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Immunology Drugs > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

What are cholinergic drugs?

A

Drugs that lead to stimulation of cholinergic receptors

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2
Q

What are the two kinds of receptors that bind acetylcholine and transmit its signal?

A

Muscarinic and Nicotinic Acetylcholine receptors

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3
Q

What is muscarine?

A

An alkaloid found in mushrooms

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4
Q

What is nicotine?

A

An alkaloid found in tobacco

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5
Q

What do cholinergic agonists do?

A

They mimic acetylcholine, called cholinomimetics

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6
Q

What is the mechanism of action of cholinomimetics?

A

Some bind and activate cholinoreceptors directly, whereas others act indirectly by inhibiting the destruction of endogenous acetylcholine

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7
Q

What are the direct-acting cholinergic agents?

A

The drugs that directly bind and activate nicotinic and muscarinic receptors with variable amounts of selectivity

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8
Q

For receptor M2, what is the target?

A

The heart

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9
Q

What is the G protein associated with the receptor M2?

A

Gi coupled

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10
Q

What is the mechanism associated with the receptor M2?

A

Decrease in adenylyl cyclase

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11
Q

What is the effect associated with the receptor M2?

A

Decrease in cAMP

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12
Q

What is the target of M3 receptor?

A

Eyes, glands etc.

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13
Q

What is the G protein associated with the M3 receptor?

A

Gq coupled

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14
Q

What is the mechanism associated with the receptor M3?

A

Increase in phospholipase C

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15
Q

What is the effect associated with the M3 receptor?

A

Increase in IP3, DAG and Ca2+

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16
Q

What are the direct-acting cholinergic agonists classified into?

A

Choline esters
Naturally occurring alkaloids

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17
Q

What are the choline esters?

A

They include natural acetylcholine and synthetic esters of choline.

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18
Q

What are the examples of choline esters?

A

Bethanechol
Carbachol
Methacholine

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19
Q

What are the examples of naturally occurring alkaloids?

A

Nicotine and pilocarpine

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20
Q

What is one characteristic of all the direct-acting cholinergic drugs?

A

They all have a longer acting duration compared to Acetylcholine

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21
Q

What are the differences between all the direct-acting cholinergic drugs?

A

Their spectrum of action and their pharmacokinetics

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22
Q

Which are the most therapeutically useful drugs from the direct-acting cholinergic drugs?

A

Pilocarpine & bethanechol

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23
Q

Are Pilocarpine and Bethanechol muscarinic or nicotinic agents?

A

Muscarinic

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24
Q

What are the PK of acetylcholine?

A

Metabolism: Rapidly hydrolyzed by AChE (acetylcholinesterase)
Lipid solubility: Poor
Duration of action: 5 to 30 seconds
Receptors: Muscarinic and nicotinic

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25
Q

What are the PK of Bethanechol?

A

Metabolism: Resistant to AChE
Lipid solubility: Poor
Duration of action: 30 minutes to 2 hours
Receptors: Muscarinic

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26
Q

What are the PK of Carbachol?

A

Metabolism: Resistant to AChE
Lipid solubility: Poor
Duration of action: 30 minutes to 2 hours
Receptors: Muscarinic and nicotinic

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27
Q

What are the PK of Pilocarpine?

A

Metabolism: Resistant to AChE
Lipid solubility: Good
Duration of action: 30 minutes to 2 hours
Receptors: Muscarinic

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28
Q

What are the PK of Nicotine?

A

Metabolism: Hepatic; CYP2A6 and CYP2B6
Lipid solubility: High
Duration of action: 1 to 6 ours
Receptors: Muscarinic and nicotinic

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29
Q

What are the PK of Veranicline?

A

Metabolism: Excreted mostly unchanged in the urine
Lipid solubility: HIgh
Duration of action: 12 to 24 hours
Receptors: Nicotinic

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30
Q

Which drug is a partial agonist to the nicotinic receptors?

A

Varenicline

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31
Q

Why are Bethanechol and Carbachol resistant to AChE?

A

Due to the esterification of carbonic acid in their structure

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32
Q

What is Pilocarpine metabolised by?

A

Serum esterase and hepatic enzyme CYP2A6

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33
Q

How is Acetylcholine administered?

A

Intraocular or IV

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34
Q

What are the primary effects of Acetylcholine?

A

Ocular system, produces miosis

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35
Q

What is the therapeutic use of Acetylcholine?

A

Surgical ocular procedures

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36
Q

What are IV acetylcholine used for?

A

The cardiovascular system

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37
Q

What is the effect of acetylcholine on the CVS?

A

Decrease in heart rate and output

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38
Q

What are the vascular effects of acetylcholine and the effect on BP?

A

Decreases BP by producing vasodilation
Mediated by muscarinic receptors

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39
Q

What are the effects of acetylcholine on the GI and the GU?

A

Increases salivation and stimulates intestinal secretions and motility

Prevents urinary retention

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40
Q

What happens to the effect of acetylcholine on GI and GU with systemic administration?

A

They are inconsistent because of the rapid inactivation of ACh by AChE

41
Q

What is the primary effect target of Bethanechol?

A

GI and GU systems

42
Q

What is the effect of Bethanechol on GI system?

A

Enhances GI motility

43
Q

What is the effect of Bethanechol on the GU system?

A

Stimulates the detrusor muscle of the bladder, promotes urination

44
Q

What are the side effects of Bethanechol?

A

CVS: Hypotension and bradycardia
Resp.: Bronchoconstriction
GI: diarrhoea
Glands: Increased sweating

45
Q

Which kind of patients is Bethanechol contraindicated for?

