Exam II CV Drugs antagonists Flashcards

1
Q

Mechanism of Action
Binds ___ or ___with alpha receptors

[Alpha-adrenergic Antagonists]

A

competitively or covalently

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2
Q

MOA:
Prevent the effect of ___ and other ___ ___from interacting with the alpha receptor

[Alpha-adrenergic Antagonists]

A

catecholamines and other alpha agonists

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3
Q

MOA:
Located in the ___ and ___
[Alpha-adrenergic Antagonists]

A

heart and peripheral vasculature

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4
Q

Effects
Vaso___
___ ___
Reflex ___
Blocks ___ of insulin secretion

[Alpha-adrenergic Antagonists]

A

dilation
Orthostatic hypotension
tachycardia
inhibition

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5
Q

Effects
Side effects prevent use as essential ____

If beta blockade is not present, ___cardiac stimulation is allowed.

[Alpha-adrenergic Antagonists]

A

antihypertensives

maximal

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6
Q

MoA – ___ ___

[Phentolamine (Regitine)]

A

competitive binding

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7
Q

Nonselective – ___ and ___

[Phentolamine (Regitine)]

A

alpha1 and alpha2

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8
Q

Effects:
___-α1 blockade and direct action on vascular smooth muscle

[Phentolamine (Regitine)]

A

Vasodilation

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9
Q

Effects:
Cardiac stimulation (increased HR and CO)-___ and ___(blocks neg. feedback of NE)

Side-effects: dysrhythmias, angina, hyper- ___, abd. pain, ___ due to ___ tone

[Phentolamine (Regitine)]

A

reflex and α2 blockade
peristalsis, diarrhea, parasympathetic

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10
Q

Uses
Acute HTN emergencies, ___

Accidental infiltration of a ___ (___-___ mg in 10 ml)

[Phentolamine (Regitine)]

A

pheochromocytoma
sympathomimetic, 5-15 mg

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11
Q

Onset –___minutes
Duration – ___-___minutes
Infusion:
[Phentolamine (Regitine)]

A

2
10-15
1 – 10 mcg/kg/min

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12
Q

MoA – ___ __binding to α-receptors
Nonselective, ___>___

[Phenoxybenzamine (Dibenzyline)]

A

irreversible covalent
α1>α2

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13
Q

Effects:
___ – orthostatic hypotension exaggerated with hypovolemia, HTN

[Phenoxybenzamine (Dibenzyline)]

A

Vasodilation

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14
Q

Effects:
Impairment of ___ ___(lower BP with hypovolemia and vasodilating drugs like volatile agents)

[Phenoxybenzamine (Dibenzyline)]

A

compensatory vasoconstriction

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15
Q

Effects:
___ CO

[Phenoxybenzamine (Dibenzyline)]

A

Increased

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16
Q

Effects:
Very little change in ___ ___ flow even with ___ BP

[Phenoxybenzamine (Dibenzyline)]

A

renal blood, decreased

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17
Q

Effects:
Prevents the inhibition of ___ ___

[Phenoxybenzamine (Dibenzyline)]

A

insulin secretion

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18
Q

Effects:
Pupil ___

[Phenoxybenzamine (Dibenzyline)]

A

constriction

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19
Q

Effects:
Chronic use may cause ___

[Phenoxybenzamine (Dibenzyline)]

A

sedation

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20
Q

Effects:
Nasal ___
[Phenoxybenzamine (Dibenzyline)]

A

congestion

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21
Q

Uses:
Control BP in ___

[Phenoxybenzamine (Dibenzyline)]

A

pheochromocytoma

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22
Q

Uses:
In trauma patients, used to ___vasoconstriction (shock), only after ___ ___

[Phenoxybenzamine (Dibenzyline)]

A

reverse, volume replacement

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23
Q

Uses:
___ syndrome
[Phenoxybenzamine (Dibenzyline)]

A

Raynaud’s

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24
Q

Onset: up to ___ minutes (IV)
Elimination ½ life: ___hours (duration can last up to 4 days)

[Phenoxybenzamine (Dibenzyline)]

