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Pharm U2 > 4) Adrenergic Receptor Agonists - Antagonists > Flashcards

4) Adrenergic Receptor Agonists - Antagonists Flashcards

1
Q

What is the class for Norepinephrine (Levophed)

A

Non-selective agonist

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2
Q

What is the mechanism for Norepinephrine (Levophed)

A

Agonist: alpha 1, alpha 2, beta 1

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3
Q

What are the therapeutics for Norepinephrine (Levophed)

A

Acute Hypotension

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4
Q

What are the important side effects for Norepinephrine (Levophed)

A

Hypertension; arrythmias; headache

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5
Q

What is the class for Epinephrine

A

Non-selective agonist

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6
Q

What is the mechanism for Epinephrine

A

Agonist: alpha 1, (alpha 2), beta 1, beta 2

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7
Q

What are the therapeutics for Epinephrine

A

Anaphylactic shock; combined with local anesthetics; glaucoma

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8
Q

What are the important side effects for Epinephrine

A

Palpitation; arrhythmias; headache

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9
Q

What is the class for Amphetamine

A

Indirect acting

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10
Q

What is the mechanism for Amphetamine

A

Increases release of NE

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11
Q

What are the therapeutics for Amphetamine

A

ADHD, narcolepsy, recreation

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12
Q

What are the important side effects for Amphetamine

A

Hypertension, insomnia, anxiety, arrhythmias

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13
Q

What is the class for Isoproterenol (Isuprel)

A

Non-selective beta agonist

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14
Q

What is the mechanism for Isoproterenol (Isuprel)

A

Agonist: beta 1, beta 2

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15
Q

What are the therapeutics for Isoproterenol (Isuprel)

A

shock; heart block

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16
Q

What are the important side effects for Isoproterenol (Isuprel)

A

Palpitation; tachyarrhythmia; headache

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17
Q

What is the class for Dobutamine

A

beta 1-selective beta agonist

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18
Q

What is the mechanism for Dobutamine

A

Agonist: beta 1

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19
Q

What are the therapeutics for Dobutamine

A

Cardiac decompensation; shock; heart block

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20
Q

What are the important side effects for Dobutamine

A

Tachyarrythmias; hypertension

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21
Q

What is the class for Albuterol (Proventil)

A

beta 2-selective beta agonist

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22
Q

What is the mechanism for Albuterol (Proventil)

A

Agonist: beta 2

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23
Q

What are the therapeutics for Albuterol (Proventil)

A

Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD

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24
Q

What are the important side effects for Albuterol (Proventil)

A

Can mask progressively severe inflammation

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25
Q

What are the other side effects for Albuterol (Proventil)

A

Tachycardia, muscle tremor

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26
Q

What are the miscellaneous for Albuterol (Proventil)

A

10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal

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27
Q

What is the class for Terbutaline (Brethine)

A

beta 2-selective beta agonist

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28
Q

What is the mechanism for Terbutaline (Brethine)

A

Agonist: beta 2

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29
Q

What are the therapeutics for Terbutaline (Brethine)

A

Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD; early labor

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30
Q

What are the important side effects for Terbutaline (Brethine)

A

Can mask progressively severe inflammation

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31
Q

What are the other side effects for Terbutaline (Brethine)

A

Tachycardia, muscle tremor

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32
Q

What are the miscellaneous for Terbutaline (Brethine)

A

10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal

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33
Q

What is the class for Phenylephrine (Neo-Synephrine)

A

alpha 1-selective alpha agonist

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34
Q

What is the mechanism for Phenylephrine (Neo-Synephrine)

A

Agonist: alpha 1

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35
Q

What are the therapeutics for Phenylephrine (Neo-Synephrine)

A

Nasal congestion; postural Hypotension

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36
Q

What are the important side effects for Phenylephrine (Neo-Synephrine)

A

Hypertension; reflex bradycardia

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37
Q

What is the class for Clonidine (Catapres)

A

alpha 2-selective alpha agonist

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38
Q

What is the mechanism for Clonidine (Catapres)

A

Agonist: CNS alpha 2

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39
Q

What are the therapeutics for Clonidine (Catapres)

A

Hypertension; shock; withdrawal from drug dependence

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40
Q

What are the important side effects for Clonidine (Catapres)

A

Sedation

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41
Q

What is the class for alpha-methyldopa (Aldomet)

A

alpha 2-selective alpha agonist

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42
Q

What is the mechanism for ?-methyldopa (Aldomet)

