Adrenergic agonists and antagonists Flashcards

1
Q

CNS Dopamine receptors and effects

A

D1, D2, D3, D4, D5

Essential NT in many neural circuits

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2
Q

Renal afferent BV Dopamine receptor and effect

A

D1

Dilation - increase flow to kidney

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3
Q

Nerve ending Dopamine receptor and effect

A

D2

Modulate NT release

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4
Q

Good treatment during shock

A

Dopamine

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5
Q

B1 receptor and heart effect

A

Stimulation of HR and force

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6
Q

Muscarinic receptor and heart effect

A

Decrease HR

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7
Q

A1 receptor and vessels

A

Vasoconstriction

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8
Q

B2 receptor and vessels

A

Vasodilation

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9
Q

Baroreceptor reflexes

A

Indirect effect on heart

Increase BP -> increase baroreceptor firing -> increase parasympathetics, decrease sympathetics

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10
Q

Norepinephrin

A

A1, A2, B1, B3 agonist
Low B2 effect -> high peripheral resistance, reflex HR decrease
Use during anesthesia and shock -> maintain stable BP

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11
Q

Epinephrin

A

A1, A2, B1, B2, B3 agonist
Good B2 agonist -> skeletal and mesentary dilation BUT some A1 constriction
Not as useful for maintaining BP artificially

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12
Q

Isoproterenol

A

B1, B2, B3 agonist

Big B2 agonist -> drop in BP and reflex increase in HR

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13
Q

CV clinical uses of epinephrin

A

During CPR for asystole
Hemodynamic support after CABG surgery
Anaphylaxis
Local or topical hemostatic

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14
Q

CV clinical uses of norepinephrin

A

Pressor agent of choice for septic shock and may be more appropriate than dopamine as first-line treatment for other types of shock as well, especially cardiogenic shock

NE can be used as a pressor agent to support blood pressure in surgery and ICU

NE decreases renal blood flow

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15
Q

Phenylephrine (Neosynephrine) actions

A

Vasoconstriction
Increase peripheral resistance and increase BP
Increased blood pressure causes reflex bradycardia - blocked by atropine

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16
Q

Phenylephrine (Neosynephrine) clinical use

A

IV vasopressor agent:
Maintain BP in hypotensive states - spinal anesthesia
Paroxysmal atrial tachycardia - induces baroreceptor reflex slowing of rate

Over-the-counter nasal decongestant

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17
Q

Dopamine receptor affinity

A

D1 > B1 > A1

Higher doses increase CO but also cause vasoconstriction

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18
Q

Dopamine effect on BV

A

Vasodilates renal, coronary, & mesenteric vascular beds

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19
Q

Dopamine effect on Heart

A

Mild increase in rate and force

B1 agonist and increase NE

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20
Q

High dose dopamine effect on BV

A

Vasoconstriction and increased BP

Bad for shock

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21
Q

Clinical uses of dopamine

A

Shock, cardiogenic shock, unstable CHF
Increases cardiac output and enhances perfusion of kidney
**Must monitor BP carefully
Sometimes used in manage acute crisis in chronic CHF

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22
Q

Dobutamine

A

B1 selective agonist
Positive inotropic and some increase HR
CO increases
Little vascular effect

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23
Q

Dobutamine clinical uses

A

Cardiogenic shock, MI, CHF

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24
Q

Adverse effects of dobutamine

A

May increase size of infarct
Potential arrhythmias
Increases work and O2 requirement

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25
Q

A1 selective receptor blocker

A

Treat essential HTN
Decrease PVR, venous return and preload
No effect on CO, HR or NE release
Decrease LDL and TG, and increase HDL

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26
Q

A1 selective receptor blocker adverse effects

A

Can cause marked postural hypotension and syncope, orthostatic hypotension, especially with initial doses
Usually given at bedtime to minimize hypotensive effects