A

60
24

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25
MoA – ___, ___binding with alpha receptors [Prazosin (Minipress)]
competitive, reversible
26
Selective – ___ ___ [Prazosin (Minipress)]
α1 antagonist
27
Effects: Vasodilation of both ___ and ___ [Prazosin (Minipress)]
arterioles and veins
28
Effects: Less reflex ____(___not blocked) [Prazosin (Minipress)]
tachycardia, alpha2
29
Uses: ___tension Severe___ Onset: within 2 hours Duration: 10-24 hours [Prazosin (Minipress)]
Hyper CHF
30
Onset: ___ hours Duration: ___-___ hours [Prazosin (Minipress)]
within 2 10-24
31
Another alpha blocker that you may see patients taking is ___(Cardura), which is used to treat both ___ and ___ [Prazosin (Minipress)]
Doxazosin HTN and benign prostatic hypertension.
32
Selective - ___ ___ [Doxazosin (Cardura)]
α1 antagonist
33
Once daily dose Peak ___ to __ hours Elimination ½ life ___hours [Doxazosin (Cardura)]
2 to 3 hours 22
34
Indications: Benign prostatic hypertrophy ___tension treatment [Doxazosin (Cardura)]
Hyper
35
Mechanism of Action Competitive binding to ___receptors to block the effect of ___and agonists on the heart and smooth muscles of airways and blood vessels [Beta-adrenergic Antagonists]
beta, catecholamines
36
MOA: Prolonged or chronic use of ___ ___causes up-regulation of ___receptors. [Beta-adrenergic Antagonists]
beta blockers, beta
37
Nonselective – block both ___ and ___ ___, ___ [Classifications]
β1 and β2 Propranolol, timolol
38
Cardioselective – block ___ ___, ___, ___ [Classifications]
β1 Metoprolol, atenolol, esmolol
39
Partial antagonist – intrinsic ___effect ___myocardial depression and HR reduction [Classifications]
sympathomimetic Less
40
Pure antagonist – ___ ___ effect [Classifications]
no sympathomimetic
41
Selectivity is ___-___. If a big enough dose of a cardioselective beta-blocker is given, the effect can impact ___receptors also. [Classifications]
dose-related, beta-2
42
Β1 blockade - Removes ___ ___ to the heart [Effects of beta-adrenergic antagonists]
sympathetic stimulation
43
Negative inotropic effects ___ ___ [Effects of beta-adrenergic antagonists]
Myocardial depression
44
Negative chronotropic effects ___, ___ [Effects of beta-adrenergic antagonists]
Slows HR, sinus rate
45
Negative dromotropic effects ___the conduction of impulse through the ___ ___ Slows rate of ___ ___ ___ [Effects of beta-adrenergic antagonists]
Slows, AV node phase 4 depolarization
46
Increase in lusitropy ___ ___ [Effects of beta-adrenergic antagonists]
Ventricular relaxation
47
Decrease in bathmotropy Reduced ___ [Effects of beta-adrenergic antagonists]
degree of excitability
48
Β2 blockade: Vaso____ [Effects of beta-adrenergic antagonists}
constriction
49
B2 Blockade Unopposed alpha vasoconstriction can cause ___ ___ ___ (increased serum K*)
decreased LV ejection
50
B2 Blockade Broncho___ [Effects of beta-adrenergic antagonists]
constriction
51
B2 Blockade ___ glycogenolysis, blocks ___ related to hypoglycemia, alters fat metabolism (lipolysis). Inhibits uptake of K into skeletal muscle cells [Effects of beta-adrenergic antagonists]
Prevents, tachycardia
52
B2 Blockade Inhibits uptake of ___into ___ ___ cells [Effects of beta-adrenergic antagonists]
K skeletal muscle
53
? Additive myocardial depressant effects with ___ ___ to continue ___ > isoflurane [Effects of beta-adrenergic antagonists]
anesthetics Safe halothane
54
CNS – cross ___ ___ ___ - fatigue, lethargy, vivid dreams, memory loss, depression [Effects of beta-adrenergic antagonists]
blood/brain barrier
55
Cross placenta – fetal ___cardia, ___tension, ___glycemia [Effects of beta-adrenergic antagonists]
Brady, hypo, hypo
56
GI – ___, ___, ___ [Effects of beta-adrenergic antagonists]
nausea, vomiting, diarrhea
57
