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PBL Spring 2015 - Block 2 > PHARM Chapter 9 - Cholinergic Pharmacology > Flashcards

PHARM Chapter 9 - Cholinergic Pharmacology Flashcards

1
Q

ME of hemicholinium-3 and vesamicol

A

Inhibit the synthesis, storage, or release of ACh

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2
Q

Uses of Hemicholinium 3 and vesamicol

A

Utilized only in research settings

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3
Q

ME of Botulinum toxin

A

Inhibits the synthesis, storage, and release of ACh, degrades SNAP25 which prevents vesicle fusion presynaptically

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4
Q

Uses of Botulinium Toxin

A

Focal dystonias, torticollis, achalasia, stabismus, etc.

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5
Q

What produces botulinum toxin

A

clostridium botulinum

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6
Q

Inhibitors of ACh Degradation

A 
Edrophonium
Neostigmine
Pyridostigmine
Ambenonium
Physostigmine
Diisopropyl fluoro-phosphate
Tacrine
Donepezil
Rivastigmine
Galantamine
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7
Q

ME of inhibitors of ACh Degradation

A

Inhibit AChE by binding to enzyme’s active site, causes increase in ACh in cleft which activates nearby receptors

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8
Q

Uses for Edrophonium, Neostigmine, Pyridostigmine, Ambenonium, Physostigmine

A

Diseases of muscle weakness (edrophoium)

Urinary or GI motility agent, NMJ diseases, glaucoma (neostigmine, pyridostigmine, ambenoium)

Reversal of anticholinergic toxicity or induced paralysis in surgery (physostigmine)

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9
Q

Short acting with rapid onset of action inhibitor of ACh degradation

A

Edrophonium

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10
Q

Topical application of cholinesterase inhibitors to the cornea has what effect?

A

decreases intraocular pressure by facilitating outflow of aqueous humor

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11
Q

Why is physostigmine used for treating CNS antichlinergic toxicity

A

nonpolar structure

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12
Q

2 carbamic acid ester AChE inhibitors

A

neostigmine and physostigmine

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13
Q

1 organophosphate AChE inhibitor

A

diisopropyl flurophosphate

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14
Q

Aging

A

oxygen-phosphorus bonds within the inhibitor are broken spontaneously in favor of stronger bonds between the enzyme and the inhibitor - essentially irreversible

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15
Q

Eaton-lambert syndrome

A

autoantibodies against calcium channels

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16
Q

how does tubocurare cause weakness or paralysis

A

acts as competitive antagonist for nAChR preventing ACh from binding to the receptor and causing nondepolarizaing blcokade of cholinergic transmission

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17
Q

Effect of AChE inhibitors on the GI system

A

increase smooth muscle motility because it enhances ganglionic transmission at auerbach’s plexus

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18
Q

SE of diisopropyl fluoro-phosphate

A

respiratory paralysis

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19
Q

organophosphate compound used as insecticide

A

diisopropyl fluoro-phosphate

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20
Q

Uses of tacrine, donepezil, rivastigmine, galantamine

A

mild to moderate Alzheimer’s disease dementia

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21
Q

Affects both AChE and butyrylcholinestarase by forming a carbamoylate complex with the enzymes

A

rivastigmine

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22
Q

ME of methacoholine

A

stimulate muscarinic receptor activity - selective for cardiovascular muscarinic cholinergic receptors

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23
Q

Uses of methacholine

A

diagnosis of asthma

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24
Q

ME of carbachol, bethanechol, cevimeline, pilocarpine

A

Stimulate muscarinic receptor activity

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25
Q

Uses for carbachol

A

glaucoma - cannot be used systemically because it is unpredicatble

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26
Q

Uses for bethanechol

A

Urinary tract motility agent - due to selective agent for muscarinic receptors

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27
Q

Uses for cevimeline and pilocarpine

A

xerostomia in sjogren’s syndrome

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28
Q

FDA approved to treat parkinson’s disease with dementia

A

rivastigmine

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29
Q

how can the GI effects of AChE inhibitors be minimized

A

administer w/ meal or in combination w/ memantine an NMDA channel blocker

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30
Q

This drug is a vasodilator and is cardiac vagomimetric

A

(mimics cardiac response to vagus nerve = parasympathetic stimulation = methacholine

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31
Q

Has enhanced nicotinic action relative to other choline esters

A

carbachol

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32
Q

Most clinically used alkaloid is ___ which is a miotic agent and sialogogue (saliva inducing) used to treat xerostomia

A

pilocarpine

33
Q

ME of succinylcholine

A

nicotinic receptor antagonist - stimulates opening of nAChR channel and produces depolarization of cell membrane - persists at neuroeffector junction and activates nicotinic receptor channels continuous resulting in inactivation of voltage-gated sodium channels (depolarizing blockade)

34
Q

uses of succinylcholine

A

induction of neuromuscular blockade in surgery, intubation

35
Q

ME of Atropine

A

selectively antagonize muscarinic receptors, marginal nicotinic affect

36
Q

Uses of atropine

A

AChE overdose, acute bradycardia, premedication for anesthetic procedure, excessive salivation during surgery, antidote to mushroom poisoning

