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Adrenergics-Chen Flashcards

1
Q

What are the alpha-1 agonists?

A

Norepinephrine, Phenylephrine, Naphazoline, Oxymetazoline

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2
Q

What is the MOA of Norepinephrine?

A

Alpha-1 at therapeutic dose, B1 and B2 with increased dose; direct action

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3
Q

What are the effects of Norepinephrine?

A

Vasoconstriction > heart stimulation; increase BP; increase TRP; reflex bradycardia

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4
Q

When would you use Norepinephrine?

A

Shock (IV) to increase BP, rapid onset, extremely short action (1-2min); slow drip, not PO

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5
Q

What are the side effects of Norepinephrine?

A

Increased BP/hypertensive crisis/hemorrhage, reflex bradycardia, excessive nasal dryness, blurred vision, IV infiltration > tissue necrosis

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6
Q

What is the MOA of Phenylephrine?

A

Selective for alpha-1

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7
Q

What are the effects of Phenylephrine?

A

Vasoconstriction > heart stimulation; increases BP; Increases TPR; reflex bradycardia

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8
Q

When would you use Phenylephrine?

A

IV to increase BP, PO or intranasally as nasal decongestant, ophthalmic drops for mydriasis

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9
Q

What are the side effects of Phenylephrine?

A

CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion

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10
Q

What is the MOA of Naphazoline?

A

Selective for alpha-1

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11
Q

What are the effects of Naphazoline?

A

Vasoconstriction > heart stimulation; increases BP; increases TPR; reflex bradycardia

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12
Q

When would you use Naphazoline?

A

PO or intranasally as nasal decongestant; ophthalmic drops for mydriasis; relief of redness of eye

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13
Q

What are the side effects of Naphazoline?

A

CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion

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14
Q

What is the MOA of Oxymetazoline?

A

Non-selective alpha agonist

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15
Q

What are the effects of Oxymetazoline?

A

Vasoconstriction > heart stimulation; increases BP; increases TPR; reflex bradycardia

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16
Q

When would you use Oxymetazoline?

A

PO or intranasally as nasal decongestant; ophthalmic drops for mydriasis; relief of redness of eye

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17
Q

What are the side effects of Oxymetazoline?

A

CVS: increase in BP, cardiac failure and arrhythmia, reflex bradycardia; infiltration necrosis after parenteral admin; rebound nasal congestion

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18
Q

What are the alpha-2 Agonists?

A

Clonidine

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19
Q

What is the MOA of Clonidine?

A

Stimulates pre-synaptic alpha-2 receptors in CNS

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20
Q

What are the effects of Clonidine?

A

Decreases sympathetic outflow to the periphery

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21
Q

Whwhen would you use Clonidine?

A

Hypertension; withdrawal symptoms from opiates, tobacco smoking, and benzodiazepines

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22
Q

What are the side effects of Clonidine?

A

Lethargy, sedation, constipation, dry mouth; abrupt discontinuance > rebound hypertension

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23
Q

What are the Beta-1 Agonists?

A

Dobutamine

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24
Q

What is the MOA of Dobutamine?

A

Selective B1 agonist

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25
Q

What are the effects of Dobutamine?

A

Increases force > HR at therapeutic concentration

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26
Q

When would you use Dobutamine?

A

Parentally for acute CHF as an inotropic drug

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27
Q

What are the side effects of Dobutamine?

A

Develop ventricular arrhythmias; development of tolerance with prolonged use (downregulate receptor)

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28
Q

What are the Beta-2 Agonists?

A

Albuterol, Terbutaline, Isoproterenol

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29
Q

What is the MOA of Albuterol?

A

Selective B2 agonist

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30
Q

What are the effects of Albuterol?

A

Relax smooth muscle, bronchodilation, relax uterus, vasodilation in skeletal muscle blood vessels

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31
Q

When would you use Albuterol?

A

PO/SC/Inhalation/IV for 3-6 hrs; acute bronchospasm in asthma; use slmeterol/formoterol for long acting and can combine with steroid for asthma

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32
Q

What are the side effects of Albuterol?

A

Tremor, tachycardia (at higher doses can cause some beta-1 stimulation on heart)

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33
Q

What is the MOA of Terbutaline?

A

Selective B2 agonist

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34
Q

What are the effects of Terbutaline?

A

Relax smooth muscle, bronchodilation, relax uterus, vasodilation in skeletal muscle blood vessels

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35
Q

When would you use Terbutaline?

A

PO/SC/Inhalation/IV for 3-6 hrs; acute bronchospasm in asthma; inhibit the uterine contractions in premature labor; use salmeterol/formoterol for long acting and can combine with steriod for asthma

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36
Q

What are the side effects of Terbutaline?

A

Tremor, tachycardia (at higher doses can cause some beta-1 stimulation on heart)

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37
Q

What is the MOA of Isoproterenol?

A

Non-selective beta agonist; direct action

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38
Q

What are the effects of Isoproterenol?