Chronic use – fever, rash, ____, alopecia, ____ [Effects of beta-adrenergic antagonists]
myopathy, thrombocytopenia
58
___ ___block – slowed conduction may be enhanced [Contraindications to beta-blockade]
AV heart
59
___ – eliminates tachycardia that is compensating for decrease in volume [Contraindications to beta-blockade]
Hypovolemia
60
____ – increased airway resistance (___ or ___) [Contraindications to beta-blockade]
COPD, nonselective or high doses
61
Diabetic – mask signs of ___ (nonselective or high doses) [Contraindications to beta-blockade]
hypoglycemia
62
Peripheral vascular disease, Raynaud’s syndrome or ____-___ agonist – vasoconstriction unopposed (nonselective), ____ extremities [Contraindications to beta-blockade]
alpha-adrenergic, V
63
Overdose of beta-adrenergic antagonist: ___cardia ___cardiac output ___tension ___shock Bronch____ ____intraventricular conduction of impulses ___glycemia - rarely
Brady Low Hypo Cardiogenic -ospasm Prolonged Hypo
64
TREATMENT: ___ ___ mcg/kg IV (0.5 mg IV) first [Overdose of beta-adrenergic antagonist]
Atropine 7
65
TREATMENT: Isoproterenol ___-___ mcg/min (with ___beta-blocker) [Overdose of beta-adrenergic antagonist]
2-25, nonselective
66
Treatment: Dobutamine (pure ___agonist) when beta-blockade is from a beta-blocker with ___ ___effects pharmacologic treatment) [Overdose of beta-adrenergic antagonist]
β1, no sympathomimetic
67
Treatment: Glucagon (___-___mg)(drug of choice due to ____ action) and CaCl (250 mg to 1 gm) increase cardiac function independent of the blocked receptors. [Overdose of beta-adrenergic antagonist]
1-10, independent, CaCl, increase
68
Treatment: If heart rate does not ___ with drugs, a ___may be necessary. [Overdose of beta-adrenergic antagonist]
increase, pacemaker
69
Treatment: Hemodialysis – only for minimally ___-___, renally excreted ___ ___(refractory to pharmacologic treatment) [Overdose of beta-adrenergic antagonist]
protein-bound, beta blockers
70
Isuprel overcomes competitive binding – requires much higher dose (___-___X) than when beta blockade is absent. [Overdose of beta-adrenergic antagonist]
5-20
71
___and ____– avoid, as alpha1 vasoconstriction occurs at the high doses required to overcome the beta blockade [Overdose of beta-adrenergic antagonist]
Epinephrine and dopamine
72
Glucagon – MOA is not via ___ receptors – stimulates ___ ___ and increases ___ ___ – especially effective in life-threatening bradycardia [Overdose of beta-adrenergic antagonist]
beta, adenylate cyclase, intracellular cAMP
73
Myocardial thresholds may be raised to prevent ___capture [Overdose of beta-adrenergic antagonist]
electromyocardial
74
Increased ___stimulation due to ____-____ of beta receptors [Acute withdrawal of beta-blockade]
sympathetic, up-regulation
75
Within ___-___hours [Acute withdrawal of beta-blockade]
24-48
76
Profound ___tension, ___cardia, contractility [Acute withdrawal of beta-blockade]
hyper, tachy
77
Avoid: ___ preoperative beta-blockade therapy Infusion of propranolol ___mg/hr IV [Acute withdrawal of beta-blockade]
continue 3
78
Treatment of hypertension: Decrease ___, decrease ___ [Uses of beta-adrenergic antagonists]
HR, CO
79
Treatment of hypertension: Decrease___ in larger doses [Uses of beta-adrenergic antagonists]
contractility
80
Treatment of hypertension: With____, prevention of ___ ___ [Uses of beta-adrenergic antagonists]
vasodilator, reflex tachycardia
81
Treatment of hypertension: Decrease___, decrease ___, prevention of Na, water retention [Uses of beta-adrenergic antagonists]
renin, aldosterone
82
Management of angina pectoris Decreased myocardial oxygen consumption – ___, ___ [Uses of beta-adrenergic antagonists]
decreased HR, contractility
83
