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Pharmacology > VIII - Adrenergic Pharmacology > Flashcards

VIII - Adrenergic Pharmacology Flashcards

1
Q

Primary neurotransmitter at the sympathetic post-ganglionic neuron effector cell synapses in most tissues

A

Norepinephrine

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2
Q

Sympathetic post-ganglionic neuron effector cell synapses use norepinephrine except

A

eccrine sweat glands, vasodilator sympathetic fibers in the skeletal muscle

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3
Q

Steps in Adrenergic Stimulation

A

synthesis, storage, release, termination

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4
Q

Adrenergic Stimulation: Step 1

A

SYNTHESIS - tyrosine is hydroxylated by tyrosine hydroxylase to DOPA which is decarboxylated to dopamine which is hydroxylated to norepinephrine

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5
Q

Adrenergic Stimulation: tyrosine hydroxylation is inhibited by

A

metyrosine

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6
Q

Adrenergic Stimulation: Step 2

A

norepinephrine and dopamine are transported into vesicles, MAOIs increase stores of NE and dopamine

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7
Q

Adrenergic Stimulation: vesicular transport is inhibited

A

reserpine

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8
Q

Adrenergic Stimulation: Step 3

A

entry of Ca triggers interaction among SNARE proteins (VAMPs and SNAPs)

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9
Q

Adrenergic Stimulation: inhibits interaction among SNARE proteins

A

guanethidine

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10
Q

Adrenergic Stimulation: promotes interaction among SNARE proteins

A

amphetamine, tyramine

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11
Q

Adrenergic Stimulation: Step 4

A

diffusion and reuptake via NET and DAT in the synaptic cleft, metabolized by MAO and COMT into metanephrines and VMA

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12
Q

Adrenergic Stimulation: diffusion and reuptake via NET and DAT is inhibited by

A

cocaine, TCAs

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13
Q

Adrenergic Stimulation: metabolism of norepinephrine into metanephrine and VMA is inhibited by

A

MAOIs, COMT Inhibitors

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14
Q

Cholinergic Inhibitors: Synthesis

A

hemicholinium

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15
Q

Cholinergic Inhibitors: Storage

A

vesamicol

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16
Q

Cholinergic Inhibitors: Release

A

botulinum

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17
Q

Cholinergic Inhibitors: Metabolism

A

neostigmine

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18
Q

Cholinergic Inhibitors: Reuptake

A

none

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19
Q

Adrenergic Inhibitors: Synthesis

A

metyrosine

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20
Q

Adrenergic Inhibitors: Storage

A

reserpine

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21
Q

Adrenergic Inhibitors: Release

A

guanethidine

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22
Q

Adrenergic Inhibitors: Metabolism

A

MAOIs, COMTIs

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23
Q

Adrenergic Inhibitors: Reuptake

A

cocaine, TCAs

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24
Q

Adrenoreceptors: effector tissues, smooth muscle, glands, Gq, inc. IP3, DAG, inc. Ca, contraction, secretion

A

Alpha 1

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25
Q

Adrenoreceptors: nerve endings, smooth muscles, Gi, dec. cAMP, dec. transmitter release, contraction

A

Alpha 2

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26
Q

Adrenoreceptors: cardiac muscle, JG apparatus, Gs, inc. cAMP, inc. heart rate and contractility, inc. renin

A

Beta 1

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27
Q

Adrenoreceptors: smooth muscle, liver, heart, Gs, inc. cAMP, relax smooth muscle, inc. glycogenolysis, inc. heart rate and contractility

A

Beta 2

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28
Q

Adrenoreceptors: adipose cells, Gs, inc. cAMP, inc. lipolysis

A

Beta 3

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29
Q

Adrenoreceptors: smooth muscle, Gs, inc. cAMP, relax renal vascular smooth muscle