37
Q

ME of scopolamine

A

selectively antagonizes muscarinic receptors - significant CNS effects

38
Q

Uses of scopolamine

A

motion sickness, nausea/vomiting

39
Q

ME of pirenzepine, methscopolamine, glycopyrrolate

A

selectively antagnoize muscarinic recpetors

40
Q

Uses of pirenzepine, methscopolamine, glycopyrrolate

A

PUD, surgically induced/vagally induced bradycardia (glycopyrrolate)

41
Q

ME of ipratropium and tiotropium

A

selectively antagonize muscarinic receptors

42
Q

Uses of ipratropium and tiotropium

A

COPD and asthma (tiotropium more superior)

43
Q

Uses of oxybutyin, propantheline, terodiline, tolterodine, fesoterodine, rospium, darifenacin, solifenacin

A

hyperrefelxic and overactive bladder, urge incontinence

44
Q

ME of oxybutyin, propantheline, terodiline, tolterodine, fesoterodine, rospium, darifenacin, solifenacin

A

selectively antagonize muscarinic receptors

45
Q

M3 receptor antagonists

A

darifenacin and solifenacin

46
Q

used clinically to dilate eyes (mydriasis)

A

atropine

47
Q

benztropine and trihexyphenidyl ME

A

muscarinic receptor antagonist

48
Q

uses of benztropine and trihexyphenidyl

A

commonly used to treat extrapyramidal symptoms and akathisia associated w/ neuroleptics

49
Q

acute cholinesterase inhibitor toxcicity

A

due to exposure of organophosphate pesticides - vomiting, diarrhea, profuse sweating, hypersalivation, miosis, bronchoconstriction followed by nicotinic toxciity

50
Q

Why are anticholinergic drugs contraindicated in elderly

A

many commonn drugs possess small measure of anticholinergic activity

elderly sensitive to choinergic blockade

polypharmacy is common practice in geriatrics, may induce acute encephalopathy, falls, urinary retension, constipation, cognitive deficits

51
Q

ME of pancuronium, tubocuraranie, vecuronium, rocuronium, mivacurium

A

selectively antagonize nicotinic recpetors preventing endogenous ACh binding and subsequent muscle cell depolarization

52
Q

Uses of pancuronium, tubocurarine, vecuronium, rocuronium, mivacurium

A

induction of neuromuscular blockade in surgery, intubation

53
Q

Long acting nicotinic receptor antagonists

A

pancuronium and tubocurarine

54
Q

Medium acting nicotinic receptor antagonists

A

vecuronium and rocuronium

55
Q

Short acting nicotinic receptor antagonists

A

mivacurium

56
Q

what can reverse the nondepolarizing blocking agent adverse effects

A

AChE inhibitors

57
Q

ME of trimethaphan and mecamylamine

A

selectively antagonize nicotinic receptors, preventing endogenous AChE binding and subsequent muscle cell depolarization

58
Q

Uses of trimethaphan and mecamylamine

A

hypertension in patients with acute aortic dissection

59
Q

When would mecamylamine and trimethaphan be administered

A

ganglionic blcokade is desired - lowers bp while blunting sympathetic reflexes

60
Q

Arterioles
Predominant tone:
Effect of ganglionic blockade

A

sympathetic

vasodilation, hypotension

61
Q

Veins
Predominant tone:
Effect of ganglionic blockade

A

symapthetic

vasodilation, pooling of blood, decreased venous return and cardiac output

62
Q

Heart
Predominant tone:
Effect of ganglionic blockade

A

Parasympathetic

Tachycardia

63
Q

Iris
Predominant tone:
Effect of ganglionic blockade

A

Parasympathetic

Mydriasis (pupil dilation)

64
Q

Ciliary muscle
Predominant tone:
Effect of ganglionic blockade

A

Parasympathetic

cycloplegia = focused to far vision

65
Q

GI
Predominant tone:
Effect of ganglionic blockade

A

Parasympathetic

Decreased tone and motility, constipation

66
Q

Urinary bladder
Predominant tone:
Effect of ganglionic blockade

A

parasymaptheitc

urinary retention

67
Q

Salivary glands
Predominant tone:
Effect of ganglionic blockade

A

parasympathetic

dry mouth

68
Q

Sweat glands
Predominant tone:
Effect of ganglionic blockade

A

Symapthetic

anhidrosis

69
Q

Effect of ACh on vasculature

A

release NO = vasodilation

70
Q

Effect of ACh on Eye iris

A

contraction and miosis

71
Q

Effect of ACh on Ciliary muscle

A

contraction and accommodation of lens to near vision

72
Q

Effect of ACh on Salivary and lacrimal galnds

A

thin and watery secretions

73
Q

Effect of ACh on bronchi

A

constriction, increased secretion

74
Q

Effect of ACh on heart

A

bradycardia, decreased conduction velocity, AV block at high doses

75
Q

Effect of ACh on GI

A

increased tone, relaxation of sphincters

76
Q

Effect of ACh on urinary bladder

A

contraction of detrusor, relaxation of sphincter

77
Q

Effect of ACh on sweat glands

A

diaphoresis

78
Q

Effect of ACh on penis

A

erect

PBL Spring 2015 - Block 2 (11 decks)

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