Post-myocardial infarction Historically - Decreases ___ and ___ Increases chances of survival ___-___% Begin within ___ to ___ days after MI and continue for 1-3 years Within ___hours of onset of ___ may actually decrease infarct size and ___ [Uses of beta-adrenergic antagonists]
mortality and reinfarctions 20-40 5 to 28 12, infarct, dysrhythmias
84
Post-myocardial infarction: Not with ___ ___ ___ with ST elevation or___shock [Uses of beta-adrenergic antagonists]
acute coronary syndrome cardiogenic
85
Post-myocardial infarction: Both ___ and ___ drugs have a cardioprotective effect; nonselective effect on ___ (prevents reduction) may decrease ___ [Uses of beta-adrenergic antagonists]
selective and nonselective K dysrhythmias
86
Cardiac dysrhythmias: Decrease activity of___ and ___ through the AV node [Uses of beta-adrenergic antagonists]
SA node and conduction
87
Cardiac dysrhythmias: Slows ___ of ectopic pacemakers [Uses of beta-adrenergic antagonists]
depolarization
88
Cardiac dysrhythmias: Suppresses both ___ and ___ ectopy [Uses of beta-adrenergic antagonists]
supraventricular and ventricular
89
Cardiac dysrhythmias: Rapid suppression of excessive___stimulation (thyrotoxicosis, pheochromocytoma, perioperative stress) [Uses of beta-adrenergic antagonists]
sympathetic
90
Cardiac dysrhythmias Decrease activity of ___ and ___ through the AV node [Uses of beta-adrenergic antagonists]
SA node and conduction
91
Cardiac dysrhythmias Slows depolarization of ___pacemakers [Uses of beta-adrenergic antagonists]
ectopic
92
Cardiac dysrhythmias Suppresses both ___ and ___ ectopy [Uses of beta-adrenergic antagonists]
supraventricular and ventricular
93
Cardiac dysrhythmias Rapid suppression of excessive ___stimulation (thyrotoxicosis, pheochromocytoma, perioperative stress) [Uses of beta-adrenergic antagonists]
sympathetic
94
Prevention of excessive sympathetic nervous system activity: Minimizes response to ___ [Uses of beta-adrenergic antagonists]
laryngoscopy
95
Prevention of excessive sympathetic nervous system activity: ___cardiomyopathies [Uses of beta-adrenergic antagonists]
Hypertrophic obstructive
96
Prevention of excessive sympathetic nervous system activity: Pheochromocytoma, ___ [Uses of beta-adrenergic antagonists]
hyperthyroidism
97
Prevention of excessive sympathetic nervous system activity: Tetralogy of Fallot – ___ cyanosis [Uses of beta-adrenergic antagonists]
minimize
98
Prevention of excessive sympathetic nervous system activity: Prevent reflex ___with ___ use in deliberate hypotension [Uses of beta-adrenergic antagonists]
tachycardia, vasodilation
99
Prevention of excessive sympathetic nervous system activity: Public speaking - ___ [Uses of beta-adrenergic antagonists]
anxiety
100
Prevention of excessive sympathetic nervous system activity: Preop prep for hyperthyroid pt – ___ or ___IV or ___-___ mg po daily [Uses of beta-adrenergic antagonists]
esmolol or propranolol 40-320
101
Management of congestive heart failure (___, ___, __) [Uses of beta-adrenergic antagonists]
metoprolol, carvedilol, bisoprolol
102
Management of congestive heart failure (metoprolol, carvedilol, bisoprolol) ___ EF Increase survival rate in ___ ___ [Uses of beta-adrenergic antagonists]
Improve chronic HF
103
Management of congestive heart failure (metoprolol, carvedilol, bisoprolol): Doses initially ___ and gradually ___ [Uses of beta-adrenergic antagonists]
small, increase
104
Rhinoplasty patients ___ postop pain Esmolol ___-___ mcg/kg/min with propofol and remifentanil [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
Decreased, 5-10
105
Rhinoplasty patients Decreased postop pain: Group E had decreased ___ ___ for first 3 hours, decreased ___ use, less variations in BP, HR [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
postop pain, morphine
106
Lap cholecystectomy Decrease ___ and ___ analgesic needs [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
