadmill test
    • get angina at same level of oxygen demand - decreases oxygen demand for a given level of exercise

Long-term:

  • start with B-adrenergic receptor blocker
  • improve survival and prevention of re-infarction
70
Q

How do you treat angina of effort for hypertensives?

A

B blockers or long acting CCB (dihydropyridine)

71
Q

How do you treat angina of effort for normotensive?

A

long acting nitrate

72
Q

What drugs are available to be combined to treat angina of effort?

A
  • nitrate
  • calcium channel blocker
  • B blocker
73
Q

Angina of effort:

is combination of products better than single therapy?

A

yes

-added drug blocks compensatory effect of the other

74
Q

Angina of effort:

Which drug combinations work?

A

B-blocker with amlodipine or nitrate

verapamil with amlodipine or nitrate

75
Q

Angina of effort:

combination effects are ______

A

additive

*amlodipine (decreases after load) + nitrate (decreases preload)

76
Q

How do you treat unstable angina?

A
  • antiplatelet therapy
    • ASA (ASAP) or clopidogrel
    • IV heparin (anticoagulant) added to ASA
  • oxygen
  • nitroglycerin (sublingual), give IV if pain persists after three tablets
  • morphine, IV for pain and anxiety
  • oral B-blockers (IV if hemodynamic stability)
  • statins

-B blockers decrease ischemic episodes but not mortality

77
Q

How do you treat vasospastic angina?

A

-calcium channel blockers (vascular) and/or nitrate

Avoid:

  • b-blockers may worsen condition (B1 selective ok?)
  • ASA - decreases prostacyclin which is a vasodilator
  • sumatriptan - used in migraine, may constrict coronary arteries

*revascularization and angioplasty not indicated

78
Q

Preferred and least preferred drugs in:

Asthma

A

Preferred:

  • CCB’s
  • nitrate

Least Preferred:
-B-blocker

79
Q

Preferred and least preferred drugs in:

Diabetes mellitus

A

Preferred:

  • CCB’s
  • nitrate

Least Preferred:
-B-blocker

80
Q

Preferred and least preferred drugs in:

Heart failure

A

Preferred:

  • nitrate
  • B -blocker

Least Preferred:
CCB’s non-dihydropyridines

81
Q

Preferred and least preferred drugs in:

Hypertension

A

Preferred:

  • B-blocker
  • CCB’s

Least Preferred:
-nitrate

82
Q

Preferred and least preferred drugs in:

Peptic ulcer

A

Preferred:

  • B-blocker
  • nitrate

Least Preferred:
-CCB’s

Pharmacology B (21 decks)

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