A

Metabolite (a-methylnorepinephrine) activates CNS a2 receptors

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43
Q

What are the therapeutics for ?-methyldopa (Aldomet)

A

Hypertension

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44
Q

What are the important side effects for ?-methyldopa (Aldomet)

A

Sedation

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45
Q

What are the miscellaneous for ?-methyldopa (Aldomet)

A

Prodrug; crosses BBB

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46
Q

What is the class for Fenoldopam (Corlopam)

A

Selective dopamine agonist

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47
Q

What is the mechanism for Fenoldopam (Corlopam)

A

Agonist: D1 only

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48
Q

What are the therapeutics for Fenoldopam (Corlopam)

A

Increase blood flow at renal, mesenteric, and cerebral arteries

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49
Q

What are the miscellaneous for Fenoldopam (Corlopam)

A

~10 minute half-life

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50
Q

What is the class for Dopamine

A

Mixed acting (direct/indirect)

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51
Q

What is the mechanism for Dopamine

A

Agonist: D1, alpha 1, beta 1

52
Q

What are the therapeutics for Dopamine

A

Shock, renal failure, hypotension

53
Q

What are the important side effects for Dopamine

A

Vasoconstriction (@ high doses)

54
Q

What are the miscellaneous for Dopamine

A

Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect

55
Q

What is the class for Phentolamine (Regitine)

A

Non-selective alpha-antagonist

56
Q

What is the mechanism for Phentolamine (Regitine)

A

Antagonist: alpha 1, alpha 2

57
Q

What are the therapeutics for Phentolamine (Regitine)

A

Pheochromocytoma, Raynaud’s, frostbite

58
Q

What are the important side effects for Phentolamine (Regitine)

A

Postural hypotension; inhibit ejaculation

59
Q

What is the class for Phenoxybenzamine (Dibenzyline)

A

Non-selective alpha-antagonist

60
Q

What is the mechanism for Phenoxybenzamine (Dibenzyline)

A

Antagonist: alpha 1, alpha 2; non-competitive blocker (covalent bond to receptor)

61
Q

What are the therapeutics for Phenoxybenzamine (Dibenzyline)

A

Pheochromocytoma, Raynaud’s, frostbite

62
Q

What are the important side effects for Phenoxybenzamine (Dibenzyline)

A

Postural hypotension; inhibit ejaculation

63
Q

What is the class for Prazosin (Minipress)

A

alpha 1-selective antagonist

64
Q

What is the mechanism for Prazosin (Minipress)

A

Antagonist: alpha 1

65
Q

What are the therapeutics for Prazosin (Minipress)

A

Primary HTN, BPH

66
Q

What are the important side effects for Prazosin (Minipress)

A

Postural hypotension (usually 1st dose)

67
Q

What is the class for Terazosin (Hytrin)

A

alpha 1-selective antagonist

68
Q

What is the mechanism for Terazosin (Hytrin)

A

Antagonist: alpha 1

69
Q

What are the therapeutics for Terazosin (Hytrin)

A

Primary HTN, BPH

70
Q

What are the important side effects for Terazosin (Hytrin)

A

Postural hypotension (usually 1st dose)

71
Q

What is the class for Propranolol (Inderal)

A

Non-selective beta-antagonist (1st generation)

72
Q

What is the mechanism for Propranolol (Inderal)

A

Antagonist: beta 1, beta 2

73
Q

What are the therapeutics for Propranolol (Inderal)

A

Angina, Hypertension, Arrythmias

74
Q

What are the important side effects for Propranolol (Inderal)

A

Bradycardia, Bronchoconstriction, Sexual Dysfunction

75
Q

What are the miscellaneous for Propranolol (Inderal)

A

Workhorse by which all the rest are judged

76
Q

What is the class for Timolol (Betimol)

A

Non-selective beta-antagonist (1st generation)

77
Q

What is the mechanism for Timolol (Betimol)

A

Antagonist: beta 1, beta 2

78
Q

What are the therapeutics for Timolol (Betimol)

79
Q

What are the important side effects for Timolol (Betimol)

A

Bradycardia, Bronchoconstriction, Sexual Dysfunction

80
Q

What is the class for Metoprolol (Lopressor)

A

beta 1-selective antagonist (2nd generation)

81
Q

What is the mechanism for Metoprolol (Lopressor)

A

Antagonist: beta 1

82
Q

What are the therapeutics for Metoprolol (Lopressor)

A

HTN, Angina, Arrythmias, CHF

83
Q

What are the important side effects for Metoprolol (Lopressor)

