Autonomic Pharmacology Flashcards

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
Q

What does tricyclic antidepressants block to treat depression?

A

NET and serotonin reuptake

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26
Q

This nonselective MAOi causes more catecholamines to be present in the presynaptic vesicles.

A

Phenelzine

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27
Q

Stimulation of a1-receptors causes what to the BP?

A

rise cuz it increased peripheral vascular resistance

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28
Q

Stimulation of a2-receptors causes what to the BP?

A

lowers by acting on brainstem centers

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29
Q

Stimulation of B1-receptors causes what to the BP?

A

increase HR and force of cardiac muscle contraction –> increase BP

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30
Q

Stimulation of B2-receptors causes what to the BP?

A

causes relaxation of vascular, bronchial, and GI smooth muscle –> decrease BP

31
Q

M1- location

A

autonomic ganglia, viscera, CNS

32
Q

M1- actions

A

EPSPs

33
Q

M2- location

A

heart

34
Q

M2-action

A

slows, decreases contractility

35
Q

M3- location

A

smooth muscle

36
Q

M3- action

A

constriction

37
Q

a1- location

A

vascular smooth muscle, gut smooth muscle

38
Q

a1- action

A

vasoconstriction, relaxation of gut

39
Q

B1- location

A

heart

40
Q

B1- action

A

increase chronotropy and ionotropy

41
Q

B2- location

A

smooth muscle, liver, SkM

42
Q

B2- action

A

SM relaxation, glycogenolysis

43
Q

What does tetrodotoxin block to cause fatal paralysis?

A

NmAchR

44
Q

What does DUMBBELSS stand for to describe Ach actions?

A

diarrhea, urination, miosis, bradycardia, bronchoconstriction, excitation, lacrimation, salivation, and sweating

45
Q

Which cholinomimetric drug ios selective for cardiovascular muscarinic R’s to Dx asthma?

A

methacholine

46
Q

What condition does carbachol treat?

A

glaucoma

47
Q

Which cholinomimetric drug is used to increase urinary and GI motility, esp after surgery since it only targets muscarinic receptors?

A

Bethanechol

48
Q

Cevimeline and Pilocarpine are cholinomimetric drugs that arre used to treat what condition?

A

Xerostomia in Sjorens syndrome

49
Q

This nicotinic agonist is used to induce a neuromuscular blockage in surgery and intubation.

A

Succinylcholine

50
Q

How do direct acting cholinomimetric agents increase Ach response?

A

by diorectly acting on the Ach R

51
Q

So how do indirect acting cholinomimetric agents increase Ach response?

A

inhibit AchE, thus inc the [Ach]synapse

52
Q

What are the actions of organophosphates to cause acute Ach toxicity?

A

strong AchE inhibitor

53
Q

Which drug can u give for acute organophosphate poisonings?

A

Pralidoxime (PAM)

54
Q

What are the Sx of atropine OD?

A

anti-DUMBBELS

cuz its a muscarinic antagonist

55
Q

Which indirect acting cholinomimetric to counter the effects of an atropine OD?

A

pilocarpine

56
Q

Mecamylamine and trimethaphan are used to treat HTN with acute aortic dissection by blocking what?

A

Nicotinic Ach R’s in ganglions

57
Q

Which drug is used to produce mydriasis and cycloplegia?

A

atropine

58
Q

Which AchE inhibitor is used to treat parkinsons?

A

rivastigmine

59
Q

Which muscarinic R antagonist is used to treat PUD?

A

methscopolamine

60
Q

Which muscarinic R antagonist is used to treat asthma?

A

Tiotropium

61
Q

Which G-subunit pathway does a1 receptors act on?

A

Gq

62
Q

Why are a2 receptors located on presynaptic sympathetic neurons?

A

to fxn as autoreceptors to mediate feedback inhibition of sympathetic transmission

63
Q

All 3 beta (B) receptors act on what G-protein subunit pathway?

A

Gs

64
Q

Methoxamine is an a1 agonist that is used to Tx what condition?

A

shock

65
Q

Phenylephrine, oxymetazoline, and tetrahydrozoline are a1 agonists that are used to Tx what conditions?

A

nasal congestion and opthalmic hyperemia

66
Q

Clinidine and methyldopa are a2 agonists that are used to Tx what condition?

A

HTN by acting in CNS

67
Q

Isoproterenol is a nonselective B agonist that is used to treat what?

A

HTN by lowering diastolic BP

68
Q

Metaproterenol, terbutaline, and albuterol are B2 agonists that are used to treat what?

A

acute bronchospasm

69
Q

Epinephrine is more selective towards which receptors, alpha or beta?

A

beta

thats why we have epi-pens with Epi, cuz it acts mainly on B2

70
Q

Propanolol is an antagonist to which B-receptors?

A

nonselective to B-receptors, so B1 and B2

71
Q

Atenolol is an antagonist to which B-receptors?

A

B1

72
Q

Esmolol is an antagonist to which B-receptors?

A

B1

73
Q

When is esmolol given?

A

in acute HTN states (given IV)

74
Q

Nadolol is an antagonist to which B-receptors?

A

Non-selective