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Pharma > Cholinomimetics > Flashcards

Cholinomimetics Flashcards

1
Q

Which receptors do cholinomimetics bind to?

A

Muscarinic or nicotinic receptors

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2
Q

Name the direct acting cholinomimetics

A

Ach
Bethanecol
Carbachol
Methacholine

Cevimeline
Varenicline

Pilocarpine 
Lobeline 
Arecoline 
Nicotine 
Muscarin
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3
Q

Name the quaternary cholinomimetics

A 
Ach
Bethanechol 
Carbachol
Methacholine 
Muscarin
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4
Q

Name the tertiary direct acting cholinomimetics

A

Pilocarpine
Lobeline
Arecoline
Nicotine

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5
Q

What are the clinical uses of Bethanechol?

A

Non-obstructive GIT dysmotility e.g., Ileus, gastric atony, post op abdominal distension
Urinary retention

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6
Q

What are the clinical uses of Carbachol?

A

Glaucoma (during surgery)

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7
Q

What are the clinical uses of Acetylcholine?

A

No clinical use due to the half life.

Exception: when short myosin is needed e.g., cataract surgery

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8
Q

What is the action of Methacholine?

A

Bronchoconstriction

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9
Q

What is the clinical use of Methacholine?

A

Methacholine challenge for the diagnosis of pulmonary function

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10
Q

What are the side effects of Bethanechol?

A 
Sweating
Salivation 
Flushing 
Decreased BP 
Nausea
Abdominal pain 
Diarrhoea
Bronchospasm
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11
Q

What is the antidote for bethanecol toxicity?

A

Atropine sulfate

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12
Q

What is the clinical use of Cevimeline?

A

Sjogren syndrome

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13
Q

What is the clinical use of Varenicline?

A

Cessation of smoking as it is a partial nicotinic agonist

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14
Q

Which cholinomimetic is a partial nicotinic agonist?

A

Varenicline

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15
Q

What are the clinical uses of Pilocarpine?

A

Glaucoma
Xerostomia
Sjogren syndrome
Salivary gland hypofunction due to radiotherapy of head and neck

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16
Q

How is pilocarpine administered in the treatment of glaucoma?

A

Topically

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17
Q

What is the mechanism of action of Pilocarpine in the treatment of glaucoma?

A

Pilocarpine causes myosin and ciliary contraction which decreases aqueous humour production which decreases IOP.

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18
Q

What are the side effects of pilocarpine?

A

Cyclopegia
Night blindness
Brow ache

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19
Q

What is the antidote for pilocarpine toxicity?

A

Parenteral atropine

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20
Q

What are the alkaloids?

A 
Pilocarpine
Lobeline
Arecoline
Arecoline
Nicotine
Muscarine
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21
Q

What is the mechanism of action of Pilocarpine?

A

increased salivation

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22
Q

What is the mechanism of action of Arecoline and Nicotine?

A

inhibits reward effect of nicotine in the limbic system

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23
Q

Is muscarine a quaternary or tertiary amine?

A

Quaternary

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24
Q

Can muscarine enter the CNS?

Why?

A

No

Quaternary amine

25
Q

What are the indirect acting cholinomimetics?

A

Ach esterase inhibitors

26
Q

What are the reversible AChEIs?

A

Edrophonium

Carbamates

27
Q

Is Edrophonium competitive or non-competitive?

A

Competitive

28
Q

Are carbamates competitive or non-competitive?

A

Non-competitive

29
Q

What are the characteristics of Edrophonium?

A

Short acting
Alcohol
Quaternary amine

30
Q

What is the duration of action of Edrophonium?

A

5-15 mins (injection)

31
Q

What is the clinical indication of Edrophonium?

A

Tensilon test

32
Q

What are the characteristics of Physostigmine?

A

Tertiary amine

Carbamate

33
Q

Can physostigmine enter the CNS?

Why

A

Yes

Tertiary amine

34
Q

What is the duration of action of Physostigmine?

A

0.5-2 hours

35
Q

What are the clinical uses of Physostigmine?

A

Glaucoma

Antidote in atropine overdose

36
Q

What are the characteristics of Rivastigmine?

A

Tertiary amine

Carbamate

37
Q

Can rivastigmine enter the CNS?

Why?

A

Yes

tertiary amine

38
Q

What is the clinical indication of Rivastigmine?

A

Alzheimer

39
Q

What is the duration of action of Neostigmine and Distigmine?

A

0.5h-2h

40
Q

What are the clinical indications of Neostigmine, Distigmine?

A

Ileus
Urinary retention
MG
Reversal of non-depolarising Nm blockers

41
Q

What are the characteristics of Neostigmine and Distigmine?

A

Quaternary amins

Carbonate

42
Q

Can Neostigmine, Distigmine, Pyridostigmine, Ambenonium and Demecarium enter the CNS?

Why?

A

No

Quatenary amine

43
Q

What is the duration of action of Pyridostigmine?

A

3-6h

44
Q

What is the duration of action of Ambenonium?

A

4-8h

45
Q

What is the duration of action of Demecarium?

A

4-6h

46
Q

What is the clinical indication of Pyridostigmine?

A
  • MG (chronic management)

- Prevention of nerve gas

47
Q

What is the clinical indication of Ambenonium?

A

MG (chronic management)

48
Q

What is the clinical indication of Demecarium?

A

Glaucoma

49
Q

What are the characteristics of Doneperzile and Tacrine?

A

Lipid soluble (CNS entry)

50
Q

What are the clinical indications of Doneperzile and Tacrine?

A

Alzheimers disease

51
Q

What are the clinical indications of Organophosphates?

A

Glaucoma

52
Q

What is the duration of action of organophosphates?

A

100 hours

53
Q

What are the characteristics of organophosphates?

A

Lipid soluble

Irreversible inhibitors

54
Q

What is the antidote given in reversible AChE inhibitors?

A

Atropine

55
Q

What are the symptoms of acute toxicity with cholinomimetics? (Muscarinic effects)

A 
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction 
Lacrimation
Salivation
Sweating
CNS stimulation
56
Q

What are the symptoms of acute toxicity with cholinomimetics? (Nicotinic effects)

A

Skeletal muscle excitation followed by paralysis (cholinergic crisis) - this is irreversible
CNS stimulation

57
Q

What are the symptoms of chronic toxicity with cholimomimetics?

A

Peripheral neuropathy causing muscle weakness and sensory loss (Like MS)
Demyelination not due to AChE inhibition

58
Q

Why does demyelination due to chronic toxicity of cholinomimetics occur?

A

AChE are very lipid soluble so they can go into the myeline sheath, bind to happen and then lead town immune response

Pharma (23 decks)

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