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Week 3 (Midterm) (Adrenergic) Flashcards

1
Q

Organs of the somatic system

A

skeletal muscle

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2
Q

Function of the somatic system

A

Voluntary movement

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3
Q

Receptor for the somatic system

A

Cholinergic (Nicotinic)

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4
Q

Sympathetic organs

A

heart, bronchiole, vascular smooth muscle

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5
Q

What type of receptor are nicotinic receptors?

A

Na+ gated channels

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6
Q

Receptor for sympathetic system

A

Adrenergic

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7
Q

What type of receptor are adrenergic receptors?

A

G-protein coupled, binds NE, Epi

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8
Q

Alpha-1, binds which G?

A

Gq

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9
Q

Alpha-1, agonistic response?

A

↑ BP (constricts smooth muscle)

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10
Q

Alpha-2, binds which G?

A

Gi

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11
Q

Alpha-2, agonistic response?

A

↓ BP, centrally (vasodilation)

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12
Q

Beta-1, binds which G?

A

Gs

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13
Q

Beta-1, agonistic response?

A

↑HR, ↑cardiac contractility

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14
Q

Beta-2, binds which G?

A

Gs

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15
Q

B-2, agonistic response?

A

bronchodilation, ↓BP (dilates arterioles), relaxation of uterus

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16
Q

Neurotransmitter for pre-ganglionic neurons?

A

ACh (somatic, sympathetic and parasympathetic)

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17
Q

Organs for parasympathetic system

A

heart, GI tract smooth muscle

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18
Q

Receptor for parasympathetic system

A

Cholinergic (muscarinic)

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19
Q

What type of receptor is muscarinic?

A

G-Protein

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20
Q

M1 and M3 bind which G?

A

Gq

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21
Q

M1 and M3 site?

A

(vasodilation) endothelium of vasculature, autonomic ganglia, gastric parietal cells, exocrine glands, smooth muscle

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22
Q

M2 and M4, which G?

A

Gi

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23
Q

M2 and M4, site?

A

SA, AV nodal cells, CNS

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24
Q

What is the exception to short preganglionic in the sympathetic system?

