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ANS Cholinergic Flashcards

1
Q

prototype that acts directly at both muscarinic and nicotinic receptors

A

Ach

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2
Q

prototype for the indirect acting cholinesterase inhibitors

A

neostigmine

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3
Q

Muscarinic mechanism of action

A

g protein and releases second messengers DAG and IP3. IP3 causes release of calcium from storage sites and causes smooth muscle contraction

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4
Q

Nicotinic mechanism of action

A

Ach receptor is located on channel protein that is selective for sodium and potassium. Receptor activation causes depolarization with influx of Na+ causes EPSP

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5
Q

drug that blocks synthesis of Ach

A

hemicholinium

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6
Q

drug that blocks storage of Ach

A

vesamicol

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7
Q

drug that blocks release of Ach

A

botulinum toxin

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8
Q

drug that block NE synthesis

A

metyrosine

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9
Q

drug that blocks catecholamine storage

A

reserpine

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10
Q

drug that blocks catecholamine release

A

guanethidine

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11
Q

drug that facilitates release of catecholamine

A

amphetamine

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12
Q

drug that impairs reuptake of catecholamines

A

cocaine

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13
Q

causes relaxation of skeletal muscle and systemic blood vessels

A

beta 2

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14
Q

causes contraction of skeletal muscle and systemic blood vessels

A

alpha 1

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15
Q

causes increase in heart rate

A

beta 1

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16
Q

causes relaxation of lungs and tracheal and bronchial smooth muscle

A

beta 2

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17
Q

short duration of action, quaternary structure , susceptible to pseudocholinesterase

A

direct acting cholinergic agonists

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18
Q

pilocarpine, bethanachol, methacholine

A

direct acting muscarinic agonists

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19
Q

Methacholine has the greatest muscarinic action on which system?

A

cardiac

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20
Q

2 drugs with very high selectivity to nicotinic receptors

A

Ach and pilocarpine

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21
Q

How do you reverse the effect of methacholine?

A

beta agonist

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22
Q

first cause depolarization at nicotinic receptor but then become antagonist

A

nicotinic receptor agonists

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23
Q

nicotine, succinylcholine varenicline

A

nicotinic receptor agonists

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24
Q

Effect of large dose of nicotine on NMJ

A

depolarization and depression of transmission, receptor desensitization

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25
Q

partial agonist of nicotinic receptors and receptor is mesolimbic nicotinic

A

varenicline

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26
Q

what is varenicline selective for?

A

alpha4 beta 2 neuronal nicotinic receptor

27
Q

adverse effects of varenicline (4)

A
  1. nausea
  2. sleep disturbances
  3. GI
  4. nicotine withdrawal
28
Q

block acetylcholinesterase from degrading Ach

A

indirect acting cholinergic agonists

29
Q

edrophonium, neostigmine, physostigmine, and malathion examples of ?

A

reversible acetylcholinesterase inhibitors (indirect acting agonists)

30
Q

example of irreversible indirect acting agonists

A

organophosphates

31
Q

Cholinesterase regenerator; reverse organophosphates

A

pralidoxime (2 PAM)

diacetylmonoxime (DAM)

32
Q

tertiary NH and antidote for antimuscarinic CNS toxicity, tx of glaucoma, tx of MG

A

physostigmine

33
Q

antibodies to alpha 1 subunit of nicotinic receptor channel complex

A

myasthenia gravis

34
Q

Which cholinesterase inhibitor has the shortest duration of action?

A

edrophonium

35
Q

prototype of antimuscarinic drugs

36
Q

use for mydriasis and cycloplegia

A

antimuscarinic drugs

37
Q

muscarinic antagonists

A

glycopyrrolate
atropine
tolterodine
ipratropium

38
Q

Which antimuscarinic has a quarternary structure and will limit distribution in the CNS?

39
Q

primary uses of muscarinic antagonists (5)

A
  1. bronchodilation
  2. treat bradyarrhythmia
  3. urinary incontinence
  4. decreased GI motility
  5. dry secretions
40
Q

large doses of this drug make it an antagonist

41
Q

Small dose of nicotine increase ___ and ___.

42
Q

Hypotension caused by larger doses of ___.

43
Q

nicotinic antagonist ganglionic blocker

A

trimethaphan

44
Q

nicotinic antagonist neuromuscular blockers

A

atracurium
pancuronium
rocuronium

45
Q

Which nicotinic antagonist neuromuscular blocker has the longest duration of action?

A

pancuronium

46
Q

membrane depolarizes resulting in an initial which produces fasciculations then flaccid paralysis

A

phase I block of depolarizing NMB

47
Q

membrane repolarizes but receptor is desensitized to effect of acetylcholine

A

phase II block of depolarizing NMB

48
Q

compete with Ach to bind with nicotinic receptor of motor end plate; blockade inhibit Ach from binding

A

Non depolarizing, competitive NMB

49
Q

Histamine release is a direct effect of ___

A

NMB nicotinic antagonists

50
Q

Phase II can be antagonized by

A

antiChE agent

51
Q

3 effects of depolarizing agents

A
  1. ) muscle fasciculation
  2. ) hyperkalemia
  3. ) masseter muscle rigidity
52
Q

can be reversed by acetylcholinesterase inhibitor agents

A

non depolarizing agents

53
Q

indirect acting cholinergic receptor antagonist

A

botulinum toxin

54
Q

adverse effects of nicotinic and muscarinic

A
  1. anaphylaxis
  2. associated with site of injection and dose
    (local effects, dry mouth, dysphagia, ptosis, vision effects)
55
Q

most likely cause of death from cholinesterase inhibitor toxicity

A

respiratory failure

56
Q

neostigmine and pyridostigmine causes ___

A

diarrhea; cholinesterase inhibitors increase bowl movement

57
Q

parasympathetic innervation and bethanechol will cause ___

A

increase bronchial smooth muscle tone

58
Q

what do muscarinic cholinergic agonists treat

A

miosis (tx of narrow angle glaucoma)

59
Q

drug with little to none vascular effect and CNS effect and duration of action of 2-4 hours

A

neostigmine

60
Q

both ganglion blockers and muscarinic blockers cause ____

61
Q

therapeutic indication for antimuscarinic drugs?

62
Q

which drug causes vasodilation and can be blocked by atropine

A

bethanechol

63
Q

beta 2 stimulants cause ___

Pharmacology (11 decks)

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