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Pharmacology. The Cholinergic Nervous System. > Cholinesterase Inhibitors. > Flashcards

Cholinesterase Inhibitors. Flashcards

1
Q

What are the functions of cholinesterase inhibitors?

A

It inhibits acetylcholinesterase.

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2
Q

What happens when acetylcholinesterase is inhibited?

A

ACH builds up in the synaptic cleft and this increases cholinergic activity.

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3
Q

What are the 2 categories of acetylcholinesterase inhibitors?

A

Reversible inhibitors.

Irreversible inhibitors.

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4
Q

What are some examples of reversible acetylcholinesterase inhibitors?

A

Physostigmine.

Pyridostigmine.

Neostigmine.

Edrophonium.

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5
Q

What are some examples of irreversible acetylcholinesterase inhibitors?

A

Organophosphate.

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6
Q

What are the 2 active sites on ACHE?

A

An anionic site.

An esteratic site.

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7
Q

What does the anionic site of ACHE bind to?

A

Positively charge molecules such as the nitrogen on ACH.

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8
Q

What does the esteratic site of ACHE bind to?

A

The carboxyl group on ACH.

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9
Q

How does ACHE break down ACH?

A

It combines with water to form acetic acid and choline.

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10
Q

What happens to the choline that is formed via the breakdown of ACH by ACHE?

A

It is recycled.

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11
Q

Is the ACHE enzyme re-usable?

A

Yes.

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12
Q

How do reversible cholinesterase inhibitors work?

A

The bind to the ionic and esteratic sites of ACHE and are then slowly broken down by ACHE.

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13
Q

How do organophosphate compounds inhibit ACHE?

A

They bind to the ionic and esteratic sites of ACHE and cannot be removed.

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14
Q

Organophosphate compounds are found in what substances?

A

Pesticides.

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15
Q

What are 4 examples of reversible cholinesterase inhibitors?

A

Physostigmine.

Neostigmine.

Pyridostigmine.

Edrophonium.

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16
Q

Can physostigmine act in the CNS?

A

Yes, as it can cross the blood brain barrier.

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17
Q

Is physostigmine a reversible or irreversible cholinesterase inhibitor?

A

A reversible cholinesterase inhibitor.

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18
Q

What conditions is physostigmine used to treat?

A

Glaucoma.

It is the antidote for atropine toxicity.

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19
Q

Physostigmine can be used as the antidote for what?

A

Atropine toxicity.

20
Q

How is neostigmine absorbed?

A

Orally.

21
Q

Does neostigmine affect the CNS?

A

Yes, but not as much as physostigmine.

22
Q

What receptors will neostigmine bind to?

A

Nicotinic receptors at the neuromuscular junction.

23
Q

What 2 conditions is neostigmine used to treat?

A

Myasthenia gravis.

Reverse neuromuscular blockade.

24
Q

Is neostigmine a reversible or irreversible cholinesterase inhibitor?

A

A reversible cholinesterase inhibitor.

25
Q

Is edrophonium a reversible or irreversible cholinesterase inhibitor?

A

A reversible cholinesterase inhibitor.

26
Q

How does edrophonium interact with ACHE?

A

It binds to the ionic site and the esteratic site.

27
Q

Edrophonium will compete with what to bind to ACHE?

A

ACH.

28
Q

Does edrophonium have a short or long duration of action?

A

A short duration of action.

29
Q

What conditions is edrophonium used for?

A

For diagnosis of myasthenia gravis.

Anti curare.

30
Q

What is a significant side effect of edrophonium?

A

Bradycardia.

31
Q

What is the preferred drug for treatment of myasthenia gravis?

A

Pyridostigmine.

32
Q

What is the pharmacological effect of neostigmine on skeletal muscle?

A

Stimulation of nicotinic receptors.

33
Q

Will neostigmine be more likely to affect skeletal muscle at high or low doses?

A

At low doses.

34
Q

What are anticurare agents?

A

Antagonists to non-depolarising neuromuscular blocking agents.

35
Q

What are common pharmacologic effects of reversible cholinesterase inhibitors?

A

Ganglionic stimulation.

Hypotension, bradycardia, arrhythmia.

Bronchoconstriction.

Contraction of the urinary bladder.

36
Q

What are the side effects of large doses of physostigmine?

A

Stimulation and then depression of the CNS.

37
Q

What are the side effects of massive doses of physostigmine?

A

Convulsions.

38
Q

What are the 6 side effects of neostigmine?

A

Skeletal muscle weakness.

Nausea.

Vomiting.

Colic.

Diarrhoea.

Bradycardia.

39
Q

What is the antidote for toxic effects caused by reversible cholinesterase inhibitors?

A

Atropine.

40
Q

Will organophosphates penetrate the blood brain barrier?

A

Yes.

41
Q

What are 3 compounds that act as irreversible cholinesterase inhibitors?

A

Pesticides.

Nerve gas.

Dichlorvos.

42
Q

What is the mode of action of irreversible cholinesterase inhibitors?

A

It binds to and irreversibly inhibits ACHE.

43
Q

What are the symptoms of organophosphate poisoning?

A

Increased salivation.

Vomiting.

Diarrhoea.

Frequent urination.

Bradycardia.

Hypotension.

Muscle twitching/paralysis.

44
Q

What are the 2 antidotes for organophosphate poisoning?

A

Atropine as it will bind to ACHE and prevent the toxin from binding.

Pralidoxime will help re-generate ACHE enzymes that are blocked.

45
Q

How does pralidoxime act as an antidote for organophosphate poisoning?

A

It removes the organophosphate from the ACHE.

46
Q

How soon should we give pralidoxime to victims of organophosphate poisoning?

A

As soon as possible.

Pharmacology. The Cholinergic Nervous System. (5 decks)

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