Autonomic Pharmacology Flashcards

(74 cards)

1
Q

Which enzymes synthesizes Ach by combining acetyl CoA + choline?

A

ChAT

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2
Q

True or False: the rate limiting step in Ach synthesis is ChAT.

A

False! it’s by the amt of choline thats available.

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3
Q

Which pump pumps chiline into presynaptic terminal?

A

Na/Choline transporter

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4
Q

What drug inhibits the Na/Choline transporter, thus increasing [choline]synapse?

A

hemocholinium

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5
Q

What is the transporter to get Ach into the secretory vesicle?

A

H/Ach antiporter

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6
Q

Which drug inhibits the H/Ach antiporter?

A

Vesamicol

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7
Q

The increase concentration of which ion causes the secretory vesicles to fuse with the terminal membrane of the presynaptic terminal?

A

Ca++

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8
Q

What is the syndrome that blocks the uptake of Ca++ into the cytoplasm, thus inhibiting Ach release?

A

Lambert-Easton syndrome

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9
Q

Which toxin blocks exocytosis of presynaptic vesicles, thus blocking the release of Ach?

A

Botulinum toxin

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10
Q

Which AA are adrenergic hormones synthesized from?

A

Tyr

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11
Q

Which transporter transports NE into the presynaptic terminal to be released?

A

NET

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12
Q

Tell me the steps of the synthesis of Tyr –> NE

A

Tyr –TH–> L-DOPA –> D –> NE –> E

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13
Q

Which enzyme is the RLS of the adrenergic synthesis pathway?

A

Tyrosine Hydroxylase (TH)

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14
Q

Tryosine degraded only to Dopamine in the cytoplasm, so how is dopamine taken up into secretory vesicles to be potentially further converted to NE/E?

A

VMAT transporter

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15
Q

Which drug inhibits VMAT, therefore decreasing release of adrenergic hormones?

A

Reserpine

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16
Q

Which drug inhibits NET, therefore increasing NE in the synpase?

A

COCAINE

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17
Q

Which drug inhibits tyrosine hydroxylase to make adrenergic hormones?

A

a-methyltyrosine

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18
Q

For what condition is a-methyltyrosine used to treat?

A

HTN with pheochromocytoma

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19
Q

True or False: reserpine isnt used any more cuz the cell can just make new vesicles with VMATs.

A

True

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20
Q

What is the action of tyramine to inhibit NE release from cells?

A

takes the place of NE in vesicles

“tyramine is MEAN”

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21
Q

Guanethidine act like tyramine by taking the place of NE in vesicles, thus decreasing what cardiovascular factor?

A

Cardiac output

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22
Q

What are the 3 actions of amphetamine to treat depression and nercolepsy?

A
  1. displaces endogenous catecholamines
  2. weak inhibitor of MAO
  3. blocks NET reuptake
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23
Q

Ephedrine/pseudoephedrine stimulate beta receptors, thus treating which condition?

A

nasal/sinus congestion

u can also make meth from this. thanks breaking bad.

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24
Q

Methylphenidate is a structural analogue of amphetamine, and is used to treat what condition?

A

ADHD

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25
What does tricyclic antidepressants block to treat depression?
NET and serotonin reuptake
26
This nonselective MAOi causes more catecholamines to be present in the presynaptic vesicles.
Phenelzine
27
Stimulation of a1-receptors causes what to the BP?
rise cuz it increased peripheral vascular resistance
28
Stimulation of a2-receptors causes what to the BP?
lowers by acting on brainstem centers
29
Stimulation of B1-receptors causes what to the BP?
increase HR and force of cardiac muscle contraction --> increase BP
30
Stimulation of B2-receptors causes what to the BP?
causes relaxation of vascular, bronchial, and GI smooth muscle --> decrease BP
31
M1- location
autonomic ganglia, viscera, CNS
32
M1- actions
EPSPs
33
M2- location
heart
34
M2-action
slows, decreases contractility
35
M3- location
smooth muscle
36
M3- action
constriction
37
a1- location
vascular smooth muscle, gut smooth muscle
38
a1- action
vasoconstriction, relaxation of gut
39
B1- location
heart
40
B1- action
increase chronotropy and ionotropy
41
B2- location
smooth muscle, liver, SkM
42
B2- action
SM relaxation, glycogenolysis
43
What does tetrodotoxin block to cause fatal paralysis?
NmAchR
44
What does DUMBBELSS stand for to describe Ach actions?
diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation, lacrimation, salivation, and sweating
45
Which cholinomimetric drug ios selective for cardiovascular muscarinic R's to Dx asthma?
methacholine
46
What condition does carbachol treat?
glaucoma
47
Which cholinomimetric drug is used to increase urinary and GI motility, esp after surgery since it only targets muscarinic receptors?
Bethanechol
48
Cevimeline and Pilocarpine are cholinomimetric drugs that arre used to treat what condition?
Xerostomia in Sjorens syndrome
49
This nicotinic agonist is used to induce a neuromuscular blockage in surgery and intubation.
Succinylcholine
50
How do direct acting cholinomimetric agents increase Ach response?
by diorectly acting on the Ach R
51
So how do indirect acting cholinomimetric agents increase Ach response?
inhibit AchE, thus inc the [Ach]synapse
52
What are the actions of organophosphates to cause acute Ach toxicity?
strong AchE inhibitor
53
Which drug can u give for acute organophosphate poisonings?
Pralidoxime (PAM)
54
What are the Sx of atropine OD?
anti-DUMBBELS | cuz its a muscarinic antagonist
55
Which indirect acting cholinomimetric to counter the effects of an atropine OD?
pilocarpine
56
Mecamylamine and trimethaphan are used to treat HTN with acute aortic dissection by blocking what?
Nicotinic Ach R's in ganglions
57
Which drug is used to produce mydriasis and cycloplegia?
atropine
58
Which AchE inhibitor is used to treat parkinsons?
rivastigmine
59
Which muscarinic R antagonist is used to treat PUD?
methscopolamine
60
Which muscarinic R antagonist is used to treat asthma?
Tiotropium
61
Which G-subunit pathway does a1 receptors act on?
Gq
62
Why are a2 receptors located on presynaptic sympathetic neurons?
to fxn as autoreceptors to mediate feedback inhibition of sympathetic transmission
63
All 3 beta (B) receptors act on what G-protein subunit pathway?
Gs
64
Methoxamine is an a1 agonist that is used to Tx what condition?
shock
65
Phenylephrine, oxymetazoline, and tetrahydrozoline are a1 agonists that are used to Tx what conditions?
nasal congestion and opthalmic hyperemia
66
Clinidine and methyldopa are a2 agonists that are used to Tx what condition?
HTN by acting in CNS
67
Isoproterenol is a nonselective B agonist that is used to treat what?
HTN by lowering diastolic BP
68
Metaproterenol, terbutaline, and albuterol are B2 agonists that are used to treat what?
acute bronchospasm
69
Epinephrine is more selective towards which receptors, alpha or beta?
beta | thats why we have epi-pens with Epi, cuz it acts mainly on B2
70
Propanolol is an antagonist to which B-receptors?
nonselective to B-receptors, so B1 and B2
71
Atenolol is an antagonist to which B-receptors?
B1
72
Esmolol is an antagonist to which B-receptors?
B1
73
When is esmolol given?
in acute HTN states (given IV)
74
Nadolol is an antagonist to which B-receptors?
Non-selective