VIII - Adrenergic Pharmacology Flashcards
(149 cards)
1
Q
Primary neurotransmitter at the sympathetic post-ganglionic neuron effector cell synapses in most tissues
A
Norepinephrine
2
Q
Sympathetic post-ganglionic neuron effector cell synapses use norepinephrine except
A
eccrine sweat glands, vasodilator sympathetic fibers in the skeletal muscle
3
Q
Steps in Adrenergic Stimulation
A
synthesis, storage, release, termination
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
5
Q
Adrenergic Stimulation: tyrosine hydroxylation is inhibited by
A
metyrosine
6
Q
Adrenergic Stimulation: Step 2
A
norepinephrine and dopamine are transported into vesicles, MAOIs increase stores of NE and dopamine
7
Q
Adrenergic Stimulation: vesicular transport is inhibited
A
reserpine
8
Q
Adrenergic Stimulation: Step 3
A
entry of Ca triggers interaction among SNARE proteins (VAMPs and SNAPs)
9
Q
Adrenergic Stimulation: inhibits interaction among SNARE proteins
A
guanethidine
10
Q
Adrenergic Stimulation: promotes interaction among SNARE proteins
A
amphetamine, tyramine
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
12
Q
Adrenergic Stimulation: diffusion and reuptake via NET and DAT is inhibited by
A
cocaine, TCAs
13
Q
Adrenergic Stimulation: metabolism of norepinephrine into metanephrine and VMA is inhibited by
A
MAOIs, COMT Inhibitors
14
Q
Cholinergic Inhibitors: Synthesis
A
hemicholinium
15
Q
Cholinergic Inhibitors: Storage
A
vesamicol
16
Q
Cholinergic Inhibitors: Release
A
botulinum
17
Q
Cholinergic Inhibitors: Metabolism
A
neostigmine
18
Q
Cholinergic Inhibitors: Reuptake
A
none
19
Q
Adrenergic Inhibitors: Synthesis
A
metyrosine
20
Q
Adrenergic Inhibitors: Storage
A
reserpine
21
Q
Adrenergic Inhibitors: Release
A
guanethidine
22
Q
Adrenergic Inhibitors: Metabolism
A
MAOIs, COMTIs
23
Q
Adrenergic Inhibitors: Reuptake
A
cocaine, TCAs
24
Q
Adrenoreceptors: effector tissues, smooth muscle, glands, Gq, inc. IP3, DAG, inc. Ca, contraction, secretion
A
Alpha 1
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Adrenoreceptors: nerve endings, smooth muscles, Gi, dec. cAMP, dec. transmitter release, contraction
Alpha 2
26
Adrenoreceptors: cardiac muscle, JG apparatus, Gs, inc. cAMP, inc. heart rate and contractility, inc. renin
Beta 1
27
Adrenoreceptors: smooth muscle, liver, heart, Gs, inc. cAMP, relax smooth muscle, inc. glycogenolysis, inc. heart rate and contractility
Beta 2
28
Adrenoreceptors: adipose cells, Gs, inc. cAMP, inc. lipolysis
Beta 3
29
Adrenoreceptors: smooth muscle, Gs, inc. cAMP, relax renal vascular smooth muscle
Dopamine 1
30
Adrenoreceptors: contracts most vascular smooth muscle
Alpha 1
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Adrenoreceptors: contracts pupillary dilator muscle
Alpha 1
32
Adrenoreceptors: contracts pilomotor smooth muscle
Alpha 1
33
Adrenoreceptors: inhibits adrenergic and cholinergic transmitter release
Alpha 2
34
Adrenoreceptors: stimulates platelet aggregation
Alpha 2
35
Adrenoreceptors: contracts some vascular smooth muscle
Alpha 2
36
Adrenoreceptors: inhibits lipolysis
Alpha 2
37
Adrenoreceptors: inhibits insulin release
Alpha 2
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Adrenoreceptors: stimulates heart rate and forces
Beta 1, Beta 2
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Adrenoreceptors: stimulates renin release from JG cells of the kidney
Beta 1
40
Adrenoreceptors: relaxes airway, uterine and vascular smooth muscle
Beta 2
41
Adrenoreceptors: stimulates glycogenolysis
Alpha 1, Beta 2
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Adrenoreceptors: stimulates insulin release
Beta 2
43
Adrenoreceptors: causes tremors by stimulating somatic motor neuron terminals
Beta 2
44
Adrenoreceptors: stimulates lipolysis
Beta 3
45
Adrenoreceptors: dilates renal and other splanchnic blood vessels
Dopamine 1
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Adrenoreceptors: inhibits adenylyl cyclase in nerve terminals
Dopamine 2
47
