Ch. 9 Cholinergic Flashcards

(78 cards)

1
Q

Hemicholinium-3

A

Blocks high-affinity transporter for choline and thereby prevents uptake of choline required for ACh synthesis
RESEARCH ONLY

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2
Q

Vesamicol

A

Blocks the ACh-H+ antiporter used to transport ACh into vesicles
RESEARCH ONLY

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3
Q

Botulinum toxin

A

Degrades synaptobrevin = prevents vesicle fusion on presynaptic membrane

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4
Q

Edrophonium

A

Inhibitor of ACh Degredation: Inhibits acetylcholinesterase (AChE) by binding to enzyme’s active site

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5
Q

Neostigmine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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6
Q

Pyridostigmine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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7
Q

Ambenonium

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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8
Q

Physostigmine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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9
Q

Diisopropyl fluorophosphate

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site
organophosphate used as insecticide, nerve gas, former topical miotic medication

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10
Q

Tacrine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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11
Q

Donepezil

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site

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12
Q

Rivastigmine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site
Also affects butyrylcholinesterase by forming a carbamoylate complex with the enzymes

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13
Q

Galantamine

A

Inhibitor of ACh Degredation: Inhibits AChE by binding to enzyme’s active site
Also acts as a nonpotentiating ligand of nicotinic receptors

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14
Q

Methacholine

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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15
Q

Carbachol

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity
Cannot be used systemically

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16
Q

Bethanechol

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity
Almost completely selective for muscarinic receptors

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17
Q

Cevimeline

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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18
Q

Pilocarpine

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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19
Q

Succinylcholine

A

Nicotinic Receptor Agonist: Stimulate opening of nicotinic ACh receptor channel and produce depolarization of the cell membrane.
Persists at the neuroeffector junction and activates the nicotinic receptor channels continuously –> inactivation of voltage-gated Na+ channels = cannot open to support further APs
Short duration = DOC for paralysis during intubation.

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20
Q

Another name for action of succinylcholine

A

“Depolarizing blockade”

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21
Q

Atropine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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22
Q

Scopolamine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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23
Q

Pirenzepine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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24
Q

Methscopolamine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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25
Glycopyrrolate
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor
26
Ipratropium
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor
27
Tiotropium
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor
28
Oxybutynin
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific
29
Propantheline
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific
30
Terodiline
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific
31
Fesoterodine
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific
32
Trospium
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific
33
Darifenacin
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective
34
Solifenacin
Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective
35
Pancuronium
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") LONG ACTING
36
Tubocurarine
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") LONG ACTING
37
Vecuronium
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") INTERMEDIATE ACTING
38
Rocuronium
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") INTERMEDIATE ACTING
39
Mivacurium
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") SHORT ACTING
40
Trimethaphan
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") Administered when ganglionic blockade is desired - HTN acute aortic dissection
41
Mecamylamine
Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization ("Nondepolarizing blockade") Administered when ganglionic blockade is desired - HTN acute aortic dissection
42
Types of cholinergic receptors
Muscarinic and Nicotinic
43
Muscarinic receptors are
G protein coupled receptors
44
Nicotinic Receptors are
ligand-gated ion channels
45
M1, M3, and M5 mAChR
Gq/11 --> PLC --> increased IP3 and DAG --> increased Ca2+ and increased PKC = excitatory
46
M2 and M4 mAChR
Beta/gamma of G protein --> inhibition of adenylyl cyclase and increased K+ channel opening = suppress cellular excitability
47
Location of M1
Autonomic ganglia = late excitatory postsynaptic potential | CNS = arousal, attention, analgesia
48
Location of M2
Heart: - SA node = slowed spontaneous depolarization; hyperpolarization - AV node = decrease conduction velocity - Atrium = decrease refractory period, decrease contractile force - Ventricle = slight decrease in contractility
49
Location of M3
Smooth muscle = contraction
50
Location of M4
CNS
51
Location of M5
CNS
52
Nicotinic receptors
Ligand-gated ion channels --> net inward Na+ depolarizing the cell -Direct ligand-gated conductance - requires binding of 2 ACh to 1 nAChR --> conformational change of 2 alpha subunits 2 alpha, 1 beta, 1 delta, 1 epsilon (mature skel m) OR 1 gamma (embryonic
53
Nicotinic Nm receptor Location
NMJ - skeletal muscle | - opening of Na+/K+ channels --> skeletal muscle contraction
54
Nicotinic Nn receptor location
Autonomic ganglia - opening of Na+/K+ channels --> depolarization and firing of postganglionic neuron Adrenal medulla - opening of Na+/K+ channels --> secretion of catecholamines CNS - opening of Na+/K+ channels --> arousal, attention analgesia
55
2 cholinesterases
1. AChE - postsyn membrane | 2. Butyrylcholinesterase (BuChE) secondary role, may be involved in path of Alzheimer's
56
Latency of mAChR
100 - 250 msec
57
Latency of nAChR
5 msec
58
Principle neurotransmitter at the NMJ that is released by alpha motor neurons --> binding of nicotinic receptors and motor end-plate depolarization
ACh | - extent of depolarization depends on QUANTITIY of ACh
59
Effect of Gaglionic Blockade on ARTERIOLES
(mainly adrenergic sympathetic tone) --> Vasodilation, increased peripheral blood flow, hypotension
60
Effect of Gaglionic Blockade on VEINS
(mainly adrenergic sympathetic tone) --> vasodilation, pooling of blood, decreased of venous return, decreased cardiac output
61
Effect of Gaglionic Blockade on HEART
(mainly parasymp cholinergic tone) --> tachycardia
62
Effect of Gaglionic Blockade on IRIS
mainly parasymp cholinergic tone --> Mydriasis (pupil dilation)
63
Effect of Gaglionic Blockade on CILIARY MUSCLE
mainly parasymp cholinergic tone --> cycloplegia (focused to far vision)
64
Effect of Gaglionic Blockade on GI TRACT
Mainly parasymp cholinergic tone --> decreased tone and motility; constipation; decreased secretions
65
Effect of Gaglionic Blockade on URINARY BLADDER
Mainly parasymp cholinergic ton --> urinary retention
66
Effect of Gaglionic Blockade on SALIVARY GLANDS
Mainly parasymp cholinergic tone --> xerostomia (dry mouth)
67
Effect of Gaglionic Blockade on SWEAT GLANDS
Mainly symp cholinergic tone --> Anhidrosis (absence of sweating)
68
Effects of ACh on VASCULATURE (endothelial cells)
Release of NO and vasodilation
69
Effects of ACh on EYE IRIS (pupillae sphincter muscle)
Contraction and miosis (constriction of pupil)
70
Effects of ACh on CILIARY MUSCLE
Contraction and accommodation for near vision
71
Effects of ACh on SALIVARY AND LACRIMAL GLANDS
Thin and watery secretions
72
Effects of ACh on BRONCHI
Constriction | Increased secretions
73
Effects of ACh on HEART
Bradycardia Decreased conduction velocity AV block at high doses Slight decrease in contractility
74
Effects of ACh on GI TRACT
Increased Tone Increased secretions Relaxation of sphincters
75
Effects of ACh on URINARY BLADDER
Contraction of detrusor muscle | Relaxation of sphincter
76
Effects of ACh on SWEAT GLANDS
Diaphoresis (sweating)
77
Effects of ACh on REPRODUCTIVE TRACT, MALE
Erection
78
Effects of ACh on UTERUS
Variable