Cardiovascular Drugs- Sympathomimetics Flashcards

1
Q

endogenous catecholamines

A
  1. epinephrine
  2. norepinephrine
  3. dopamine
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2
Q

synthetic catecholamines

A
  1. isoproterenol
  2. dobutamine
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3
Q

synthetic noncatecholamines

A
  1. ephedrine
  2. amphetamine
  3. phenylephrine
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4
Q

selective alpha2-adrenergic agonists

A
  1. clonidine
  2. dexmedetomidine
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5
Q

selective beta2-adrenergic agonists

A
  1. albuterol
  2. terbutaline
  3. ritodrine
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6
Q

sympathetic nervous system activation causes

A
  1. cardiac stimulation (increased HR and BP, contractility, susceptibility to ectopy)
  2. bronchdilation
  3. vasoconstriction (decreased flow to skin, GI tract, renal)
  4. vasodilation (improved blood flow to skeletal muscle)
  5. CNS stimulation- increased cognition (except alpha 2)
  6. increased blood sugar (lipolysis & glycogenolysis)
  7. increased rate of coagulation
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7
Q

lipolysis is

A

breakdown of lipids

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8
Q

glycogenolsysi is

A

splitting up of glycogen in the liver, yielding glucose

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9
Q

used to increase __ or increase __ after sympathetic blockade caused by regional anesthesia

A

contractility

vasular tone

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10
Q

used to __ or __ BP (to prevent tissue ischemia) during the time required to correct for hypovolemia or excessive inhaled anesthesia

A

increase or maintain

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11
Q

used to __ of asthmatic

A

relax bronchoconstriction

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12
Q

used to manage __

A

anaphylaxis

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13
Q

used to prolong __

A

regional anesthesia

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14
Q

direct

A

bind to receptors and activate them directly (catecholamines and phenylephrine)

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15
Q

indirect causes the release of

A

norepinephrine from postganglionic sympathetic nerve endings (amphetamine)

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16
Q

indirect blocks

A

the reuptake of norepinephrine to make more in circulation (cocaine, tricyclic antidepressants)

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17
Q

indirect agent might not be effective if patient has

A

denervation injury, or depletion of NT

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18
Q

tachyphylaxis

A

the greater the concentration of the sympathomimetic, the lower the number of receptors in tissues or decreased response

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19
Q

catecholamines are inactivated by enzymes

A
  1. monoamine oxidase (MAO)
  2. Catechol-O-methyltransferase (COMT)
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20
Q

catecholamines termination of effect influenced more by

A

uptake back into postganglion sympathetic nerve endings

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21
Q

catecholamines are filtrated by

A

the lungs of norepinephrine and dopamine

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22
Q

noncatecholamines are inactivated by

A

MAO only- slower

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23
Q

epinephrine stimulates

A

both alpha and beta

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24
Q

most potent alpha stimulator

A

epinephrine

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25
Q

epinephrine stimulation

A

alpha1=alpha2; beta1=beta2

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26
Q

epinephrine is given

A

IV or subq (causes vasoconstriction which slows absorption)

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27
Q

epinephrine __ soluble

A

poorly lipid; lack of cerebral effects

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28
Q

epinephrine uses

A
  1. decrease absorption and prolong duration of local anesthetics
  2. treatment of anaphylactic reactions
  3. treatment of cardiac arrest
  4. increase myocardial contractility
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29
Q

low dose epinephrine dose

A

0.01-0.03 mcg/kg/min

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30
Q

low dose epinephrine beta 1

A

increases HR, BP, CO, inotropy

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31
Q

low dose epinephrine beta 2

A

decrease in DBP due to decrease in SVR (vasodilation in skeletal muscle vessels)

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32
Q

moderate dose epinephrine dose

A

0.03-0.15 mcg/kg/min

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33
Q

moderate dose epinephrine beta 1

A
  1. increase in SBP, HR, CO, inotropy (increase in venous return)
  2. increase in susceptibility to arrhythmias
  3. mixed with alpha
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34
Q

large dose epinephrine dose

A

> 0.15 mcg/kg/min

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35
Q

large dose of epinephrine stimulates

A

beta and alpha-1 but alpha predominates

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36
Q

large dose epinephrine beta and alpha 1

A

vasoconstriction of the skin, mucosa, and hepatorenal vessels (decreased renal blood flow), SVT common

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37
Q

epinephrine respiratory effects

A

smooth muscle relaxed in the bronchi (beta 2)