A

Relaxation of smooth muscle of bronchioles and intestinal tract; vasodilation within the skeletal muscles > drop in TPR and diastolic pressure; chronotropic actions > rise in systolic pressure; glycogenolysis and hyperlipidemia; myometrial relaxation

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39
Q

When would you use Isoproterenol?

A

IV metabolized by COMT, not MAO; longer half life than epinephrine; treat heart block, bradycardia, ventricular arrhythmia (torsades de pointes)

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40
Q

What are the side effects of Isoproterenol?

A

Tachycardia, headache, flushing, ischemia, arrhythmia in coronary artery disease patients; palpitations, increased BP, CNS stimulation/anxiety overdoses; treamors (A HINT)

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41
Q

What is the MOA of Epinephrine?

A

Works as A1, B1 and B2 agonist; direct action

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42
Q

What are the effects of Epinephrine?

A

Regional vasoconstriction > increased systolic BP (A1); Increased CO > increased systolic BP (HR/Contractility increase B1); Skeletal muscle vasodilation > decrease diastolic pressure (B2); Broncorelaxation (B2); hyperglycemic effect (B2/A1); lipolysis

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43
Q

When would you use Epinephrine?

A

IM/IV/SC/Inhalation; rapid onset but brief duration of action; asthma; anaphylactic shock (IM) and angioedema; prolongation of local anesthetics; cardiac arrest, bradycardia, complete heart block in emergency; bleeding ulcers, calrogenic effects/metabolism

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44
Q

What are the side effects of Epinephrine?

A

Ventricular arrhythmias, headache, restlessness

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45
Q

What is the MOA of Dopamine?

A

Dose-dependent response on receptors; low= dopaminergic; medium=B1; high=A

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46
Q

What are the effects of Dopamine?

A

Low= vasodilation; medium= force > rate; High= vasoconstriction

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47
Q

When would you use Dopamine?

A

Circulatory shock, acute heart failure

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48
Q

What are the side effects of Dopamine?

A

Tachycardia, anginal pain, arrhythmias, headache

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49
Q

What is the MOA of Fenoldopam?

A

Peripheral D1 agonist

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50
Q

What are the effects of Fenoldopam?

A

Rapid vasodilation

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51
Q

When would you use Fenoldopam?

A

Severe hypertension

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52
Q

What are the side effects of Fenoldopam?

A

Tachycardia, anginal pain, arrhythmias, headache

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53
Q

What are the alpha antagonists?

A

Pentolamine, Phenoxybenzamine, Prazosin, Terazosin, Tamsulosin, Alfusozin, Doxazosin, Labetalol, Carvedilol

54
Q

What is the MOA of Phentolamine?

A

Nonselective block of A1 and A2

55
Q

What are the effects of Phentolamine?

A

Reversible; short acting

56
Q

When would you use Phentolamine?

A

For diagnosis and treatment of pheochromocytoma

57
Q

What are the side effects of Phentolamine?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

58
Q

What is the MOA of Phenoxybenzamine?

A

Nonselective block of A1 and A2

59
Q

What are the effects of Phenoxybenzamine?

A

Irreversible; long-acting

60
Q

When would you use Phenoxybenzamine?

A

Preoperative management of pheochromocytoma

61
Q

What are the side effects of Phenoxybenzamine?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

62
Q

What is the MOA of Prazosin?

A

Selective block of A1

63
Q

What are the effects of Prazosin?

A

Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle

64
Q

When would you use Prazosin?

A

Hypertension

65
Q

What are the side effects of Prazosin?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

66
Q

What is the MOA of Terazosin?

A

Selective Block of A1

67
Q

What are the effects of Terazosin?

A

Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle

68
Q

When would you use Terazosin?

A

Hypertension

69
Q

What are the side effects of Terazosin?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

70
Q

What is the MOA of Tamsulosin?

A

Selective block of A1

71
Q

What are the effects of Tamsulosin?

A

Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle

72
Q

When would you use Tamsulosin?

A

Benign prostate hyperplasia

73
Q

What are the side effects of Tamsulosin?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

74
Q

What is the MOA of Alfusozin?

A

Selective block of A1

75
Q

What are the effects of Alfusozin?

A

Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle

76
Q

When would you use Alfusozin?

A

Benign prostate hyperplasia

77
Q

What are the side effects of Alfusozin?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

78
Q

What is the MOA of Doxazosin?

A

Selective block of A1

79
Q

What are the effects of Doxazosin?

A

Reduce BP with less reflex tachycardia than non-selective; relax prostate smooth muscle

80
Q

When would you use Doxazosin?

A

Hypertension and benign prostate hyperplasia

81
Q

What are the side effects of Doxazosin?

A

Excessive/postural hypertension (syncope at first-dose effect), headache and dizziness, nasal congestion, blurred vision, reflex tachycardia, sexual dysfunction, epinephrine reversal

82
Q

What is the MOA of Labetalol?

A

A1 and NS beta blocker

83
Q

What are the effects of Lebetalol?

