Exam II CV Drugs antagonists Flashcards
Mechanism of Action
Binds ___ or ___with alpha receptors
[Alpha-adrenergic Antagonists]
competitively or covalently
MOA:
Prevent the effect of ___ and other ___ ___from interacting with the alpha receptor
[Alpha-adrenergic Antagonists]
catecholamines and other alpha agonists
MOA:
Located in the ___ and ___
[Alpha-adrenergic Antagonists]
heart and peripheral vasculature
Effects
Vaso___
___ ___
Reflex ___
Blocks ___ of insulin secretion
[Alpha-adrenergic Antagonists]
dilation
Orthostatic hypotension
tachycardia
inhibition
Effects
Side effects prevent use as essential ____
If beta blockade is not present, ___cardiac stimulation is allowed.
[Alpha-adrenergic Antagonists]
antihypertensives
maximal
MoA – ___ ___
[Phentolamine (Regitine)]
competitive binding
Nonselective – ___ and ___
[Phentolamine (Regitine)]
alpha1 and alpha2
Effects:
___-α1 blockade and direct action on vascular smooth muscle
[Phentolamine (Regitine)]
Vasodilation
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)]
reflex and α2 blockade
peristalsis, diarrhea, parasympathetic
Uses
Acute HTN emergencies, ___
Accidental infiltration of a ___ (___-___ mg in 10 ml)
[Phentolamine (Regitine)]
pheochromocytoma
sympathomimetic, 5-15 mg
Onset –___minutes
Duration – ___-___minutes
Infusion:
[Phentolamine (Regitine)]
2
10-15
1 – 10 mcg/kg/min
MoA – ___ __binding to α-receptors
Nonselective, ___>___
[Phenoxybenzamine (Dibenzyline)]
irreversible covalent
α1>α2
Effects:
___ – orthostatic hypotension exaggerated with hypovolemia, HTN
[Phenoxybenzamine (Dibenzyline)]
Vasodilation
Effects:
Impairment of ___ ___(lower BP with hypovolemia and vasodilating drugs like volatile agents)
[Phenoxybenzamine (Dibenzyline)]
compensatory vasoconstriction
Effects:
___ CO
[Phenoxybenzamine (Dibenzyline)]
Increased
Effects:
Very little change in ___ ___ flow even with ___ BP
[Phenoxybenzamine (Dibenzyline)]
renal blood, decreased
Effects:
Prevents the inhibition of ___ ___
[Phenoxybenzamine (Dibenzyline)]
insulin secretion
Effects:
Pupil ___
[Phenoxybenzamine (Dibenzyline)]
constriction
Effects:
Chronic use may cause ___
[Phenoxybenzamine (Dibenzyline)]
sedation
Effects:
Nasal ___
[Phenoxybenzamine (Dibenzyline)]
congestion
Uses:
Control BP in ___
[Phenoxybenzamine (Dibenzyline)]
pheochromocytoma
Uses:
In trauma patients, used to ___vasoconstriction (shock), only after ___ ___
[Phenoxybenzamine (Dibenzyline)]
reverse, volume replacement
Uses:
___ syndrome
[Phenoxybenzamine (Dibenzyline)]
Raynaud’s
Onset: up to ___ minutes (IV)
Elimination ½ life: ___hours (duration can last up to 4 days)
[Phenoxybenzamine (Dibenzyline)]
60
24
MoA – ___, ___binding with alpha receptors
[Prazosin (Minipress)]
competitive, reversible
Selective – ___ ___
[Prazosin (Minipress)]
α1 antagonist
Effects:
Vasodilation of both ___ and ___
[Prazosin (Minipress)]
arterioles and veins
Effects:
Less reflex ____(___not blocked)
[Prazosin (Minipress)]
tachycardia, alpha2
Uses:
___tension
Severe___
Onset: within 2 hours
Duration: 10-24 hours
[Prazosin (Minipress)]
Hyper
CHF
Onset: ___ hours
Duration: ___-___ hours
[Prazosin (Minipress)]
within 2
10-24
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.