intraop and postop
107
Lap cholecystectomy Esmolol ___ mg/kg IV, followed by infusion of ___mcg/kg/min through surgery [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
0.5, 0.05
108
Lap cholecystectomy Control group required additional doses of ___ [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
fentanyl
109
Lap cholecystectomy “Modulation of the ___ component of pain” [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
sympathetic
110
Lap cholecystectomy patients ___ infusion added to either ___/___ or desflurane/remifentanil anesthetics with two groups without esmolol [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
Esmolol, propofol/remifentanil
111
Lap cholecystectomy patients: Pain score and PONV incidence was ___ in p/r/e group. [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
lowest
112
Lap cholecystectomy patients: D/r/e group had ___pain score and PONV incidence compared to d/r group [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
lower
113
Lap cholecystectomy patients: Both groups receiving esmolol had ___ HR, but ___BP compared to controls. [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
lower, similar
114
Lap cholecystectomy patients: Both groups receiving esmolol had significantly ___ and ___ [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
lower anesthesia and opioid requirements.
115
Preoperative beta-blocker therapy ___ 30-day mortality in coronary surgery Br J of Anaes 2003;90:27-31 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
reduces
116
Perioperative beta-blockade ___perioperative ischemia, mortality, and cardiovascular complications for up to ___ ___post-op. N Engl J Med 1996;335:1713-20 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
reduced, 2 years
117
Preoperative beta-blockade improved ___ and ___in CABG patients JAMA 2002;287:2221-7 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
mortality and morbidity
118
beta-blockade in elderly patients having ___-___ surgery reduced analgesic requirements, allowed ___recovery from anesthesia, and ___hemodynamic stability Anesthesiology 1999;91:1674-86 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
non-cardiac, faster, improved
119
Preoperative ___-___to uncontrolled hypertensive patients reduced myocardial ischemia from ___ to ___% Anesthesiology 1988;68:495-500 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
beta-blockade 28% to 2%
120
Preoperative, perioperative, and postoperative beta-blockade reduced post-op ___ ___ in at-risk patients after ___ surgery Anesthesiology 1998;88:7-17 N Engl J Med 1996;335:1713-20 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
myocardial ischemia noncardiac
121
Esmolol ___ anesthetic requirements Anesthesiology 1997;86:364-71 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
reduces
122
Propranolol___opioid analgesia Can Anaesth Soc J 1983;29:319-24 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
potentiates
123
___-___ reduces perception of noxious stimuli and has an anxiolytic effect J Pharm Pharmacol 1966;18:317-8 Lancet 1966;1:788-90 [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
beta-blockade
124
Effects of beta-blockade that causes cardioprotection during surgery: Improvement of the ___ ___ supply-demand balance [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
myocardial oxygen
125
Effects of beta-blockade that causes cardioprotection during surgery: Decrease oxygen requirements by ___ and ___ [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
slowing HR and decreasing contractility
126
Effects of beta-blockade that causes cardioprotection during surgery: Blocks ___from the receptors to avoid increased sympathetic stimulation. [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
