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

PHARM Chapter 9 - Cholinergic Pharmacology Flashcards

(78 cards)

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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
Uses for carbachol
glaucoma - cannot be used systemically because it is unpredicatble
26
Uses for bethanechol
Urinary tract motility agent - due to selective agent for muscarinic receptors
27
Uses for cevimeline and pilocarpine
xerostomia in sjogren's syndrome
28
FDA approved to treat parkinson's disease with dementia
rivastigmine
29
how can the GI effects of AChE inhibitors be minimized
administer w/ meal or in combination w/ memantine an NMDA channel blocker
30
This drug is a vasodilator and is cardiac vagomimetric
(mimics cardiac response to vagus nerve = parasympathetic stimulation = methacholine
31
Has enhanced nicotinic action relative to other choline esters
carbachol
32
Most clinically used alkaloid is ___ which is a miotic agent and sialogogue (saliva inducing) used to treat xerostomia
pilocarpine
33
ME of succinylcholine
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
uses of succinylcholine
induction of neuromuscular blockade in surgery, intubation
35
ME of Atropine
selectively antagonize muscarinic receptors, marginal nicotinic affect
36
Uses of atropine
AChE overdose, acute bradycardia, premedication for anesthetic procedure, excessive salivation during surgery, antidote to mushroom poisoning
37
ME of scopolamine
selectively antagonizes muscarinic receptors - significant CNS effects
38
Uses of scopolamine
motion sickness, nausea/vomiting
39
ME of pirenzepine, methscopolamine, glycopyrrolate
selectively antagnoize muscarinic recpetors
40
Uses of pirenzepine, methscopolamine, glycopyrrolate
PUD, surgically induced/vagally induced bradycardia (glycopyrrolate)
41
ME of ipratropium and tiotropium
selectively antagonize muscarinic receptors
42
Uses of ipratropium and tiotropium
COPD and asthma (tiotropium more superior)
43
Uses of oxybutyin, propantheline, terodiline, tolterodine, fesoterodine, rospium, darifenacin, solifenacin
hyperrefelxic and overactive bladder, urge incontinence
44
ME of oxybutyin, propantheline, terodiline, tolterodine, fesoterodine, rospium, darifenacin, solifenacin
selectively antagonize muscarinic receptors
45
M3 receptor antagonists
darifenacin and solifenacin
46
used clinically to dilate eyes (mydriasis)
atropine
47
benztropine and trihexyphenidyl ME
muscarinic receptor antagonist
48
uses of benztropine and trihexyphenidyl
commonly used to treat extrapyramidal symptoms and akathisia associated w/ neuroleptics
49
acute cholinesterase inhibitor toxcicity
due to exposure of organophosphate pesticides - vomiting, diarrhea, profuse sweating, hypersalivation, miosis, bronchoconstriction followed by nicotinic toxciity
50
Why are anticholinergic drugs contraindicated in elderly
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
ME of pancuronium, tubocuraranie, vecuronium, rocuronium, mivacurium
selectively antagonize nicotinic recpetors preventing endogenous ACh binding and subsequent muscle cell depolarization
52
Uses of pancuronium, tubocurarine, vecuronium, rocuronium, mivacurium
induction of neuromuscular blockade in surgery, intubation
53
Long acting nicotinic receptor antagonists
pancuronium and tubocurarine
54
Medium acting nicotinic receptor antagonists
vecuronium and rocuronium
55
Short acting nicotinic receptor antagonists
mivacurium
56
what can reverse the nondepolarizing blocking agent adverse effects
AChE inhibitors
57
ME of trimethaphan and mecamylamine
selectively antagonize nicotinic receptors, preventing endogenous AChE binding and subsequent muscle cell depolarization
58
Uses of trimethaphan and mecamylamine
hypertension in patients with acute aortic dissection
59
When would mecamylamine and trimethaphan be administered
ganglionic blcokade is desired - lowers bp while blunting sympathetic reflexes
60
Arterioles Predominant tone: Effect of ganglionic blockade
sympathetic | vasodilation, hypotension
61
Veins Predominant tone: Effect of ganglionic blockade
symapthetic | vasodilation, pooling of blood, decreased venous return and cardiac output
62
Heart Predominant tone: Effect of ganglionic blockade
Parasympathetic | Tachycardia
63
Iris Predominant tone: Effect of ganglionic blockade
Parasympathetic | Mydriasis (pupil dilation)
64
Ciliary muscle Predominant tone: Effect of ganglionic blockade
Parasympathetic | cycloplegia = focused to far vision
65
GI Predominant tone: Effect of ganglionic blockade
Parasympathetic | Decreased tone and motility, constipation
66
Urinary bladder Predominant tone: Effect of ganglionic blockade
parasymaptheitc | urinary retention
67
Salivary glands Predominant tone: Effect of ganglionic blockade
parasympathetic | dry mouth
68
Sweat glands Predominant tone: Effect of ganglionic blockade
Symapthetic | anhidrosis
69
Effect of ACh on vasculature
release NO = vasodilation
70
Effect of ACh on Eye iris
contraction and miosis
71
Effect of ACh on Ciliary muscle
contraction and accommodation of lens to near vision
72
Effect of ACh on Salivary and lacrimal galnds
thin and watery secretions
73
Effect of ACh on bronchi
constriction, increased secretion
74
Effect of ACh on heart
bradycardia, decreased conduction velocity, AV block at high doses
75
Effect of ACh on GI
increased tone, relaxation of sphincters
76
Effect of ACh on urinary bladder
contraction of detrusor, relaxation of sphincter
77
Effect of ACh on sweat glands
diaphoresis
78
Effect of ACh on penis
erect

PBL Spring 2015 - Block 2 (11 decks)

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