Selective - ___ ___
[Doxazosin (Cardura)]
α1 antagonist
Once daily dose
Peak ___ to __ hours
Elimination ½ life ___hours
[Doxazosin (Cardura)]
2 to 3 hours
22
Indications:
Benign prostatic hypertrophy
___tension treatment
[Doxazosin (Cardura)]
Hyper
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
MOA:
Prolonged or chronic use of ___ ___causes up-regulation of ___receptors.
[Beta-adrenergic Antagonists]
beta blockers, beta
Nonselective – block both ___ and ___
___, ___
[Classifications]
β1 and β2
Propranolol, timolol
Cardioselective – block ___
___, ___, ___
[Classifications]
β1
Metoprolol, atenolol, esmolol
Partial antagonist – intrinsic ___effect
___myocardial depression and HR reduction
[Classifications]
sympathomimetic
Less
Pure antagonist – ___ ___ effect
[Classifications]
no sympathomimetic
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
Β1 blockade - Removes ___ ___ to the heart
[Effects of beta-adrenergic antagonists]
sympathetic stimulation
Negative inotropic effects
___ ___
[Effects of beta-adrenergic antagonists]
Myocardial depression
Negative chronotropic effects
___, ___
[Effects of beta-adrenergic antagonists]
Slows HR, sinus rate
Negative dromotropic effects
___the conduction of impulse through the ___ ___
Slows rate of ___ ___ ___
[Effects of beta-adrenergic antagonists]
Slows, AV node
phase 4 depolarization
Increase in lusitropy
___ ___
[Effects of beta-adrenergic antagonists]
Ventricular relaxation
Decrease in bathmotropy
Reduced ___
[Effects of beta-adrenergic antagonists]
degree of excitability
Β2 blockade:
Vaso____
[Effects of beta-adrenergic antagonists}
constriction
B2 Blockade
Unopposed alpha vasoconstriction can cause ___ ___ ___
(increased serum K*)
decreased LV ejection
B2 Blockade
Broncho___
[Effects of beta-adrenergic antagonists]
constriction
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
B2 Blockade
Inhibits uptake of ___into ___ ___ cells
[Effects of beta-adrenergic antagonists]
K
skeletal muscle
? Additive myocardial depressant effects with ___
___ to continue
___ > isoflurane
[Effects of beta-adrenergic antagonists]
anesthetics
Safe
halothane
CNS – cross ___ ___ ___ - fatigue, lethargy, vivid dreams, memory loss, depression
[Effects of beta-adrenergic antagonists]
blood/brain barrier
Cross placenta – fetal ___cardia, ___tension, ___glycemia
[Effects of beta-adrenergic antagonists]
Brady, hypo, hypo
GI – ___, ___, ___
[Effects of beta-adrenergic antagonists]
nausea, vomiting, diarrhea
Chronic use – fever, rash, ____, alopecia, ____
[Effects of beta-adrenergic antagonists]
myopathy, thrombocytopenia
___ ___block – slowed conduction may be enhanced
[Contraindications to beta-blockade]
AV heart
___ – eliminates tachycardia that is compensating for decrease in volume
[Contraindications to beta-blockade]
Hypovolemia
____ – increased airway resistance (___ or ___)
[Contraindications to beta-blockade]
COPD, nonselective or high doses
Diabetic – mask signs of ___ (nonselective or high doses)
[Contraindications to beta-blockade]
hypoglycemia
Peripheral vascular disease, Raynaud’s syndrome or ____-___ agonist – vasoconstriction unopposed (nonselective), ____ extremities
[Contraindications to beta-blockade]
alpha-adrenergic, V
Overdose of beta-adrenergic antagonist:
___cardia
___cardiac output
___tension
___shock
Bronch____
____intraventricular conduction of impulses
___glycemia - rarely
Brady
Low
Hypo
Cardiogenic
-ospasm
Prolonged
Hypo
TREATMENT:
___ ___ mcg/kg IV (0.5 mg IV) first
[Overdose of beta-adrenergic antagonist]
Atropine 7
TREATMENT:
Isoproterenol ___-___ mcg/min (with ___beta-blocker)
[Overdose of beta-adrenergic antagonist]
2-25, nonselective
Treatment:
Dobutamine (pure ___agonist) when beta-blockade is from a beta-blocker with ___ ___effects
pharmacologic treatment)
[Overdose of beta-adrenergic antagonist]
β1, no sympathomimetic
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
Treatment:
If heart rate does not ___ with drugs, a ___may be necessary.