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38
Q

if beta antagonist is present with epinephrine the respiratory effects is

A

the alpha1 effect causes bronchoconstriction

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39
Q

epinephrine metabolic effect

A

most significant effect of all catecholamines

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40
Q

epinephrine __ blood glucose

A

increase

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41
Q

metabolic effect of epinephrine of beta 2

A

increase glycogenolysis and lipolysis

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42
Q

metabolic effect of epinephrine of alpha 2

A

inhibits release of insulin (hyperglycemia)

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43
Q

epinephrine effects on electrolytes

A

beta 2- stress induced hypokalemia (activation of the sodium-potassium pump on RBCs)

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44
Q

epinephrine causes __ K

A

initial increased

it follows glucose out of hepatic cells

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45
Q

epinephrine ocular effects

A

alpha 1- contraction of the radial muscles of the iris causes pupil dilation; contraction of the orbital muscles causing bulging of the eyes (exophthalmus)

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46
Q

epinephrine GI/GU effects

A

relaxation of GI smooth muscle

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47
Q

epinephrine GI/GU beta effects

A

relaxation of the detrusor muscle of the bladder

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48
Q

epinephrine GI/GU alpha1 effects

A

contracts the sphincter muscles

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49
Q

norepinephrine is

A

a naturally occurring catecholamines released from postganglionic sympathetic nerve endings

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50
Q

norepinephrine is a potent __ agonist with __ agonist effect, but little __ effect

A

alpha

beta1

beta2

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51
Q

norepinephrine stimulation

A

alpha1=alpha2; beta1»beta2

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52
Q

norepinephrine clinical use

A

vasoconstrictor to increase SVR and raise BP

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53
Q

infiltration of norepinephrine into subq tissue can

A

cause necrosis due to vasoconstriction

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54
Q

can treat infiltration for norepinephrine with

A

phentolamine

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55
Q

norepinephrine alpha 1 CV effects

A
  1. vasoconstriction of both arterial and venous vessels of all vascular beds
  2. increased SVR, MAP, increased venous return
  3. decreased HR
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56
Q

norepinephrine beta 1 CV effects

A

overshadowed by the alpha 1 effects causing a decrease in CO, decreased tissue perfusion, decreased kidney blood flow

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57
Q

norepinephrine respiratory effects

A

no beta 2

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58
Q

norepinephrine metabolic effects

A

hyperglycemia unlikely

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59
Q

norepinephrine dose

A

0.02-0.4 mcg/kg/min

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60
Q

low dose norepinephrine stimulation

A

beta 1 selective; increase HR, inotropy

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61
Q

high dose norepinephrine stimulation

A

alpha 1, alpha 2, beta 1; increase SVR, BP, but decreased HR (baroreceptor reflex)

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62
Q

norepinephrine bolus

A

dilute; 4-16 mcgs (intermittent boluses- less bradycardia than phenylephrine)

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63
Q

dopamine

A

endogenous NT in the nervous system (central and peripheral)

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64
Q

dopamine stimulation

A

D1=D2»beta»alpha

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65
Q

low dose dopamine dose

A

1-2 mcg/kg/min

66
Q

low dose dopamine

A

D1 renal vasodilation, may have decreased BP

67
Q

moderate dose dopamine dose

A

2-10 mcg/kg/min

68
Q

moderate dose dopamine

A

beta 1 in the heart (increased HR, inotropy, CO)

69
Q

high dose dopamine dose

A

10-20 mcg/kg/min

70
Q

high dose dopamine

A

alpha1 in the peripheral vessels overrides D and beta

71
Q

dopamine indications

A
  1. increase CO in patients with low BP, elevated atrial filling pressure, and low urine output
  2. increase renal blood flow, GFR, excretion of sodium and urine output
72
Q

renal dose dopamine

A

no studies have shown that dopamine decreases the incidence of acute renal failure of those at risk (UOP increases, mortality and morbidity do not improve)

73
Q

dopamine renal effects antagonized by

A

arterial hypoxemia and droperidol and metoclopramide

74
Q

dopamine beta 1 CV effects

A

increases CO; increased HR, BP, SVR

75
Q

dopamine release of norepinephrine

A

inotropic and susceptible to dysrhythmias (less than epinephrine)

