Cholinergic Effects Flashcards

1
Q

What are 2 examples of receptor super classes?

A

Nicotinic + muscarinic

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2
Q

What do muscarinic receptors do?

A

Mediate response of PNS

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3
Q

What are selective agonists of nicotinic receptors?

A

Nicotine and labeline

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4
Q

What are selective antagonist of nicotinic receptors?

A

Tubocurarine, hexamethonium + pancuronium

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5
Q

What are selective agonist of muscarinic receptors?

A

Muscarine, bethanecol, pilocarpine

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6
Q

What are selective antagonist of muscarinic receptors?

A

Pirenzepine , ipratropium

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7
Q

What are main parasympathetic effects?

A

Reduce heart rate
Vasodilation
Increased saliva + gastric acid production
Increased tear formation
Visceral smooth muscle contraction e.g. gut, bladder
Pupil constriction

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8
Q

What does expression of M1,M3,M5 lead to?

A

Lead to stimulation of phospholipase C

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9
Q

What does expression of M2 and M4 muscarinic receptors lead?

A

Are negatively coupled to adenylate cyclase

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10
Q

Cardiac effects

A

In heart, parasympathetic nerve releases Ach + interacts with M2 receptor
M2 receptor is negatively coupled with adenylate cyclase
Less cAMP
less stimulation of funny channel
Less PKA so less stimulation of Ca channel + calcium release

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11
Q

Describe vascular effects- arterial relaxation

A

Ach will lead to vasodilation
There is no parasympathetic nerves going to arteries
M3 receptors are on endothelial cells
Endothelial cells make gas called nitric oxide which is made by NO synthase from arginine
NO diffuses short distance + leads to relaxation of smooth muscle cell

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12
Q

Describe the contraction of non vascular smooth muscle

A

Activation of M3 receptors leads to increased activation of phospholipase + calcium release
M3 receptors are on endothelial cells
In particular: GI tract, bladder + airways => M3 receptors are on muscle

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13
Q

Where is M1 receptors found?

A

CNS
peripheral neurone
Gastric parietal cells

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14
Q

Where is M2 receptors found?

A

Heart-> atria, SAN , AVN

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15
Q

Where is M3 receptors found?

A

Visceral smooth muscle
Secretory glands
Endothelial cells

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16
Q

Where is M4 receptors found?

A

CNS

17
Q

Where is M5 receptors found?

A

CNS

18
Q

What does atropine do?

A

Blocks muscarinic receptors

19
Q

What is parasympathomimetic?

A

Drugs that mimic PNS

20
Q

What are some clinical uses of parasympathomietics?

A

Directly acting;
Pilocarpine(mAchR agonist)-used to treat glaucoma and dry mouth
Bethanecol (mAchR agonist)- used to aid bladder / gastric emptying
Succinylcholine (high affinity nAchR) used in surgery for depolarising paralysis
Indirectly acting;
AchE inhibitors such as Tacrine, donepezil or rivastigmine used in dementia
Neuromuscular disease such as myasthesia gravis

21
Q

What are clinical uses of nicotinic blockers?

A

Muscle relaxants

Depolarising blockers