A

Bradycardia, Sexual Dysfunction

84
Q

What is the class for Atenolol (Tenormin)

A

beta 1-selective antagonist (2nd generation)

85
Q

What is the mechanism for Atenolol (Tenormin)

A

Antagonist: beta 1

86
Q

What are the therapeutics for Atenolol (Tenormin)

A

HTN, Angina, Arrythmias, CHF

87
Q

What are the important side effects for Atenolol (Tenormin)

A

Bradycardia, Sexual Dysfunction

88
Q

What is the class for Bisoprolol (Zebeta)

A

beta 1-selective antagonist (2nd generation)

89
Q

What is the mechanism for Bisoprolol (Zebeta)

A

Antagonist: beta 1

90
Q

What are the therapeutics for Bisoprolol (Zebeta)

A

HTN, Angina, Arrythmias, CHF

91
Q

What are the important side effects for Bisoprolol (Zebeta)

A

Bradycardia, Sexual Dysfunction

92
Q

What is the class for Carvedilol (Coreg)

A

Non-selective beta-antagonist (3rd generation “A”)

93
Q

What is the mechanism for Carvedilol (Coreg)

A

Antagonist: beta 1, beta 2

94
Q

What are the therapeutics for Carvedilol (Coreg)

95
Q

What are the important side effects for Carvedilol (Coreg)

A

Bradycardia, Fatigue

96
Q

What is the class for Labetalol (Trandate)

A

Non-selective beta-antagonist (3rd generation “A”)

97
Q

What is the mechanism for Labetalol (Trandate)

A

Antagonist: beta 1, beta 2

98
Q

What are the therapeutics for Labetalol (Trandate)

99
Q

What are the important side effects for Labetalol (Trandate)

A

Bradycardia, Fatigue

100
Q

What is the class for Betaxolol (Kerlone)

A

beta 1-selective antagonist (3rd generation “B”)

101
Q

What is the mechanism for Betaxolol (Kerlone)

A

Antagonist: beta 1

102
Q

What are the therapeutics for Betaxolol (Kerlone)

103
Q

What are the important side effects for Betaxolol (Kerlone)

A

Bradycardia

104
Q

What is the class for Tyramine

A

Indirect acting agonist

105
Q

What is the mechanism for Tyramine

A

Increases cytoplasmic NE release

106
Q

What are the miscellaneous for Tyramine

A

Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out

107
Q

What is the mechanism for Cocaine

A

Prevents NE reuptake

108
Q

What are the therapeutics for Cocaine

A

Local anesthetic, vasoconstrictor

109
Q

What are the important side effects for Cocaine

A

Insomnia, anxiety, arrhythmias

110
Q

What is the class for Guanethidine (Ismelin)

A

Nerve ending blocker

111
Q

What is the mechanism for Guanethidine (Ismelin)

A

False neurotransmitter (vesicles become full of guanethidine rather than NE)

112
Q

What are the therapeutics for Guanethidine (Ismelin)

A

Antihypertensive

113
Q

What are the important side effects for Guanethidine (Ismelin)

A

Many and serious

114
Q

What are the miscellaneous for Guanethidine (Ismelin)

A

Don’t really use this in US; doesn’t cross BBB

115
Q

What is the class for Reserpine

A

Nerve ending blocker

116
Q

What is the mechanism for Reserpine

A

Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it)

117
Q

What are the therapeutics for Reserpine

A

Older antihypertensive

118
Q

What are the important side effects for Reserpine

A

Many and serious (depression and suicide are major ones)

119
Q

What are the miscellaneous for Reserpine

A

Cheap! (used abroad, not here)

120
Q

What is the class for ?-me-tyrosine (Metirosine)

A

Nerve ending blocker

121
Q

What is the mechanism for ?-me-tyrosine (Metirosine)

A

Inhibit tyrosine hydroxylase (decreases NE synthesis)

122
Q

What are the therapeutics for ?-me-tyrosine (Metirosine)

A

Pheochromocytoma

123
Q

What are the important side effects for ?-me-tyrosine (Metirosine)

A

Many and serious

124
Q

What are the miscellaneous for ?-me-tyrosine (Metirosine)

A

Still used for this

125
Q

What is the class for Ephedrine (Pretz-D)

A

Mixed, direct (beta 2)/indirect agonist

126
Q

What are the therapeutics for Ephedrine (Pretz-D)

A

Nasal decongestion, anorexic

Pharm U2 (11 decks)

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