[Overdose of beta-adrenergic antagonist]
increase, pacemaker
Treatment:
Hemodialysis – only for minimally ___-___, renally excreted ___ ___(refractory to pharmacologic treatment)
[Overdose of beta-adrenergic antagonist]
protein-bound, beta blockers
Isuprel overcomes competitive binding – requires much higher dose (___-___X) than when beta blockade is absent.
[Overdose of beta-adrenergic antagonist]
5-20
___and ____– avoid, as alpha1 vasoconstriction occurs at the high doses required to overcome the beta blockade
[Overdose of beta-adrenergic antagonist]
Epinephrine and dopamine
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
Myocardial thresholds may be raised to prevent ___capture
[Overdose of beta-adrenergic antagonist]
electromyocardial
Increased ___stimulation due to ____-____ of beta receptors
[Acute withdrawal of beta-blockade]
sympathetic, up-regulation
Within ___-___hours
[Acute withdrawal of beta-blockade]
24-48
Profound ___tension, ___cardia, contractility
[Acute withdrawal of beta-blockade]
hyper, tachy
Avoid: ___ preoperative beta-blockade therapy
Infusion of propranolol ___mg/hr IV
[Acute withdrawal of beta-blockade]
continue
3
Treatment of hypertension:
Decrease ___, decrease ___
[Uses of beta-adrenergic antagonists]
HR, CO
Treatment of hypertension:
Decrease___ in larger doses
[Uses of beta-adrenergic antagonists]
contractility
Treatment of hypertension:
With____, prevention of ___ ___
[Uses of beta-adrenergic antagonists]
vasodilator, reflex tachycardia
Treatment of hypertension:
Decrease___, decrease ___, prevention of Na, water retention
[Uses of beta-adrenergic antagonists]
renin, aldosterone
Management of angina pectoris
Decreased myocardial oxygen consumption – ___, ___
[Uses of beta-adrenergic antagonists]
decreased HR, contractility
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
Post-myocardial infarction:
Not with ___ ___ ___ with ST elevation or___shock
[Uses of beta-adrenergic antagonists]
acute coronary syndrome
cardiogenic
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
Cardiac dysrhythmias:
Decrease activity of___ and ___ through the AV node
[Uses of beta-adrenergic antagonists]
SA node and conduction
Cardiac dysrhythmias:
Slows ___ of ectopic pacemakers
[Uses of beta-adrenergic antagonists]
depolarization
Cardiac dysrhythmias:
Suppresses both ___ and ___ ectopy
[Uses of beta-adrenergic antagonists]
supraventricular and ventricular
Cardiac dysrhythmias:
Rapid suppression of excessive___stimulation (thyrotoxicosis, pheochromocytoma, perioperative stress)
[Uses of beta-adrenergic antagonists]
sympathetic
Cardiac dysrhythmias
Decrease activity of ___ and ___ through the AV node
[Uses of beta-adrenergic antagonists]
SA node and conduction
Cardiac dysrhythmias
Slows depolarization of ___pacemakers
[Uses of beta-adrenergic antagonists]
ectopic
Cardiac dysrhythmias
Suppresses both ___ and ___ ectopy
[Uses of beta-adrenergic antagonists]
supraventricular and ventricular
Cardiac dysrhythmias
Rapid suppression of excessive ___stimulation (thyrotoxicosis, pheochromocytoma, perioperative stress)
[Uses of beta-adrenergic antagonists]
sympathetic
Prevention of excessive sympathetic nervous system activity:
Minimizes response to ___
[Uses of beta-adrenergic antagonists]
laryngoscopy
Prevention of excessive sympathetic nervous system activity:
___cardiomyopathies
[Uses of beta-adrenergic antagonists]
Hypertrophic obstructive
Prevention of excessive sympathetic nervous system activity:
Pheochromocytoma, ___
[Uses of beta-adrenergic antagonists]
hyperthyroidism
Prevention of excessive sympathetic nervous system activity:
Tetralogy of Fallot – ___ cyanosis
[Uses of beta-adrenergic antagonists]
minimize
Prevention of excessive sympathetic nervous system activity:
Prevent reflex ___with ___ use in deliberate hypotension
[Uses of beta-adrenergic antagonists]
tachycardia, vasodilation
Prevention of excessive sympathetic nervous system activity:
Public speaking - ___
[Uses of beta-adrenergic antagonists]
anxiety
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
Management of congestive heart failure (___, ___, __)
[Uses of beta-adrenergic antagonists]
metoprolol, carvedilol, bisoprolol
Management of congestive heart failure (metoprolol, carvedilol, bisoprolol)
___ EF
Increase survival rate in ___ ___
[Uses of beta-adrenergic antagonists]
Improve
chronic HF
Management of congestive heart failure (metoprolol, carvedilol, bisoprolol):
Doses initially ___ and gradually ___
[Uses of beta-adrenergic antagonists]
small, increase
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
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
Lap cholecystectomy
Decrease ___ and ___ analgesic needs
[Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
intraop and postop
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
Lap cholecystectomy
Control group required additional doses of ___
[Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
fentanyl
Lap cholecystectomy
“Modulation of the ___ component of pain”
[Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
sympathetic
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
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
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
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
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.