A

adrenal medula

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25
What are the 4 cranial nerves involved in parasympathetic functions?
3, 7, 9, 10
26
Adrenergic pre-ganglionic neurons secrete:
ACh (receptor is nicotinic)
27
Adrenergic post-ganglionic neurons secrete:
NE (receptor is adrenergic)
28
Where does NE go to Epi?
In the adrenal medulla
29
Step 1: Tyrosine to _____
L-DOPA
30
Step 1: Tyrosine to L-DOPA (Enzyme)
Tyrosine hydroxylase
31
Step 1: Tyrosine to L-DOPA (inhibited by)
metyrosine and NE
32
What is the rate limiting step in synthesizing NE?
Tyrosine --> L-DOPA
33
What is metyrosine used to treat?
pheochromocytoma
34
Step 2: L-DOPA to _____
Dopamine
35
Step 2: L-DOPA to Dopamine (Enzyme)
AAAD | L-DOPA decarboxylase
36
Step 2: L-DOPA to Dopamine (inhibited by)
Carbidopa
37
Breakdown of Dopamine enzyme
MAO-B
38
MAO-B inhibitor
Deprenyl
39
Step 3: Dopamine to ____
NE
40
Step 3: Dopamine to NE (enzyme)
Dopamine Beta-hydroxylase
41
Step 3: Dopamine to NE (inhibited by)
Copper chelators i.e. Disulfiram
42
Step 4: NE to Epi (enzyme)
PNMT
43
Carbidopa and parkinson's
Given to build-up L-DOPA in plasma, which can cross the BBB to be converted to dopamine
44
Amantadine and parkinson's
Stimulates release of dopamine in vesicles
45
MPTP
Heroine substitute metabolized by MAO-B into toxin --> presents like PD
46
What inhibits the release of catecholamines?
Adrenergics (a2) attached to Gi subunits
47
Catecholamines are taken back up by:
Sodium channels (uptake-1)
48
Catecholamines are broken down by:
COMT
49
INDIRECT CATECHOLAMINE ANTAGONISTS: Reserpine and BBB
Crosses the BBB
50
INDIRECT CATECHOLAMINE ANTAGONISTS: Reserpine and action
permanent inhibition of amine-H+ for catecholamine packaging into vesicles; action duration much longer than plasma half-life
51
INDIRECT CATECHOLAMINE ANTAGONISTS: Reserpine and effect
Deplete catecholamine stores
52
INDIRECT CATECHOLAMINE ANTAGONISTS: Reserpine and use
Hypertension
53
INDIRECT CATECHOLAMINE ANTAGONISTS: Reserpine and side effects
Depression, parkinsonism, gynecomastia
54
INDIRECT CATECHOLAMINE ANTAGONISTS: Clonidine action
alpha-2 agonist --> inhibits release of catecholamine vesicles
55
INDIRECT CATECHOLAMINE ANTAGONISTS: Clonidine effect
decreased catecholamines in synapse
56
INDIRECT CATECHOLAMINE ANTAGONISTS: Clonidine use
hypertension
57
INDIRECT CATECHOLAMINE ANTAGONISTS: Clonidine side effects
dry mouth, drowsiness (somnolence)
58
INDIRECT CATECHOLAMINE ANTAGONISTS: Metyrosine action
inhibits tyrosine
59
INDIRECT CATECHOLAMINE ANTAGONISTS: Metyrosine effect
no neurotransmitter stored
60
INDIRECT CATECHOLAMINE ANTAGONISTS: Metyrosine use
pheochromocytoma
61
INDIRECT CATECHOLAMINE ANTAGONISTS: Metyrosine side effects
Hypotension, sedation
62
INDIRECT CATECHOLAMINE AGONISTS: Guanethdine/Guanadrel action
inhibits release of packaged catecholamine stores by inhibitig vesicle fusion; competitive inhibition of Uptake-1
63
INDIRECT CATECHOLAMINE AGONISTS: Guanethdine/Guanadrel effect
depletes catecholamine stores by inhibiting vesicle fusion
64
INDIRECT CATECHOLAMINE AGONISTS: Guanethdine/Guanadrel use
Hypertension (obsolete)
65
INDIRECT CATECHOLAMINE AGONISTS: Guanethdine/Guanadrel side effects
Postural hypotension; hypertension on first administration
66
Which has a longer half-life? Guanethidine or Guanadrel?
Guanethidine
67
INDIRECT CATECHOLAMINE AGONISTS: Tyramine action
Displaces catecholamines out of nerve terminal; competitive inhibition of uptake-1
68
INDIRECT CATECHOLAMINE AGONISTS: Tyramine Effect
↑ catecholamine in synapse
69
INDIRECT CATECHOLAMINE AGONISTS: Tyramine side effects
"cheese syndrome", hypertensive crisis, hypertension, vasoconstriction, tachycardia
70
What is tyramine metabolized by?
MAO
71
INDIRECT CATECHOLAMINE AGONISTS: Amphetamines /Ephedrine/ Pseudoephedrine action
Displaces catecholamines out of nerve terminal; competitive inhibition of uptake-1
72
INDIRECT CATECHOLAMINE AGONISTS: Amphetamines /Ephedrine/ Pseudoephedrine effect
↑ catecholamine in synapse (indirect release of catecholamines)
73
INDIRECT CATECHOLAMINE AGONISTS: Amphetamines /Ephedrine/ Pseudoephedrine use
Amphetamine: stimulant, ↑ wakefulness, appetite suppressant, and recreational drug Ephedrine: decongestant
74