A

Dopamine 1

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30
Q

Adrenoreceptors: contracts most vascular smooth muscle

A

Alpha 1

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31
Q

Adrenoreceptors: contracts pupillary dilator muscle

A

Alpha 1

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32
Q

Adrenoreceptors: contracts pilomotor smooth muscle

A

Alpha 1

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33
Q

Adrenoreceptors: inhibits adrenergic and cholinergic transmitter release

A

Alpha 2

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34
Q

Adrenoreceptors: stimulates platelet aggregation

A

Alpha 2

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35
Q

Adrenoreceptors: contracts some vascular smooth muscle

A

Alpha 2

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36
Q

Adrenoreceptors: inhibits lipolysis

A

Alpha 2

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37
Q

Adrenoreceptors: inhibits insulin release

A

Alpha 2

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38
Q

Adrenoreceptors: stimulates heart rate and forces

A

Beta 1, Beta 2

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39
Q

Adrenoreceptors: stimulates renin release from JG cells of the kidney

A

Beta 1

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40
Q

Adrenoreceptors: relaxes airway, uterine and vascular smooth muscle

A

Beta 2

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41
Q

Adrenoreceptors: stimulates glycogenolysis

A

Alpha 1, Beta 2

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42
Q

Adrenoreceptors: stimulates insulin release

A

Beta 2

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43
Q

Adrenoreceptors: causes tremors by stimulating somatic motor neuron terminals

A

Beta 2

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44
Q

Adrenoreceptors: stimulates lipolysis

A

Beta 3

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45
Q

Adrenoreceptors: dilates renal and other splanchnic blood vessels

A

Dopamine 1

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46
Q

Adrenoreceptors: inhibits adenylyl cyclase in nerve terminals

A

Dopamine 2

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47
Q

Activate adrenoreceptors directly and indirectly by increasing concentration of available catecholamines in the synapses (release of stored catecholamines, inhibition of reuptake)

A

Sympathomimetics

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48
Q

Epinephrine: Class

A

sympathomimetic - non-selective, direct-acting

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49
Q

Epinephrine: MOA

A

activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)

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50
Q

Epinephrine: Uses

A

cardiac arrest, anaphylaxis, asthma, COPD, hemostasis

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51
Q

Epinephrine: Side Effects

A

hypertension, tachycardia, ischemia, hyperglycemia

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52
Q

Norepinephrine: Class

A

sympathomimetic - non-selective, direct-acting

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53
Q

Norepinephrine: MOA

A

activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)

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54
Q

Norepinephrine: Uses

A

neurogenic shock, cardiogenic shock (last resort)

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55
Q

Norepinephrine: Side Effects

A

extreme vasospasm, tissue necrosis, excessive blood pressure increase, arrythmias, infarction, reflex bradycardia

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56
Q

Norepinephrine: Compensatory vagal reflexes tend to overcome

A

the direct positive chronotropic effects

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57
Q

Dopamine: Class

A

sympathomimetic - non-selective, direct-acting

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58
Q

Dopamine: MOA

A

activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), dopamine 1 (vasodilation of splanchnic and renal muscles)

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59
Q

Dopamine: Uses

A

shock, heart failure

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60
Q

Dopamine: Side Effects

A

cardiovascular disturbance, arrythmias

61
Q

Dopamine: Low-Dose

A

1-5 mcg/kg/min, D1 receptors, vasodilation in the splanchnic and renal vascular beds

62
Q

Dopamine: Medium Dose

A

5-15 mcg/kg/min, B1 receptors, increase renal blood flow, heart rate, cardiac contractility and cardiac output

63
Q

Dopamine: High Dose

A

> 15 mcg/kg/min, alpha receptors, vasoconstriction, increased BP

64
Q

Isoproterenol: Class

A

sympathomimetic - beta-non-selective

65
Q

Isoproterenol: MOA

A

non-selectively activates beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)

66
Q

Isoproterenol: Uses

67
Q

Isoproterenol: Side Effects

A

cardiovascular disturbance, arrhythmias

68
Q

Phenylephrine: Similar Drugs

A

pseudoephedrine

69
Q

Phenylephrine: Class

A

sympathomimetic - alpha 1-selective

70
Q

Phenylephrine: MOA

A

selectively activates alpha 1 (vasoconstricion, increases BP)