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27
Q

Prazosin

A

A1 selective receptor blocker
VERY selective
Short half life

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28
Q

Terazosin

A

A1 selective receptor blocker

High bioavailability

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29
Q

Doxazosin

A

A1 selective receptor blocker

High bioavailability

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30
Q

1st generation B blockers

A
Both B1 and B2 blocker
*Propranolol (prototype)
Nadolol
Timolol
Pindolol - partial agonist
Carteolol - partial agonist
Sotalol - ISA
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31
Q

2nd generation B blockers

A
Cardioselective
*Atenolol 
*Metoprolol
Bisoprolol
*Esmolol - very short acting, use during surgery
Acebutolol - partial agonist, ISA
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32
Q

Alpha and beta blockers (3rd generation)

A

Labetolol

Carvedilol

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33
Q

Nonselective Vasodilating (3rd generation B blocker)

A

Carteolol

Bucindolo

34
Q

Selective Vasodilating (3rd generation B blocker)

A

Betaxolol

Carteolol

35
Q

Mechanism of vasodilation of 3rd generation B blocker

A

Block Ca -> block contraction

Antioxidant

36
Q

Clinical uses of B blocker

A

HTN - decrease CO and slowly decrease peripheral resistance
Ischemic Heart Disease - Angina, myocardial infarction, acute coronary syndromes
MI prophylaxis
CHF
Arrhythmias - tachycardia

37
Q

Thyrotoxicosis and B blocker

A

Hyperthyroid - B receptor sensitivity

Use B blocker to alleviate effects

38
Q

Other B blocker uses

A

Anxiety
Migraines
Pheochromocytoma

39
Q

Pharmacologic effect of B blocker

A

Based on existing sympathetic tone
Increased sympathetic tone (exercise) means greater effect of blocker
HTN and ischemia effect B blocker effects

Decrease HR, CO, exercise tolerance, O2 demand, ectopic foci firing, AV node conduction, infarct size

40
Q

CV effect of B blocker short term

A

Decrease CO and HR

PVR increases to maintain BP

41
Q

CV effect of B blocker long term

A

PVR returns to normal or decreases

A/B blocker - CO maintained with greater decrease in PVR

42
Q

Rhythm effect of B blocker

A

Decrease sinus rate and spontaneous depolarization of foci
Slow conduction
Increase refractory period of AV node

43
Q

B blocker effect on exercise tolerance

A

Blunt increase in HR and contractility
CO less effected because SV increased
Decrease work capacity
B1 selective less problematic

44
Q

CV exercise effects

A

Coronary blood flow increase to meet the demands

Increased catecholamines increase the work of the heart and myocardial oxygen demand

Patients with CAD have fixed narrowing of these vessels which prevents the expected increase in flow, leading to ischemia

45
Q

Beta blockers and myocardial oxygen consumption

A

Decrease oxygen demand (improve relationship of supply and demand)

May increase oxygen demand by increasing end-diastolic pressure and systolic ejection time

Exercise tolerance is improved in those with angina

46
Q

Antihypertensive effects of B blocker

A

Decrease HTN

No decrease in BP of normal patient

47
Q

B blocker effect on plasma renin

A

Block increase in renin (B1)

48
Q

Antihypertensive mechanisms of B blocker

A

Ultimate decrease in PVR

Also decrease in CO

49
Q

Non-selective vasodilating B blockers

A

Carteolol, carvedilol, bucindolol, labetolol

50
Q

B1-selective vasodilating B blockers

A

Betaxolol, celiprolol, nebivolol

51
Q

Mechanism of peripheral vasodilation from B blockers

A
Increase NO
Activate B2 receptors
Block of A1 receptors
Block Ca++ entry
Open K+ channels
Antioxidant activity
Antiproliferative effects
52
Q

Vasodilating B blockers also associated with decreased incidence of

A

Bronchospasm, impaired lipid metabolism, impotence, reduced regional blood flow, increased vascular resistance, and withdrawal symptoms

**Beneficial in patients with insulin resistance, diabetes mellitus, and metabolic syndrome

May be helpful with congestive heart failure and peripheral arterial disease

53
Q

Treatment of angina and MI with B blockers

A

Reduce the severity and frequency of attacks of exertional angina
Improve survival in patients with MI (25%)

Fall in myocardial oxygen demand and increased flow to ischemic areas
Decrease HR, contractility, and arterial BP
Antiarrhythmic effects

54
Q

What type of angina are B blockers not useful for?