INDIRECT CATECHOLAMINE AGONISTS: Amphetamines /Ephedrine/ Pseudoephedrine side effects
hyperactivity, dilated pupils, ED, ↑BR and HR, sweating, hypertension, insomnia, dependence
75
INDIRECT CATECHOLAMINE AGONISTS: Tricyclic Anti-Depressents and BBB
Crosses BBB
76
INDIRECT CATECHOLAMINE AGONISTS: Tricyclic Anti-Depressents action
inhibits uptake-1
77
INDIRECT CATECHOLAMINE AGONISTS: Tricyclic Anti-Depressents effect
increase catecholamine in synapse
78
INDIRECT CATECHOLAMINE AGONISTS: Tricyclic Anti-Depressents use
depression
79
INDIRECT CATECHOLAMINE AGONISTS: Tricyclic Anti-Depressents side effects
sudden death
80
INDIRECT CATECHOLAMINE AGONISTS: Cocaine action
CNS: inhibits Uptake-1 PNS: inhibits Na+ channels
81
INDIRECT CATECHOLAMINE AGONISTS: Cocaine effect
increased catecholamine in synapse; prevents neuronal excitation
82
INDIRECT CATECHOLAMINE AGONISTS: Cocaine use
local anesthetic, recreational drug
83
INDIRECT CATECHOLAMINE AGONISTS: Cocaine side effects
euphoria, increased HR and BP, convulsions, dependence
84
Epinephrine (adrenaline) Mechanism
α1, α2, β1, β2 agonist (even split between α and β)
85
Epinephrine Use
cardiac arrest, correct low cardiac output, anaphylaxis, added to local anesthetics
86
Epinephrine SE
hypertension*, vasoconstriction, tachycardia, ventricular dysrhythmias
87
Norepinephrine mechanism
predominantly α1 and α2 agonist; mild β1 agonist
88
Norepinephrine use
correct hypotension (critical care setting) - probably mainly via α1 vasoconstriction action
89
Norepinephrine SE
hypertension*, vasoconstriction, tachycardia, ventricular dysrhythmias
90
Which causes less hypertension, epi or NE?
Epi b/c NE prefers alpha receptors
91
Phenylephrine, Methoxamine mechanism
alpha-1 agonist
92
Phenylephrine, methoxamine use
Decongestant, pupil dilator, for septic shock or profound hypotension
93
Phenylephrine, methoxamine SE
hypertension, reflex bradycardia
94
Clonidine, alpha-methylnoradrenaline mechanism
alpha-2 partial agonist
95
Clonidine, alpha-methylnoradrenaline use
hypertension, migraine
96
Clonidine, alpha-methylnoradrenaline SE
somnolence, orthostatic hypotension, edema, weight gain, rebound hypertension
97
Isoproterenol mechanism
Beta-1, beta-2 agonist
98
Isoproterenol use
Heart failure, asthma - obsolete
99
Isoproterenol SE
Tachycardia, dysrhythmias
100
Dobutamine mechanism
Beta-1 agonist
101
Dobutamine use
stress test, heart failure, shock
102
Dobutamine SE
dysrhythmias
103
Albuterol, terbutaline mechanism
beta-2 agonist
104
Albuterol, terbutaline use
asthma, pre-term labor (tocolytic anti-contraction)
105
Albuterol, terbutaline SE
tachycardia, dysrhythmias, tremor, peripheral vasodilation
106
Phenoxybenzamine, phentolamine mechanism
alpha-1, alpha-2 antagonist
107
Phenoxybenzamine, phentolamine use
pheochromocytoma (neuroendocrine tumor of adrenal medulla)
108
Phenoxybenzamine, phentolamine SE
hypotension, flushing, tachycardia, nasal congestion, impotence
109
Prazosin mechanism
alpha-1 antagonist
110
Prazosin use
hypertension
111
Prazosin SE
hypotension, flushing, tachycardia, nasal congestion, impotence
112
Yohimbine mechanism
alpha-2 antagonist
113
Yohimbine use
not used clinically
114
Carvedilol mechanism
alpha-1, beta-1, beta-2 antagonist
115
Carvedilol use
heart failure
116
Carvedilol SE
exacerbation of initial heart failure, renal failure
117
Nebivolol mechanism
Beta-1 antagonist + vasodilation
118
Nebivolol use
hypertension, heart failure
119
Nebivolol SE
fatigue, headache
120
Propanolol mechanism
beta-1, beta-2 antagonist
121
Propanolol use
hypertension, migraine prophylaxis, angina, anxiety tremor, glaucoma
122
Propanolol SE
bronchoconstriction, cardiac failure, cold extremities, fatigue, depression, hypoglycemia]
123
Atenolol, metoprolol mechanism
Beta-1 antagonist
124
Atenolol, metoprolol use
hypertension, arrhythmia, angina at MI
125
Atenolol, metoprolol SE
cardiac failure, cold extremities, fatigue, depression, hypoglycemia
126
Prazosin + epinephrine =
decreased BP (unopposed alpha-2, beta-2 agonism)
127
Tyramine + MAO-inhibitors =
Causes hypertensive crisis
128
Tyramine + MAO-Inhibitors + TCA (imipramine) =
TCA blocks Uptake 1 --> no tyramine inside terminal --> no effect

Pharm (9 decks)

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