Ch. 9 Cholinergic Flashcards by Anna Miller | Brainscape

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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Q

Vesamicol

A

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

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Q

Botulinum toxin

A

Degrades synaptobrevin = prevents vesicle fusion on presynaptic membrane

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Q

Edrophonium

A

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

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Q

Neostigmine

A

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

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Q

Pyridostigmine

A

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

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Q

Ambenonium

A

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

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Q

Physostigmine

A

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

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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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Q

Tacrine

A

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

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Q

Donepezil

A

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

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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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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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Q

Methacholine

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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Q

Carbachol

A

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

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Q

Bethanechol

A

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

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Q

Cevimeline

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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Q

Pilocarpine

A

Muscarinic Receptor Agonist: Stimulates muscarinic receptor activity

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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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Q

Another name for action of succinylcholine

A

“Depolarizing blockade”

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Q

Atropine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Scopolamine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Pirenzepine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Methscopolamine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Glycopyrrolate

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Ipratropium

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Tiotropium

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor

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Q

Oxybutynin

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

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Q

Propantheline

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

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Q

Terodiline

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

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Q

Fesoterodine

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

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Q

Trospium

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - nonspecific

Q

Darifenacin

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective

Q

Solifenacin

A

Muscarinic Receptor Antagonist: Selectively antagonizes muscarinic receptor - M3 selective

Q

Pancuronium

A

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization (“Nondepolarizing blockade”)
LONG ACTING

Q

Tubocurarine

A

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization (“Nondepolarizing blockade”)
LONG ACTING

Q

Vecuronium

A

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization (“Nondepolarizing blockade”)
INTERMEDIATE ACTING

Q

Rocuronium

A

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization (“Nondepolarizing blockade”)
INTERMEDIATE ACTING

Q

Mivacurium

A

Nicotinic Receptor Antagonist: Selectively antagonizes nicotinic receptor preventing endogenous ACh binding and subsequent muscle cell depolarization (“Nondepolarizing blockade”)
SHORT ACTING

Q

Trimethaphan

A

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

Q

Mecamylamine

A

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

Q

Types of cholinergic receptors

A

Muscarinic and Nicotinic

Q

Muscarinic receptors are

A

G protein coupled receptors

Q

Nicotinic Receptors are

A

ligand-gated ion channels

Q

M1, M3, and M5 mAChR

A

Gq/11 –> PLC –> increased IP3 and DAG –> increased Ca2+ and increased PKC = excitatory

Q

M2 and M4 mAChR

A

Beta/gamma of G protein –> inhibition of adenylyl cyclase and increased K+ channel opening = suppress cellular excitability

Q

Location of M1

A

Autonomic ganglia = late excitatory postsynaptic potential

CNS = arousal, attention, analgesia

Q

Location of M2

A

Heart:

SA node = slowed spontaneous depolarization; hyperpolarization
AV node = decrease conduction velocity
Atrium = decrease refractory period, decrease contractile force
Ventricle = slight decrease in contractility

Q

Location of M3

A

Smooth muscle = contraction

Q

Location of M4

A

CNS

Q

Location of M5

A

CNS

Q

Nicotinic receptors

A

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

Q

Nicotinic Nm receptor Location

A

NMJ - skeletal muscle

- opening of Na+/K+ channels –> skeletal muscle contraction

Q

Nicotinic Nn receptor location

A

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

Q

2 cholinesterases

A

AChE - postsyn membrane

2. Butyrylcholinesterase (BuChE) secondary role, may be involved in path of Alzheimer’s

Q

Latency of mAChR

A

100 - 250 msec

Q

Latency of nAChR

A

5 msec

Q

Principle neurotransmitter at the NMJ that is released by alpha motor neurons –> binding of nicotinic receptors and motor end-plate depolarization

A

ACh

- extent of depolarization depends on QUANTITIY of ACh

Q

Effect of Gaglionic Blockade on ARTERIOLES

A

(mainly adrenergic sympathetic tone) –> Vasodilation, increased peripheral blood flow, hypotension

Q

Effect of Gaglionic Blockade on VEINS

A

(mainly adrenergic sympathetic tone) –> vasodilation, pooling of blood, decreased of venous return, decreased cardiac output

Q

Effect of Gaglionic Blockade on HEART

A

(mainly parasymp cholinergic tone) –> tachycardia

Q

Effect of Gaglionic Blockade on IRIS

A

mainly parasymp cholinergic tone –> Mydriasis (pupil dilation)

Q

Effect of Gaglionic Blockade on CILIARY MUSCLE

A

mainly parasymp cholinergic tone –> cycloplegia (focused to far vision)

Q

Effect of Gaglionic Blockade on GI TRACT

A

Mainly parasymp cholinergic tone –> decreased tone and motility; constipation; decreased secretions

Q

Effect of Gaglionic Blockade on URINARY BLADDER

A

Mainly parasymp cholinergic ton –> urinary retention

Q

Effect of Gaglionic Blockade on SALIVARY GLANDS

A

Mainly parasymp cholinergic tone –> xerostomia (dry mouth)

Q

Effect of Gaglionic Blockade on SWEAT GLANDS

A

Mainly symp cholinergic tone –> Anhidrosis (absence of sweating)

Q

Effects of ACh on VASCULATURE (endothelial cells)

A

Release of NO and vasodilation

Q

Effects of ACh on EYE IRIS (pupillae sphincter muscle)

A

Contraction and miosis (constriction of pupil)

Q

Effects of ACh on CILIARY MUSCLE

A

Contraction and accommodation for near vision

Q

Effects of ACh on SALIVARY AND LACRIMAL GLANDS

A

Thin and watery secretions

Q

Effects of ACh on BRONCHI

A

Constriction

Increased secretions

Q

Effects of ACh on HEART

A

Bradycardia
Decreased conduction velocity
AV block at high doses
Slight decrease in contractility

Q

Effects of ACh on GI TRACT

A

Increased Tone
Increased secretions
Relaxation of sphincters

Q

Effects of ACh on URINARY BLADDER

A

Contraction of detrusor muscle

Relaxation of sphincter

Q

Effects of ACh on SWEAT GLANDS

A

Diaphoresis (sweating)

Q

Effects of ACh on REPRODUCTIVE TRACT, MALE

A

Erection

Q

Effects of ACh on UTERUS

A

Variable