76
Q

dopamine CV effects can raise

A

myocardial O2 demand > O2 supply

77
Q

dopamine D1 CV effects

A

dilates renal and mesenteric vascular beds

78
Q

dopamine respiratory effects

A

inhibits the ventilatory response to arterial hypoxemia

79
Q

dobutamine stimulation

A

selective beta1; beta1>beta2»»alpha

80
Q

dobutamine indication

A

CO in patients with CHF

81
Q

dobutamine dose

A

0.1-15 mcg/kg/min

82
Q

dobutamine causes

A

increase HR, inotropy, CO

83
Q

dobutmaine is combined with dopamine to

A

improve renal blood flow

84
Q

dobutmaine is combined with a vasodilator to

A

decrease SVR and further improve CO

85
Q

dobutamine beta1 CV effects

A

increase in CO with little increase in HR or BP (minimal increase in oxygen demand), decreases SVR and PVR

86
Q

dobutamine is a __ vasodilator and cannot cause __

A

coronary artery

renal vasodilation

87
Q

high doses of dobutamine cause

A

increased HR and dysrhythmias (otherwise unlikely due to no release of norepinephrine)

88
Q

most potent beta agonist

A

isoproterenol

89
Q

isoproterenol stimulates

A

beta1=beta2»»alpha

90
Q

isoproterenol indications

A
  1. increase heart rate with heart block
  2. decrease pulmonary vascular resistance
  3. bronchodilation
91
Q

isoproterenol beta1 CV effects

A
  1. increased HR
  2. inotropic effect
  3. susceptibility to dysrhythmias
92
Q

isoproterenol beta2 CV effects

A

decreased SVR due to vasodilation in skeletal muscle

93
Q

isoproterenol summary

A
  1. decreased MAP
  2. decreased coronary blood flow
  3. increased oxygen demand
94
Q

isoproterenol is not good for

A

patients with coronary artery disease

95
Q

ephedrine stimulates

A

alpha and beta

96
Q

ephedrine is __ acting

A

indirect

97
Q

ephedrine effects are due to

A

release of norepinephrine and the direct effect of ephedrine on beta adrenergic receptors

98
Q

ephedrine may be given

A

orally, IM, IV

99
Q

ephedrine dose

A

2.5-10 mg (must increase subsequent doses to obtain same response, tachyphylaxis)

100
Q

ephedrine __ duration as a __

A

prolonged

noncatecholamine

101
Q

ephedrine indications

A
  1. temporarily increase BO due to sympathetic blockade from regional or hypotension due to inhaled or IV anesthesia
  2. bronchdilation (slow onset) or nasal decongestant
  3. antiemetic (0.5 mg/kg IM)
102
Q

ephedrine CV effects are similar to

A

epinephrine but not as intense (250X)

103
Q

ephedrine beta1 CV effects

A

increased systolic and diastolic BP, HR, and CO

104
Q

principle CV effect of ephedrine beta1

A

increased contractility

105
Q

ephedrine alpha1 CV effects

A

vasoconstriction, renal and splanchnic flow decreased

106
Q

ephedrine beta2 CV effects

A

vasodilation, coronary artery and skeletal muscle vessels flow increased

107
Q

ephedrine beta2 CV effects- SVR may not change much as

A

vasodilation of some vessels offset the vasoconstriction of others

108
Q

ephedrine respiratory effects

A

beta1- bronchodilation

109
Q

ephedrine CNS effects

A

stimulation; increases MAC- less than amphetamine

110
Q

ephedrine ocular effects

A

mydriasis

111
Q

ephedrine metabolic effects

A

no hyperglycemia

112
Q

ephedrine effects of uterine blood flow

A

not** the drug of choice, higher incidence of fetal acidosis

113
Q

phenylephrine is mostly __ by __ effect

A

alpha1

direct

114
Q

phenylephrine stimulation

A

alpha1>alpha2»»>beta

115
Q

phenylephrine __ effect

A

very small indirect

116
Q

phenylephrine acts more like

A

norepinephrine

117
Q

phenylephrine indications

A
  1. increased BP due to sympathetic blockade or peripheral vasodilation
  2. increase BP in patients with CAD or aortic stenosis to avoid increased HR
  3. maintain BP during carotid endarterectomy
  4. slow HR from SVT
  5. nasal decongestant, mydriasis
  6. prolong duration of spinal anesthesia
118
Q

phenylephrine alpha1 CV effects

A
  1. peripheral vasoconstriction
  2. increase in BP
  3. increased susceptibility to dysrhythmias
119
Q

phenylephrine CV effects

A
  1. decrease in CO due to increased afterload or reflex bradycardia
  2. decreased blood flow to the kidneys, skin, and splanchnic system
  3. increased flow to the coronary arteries
  4. decreased cerebral oxygen saturation
120
Q

