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Fundamentals of pharmocology and physiolgy > Cholinergic effects > Flashcards

Cholinergic effects Flashcards

1
Q

What are some cholinergic esterase inhibitors

A

Neostigmine, physostigmine, edrophonium and parathion

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2
Q

What are nicotinic acetylcholine receptors

A

Ligand gated ion channels

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3
Q

Where are N1/Nm receptors found

A

Skeletal muscle

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4
Q

Where are N2/Nn receptors found

A

Autonomic ganglia/CNA

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5
Q

What are muscarinic acetylcholine receptors

A

G-coupled receptors

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6
Q

Where are M1 receptors found

A

CNS, peripheral neurones and gastric parietal cells

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7
Q

Where are M2 receptors found

A

Atria, SAN and AVN

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8
Q

Where are M3 receptors found

A

Visceral smooth muscle, secretory glands and endothelial cells

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9
Q

Where are M4 and M5 receptors found

A

CNS

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10
Q

What are some nicotinic agonists

A

Nicotine and lobeline

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11
Q

What are some nicotinic antagonists

A

Tubocararine, hexamhonium and pancuronium

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12
Q

What are some muscarinic agonists

A

Muscarine, bethanecol (longer lasting) and pilocarpine

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13
Q

What are some muscarinic antagonists

A

Atropine, hyoscine, pirenzepine and ipratropium

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14
Q

What are some parasympathetic effects

A
  • Reduced heart rate
  • Vasodilation
  • Increased saliva and gastric acid production
  • Increased tear formation
  • Visceral smooth muscle contraction
  • Pupil constriction
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15
Q

Which muscarinic receptors are G alpha q/11 receptors

A

M1, M3 and M5

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16
Q

Which muscarinic receptors are G alpha i receptors

A

M2 and M4

17
Q

What are some cardiac effects and how are they achieved

A

Limited parasympathetic innervation to the heart

Stimulated through the vagus to reach the SAN and atria M2 receptors

18
Q

How does arterial relaxation occur

A

Stimulated by acetylcholine on M3 receptors situated on endothelial cells on the monolayer in arteries

19
Q

How does rapid relaxation of smooth muscle cell occur

A

NO is released which binds to guanylate cyclase and GTP is converted to cGMP

20
Q

What is a cardiovascular effect

A

Blood pressure drops however there is no change in heart rate

21
Q

How is acid production augmented

A

Acetylcholine from the vagus nerve activates M1 receptors

22
Q

How are salivary glands activated

A

M3

23
Q

How are sweat glands activated

A

M3 receptors which are under sympathetic control

24
Q

How is the pupil narrowed

A

Parasympathetic stimulation of M3 receptors causing contraction of circular muscle

25
Q

How is the pupil widened

A

Sympathetic stimulation of alpha 1 receptors causing contraction of radial muscle

26
Q

What happens in glaucoma

A

Poor drainage of fluid through the trabecular network, often due to dilated iris

27
Q

What is pilocarpine and how is it used

A

A directly acting mAchR agonist that is used to treat glaucoma and dry mouth and its used in sweat tests

28
Q

What is bethanecol and how is it used

A

A directly acting mAchR agonist occasionally used to aid bladder/gastric emptying

29
Q

What is succinylcholine and how is it used

A

A directly acting high affinity nAChR agonist used in surgery, depolarising paralysis

30
Q

What are some indirectly acting clinical uses of parasympathetics

A

Choline esterase inhibitors such as tacrine, donepezil and rivastigmine used in dementia

31
Q

What are some clinical uses of muscarinic blockers

A
  • Dry up secretions before surgery and prevent vagal slowing of the heart
  • In heart block to increase AV conduction
  • Ophthalmology to produce mydriasis for examination
  • Bronchodilatation in COPD
  • Anti-spasmodic in GI colic
  • Treatment of anticholinergic poisoning
  • Motion sickness
32
Q

What are some clinical uses of cholinergic blockers

A
  • Muscle relaxants, direct nAchR blockers
  • Tubocurarine, pancoronium, vecuronium and atarcurium
  • Depolarising blockers, direct nAchR agonists
  • Suxamethonium

Fundamentals of pharmocology and physiolgy (12 decks)

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