catecholamines
127
Effects of beta-blockade that causes cardioprotection during surgery: Prolongs ___ and increases time for oxygen delivery [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
diastole
128
Effects of beta-blockade that causes cardioprotection during surgery: Suppression of dysrhythmias – improves long-term ___ [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
mortality
129
Effects of beta-blockade that causes cardioprotection during surgery: Increase blood flow to ___myocardium [Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
ischemic
130
POISE = Peri-Operative Ischemic Evaluation randomized, controlled clinical trial 8,351 patients from 190 hospitals 23 countries patients accepted from 2002-2007 ___-___surgical procedures greater than ___ years of age hospitalized at least ___hours post-op [POISE trial, 2008]
non-cardiac 45 24
131
30 day results of PBB - positive: -Significant reduction in___ (4.2% in metoprolol group vs. 5.7% in placebo group) -Reduced need for ___ revascularization -Reduction in number of patients developing ___ ___ [POISE trial]
MI’s coronary atrial fibrillation
132
30 day results of PBB - negative: -Increase in total ___(3.1% from metoprolol group vs. 2.3% placebo group) -Increase in ___incidence -Increase in clinically significant ___ and ___ [POISE trial]
mortality stroke hypotension and bradycardia
133
Strokes seen in the POISE trial: excessive hypotension likely explains these strokes as the etiology of 47 of the 60 observed strokes was ___. For every 1000 patients undergoing non-cardiac surgery, the administration of ____perioperatively may prevent: 15 patients from suffering an MI 3 from undergoing coronary revascularization 7 from developing new significant A fib. But may contribute to: More than 8 patient deaths and 5 strokes [POISE trial]
ischemic metoprolol
134
PBB in patients having non-cardiac surgery: a meta-analysis Trial
135
[2009 ACCF/AHA Focused Update on Perioperative Beta-blockade] Recommends PBB for: Patients who are receiving ___-___ for the treatment of conditions with ACC/AHA Class I indication for the drug (I C)
beta-blockers
136
Beta-blockers are probably recommended in patients: Undergoing ___surgery who suffer from CAD or show ischemia on ____ testing (IIa B) In the presence of CAD or high cardiac risk (more than one risk factor) who are undergoing intermediate-risk surgery (IIa B) Where preoperative assessment for vascular surgery identifies ___ ___ ___ (more than one risk factor; IIa C) [2009 ACCF/AHA Focused Update on Perioperative Beta-blockade]
vascular, preoperative high cardiac risk
137
The usefulness of beta-blockers is uncertain in patients: Undergoing vascular surgery with no risk factors who are not currently taking ___ ___ [2009 ACCF/AHA Focused Update on Perioperative Beta-blockade]
beta-blockers (IIb B
138
Undergoing either ___-___procedures or vascular surgery with a single clinical risk factor in the absence of ___ (IIb C) [2009 ACCF/AHA Focused Update on Perioperative Beta-blockade]
immediate-risk, CAD
139
Beta blockers are not to be given: ____-___ ___-___without titration are not useful and may be harmful to patients not currently taking beta-blockers who are undergoing surgery (III B). Patients undergoing surgery who have an absolute contraindication to ____-____ (III C) [2009 ACCF/AHA Focused Update on Perioperative Beta-blockade]
High-dose beta-blockers beta-blockade
140
Should be continued in patients on ___treatment [Perioperative Beta-blockade]
chronic
141
Cardiac surgery – benefit reduces risk of ___, ___ [Perioperative Beta-blockade]
SVT, vent arrhythmias
142
Should they be indicated perioperatively, should be started between ___ and ___ week before surgery or days to weeks before surgery (this is based on limited evidence). [Perioperative Beta-blockade]