A

Decreases PR and CO, more balanced approach to inhibiting the SNS

84
Q

When would you use Lebetalol?

A

IV for hypertension and hypertensive emergencies, pheochromocytoma

85
Q

What are the side effects of Labetalol?

A

Combination of alpha/beta blockade, hepatic injury

86
Q

What is the MOA of Carvedilol?

A

A1 and NS Beta blocker

87
Q

What are the effects of Carvedilol?

A

Decreases PR and CO, more balanced approach to inhibiting the SNS

88
Q

When would you use Carvedilol?

A

Heart failure

89
Q

What are the side effects of Carvedilol?

A

Combination of alpha/beta blockade, hepatic injury

90
Q

What are the beta antagonists?

A

Propranolol, Timolol, Nadolol, Metoprolol, Atenolol, Acebutolol, Esmolol, Nebivolol, Pindolol

91
Q

What is the MOA of Propranolol?

A

Nonselective B antagonist

92
Q

What are the effects of Propranolol?

A

Prototype; most lipid soluble beta blocker; highest membrane stabilizing effect

93
Q

What are the side effects of Propranolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

94
Q

What is the MOA of Timolol?

A

Nonselective B antagonist

95
Q

When would you use Timolol?

A

Chronic open-angle glaucoma (topical); hypertension and migraine prophylaxis

96
Q

What are the side effects of Timolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

97
Q

What is the MOA of Nadolol?

A

Nonselective B antagonist

98
Q

What are the effects of Nadolol?

A

More potent than Propranolol; long duration of action (HL= 20-24 hrs)

99
Q

When would you use Nadolol?

A

Hypertension, angina, migraine prophylaxis

100
Q

What are the side effects of Nadolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

101
Q

What is the MOA of Metoprolol?

A

Selective B1 blocker

102
Q

What are the effects of Metoprolol?

A

Cardioselective

103
Q

When would you use Metoprolol?

A

Safer than non-selective for COPD and asthma; hypertension, angina, acute MI, heart failure, tachycardia

104
Q

What are the side effects of Metoprolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

105
Q

What is the MOA of Atenolol?

A

Selective B1 blocker

106
Q

What are the effects of Atenolol?

A

Reduces CO

107
Q

When would you use Atenolol?

A

Safer than non-selective for COPD and asthma; hypertension, angina, acute MI, heart failure, tachycardia

108
Q

What are the side effects of Atenolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

109
Q

What is the MOA of Acebutolol?

A

Selective B1 blocker

110
Q

What are the effects of Acebutolol?

A

Half life= 3hrs; active metabolite (diacetolol) half life= 8-12hrs; membrane stabilization and ISA

111
Q

When would you use Acebutolol?

A

Ventricular arrhythmias

112
Q

What are the side effects of Acebutolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

113
Q

What is the MOA of Esmolol?

A

Selective B1 blocker

114
Q

What are the effects of Esmolol?

A

Short half-life (8-9min)

115
Q

When would you use Esmolol?

A

Safer than non-selective for COPD and asthma; IV for hypertensive crisis and acute SVT

116
Q

What are the side effect of Esmolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

117
Q

What is the MOA of Nebivolol?

A

Selective block of B1; Release of NO > vasodilation

118
Q

What are the effects of Nebivolol?

A

Vasodilation

119
Q

When would you use Nebivolol?

A

Safer than non-selective for COPD and asthma; hypertension

120
Q

What are the side effects of Nebivolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

121
Q

What is the MOA of Pindolol?

A

Nonselective Beta antagonist

122
Q

What are the effects of Pindolol?

A

IS and membrane stabilization

123
Q

When would you use Pindolol?

A

Antihypertensive drug when people have diminished cardiac reserve

124
Q

What are the side effects of Pindolol?

A

Weakness, dizziness, tiredness, minor GI disturbances, sexual dysfunction; CVS: bradycardia, AV block, CHF, hypotension, chest pain, aggravation of peripheral vascular disease; CNS: sedation, confusion, nightmares, rare psychotic reactions (lipid soluble drugs); asthmatic and diabetic difficulties; abrupt withdrawal due to receptor up-regulation

125
Q

What is the MOA of Reserpine?

A

Blocks ventricular amine transporter

126
Q

What are the effects of Reserpine?

A

Reduces SNS activity (storage/release); depletes serotonin and dopamine in CNS

127
Q

When would you use Reserpine?

A

Hypertension, used to be used as antipsychotic

128
Q

What are the side effects of Reserpine?

A

Hypotension, reflex tachycardia; increase GI/CNS depression; sedation

129
Q

What is the MOA of Guanethidine?

A

Displaces NE from storage vesicles; acts as false NT

130
Q

What are the effects of Guanethidine?

A

Reduces SNS activity (storage/release)

131
Q

When would you use Guanethidine?

A

Hypertension

132
Q

What are the side effects of Guanethidine?

A

Hypotension, reflex tachycardia; increase GI/CNS depression; sedation

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