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
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
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
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
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%
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
Esmolol ___ anesthetic requirements
Anesthesiology 1997;86:364-71
[Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
reduces
Propranolol___opioid analgesia
Can Anaesth Soc J 1983;29:319-24
[Uses of beta-adrenergic antagonists – related to anesthesia and surgery]
potentiates
___-___ 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
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
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
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
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
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
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
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
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
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
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
PBB in patients having non-cardiac surgery: a meta-analysis Trial
[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
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
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
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
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
Should be continued in patients on ___treatment
[Perioperative Beta-blockade]
chronic
Cardiac surgery – benefit reduces risk of ___, ___
[Perioperative Beta-blockade]
SVT, vent arrhythmias
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
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
Non-cardiac – no benefit – reduction in arrhythmias, acute MI is offset by increase in ___, ___
[Perioperative Beta-blockade]
mortality, stroke
Nonselective, pure antagonist, ___=___
Effects:
Decreases HR and contractility (and CO)
Increases peripheral vascular resistance (beta2), including coronary vascular resistance
[Propranolol (Inderal)]
beta1=beta2
Effects:
Decreases ___ and ____(and ___)
[Propranolol (Inderal)]
HR, contractility, CO
Effects:
Increases ____ ____ ____ (beta2), including ___ ___ ___
[Propranolol (Inderal)]
peripheral vascular resistance,
coronary vascular resistance
First ___-___introduced clinically.
[Propranolol (Inderal)]
beta-blocker
____ that other drugs are compared to.
[Propranolol (Inderal)]
Standard
Decreased ___ ___ is bigger than decreased ____ ___ flow due to increased vascular resistance.
[Propranolol (Inderal)]
oxygen requirement
coronary blood
Dose: ___mg/kg IV in increments of ___-___ mg q 5 minutes
[Propranolol (Inderal)]
0.05, 0.5-1.0
Metabolism: ____
____ is decreased with decreases in hepatic blood flow; it can decrease its own metabolism.
[Propranolol (Inderal)]
hepatic
Clearance
Elimination ½ life: ___-___hours
[Propranolol (Inderal)]
2-3
Special effects
The metabolism of___local anesthetics is decreased by propranolol due to decreased___ and more.
[Propranolol (Inderal)]
amide, CO
More ____ enters the circulation of a patient on propranolol due to ____pulmonary uptake
[Propranolol (Inderal)]
fentanyl
decreased
____selective
[Nadolol (Corgard)]
Non
Long duration of action – given ___daily
[Nadolol (Corgard)]
once
Metabolism – ___excreted unchanged by the ____, in the bile
[Nadolol (Corgard)]
75%, kidneys
Elimination 1/2 life: ___-___hours
[Nadolol (Corgard)]
20-40
___selective
[Timolol]
Non
Topical eye gtts for ____
[Timolol]
glaucoma
___ and ___ caused by gtts during anesthesia
[Timolol]
Bradycardia and hypotension
Can cause apnea in neonates with immature ___ ___ ___
[Timolol]
blood brain barrier
Selective for ___-receptors
[Metoprolol (Lopressor)]
beta1
Effects:
Blocks ___ and chronotropic responses
[Metoprolol (Lopressor)]
inotropic
___ receptors remain unblocked allowing bronchodilation, vasodilation, and metabolic stability (unless ___ doses are used)
[Metoprolol (Lopressor)]
beta2, higher
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
Metabolism: ___
Elimination ½ life: ___hours
[Metoprolol (Lopressor)]
hepatic
Elimination ½ life: ___hours
[Metoprolol (Lopressor)]
3-4
MOST selective ___ ___
[Atenolol (Tenormin)]
beta1 antagonist
Elimination: ___ ___
[Atenolol (Tenormin)]
renal excretion
Elimination ½ life: ___hours
[Atenolol (Tenormin)]
6-7
Does not interfere with ___, can be given with caution to ___patients.