30 days and 1
143
Titration of the beta-blocker to ___ and ___ is necessary in order to minimize or reduce the risk of hypotension. -Heart rate are ___-___ beats per minute -Systolic arterial pressure ___ [Perioperative Beta-blockade]
heart rate and arterial blood pressure 60-80 >100 mm Hg
144
Non-cardiac – no benefit – reduction in arrhythmias, acute MI is offset by increase in ___, ___ [Perioperative Beta-blockade]
mortality, stroke
145
Nonselective, pure antagonist, ___=___ Effects: Decreases HR and contractility (and CO) Increases peripheral vascular resistance (beta2), including coronary vascular resistance [Propranolol (Inderal)]
beta1=beta2
146
Effects: Decreases ___ and ____(and ___) [Propranolol (Inderal)]
HR, contractility, CO
147
Effects: Increases ____ ____ ____ (beta2), including ___ ___ ___ [Propranolol (Inderal)]
peripheral vascular resistance, coronary vascular resistance
148
First ___-___introduced clinically. [Propranolol (Inderal)]
beta-blocker
149
____ that other drugs are compared to. [Propranolol (Inderal)]
Standard
150
Decreased ___ ___ is bigger than decreased ____ ___ flow due to increased vascular resistance. [Propranolol (Inderal)]
oxygen requirement coronary blood
151
Dose: ___mg/kg IV in increments of ___-___ mg q 5 minutes [Propranolol (Inderal)]
0.05, 0.5-1.0
152
Metabolism: ____ ____ is decreased with decreases in hepatic blood flow; it can decrease its own metabolism. [Propranolol (Inderal)]
hepatic Clearance
153
Elimination ½ life: ___-___hours [Propranolol (Inderal)]
2-3
154
Special effects The metabolism of___local anesthetics is decreased by propranolol due to decreased___ and more. [Propranolol (Inderal)]
amide, CO
155
More ____ enters the circulation of a patient on propranolol due to ____pulmonary uptake [Propranolol (Inderal)]
fentanyl decreased
156
____selective [Nadolol (Corgard)]
Non
157
Long duration of action – given ___daily [Nadolol (Corgard)]
once
158
Metabolism – ___excreted unchanged by the ____, in the bile [Nadolol (Corgard)]
75%, kidneys
159
Elimination 1/2 life: ___-___hours [Nadolol (Corgard)]
20-40
160
___selective [Timolol]
Non
161
Topical eye gtts for ____ [Timolol]
glaucoma
162
___ and ___ caused by gtts during anesthesia [Timolol]
Bradycardia and hypotension
163
Can cause apnea in neonates with immature ___ ___ ___ [Timolol]
blood brain barrier
164
Selective for ___-receptors [Metoprolol (Lopressor)]
beta1
165
Effects: Blocks ___ and chronotropic responses [Metoprolol (Lopressor)]
inotropic
166
___ receptors remain unblocked allowing bronchodilation, vasodilation, and metabolic stability (unless ___ doses are used) [Metoprolol (Lopressor)]
beta2, higher
167
Bolus: ___ mg IV (if HR > ___); 2.5 mg IV (if HR 60-80); hold if HR <___ or SBP ___mm Hg [Metoprolol (Lopressor)]
5, 80, 60, <100
168
Metabolism: ___ Elimination ½ life: ___hours [Metoprolol (Lopressor)]
hepatic
169
Elimination ½ life: ___hours [Metoprolol (Lopressor)]
3-4
170
MOST selective ___ ___ [Atenolol (Tenormin)]
beta1 antagonist
171
Elimination: ___ ___ [Atenolol (Tenormin)]
renal excretion
172
Elimination ½ life: ___hours [Atenolol (Tenormin)]
6-7
173
Does not interfere with ___, can be given with caution to ___patients. [Atenolol (Tenormin)]
metabolism, diabetic
174
Betaxolol Alternative to___(nonselective) [Cardioselective beta1 antagonists]
timolol
175
Betaxolol Reduces ___ as well as ___intraocular pressure, whether or not accompanied by glaucoma [Cardioselective beta1 antagonists]
elevated, normal,
176
Betaxolol Minimal ___ and ___effects with clinical doses [Cardioselective beta1 antagonists]
pulmonary and cardiac
177
Bisoprolol Prominent effect – ___ ___ [Cardioselective beta1 antagonists]
decreased HR
178