71
Q

Phenylephrine: Uses

A

decongestant, mydriatic, drug-induced hypotension, spinal shock

72
Q

Phenylephrine: Side Effects

A

rebound nasal congestion, hypertension, stroke, myocardial infarction

73
Q

Phenylephrine: Ocular administration causes mydriasis without

A

cyclopegia

74
Q

Clonidine: Class

A

sympathomimetic - alpha 2-selective

75
Q

Clonidine: MOA

A

selectively activates alpha 2 (decreases central sympathetic outflow)

76
Q

Clonidine: Uses

A

hypertension, cancer pain, opioid withdrawal

77
Q

Clonidine: Side Effects

A

sedation, rebound hypertension, dry mouth

78
Q

Clonidine: Avoid rebound hypertension by

A

tapering use to discontinuation

79
Q

Clonidine: Treat rebound hypertension with

A

phentolamine

80
Q

Methyldopa: Class

A

sympathomimetic - alpha 2-selective

81
Q

Methyldopa: MOA

A

selectively activates alpha 2 (decreases central sympathetic outflow)

82
Q

Methyldopa: Uses

A

pre-eclampsia

83
Q

Methyldopa: Side Effects

A

sedation, hemolytic anemia (positive Coomb’s test)

84
Q

Apraclonidine: Similar Drugs

A

brimonidine

85
Q

Apraclonidine: Class

A

sympathomimetic - alpha 2-selective

86
Q

Apraclonidine: MOA

A

selectively activates alpha 2 (decreases secretion of aqueous humor)

87
Q

Apraclonidine: Uses

88
Q

Apraclonidine: Side Effects

A

BOV, dry mouth, conjunctivitis

89
Q

Dobutamine: Class

A

sympathomimetic - beta 1-selective

90
Q

Dobutamine: MOA

A

selectively activates beta 1 (increased HR and contractility)

91
Q

Dobutamine: Uses

A

acute heart failure, cardiogenic shock

92
Q

Dobutamine: Side Effects

A

tachycardia, arrhythmias, tachyphylaxis

93
Q

Dobutamine: May also be used in

A

cardiac stress testing

94
Q

Albuterol/Salbutamol: Similar Drugs

A

terbutaline, ritodrine

95
Q

Albuterol/Salbutamol: Class

A

sympathomimetic - beta 2-selective

96
Q

Albuterol/Salbutamol: MOA

A

selectively activates beta 2 (bronchodilation)

97
Q

Albuterol/Salbutamol: Uses

A

acute asthma attack (drug of choice), tocolysis for preterm labor (terbutaline, ritodrine)

98
Q

Albuterol/Salbutamol: Side Effects

A

tachycardia, tremors, nervousness, restlessness, arrhythmias when used excessively, loss of responsiveness (tolerance, tachyphylaxis)

99
Q

Albuterol/Salbutamol: May precipitate arrythmias in a patient with

A

COPD and heart disease

100
Q

Sympathomimetics: acute heart failure tx

A

β1 & D1 agonists

101
Q

Sympathomimetics: septic shock tx

A

β1 & D1 agonists

102
Q

Sympathomimetics: increased cardiac output

A

β1 & D1 agonists

103
Q

Sympathomimetics: hemostasis

A

α1 agonist

104
Q

Sympathomimetics: decongestion

A

α1 agonist

105
Q

Sympathomimetics: vasoconstriction

A

α1 agonist

106
Q

Sympathomimetics: temporary maintenance of BP

A

α1 agonist

107
Q

Sympathomimetics: bronchospasm tx

A

β2 agonist

108
Q

Sympathomimetics: premature labor tx

A

β2 agonist

109
Q

Sympathomimetics: bronchodilation

A

β2 agonist

110
Q

Sympathomimetics: uterine smooth muscle relaxation

A

β2 agonist

111
Q

Sympathomimetics: hypertension tx

A

α2 agonist

112
Q

Sympathomimetics: glaucoma tx

A

α2 agonist

113
Q

Sympathomimetics: spinal shock tx

A

α2 agonist

114
Q

Sympathomimetics: decrease BP

A

α2 agonist

115
Q

Phenoxybenzamine: Class

A

adrenergic antagonist - alpha-non-selective

116
Q

Phenoxybenzamine: MOA

A

irreversibly blocks alpha adrenergic receptors (α1 > α2)