clonidine is __ acting __

A

centrally

partial alpha2-adrenergic agonist

121
Q

clonidine stimulation

A

antihypertensive, alpha2>alpha2»»>beta

122
Q

clonidine decreases

A

sympathetic output from the CNS

123
Q

clonidine MOA- stimulates

A

alpha1 inhibitory neurons in the medullary vasomotor center

124
Q

clonidine MOA- __ sympathetic outflow

A

decreased

125
Q

clonidine MOA- cell membranes

A

hyper polarized in the CNS

126
Q

clonidine MOA- neuraxial

A

inhibits spinal substance P release and blunts perception of noxious stimuli

127
Q

clonidine CV effects

A
  1. decrease in BP, HR, CO
  2. reflexes are maintained; avoid orthostatic hypotension
  3. renal blood flow is maintained
128
Q

clonidine indications

A
  1. analgesia
  2. premedication
  3. prolongs the effect of regional anesthesia
  4. diagnose pheochromocytoma
  5. treatment of opioid withdrawal
  6. treatment of shivering
129
Q

clonidine for analgesia

A

neuraxial- without depression of ventilation, pruritus, N/V, or delayed gastric emptying

130
Q

clonidine as premedication

A
  1. blunts response from laryngoscopy
  2. decrease lability of BP and HR
  3. decrease catecholamine concentrations
  4. decreases MAC and requirements of injected drugs
  5. accentuates effect of ephedrine
  6. decreases incidence of myocardial ischemic episodes in patients with CAD
131
Q

clonidine to diagnose pheochromocytoma

A

reduces release of catecholamines from nerve endings, not pheo

132
Q

clonidine for treatment of opioid withdrawal

A

inhibition of CNS

133
Q

clonidine for treatment for shivering

A

inhibit central thermoregulatory control, vasoconstriction- more susceptible to hypothermia

134
Q

most common side effect of clonidine

A

sedation

135
Q

clonidine has agonist effect on

A

postsynaptic alpha2- 50% reduction in anesthetic requirements of MAC

136
Q

clonidine decreased catecholamine levels so may require

A

anticholinergic to treat bradycardia

137
Q

clonidine has __ if abruptly stopped

A

rebound hypertension

138
Q

dexmedetomidine is a

A

alpha2-adrenergic agonist

139
Q

dexmedetomidine is selective for

A

7X more selective for alpha2 receptors than clonidine

140
Q

dexmedetomidine duration of action

A

shorter than clonidine (2hr 1/2life)

141
Q

dexmedetomidine decrease

A

MAC by > 90%

142
Q

dexmedetomidine causes __ and __ with little __

A

sedation and analgesia

depression of ventilation

143
Q

dexmedetomidine increased likelihood of

A

hypotension and hypothermia

144
Q

albuterol is selective

A

beta2

145
Q

albuterol stimulation

A

beta2»beta1»»alpha

146
Q

albuterol indications

A
  1. prevention and treatment of bronchoconstriction in asthma or COPD
  2. stop premature uterine contractions
147
Q

albuterol- inhaled route minimizes __; inhaler delivers __ of dose to lungs; an ETT decreases that amount by __

A

side effects

12%

50-70%

148
Q

albuterol side effects

A
  1. tremors
  2. increased HR, vasodilation
  3. relaxation of compensatory vasoconstriction
  4. hyperglycemia, hypokalemia, hypomagnesium with acute admin
149
Q

albuterol is __ with volatile agent

A

additive (bronchodilation)

150
Q

alpha agonist

A
  1. phenylephrine alpha1>alpha2»»>beta
  2. clonidine alpha2>alpha1»»>beta
151
Q

mixed alpha and beta agonist

A
  1. epinephrine alpha1=alpha2; beta1=beta2
  2. norepinephrine alpha1=alpha2; beta1»beta2
152
Q

beta agonists

A
  1. isoproterenol beta1=beta2»»alpha
  2. dobutamine beta1>beta2»»alpha
  3. albuterol, terbutaline beta2»beta1»»alpha
153
Q

dopamine agonist

A

dopamine d1=d2»beta»alpha

154
Q

vasopressin (arginine vasopressin) antidiuretic hormone (ADH) regulates

A

extracellular fluid by affecting the kidney’s handling of water

155
Q

vasopressin principle sites of action

A
  1. kidneys
  2. vessels
156
Q

vasopressin action on kidneys

A

water reabsorption V2

157
Q

vasopressin action on vessels

A

arterial vasoconstriction V1

158
Q

vasopressin dose

A

20 units, diluted to 1U/cc

159
Q

1 unit of vasopressin

A

approximately increases systolic BP 20mmHg

160
Q

vasopressin is used to treat

A

refractory hypotension after ephedrine, phenylephrine, etc.