Activate adrenoreceptors directly and indirectly by increasing concentration of available catecholamines in the synapses (release of stored catecholamines, inhibition of reuptake)
Sympathomimetics
48
Epinephrine: Class
sympathomimetic - non-selective, direct-acting
49
Epinephrine: MOA
activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)
50
Epinephrine: Uses
cardiac arrest, anaphylaxis, asthma, COPD, hemostasis
51
Epinephrine: Side Effects
hypertension, tachycardia, ischemia, hyperglycemia
52
Norepinephrine: Class
sympathomimetic - non-selective, direct-acting
53
Norepinephrine: MOA
activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)
54
Norepinephrine: Uses
neurogenic shock, cardiogenic shock (last resort)
55
Norepinephrine: Side Effects
extreme vasospasm, tissue necrosis, excessive blood pressure increase, arrythmias, infarction, reflex bradycardia
56
Norepinephrine: Compensatory vagal reflexes tend to overcome
the direct positive chronotropic effects
57
Dopamine: Class
sympathomimetic - non-selective, direct-acting
58
Dopamine: MOA
activates alpha 1 (vasoconstricion, increases BP), beta 1 (increased HR, conduction and contractility), dopamine 1 (vasodilation of splanchnic and renal muscles)
59
Dopamine: Uses
shock, heart failure
60
Dopamine: Side Effects
cardiovascular disturbance, arrythmias
61
Dopamine: Low-Dose
1-5 mcg/kg/min, D1 receptors, vasodilation in the splanchnic and renal vascular beds
62
Dopamine: Medium Dose
5-15 mcg/kg/min, B1 receptors, increase renal blood flow, heart rate, cardiac contractility and cardiac output
63
Dopamine: High Dose
> 15 mcg/kg/min, alpha receptors, vasoconstriction, increased BP
64
Isoproterenol: Class
sympathomimetic - beta-non-selective
65
Isoproterenol: MOA
non-selectively activates beta 1 (increased HR, conduction and contractility), beta 2 (bronchodilation)
66
Isoproterenol: Uses
asthma
67
Isoproterenol: Side Effects
cardiovascular disturbance, arrhythmias
68
Phenylephrine: Similar Drugs
pseudoephedrine
69
Phenylephrine: Class
sympathomimetic - alpha 1-selective
70
Phenylephrine: MOA
selectively activates alpha 1 (vasoconstricion, increases BP)
71
Phenylephrine: Uses
decongestant, mydriatic, drug-induced hypotension, spinal shock
72
Phenylephrine: Side Effects
rebound nasal congestion, hypertension, stroke, myocardial infarction
73
Phenylephrine: Ocular administration causes mydriasis without
cyclopegia
74
Clonidine: Class
sympathomimetic - alpha 2-selective
75
Clonidine: MOA
selectively activates alpha 2 (decreases central sympathetic outflow)
76
Clonidine: Uses
hypertension, cancer pain, opioid withdrawal
77
Clonidine: Side Effects
sedation, rebound hypertension, dry mouth
78
Clonidine: Avoid rebound hypertension by
tapering use to discontinuation
79
Clonidine: Treat rebound hypertension with
phentolamine
80
Methyldopa: Class
sympathomimetic - alpha 2-selective
81
Methyldopa: MOA
selectively activates alpha 2 (decreases central sympathetic outflow)
82
Methyldopa: Uses
pre-eclampsia
83
Methyldopa: Side Effects
sedation, hemolytic anemia (positive Coomb's test)
84
Apraclonidine: Similar Drugs
brimonidine
85
Apraclonidine: Class
sympathomimetic - alpha 2-selective
86
Apraclonidine: MOA
selectively activates alpha 2 (decreases secretion of aqueous humor)
87
Apraclonidine: Uses
glaucoma
88
Apraclonidine: Side Effects
BOV, dry mouth, conjunctivitis
89
Dobutamine: Class
sympathomimetic - beta 1-selective
90
Dobutamine: MOA
selectively activates beta 1 (increased HR and contractility)
91
Dobutamine: Uses
acute heart failure, cardiogenic shock
92
Dobutamine: Side Effects
tachycardia, arrhythmias, tachyphylaxis
93
Dobutamine: May also be used in
cardiac stress testing
94
Albuterol/Salbutamol: Similar Drugs
terbutaline, ritodrine
95
Albuterol/Salbutamol: Class
sympathomimetic - beta 2-selective
96
Albuterol/Salbutamol: MOA
selectively activates beta 2 (bronchodilation)
97
Albuterol/Salbutamol: Uses
acute asthma attack (drug of choice), tocolysis for preterm labor (terbutaline, ritodrine)
98