Bisprolol Treatment of essential ___ ___CHF [Cardioselective beta1 antagonists]
HTN,mild to moderate
179
Selective ___ ___ [Esmolol (Brevibloc)]
beta1 antagonist
180
Dose: ___mg/kg IV over ___seconds [Esmolol (Brevibloc)]
0.5, 60
181
Onset: within ___minutes [Esmolol (Brevibloc)]
5
182
Duration: ___-___ minutes [Esmolol (Brevibloc)]
10-30
183
Metabolism: rapid hydrolysis by ___ ___(independent of renal and hepatic function) [Esmolol (Brevibloc)]
plasma esterases
184
Elimination ½ life:___minutes [Esmolol (Brevibloc)]
9
185
Uses: Protection against ___ and ___ related to laryngoscopy – give esmolol ____ 2 minutes prior to laryngoscopy. Better protection than ___ or ___against HR. [Esmolol (Brevibloc)]
tachycardia and hypertension 150 mg lidocaine or fentanyl
186
Pheochromocytoma, thyrotoxicosis, ___-___ cardiovascular toxicity* [Esmolol (Brevibloc)]
cocaine-induced
187
Tetralogy of Fallot and ___ ___ cardiomyopathy [Esmolol (Brevibloc)]
hypertrophic obstructive
188
Cardiac surgery – ___ ___ [Esmolol (Brevibloc)]
off bypass
189
Reduce requirements of ___, ___** [Esmolol (Brevibloc)]
propofol, opioids
190
ECT – ___mcg/kg/min [Esmolol (Brevibloc)]
500
191
*be careful when treating excessive SNS activity produced by ____ or systemic absorption of topical or subcutaneous ____ = fulminant pulm edema and ____ cardiac collapse (can’t increase HR or contractility to handle increased afterload) [Esmolol (Brevibloc)]
cocaine, epinephrine, irreversible
192
Labetalol (Normodyne, Trandate) Selective ____ [Combined alpha- and beta-adrenergic antagonist'
alpha1
193
Labetalol (Normodyne, Trandate) Nonselective ____ and ___ [Combined alpha- and beta-adrenergic antagonist'
beta1 and beta2
194
Labetalol (Normodyne, Trandate) 1/4 to 1/3 as potent as ____ in beta blockade [Combined alpha- and beta-adrenergic antagonist'
propranolol
195
Labetalol (Normodyne, Trandate) CV effects: __creases SVR (vasodilation-alpha1antagonist and beta2 agonist effect) Prevents reflex ____cardia ____ CO [Combined alpha- and beta-adrenergic antagonist'
Decreases tachycardia Unchanged
196
Labetalol Alpha to beta blockade ratio is ___:___ for IV labetalol ___to ___ as potent as phentolamine [Combined alpha- and beta-adrenergic antagonist'
1:7 1/5 to 1/10
197
Dose: ___ to ___ mg/kg IV [Labetalol]
0.1 to 0.5
198
Onset of peak effect: ___-___ minutes [Labetalol]
5-10
199
Metabolism: conjugation of glucuronic acid (hepatic) [Labetalol]
conjugation of glucuronic acid (hepatic)
200
Elimination ½ life: ___-__ hours [Labetalol]
5-8
201
Uses: Hyp__tensive emergencies, ___creased sympathetic activity, pheochromocytoma Angina pectoris Controlled, deliberate ___tension [Labetalol]
Hypertensive, increased, hypotension
202
___-___ mg IV decrease BP, but not excessively – may repeat as needed [Labetalol]
20-80
203
Side effects ___ ___ – most common ___ – nonspecific beta* Congestive heart failure, bradycardia, heart block (incidence and severity decreased) – beta effects Fluid retention – chronic use necessitates addition diuretic [Labetalol]
Orthostatic hypotension Bronchospasm
204
Esmolol compared to labetalol Selective vs Nonselective and for what? Duration: Prolonged vs short acting what is the duration? Metbolized: plasma esterases vs hepatic? Bronchospam vs selective Onset: Slower vs rapid and what is the time?
Esmolol Labetalol Selective B1 NS B & A1 Short acting 9 min. Prolonged 6-8 hr Plasma esterases Hepatic Selective Bronchospasm* Rapid onset w/i 5 min Slow onset 5-10 m
205
Combination – ___ blocking activity [Carvedilol (Coreg)]
alpha1
206
Nonselective or selective beta blocking [Carvedilol (Coreg)]
Nonselective
207
No intrinsic ___agonist effect (different from labetalol) [Carvedilol (Coreg)]
beta
208
Metabolites produce weak ___ effect [Carvedilol (Coreg)]
vasodilating