A

Vasospastic angina

55
Q

Which B blockers exert cardioprotective effects?

A

Timolol, metoprolol, atenolol, and propranolol

56
Q

In what patients do B blockers decrease left ventricular function

A

Those with limited cardiac reserve that depend on sympathetic stimulation

57
Q

Treating CHF with B blocker

A

Prevent HF in greater than 50%
Reduce strokes by 38%
CAD and CV events decreased
Improve ventricular remodeling - increase LVEF

**Only in stable CHF
Use with ACE, digoxin, and diuretic

58
Q

Decrease mortality rate of CHF with B blockers:

A

65% by carvedilol
35% by metoprolol
35% by bisoprolol

59
Q

Bronchial SM contraindications with B blockers

A

Block bronchodilation

Precaution or contraindication in asthma and COPD

60
Q

Metabolic contraindications with B blockers

A

Effects on lipolysis and glycogenolysis

May mask signs of hypoglycemia in DM

61
Q

Common side effects of B blockers

A

Dizziness, fatigue, diarrhea, constipation, nausea, depression, sexual dysfunction, bizarre dreams

62
Q

Severe but rare side effects of B blockers

A

Purpura, rash, fever

63
Q

B blockers may interfere with what tests?

A

SGOT and BUN

64
Q

Chronic use of B blockers

A

Increase VLDL and decrease HDL

65
Q

Sudden withdrawal of B blockers

A

Rebound HTN, anginal attack and possibly MI

Chronic therapy increase B receptors (increase sensitivity)

66
Q

Other contraindications of B blockers

A

Acute treatment of decompensated heart failure
2nd and 3rd degree heart block
Cardiogenic shock

67
Q

Drug interactions with B blockers

A

Other hypotensive medications (reserpine, guanethidine, methyldopa)
Other antiarrhythmic agents (CCBs, lidocaine)
Insulin and oral hypoglycemic drugs
Masks symptoms of hyperthyroidism

68
Q

Nadolol

A

Nonselective B blocker

Longer acting, once-per-day dosing

69
Q

Timolol

A

Nonselective B blocker

More potent than propranolol

70
Q

Pindolol

A

Nonselective B blocker
Partial agonist and blockade
Less incidence of rebound hypertension
Less bradycardia

71
Q

Carteolol

A

Nonselective B blocker

Vasodilating properties

72
Q

B1 selective blockers

A

B1»>B2
High enough doses activate B2
Less bronchospasm but still no use with asthma
Does not prolong hypoglycemia

73
Q

Atenolol

A

B1 selective

Use for HTN

74
Q

Metoprolol

A

B1 selective

Use for HTN and CHF

75
Q

Acebutolol

A

B1 selective
Partial agonist
Use for HTN and arrhythmias

76
Q

Bisoprolol

A

B1 selective

Dramatic benefits for CHF

77
Q

Esmolol

A

B1 selective
Short acting and rapid onset
Use for tachycardia and HTN around surgery
Use in electroconvulsive therapy

78
Q

Labetolol

A

Selective A1 blocker
Nonselective B1 and B2 blocker
Partial agonist at B2
Use with HTN and pheochromocytoma

79
Q

Carvedilol

A

Nonselective B blocker and A blocker

Use for CHF

80
Q

Methyldopa

A

False NT
Centrally acting A2 agonist
Decrease sympathetic flow and decrease BP
**Use in pregnant women
Can cause dry mouth, sedation and sexual dysfunction

81
Q

Clonidine

A

Centrally acting A2 agonist
Use for essential HTN
Off label use for withdrawal symptoms
Can cause dry mouth, sedation and impotence

82
Q

Sudden withdrawal of clonidine

A

HTN crisis