A

Asthmatic / COPD patients due to the bronchoconstriction

46
Q

The side effects of Bethanechol are a consequence of:

A

Muscarinic receptor stimulation

47
Q

What is Atropine?

A

An anticholinergic drug

48
Q

How are treatments of Bethanchol administred?

A

Treatment consists of IV/IM administration of Atropine in doses sufficient to cross the BBB

49
Q

What is the primary use of Carbachol?

A

used topically in the eye to induce miosis

50
Q

What is the function of Carbachol?

A

It decreases the pressure in the eye by increasing the amount of fluid that is drained from the eye.

51
Q

What is the main therapeutic use of Carbachol?

A

Ophthalmological surgeries and treatment of open angle or narrow angle glaucoma

52
Q

Where is Pilocarpine used?

A

Topically in the eye and the mouth

53
Q

What is the therapeutic treatment of Pilocarpine?

A

Open angle or narrow angle glaucoma

54
Q

When Pilocarpine is given oral spray or tablets what does it induce?

A

Promotes salivation and is used in the treatment of xerostomia

55
Q

Which other direct-acting cholinergic agonist can have the same effect as Pilocarpine when given orally?

A

Cevimeline

56
Q

What is the toxicity of Pilocarpine characterised by?

A

Excessive sweating and salivation

57
Q

What drug could be used to counter-act the toxicity of Pilocarpine?

A

Atropine

58
Q

What are the indirect-acting cholinergic agonists?

A

Anticholinergic agents or cholinesterase inhibitors

59
Q

What is the function of indirect-acting cholinergic agonists?

A

They inhibit acetylcholinesterase (AChE), the enzyme that destroys acetylcholine secreted into the synapse

60
Q

What is the main effect of indirect-acting cholinergic agonists?

A

They extend the half-life of synaptic Ache and boost the cholinergic activity

61
Q

What is the effect of the boost in cholinergic activity because of the indirect-acting cholinergic agonists?

A

It is non-specific and acts in both nicotinic and muscarinic receptors –> occur at all physiological sites of action

62
Q

What is the consequence of the boost of cholinergic activity?

A

The drugs have a wide range of effects that depend on their pharmacological properties (half life, solubility etc.)

63
Q

What is the chemical class of Edrophonium?

A

Alcohol

64
Q

What is the duration cation of Edrophonium?

A

Short (10 to 20 minutes)

65
Q

What is the lipid solubility of Edrophonium?

A

Poor

66
Q

Which anticholinesterase agent is no longer clinically used?

A

Edrophonium

67
Q

What is the chemical class of Physostigmine?

A

Carbamic acid ester

68
Q

What is the duration of Physostigmine?

A

Intermediate (30 minutes to 2 hours)

69
Q

What is the lipid solubility of Physostigmine?

A

Good

70
Q

What is the clinical use of Physostigmine?

A

Increases intestinal and bladder motility
Reverses the effects of atropine

71
Q

What is the chemical class of Neostigmine?

A

Carbamic acid ester

72
Q

What is the duration of Neostigmine?

A

Intermediate (30 minutes to 2 hours)

73
Q

What is the lipid solubility of Neostigmine?

A

Poor

74
Q

What are the clinical uses of Neostigmine?

A

Prevents urinary retention
Management of myasthenia gravis
Antidote for competitive neuromuscular-blocking gents

75
Q

What is the chemical class of Pyridostigmine?

A

Carbamic acid ester

76
Q

What is the duration of action of Pyridostigmine?

A

Long (3 to 6 hours)

77
Q

What is the lipid solubility of Pyridostigmine?

A

Poor

78
Q

What are the clinical uses of Pyridostigmine?

A

Management of myasthenia gravis

79
Q

Which drugs are used as treatment for Alzheimer’s disease?

A

Donepezil & Rivastigmine

80
Q

Why were anticholinesterase agents developed?

A

By the military as nerve agents

81
Q

What are the related compounds of anticholinesterase agents that are used as insecticides?

A

Parathion and Malathion

82
Q

What is the MOA of anticholinesterase agents?

A

Once bound to AChE, they phosphorylate the esteratic site on AChE –> permanently inactivates the enzyme

83
Q

What are the actions of Echothiophate?

A

Cholinergic stimulation, paralysis of motor function –> breathing difficulties

84
Q

What is the antidote of Echothiophate?

A

Atropine in high doses

85
Q

What is therapeutic use of Echothiophate?

A

Open angle glaucoma, especially after cataract surgery.

86
Q

Which drug should NOT be used for narrow angle glaucoma?

A

Echothiophate

87
Q

What is the main reason of death when it comes to anticholinesterase agents?

A

Respiratory failure due to respiratory depression, respiratory muscle weakness and direct pulmonary effects

88
Q

What are the different management methods of anticholinesterase agents toxicity?

A

Pralidoxime
Atropine
Diazepam

89
Q

Where is acetyl-coa synthesised?

A

Mitochondria

90
Q

How is choline transported into the presynaptic nerve?

A

Sodium dependent choline transporter (CHT)

91
Q

What drug is the CHT transporter inhibited by?

A

Hemicholinium

92
Q

How is ACh transported form the cytoplasm into the synaptic vesicles?

A

Vesicle-associated transporter (VAT)

93
Q

What drug inhibits VAT?

A

Vesamicol

94
Q

Which toxin interacts with the synaptobrevin and other proteins to prevent ACh release?

A

Botulinum toxin

95
Q

When does the release of transmitters occurs?

A

When voltage sensitive calcium channels in terminal membrane are opened

96
Q

What is Botox?

A

Botulinum toxin

97
Q

How does Botox work?

A

Blocks ACh release by nerve impulses

98
Q

How long after the Botox will the muscles start regaining function?

A

Six months after treatment

Immunology Drugs (7 decks)

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