Adrenergics Flashcards

1
Q

Rate limiter in NE synthesis

A

conversion of tyrosine to DOPA

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2
Q

Dopamine is converted into…..

A

NE

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3
Q

Causes opening of vesicles to release NE

A

opening of Ca channels

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4
Q

NE Presynaptic receptor

A

a2 - Gi

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5
Q

Fates of NE

A

response on target organ- a or B
metabolized to inactive metabolites
reuptake

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6
Q

COMT

A

metabolizes NE into inactive metabolites

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7
Q

Reason for short half life of NE

A

rapid reuptake

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8
Q

Reason for short half life of Ach

A

rapid metabolism

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9
Q

a2 Agonist

A

more feedback

stops NE release

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10
Q

a2 Antagonist

A

more NE released

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11
Q

COMT Inhibitors

A

less metabolism, more NE available

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12
Q

Cocaine

A

blocks reuptake at Na/ K pump

more NE available

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13
Q

Imipramine

A

blocks reuptake

more NE available

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14
Q

MOAI

Monoamine oxidase inhibitor

A

increases recycling, more NE released

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15
Q

a1 Receptor

A

on target organ

use Gq

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16
Q

a2 Receptor

A

negative feedback presynaptic receptors

Gi

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17
Q

B Receptors

A

Gs

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18
Q

B1 has higher affinity for Epi or NE?

A

equal

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19
Q

B2 has higher affinity for Epi or NE?

A

Epi

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20
Q

Catecholamines

A

Epi, NE, dopamine

have short half lives

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21
Q

a1 Locations

A

vascular smooth muscle
pupillary dilator
prostate (a1A)

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22
Q

a1 Effects

A

muscle contraction
pupil dilation
prostate contraction; decrease urine output
raises blood pressure

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23
Q

Enlarged Prostate

A

a1A blocker to relax

avoid a agonists and M antagonists

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24
Q

a2 Locations

A

adrenergic presynaptic nerve terminals

pancreatic B cells

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25
a2 Effects
negative feedback/ inhibit NE release | inhibits insulin release/ decreases storage
26
B1 Locations
``` heart juxtaglomerular cells (JGA) ```
27
B1 Effects
increase heart rate and force | stim renin release
28
B2 Locations
respiratory, uterine, vascular smooth muscle liver voluntary muscle
29
B2 Effects
relaxes smooth muscle- bronchodilation, stop premature labor, decrease BP stimulates glycogenesis causes tremor
30
How is B2 activated?
Epi in blood | not innervated
31
B3 Locations
fat cells
32
B3 Effects
stim lipolysis
33
Dopamine Receptor Locations
renal and blood vessels
34
Dopamine Receptor Effects
relaxes renal and blood vessels - vasodilation
35
CNS Effects
do not enter except for amphetamines
36
Eye Effect
mydriasis (a1)
37
Bronchi Effects
relax (B2)
38
GI Effects
relax (B2)
39
Urinary Effects
``` contract (a1) relax detrusor (B3) ```
40
a1 Effects on Vascular System
increase pressure | reflex bradycardia
41
B2 Effects on Vascular System
reduce pressure | reflex tachycardia
42
Low Dose Dopamine
vasodilation of renal vessels (D1)
43
Medium Dose Dopamine
has B1 effect on heart- increases rate
44
High Dose Dopamine
acts on a1 to increase TPR and BP
45
Direct Acting Adrenergic Agonists | NE
a1, a2, B1 increase TPR and BP long term reflex bradycardia
46
Direct Acting Adrenergic Agonists | Epi
a1, a2, B1, B2
47
Direct Acting Adrenergic Agonists | Epi Low Dose
lowers BP and increases HR
48
Direct Acting Adrenergic Agonists | Epi High Dose
increase BP | initial tachycardia followed by long term bradycardia
49
Examples of Direct Acting Adrenergic Agonists
Isoproterenol Phenylephrine Albuterol Mirabegron
50
Isoproterenol
B1, B2 agonist | not used
51
Phenylephrine
a1 agonist | mydriasis
52
Albuterol
B2 agonist
53
Mirabegron
B3 agonist for urinary incontinence
54
Indirect Acting Adrenergic Agonists
don't act on a or B receptors | go into nerve and release NE from vesicles
55
Indirect Acting Adrenergic Agonists Examples
Amphetamine Tyramine Cocaine
56
Amphetamine
increases NE release a1 for vasoconstriction B1 increased heart rate
57
Tyramine
increases NE release in ripe cheese and red wine oxidized by MAO and normally has no effect
58
Combining Tyramine and MOAI
hypertensive crisis
59
Cocaine
blocks reuptake of NE a1 vasoconstriction B1 increased heart rate
60
Ephedrine
mixed action adrenergic agonist increases NE release direct action on a and B like Epi
61
Treating Anaphylactic Shock
Ephedrine
62
Treating Acute Asthmatic Bronchoconstriction
B2 agonists
63
Irreversible a-Adrenergic Blockers
long lasting | nonselective so blocks a1 and a2
64
Phenoxybenzamine
Irreversible a-Adrenergic Blocker | lasts 48 hours
65
Examples of Reversible a-Adrenergic Blockers
Zosins (a1) | mirtazapine (a2)
66
a2 Block at Heart
increased levels of NE- tachycardia
67
Pheochromocytoma
tumor of adrenal medulla increases NE and Epi = increase BP uses phenoxybenzamine before surgery (a1 block)
68
Benign Prostatic Hyperplasia
enlarged prostate | treat with Zosins (a1A block)
69
Hypertension Treatment
Zosins | a1 block
70
a Blocker Toxicity
hypotension and reflex tachycardia | first dose should be slow
71
B Blocker Examples
Olols | labetalol and carvedilol
72
Nonspecific B Blockers Examples
N-Z Olols
73
B1 Specific B Blockers Examples
A-M Olols
74
a1 and B Blockers
labetalol | carvedilol
75
B Blockers and Heart
blocks B1 for decreased rate | blocks B2 to prevent vasodilation
76
B Blockers and Renal
block B1 to inhibit renin release
77
B Blockers and Lungs
block B2 to cause bronchoconstriction
78
B Blockers and Glucose Metabolism
block B2 causing decreased glycogenolysis and lowers blood glucose
79
Glaucoma Treatment
B blocker decreases aqueous humor production
80
B Blocker Toxicity
Hypotension, bradycardia fatigue and sleep disturbance (CNS) increase plasma lipids (decrease insulin)