Albuterol/Salbutamol: Side Effects
tachycardia, tremors, nervousness, restlessness, arrhythmias when used excessively, loss of responsiveness (tolerance, tachyphylaxis)
99
Albuterol/Salbutamol: May precipitate arrythmias in a patient with
COPD and heart disease
100
Sympathomimetics: acute heart failure tx
β1 & D1 agonists
101
Sympathomimetics: septic shock tx
β1 & D1 agonists
102
Sympathomimetics: increased cardiac output
β1 & D1 agonists
103
Sympathomimetics: hemostasis
α1 agonist
104
Sympathomimetics: decongestion
α1 agonist
105
Sympathomimetics: vasoconstriction
α1 agonist
106
Sympathomimetics: temporary maintenance of BP
α1 agonist
107
Sympathomimetics: bronchospasm tx
β2 agonist
108
Sympathomimetics: premature labor tx
β2 agonist
109
Sympathomimetics: bronchodilation
β2 agonist
110
Sympathomimetics: uterine smooth muscle relaxation
β2 agonist
111
Sympathomimetics: hypertension tx
α2 agonist
112
Sympathomimetics: glaucoma tx
α2 agonist
113
Sympathomimetics: spinal shock tx
α2 agonist
114
Sympathomimetics: decrease BP
α2 agonist
115
Phenoxybenzamine: Class
adrenergic antagonist - alpha-non-selective
116
Phenoxybenzamine: MOA
irreversibly blocks alpha adrenergic receptors (α1 > α2)
117
Phenoxybenzamine: Uses
pheochromocytoma (pre-op)
118
Phenoxybenzamine: Side Effects
orthostatic hypotension, reflex tachycardia, GI irritation
119
Phenoxybenzamine: Forms covalent bond with
alpha receptors - lasts for days
120
Phentolamine: Class
adrenergic antagonist - alpha-non-selective
121
Phentolamine: MOA
reversibly blocks alpha adrenergic receptors (α1 > α2)
122
Phentolamine: Uses
pheochromocytoma (pre-op), antidote to alpha 1 agonist overdose, rebound hypertension
123
Phentolamine: Side Effects
orthostatic hypotension, reflex tachycardia, GI irritation
124
Prazosin: Similar Drugs
doxazosin, terazosin, tamsulosin, silodosin
125
Prazosin: Class
adrenergic antagonist - alpha 1-selective
126
Prazosin: MOA
selectively blocks alpha 1 adrenergic receptors
127
Prazosin: Uses
benign prostatic hyperplasia, hypertension
128
Prazosin: Side Effects
first dose orthostatic hypotension, reflex tachycardia
129
Prazosin: Most selective for prostatic smooth muscle
tamsulosin
130
Pharmacologic advantage of alpha 1 selectivity
reflex tachycardia is less common and less severe
131
Propranolol: Similar Drugs
pindolol, timolol, labetalol, carvedilol, nadolol
132
Propranolol: Class
adrenergic antagonist - beta-non-selective
133
Propranolol: MOA
blocks beta 1 and 2 receptors, blocks sympathetic effects on heart and BP, reduces renin release
134
Propranolol: Uses
angina prophylaxis, hypertension, arrhythmias, migraine, performance anxiety, hyperthyroidism
135
Propranolol: Side Effects
bronchospasm, AV block, heart failure, CNS sedation, erectile dysfunction
136
Propranolol: Masks symptoms of
hypoglycemia in diabetics
137
Propranolol: Carvedilol and Labetalol have combined
alpha and beta blockade (pheochromocytoma)
138
In diabetics beta-blockers impair
hepatic mobilization of glucose
139
Beta-Blockers: partial agonist activity, advantage in treating patients with asthma because these drugs are less likely to cause bronchospasm
Acebutolol, Pindolol (Intrinsic Sympathomimetic Activity)
140
Beta-Blockers: membrane-stabilizing activity, decreases protective reflexes, increases risk of corneal ulceration
Local Anesthetic Activity
141
Beta-Blockers that lack Local Anesthetic Activity
Timolol, Betaxolol (glaucoma)
142
Beta-Blockers: Longest Half-Life
Nadolol
143
Beta-Blockers: Shortest Half-Life
Esmolol
144
Atenolol: Similar Drugs
betaxolol, esmolol, acebutolol, metoprolol
145
Atenolol: Class
adrenergic antagonist - beta 1-selective
146
Atenolol: MOA
selectively blocks beta 1, blocks sympathetic effects on heart and BP
147
Atenolol: Uses
angina, hypertension, heart failure, supraventricular tachycardia (esmolol)
148
Atenolol: Side Effects
bronchospasm, AV block, heart failure, CNS sedation, erectile dysfunction
149
Atenolol: Masks symptoms of
hypoglycemia in diabetics