[Atenolol (Tenormin)]
metabolism, diabetic
Betaxolol
Alternative to___(nonselective)
[Cardioselective beta1 antagonists]
timolol
Betaxolol
Reduces ___ as well as ___intraocular pressure, whether or not accompanied by glaucoma
[Cardioselective beta1 antagonists]
elevated, normal,
Betaxolol
Minimal ___ and ___effects with clinical doses
[Cardioselective beta1 antagonists]
pulmonary and cardiac
Bisoprolol
Prominent effect – ___ ___
[Cardioselective beta1 antagonists]
decreased HR
Bisprolol
Treatment of essential ___ ___CHF
[Cardioselective beta1 antagonists]
HTN,mild to moderate
Selective ___ ___
[Esmolol (Brevibloc)]
beta1 antagonist
Dose: ___mg/kg IV over ___seconds
[Esmolol (Brevibloc)]
0.5, 60
Onset: within ___minutes
[Esmolol (Brevibloc)]
5
Duration: ___-___ minutes
[Esmolol (Brevibloc)]
10-30
Metabolism: rapid hydrolysis by ___ ___(independent of renal and hepatic function)
[Esmolol (Brevibloc)]
plasma esterases
Elimination ½ life:___minutes
[Esmolol (Brevibloc)]
9
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
Pheochromocytoma, thyrotoxicosis, ___-___ cardiovascular toxicity*
[Esmolol (Brevibloc)]
cocaine-induced
Tetralogy of Fallot and ___ ___ cardiomyopathy
[Esmolol (Brevibloc)]
hypertrophic obstructive
Cardiac surgery – ___ ___
[Esmolol (Brevibloc)]
off bypass
Reduce requirements of ___, ___**
[Esmolol (Brevibloc)]
propofol, opioids
ECT – ___mcg/kg/min
[Esmolol (Brevibloc)]
500
*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
Labetalol (Normodyne, Trandate)
Selective ____
[Combined alpha- and beta-adrenergic antagonist’
alpha1
Labetalol (Normodyne, Trandate)
Nonselective ____ and ___
[Combined alpha- and beta-adrenergic antagonist’
beta1 and beta2
Labetalol (Normodyne, Trandate)
1/4 to 1/3 as potent as ____ in beta blockade
[Combined alpha- and beta-adrenergic antagonist’
propranolol
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
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
Dose: ___ to ___ mg/kg IV
[Labetalol]
0.1 to 0.5
Onset of peak effect: ___-___ minutes
[Labetalol]
5-10
Metabolism: conjugation of glucuronic acid (hepatic)
[Labetalol]
conjugation of glucuronic acid (hepatic)
Elimination ½ life: ___-__ hours
[Labetalol]
5-8
Uses:
Hyp__tensive emergencies, ___creased sympathetic activity, pheochromocytoma
Angina pectoris
Controlled, deliberate ___tension
[Labetalol]
Hypertensive, increased, hypotension
___-___ mg IV decrease BP, but not excessively – may repeat as needed
[Labetalol]
20-80
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
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
Combination –
___ blocking activity
[Carvedilol (Coreg)]
alpha1
Nonselective or selective beta blocking
[Carvedilol (Coreg)]
Nonselective
No intrinsic ___agonist effect (different from labetalol)
[Carvedilol (Coreg)]
beta
Metabolites produce weak ___ effect
[Carvedilol (Coreg)]
vasodilating