117
Q

Phenoxybenzamine: Uses

A

pheochromocytoma (pre-op)

118
Q

Phenoxybenzamine: Side Effects

A

orthostatic hypotension, reflex tachycardia, GI irritation

119
Q

Phenoxybenzamine: Forms covalent bond with

A

alpha receptors - lasts for days

120
Q

Phentolamine: Class

A

adrenergic antagonist - alpha-non-selective

121
Q

Phentolamine: MOA

A

reversibly blocks alpha adrenergic receptors (α1 > α2)

122
Q

Phentolamine: Uses

A

pheochromocytoma (pre-op), antidote to alpha 1 agonist overdose, rebound hypertension

123
Q

Phentolamine: Side Effects

A

orthostatic hypotension, reflex tachycardia, GI irritation

124
Q

Prazosin: Similar Drugs

A

doxazosin, terazosin, tamsulosin, silodosin

125
Q

Prazosin: Class

A

adrenergic antagonist - alpha 1-selective

126
Q

Prazosin: MOA

A

selectively blocks alpha 1 adrenergic receptors

127
Q

Prazosin: Uses

A

benign prostatic hyperplasia, hypertension

128
Q

Prazosin: Side Effects

A

first dose orthostatic hypotension, reflex tachycardia

129
Q

Prazosin: Most selective for prostatic smooth muscle

A

tamsulosin

130
Q

Pharmacologic advantage of alpha 1 selectivity

A

reflex tachycardia is less common and less severe

131
Q

Propranolol: Similar Drugs

A

pindolol, timolol, labetalol, carvedilol, nadolol

132
Q

Propranolol: Class

A

adrenergic antagonist - beta-non-selective

133
Q

Propranolol: MOA

A

blocks beta 1 and 2 receptors, blocks sympathetic effects on heart and BP, reduces renin release

134
Q

Propranolol: Uses

A

angina prophylaxis, hypertension, arrhythmias, migraine, performance anxiety, hyperthyroidism

135
Q

Propranolol: Side Effects

A

bronchospasm, AV block, heart failure, CNS sedation, erectile dysfunction

136
Q

Propranolol: Masks symptoms of

A

hypoglycemia in diabetics

137
Q

Propranolol: Carvedilol and Labetalol have combined

A

alpha and beta blockade (pheochromocytoma)

138
Q

In diabetics beta-blockers impair

A

hepatic mobilization of glucose

139
Q

Beta-Blockers: partial agonist activity, advantage in treating patients with asthma because these drugs are less likely to cause bronchospasm

A

Acebutolol, Pindolol (Intrinsic Sympathomimetic Activity)

140
Q

Beta-Blockers: membrane-stabilizing activity, decreases protective reflexes, increases risk of corneal ulceration

A

Local Anesthetic Activity

141
Q

Beta-Blockers that lack Local Anesthetic Activity

A

Timolol, Betaxolol (glaucoma)

142
Q

Beta-Blockers: Longest Half-Life

143
Q

Beta-Blockers: Shortest Half-Life

144
Q

Atenolol: Similar Drugs

A

betaxolol, esmolol, acebutolol, metoprolol

145
Q

Atenolol: Class

A

adrenergic antagonist - beta 1-selective

146
Q

Atenolol: MOA

A

selectively blocks beta 1, blocks sympathetic effects on heart and BP

147
Q

Atenolol: Uses

A

angina, hypertension, heart failure, supraventricular tachycardia (esmolol)

148
Q

Atenolol: Side Effects

A

bronchospasm, AV block, heart failure, CNS sedation, erectile dysfunction

149
Q

Atenolol: Masks symptoms of

A

hypoglycemia in diabetics

Pharmacology (34 decks)

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