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CV II Exam 3 > Adrenergic agonists and antagonists > Flashcards

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
A1 selective receptor blocker
Treat essential HTN Decrease PVR, venous return and preload No effect on CO, HR or NE release Decrease LDL and TG, and increase HDL
26
A1 selective receptor blocker adverse effects
Can cause marked postural hypotension and syncope, orthostatic hypotension, especially with initial doses Usually given at bedtime to minimize hypotensive effects
27
Prazosin
A1 selective receptor blocker VERY selective Short half life
28
Terazosin
A1 selective receptor blocker | High bioavailability
29
Doxazosin
A1 selective receptor blocker | High bioavailability
30
1st generation B blockers
``` Both B1 and B2 blocker *Propranolol (prototype) Nadolol Timolol Pindolol - partial agonist Carteolol - partial agonist Sotalol - ISA ```
31
2nd generation B blockers
``` Cardioselective *Atenolol *Metoprolol Bisoprolol *Esmolol - very short acting, use during surgery Acebutolol - partial agonist, ISA ```
32
Alpha and beta blockers (3rd generation)
Labetolol | Carvedilol
33
Nonselective Vasodilating (3rd generation B blocker)
Carteolol | Bucindolo
34
Selective Vasodilating (3rd generation B blocker)
Betaxolol | Carteolol
35
Mechanism of vasodilation of 3rd generation B blocker
Block Ca -> block contraction | Antioxidant
36
Clinical uses of B blocker
HTN - decrease CO and slowly decrease peripheral resistance Ischemic Heart Disease - Angina, myocardial infarction, acute coronary syndromes MI prophylaxis CHF Arrhythmias - tachycardia
37
Thyrotoxicosis and B blocker
Hyperthyroid - B receptor sensitivity | Use B blocker to alleviate effects
38
Other B blocker uses
Anxiety Migraines Pheochromocytoma
39
Pharmacologic effect of B blocker
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
CV effect of B blocker short term
Decrease CO and HR | PVR increases to maintain BP
41
CV effect of B blocker long term
PVR returns to normal or decreases A/B blocker - CO maintained with greater decrease in PVR
42
Rhythm effect of B blocker
Decrease sinus rate and spontaneous depolarization of foci Slow conduction Increase refractory period of AV node
43
B blocker effect on exercise tolerance
Blunt increase in HR and contractility CO less effected because SV increased Decrease work capacity B1 selective less problematic
44
CV exercise effects
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
Beta blockers and myocardial oxygen consumption
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
Antihypertensive effects of B blocker
Decrease HTN No decrease in BP of normal patient
47
B blocker effect on plasma renin
Block increase in renin (B1)
48
Antihypertensive mechanisms of B blocker
Ultimate decrease in PVR | Also decrease in CO
49
Non-selective vasodilating B blockers
Carteolol, carvedilol, bucindolol, labetolol
50
B1-selective vasodilating B blockers
Betaxolol, celiprolol, nebivolol
51
Mechanism of peripheral vasodilation from B blockers
``` Increase NO Activate B2 receptors Block of A1 receptors Block Ca++ entry Open K+ channels Antioxidant activity Antiproliferative effects ```
52
Vasodilating B blockers also associated with decreased incidence of
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
Treatment of angina and MI with B blockers
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
What type of angina are B blockers not useful for?
Vasospastic angina
55
Which B blockers exert cardioprotective effects?
Timolol, metoprolol, atenolol, and propranolol
56
In what patients do B blockers decrease left ventricular function
Those with limited cardiac reserve that depend on sympathetic stimulation
57
Treating CHF with B blocker
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
Decrease mortality rate of CHF with B blockers:
65% by carvedilol 35% by metoprolol 35% by bisoprolol
59
Bronchial SM contraindications with B blockers
Block bronchodilation | Precaution or contraindication in asthma and COPD
60
Metabolic contraindications with B blockers
Effects on lipolysis and glycogenolysis | May mask signs of hypoglycemia in DM
61
Common side effects of B blockers
Dizziness, fatigue, diarrhea, constipation, nausea, depression, sexual dysfunction, bizarre dreams
62
Severe but rare side effects of B blockers
Purpura, rash, fever
63
B blockers may interfere with what tests?
SGOT and BUN
64
Chronic use of B blockers
Increase VLDL and decrease HDL
65
Sudden withdrawal of B blockers
Rebound HTN, anginal attack and possibly MI Chronic therapy increase B receptors (increase sensitivity)
66
Other contraindications of B blockers
Acute treatment of decompensated heart failure 2nd and 3rd degree heart block Cardiogenic shock
67
Drug interactions with B blockers
Other hypotensive medications (reserpine, guanethidine, methyldopa) Other antiarrhythmic agents (CCBs, lidocaine) Insulin and oral hypoglycemic drugs Masks symptoms of hyperthyroidism
68
Nadolol
Nonselective B blocker | Longer acting, once-per-day dosing
69
Timolol
Nonselective B blocker | More potent than propranolol
70
Pindolol
Nonselective B blocker Partial agonist and blockade Less incidence of rebound hypertension Less bradycardia
71
Carteolol
Nonselective B blocker | Vasodilating properties
72
B1 selective blockers
B1>>>B2 High enough doses activate B2 Less bronchospasm but still no use with asthma Does not prolong hypoglycemia
73
Atenolol
B1 selective | Use for HTN
74
Metoprolol
B1 selective | Use for HTN and CHF
75
Acebutolol
B1 selective Partial agonist Use for HTN and arrhythmias
76
Bisoprolol
B1 selective | Dramatic benefits for CHF
77
Esmolol
B1 selective Short acting and rapid onset Use for tachycardia and HTN around surgery Use in electroconvulsive therapy
78
Labetolol
Selective A1 blocker Nonselective B1 and B2 blocker Partial agonist at B2 Use with HTN and pheochromocytoma
79
Carvedilol
Nonselective B blocker and A blocker | Use for CHF
80
Methyldopa
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
Clonidine
Centrally acting A2 agonist Use for essential HTN Off label use for withdrawal symptoms Can cause dry mouth, sedation and impotence
82
Sudden withdrawal of clonidine
HTN crisis

CV II Exam 3 (13 decks)

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