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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
What are the PK of Bethanechol?
Metabolism: Resistant to AChE Lipid solubility: Poor Duration of action: 30 minutes to 2 hours Receptors: Muscarinic
26
What are the PK of Carbachol?
Metabolism: Resistant to AChE Lipid solubility: Poor Duration of action: 30 minutes to 2 hours Receptors: Muscarinic and nicotinic
27
What are the PK of Pilocarpine?
Metabolism: Resistant to AChE Lipid solubility: Good Duration of action: 30 minutes to 2 hours Receptors: Muscarinic
28
What are the PK of Nicotine?
Metabolism: Hepatic; CYP2A6 and CYP2B6 Lipid solubility: High Duration of action: 1 to 6 ours Receptors: Muscarinic and nicotinic
29
What are the PK of Veranicline?
Metabolism: Excreted mostly unchanged in the urine Lipid solubility: HIgh Duration of action: 12 to 24 hours Receptors: Nicotinic
30
Which drug is a partial agonist to the nicotinic receptors?
Varenicline
31
Why are Bethanechol and Carbachol resistant to AChE?
Due to the esterification of carbonic acid in their structure
32
What is Pilocarpine metabolised by?
Serum esterase and hepatic enzyme CYP2A6
33
How is Acetylcholine administered?
Intraocular or IV
34
What are the primary effects of Acetylcholine?
Ocular system, produces miosis
35
What is the therapeutic use of Acetylcholine?
Surgical ocular procedures
36
What are IV acetylcholine used for?
The cardiovascular system
37
What is the effect of acetylcholine on the CVS?
Decrease in heart rate and output
38
What are the vascular effects of acetylcholine and the effect on BP?
Decreases BP by producing vasodilation Mediated by muscarinic receptors
39
What are the effects of acetylcholine on the GI and the GU?
Increases salivation and stimulates intestinal secretions and motility Prevents urinary retention
40
What happens to the effect of acetylcholine on GI and GU with systemic administration?
They are inconsistent because of the rapid inactivation of ACh by AChE
41
What is the primary effect target of Bethanechol?
GI and GU systems
42
What is the effect of Bethanechol on GI system?
Enhances GI motility
43
What is the effect of Bethanechol on the GU system?
Stimulates the detrusor muscle of the bladder, promotes urination
44
What are the side effects of Bethanechol?
CVS: Hypotension and bradycardia Resp.: Bronchoconstriction GI: diarrhoea Glands: Increased sweating
45
Which kind of patients is Bethanechol contraindicated for?
Asthmatic / COPD patients due to the bronchoconstriction
46
The side effects of Bethanechol are a consequence of:
Muscarinic receptor stimulation
47
What is Atropine?
An anticholinergic drug
48
How are treatments of Bethanchol administred?
Treatment consists of IV/IM administration of Atropine in doses sufficient to cross the BBB
49
What is the primary use of Carbachol?
used topically in the eye to induce miosis
50
What is the function of Carbachol?
It decreases the pressure in the eye by increasing the amount of fluid that is drained from the eye.
51
What is the main therapeutic use of Carbachol?
Ophthalmological surgeries and treatment of open angle or narrow angle glaucoma
52
Where is Pilocarpine used?
Topically in the eye and the mouth
53
What is the therapeutic treatment of Pilocarpine?
Open angle or narrow angle glaucoma
54
When Pilocarpine is given oral spray or tablets what does it induce?
Promotes salivation and is used in the treatment of xerostomia
55
Which other direct-acting cholinergic agonist can have the same effect as Pilocarpine when given orally?
Cevimeline
56
What is the toxicity of Pilocarpine characterised by?
Excessive sweating and salivation
57
What drug could be used to counter-act the toxicity of Pilocarpine?
Atropine
58
What are the indirect-acting cholinergic agonists?
Anticholinergic agents or cholinesterase inhibitors
59
What is the function of indirect-acting cholinergic agonists?
They inhibit acetylcholinesterase (AChE), the enzyme that destroys acetylcholine secreted into the synapse
60
What is the main effect of indirect-acting cholinergic agonists?
They extend the half-life of synaptic Ache and boost the cholinergic activity
61
What is the effect of the boost in cholinergic activity because of the indirect-acting cholinergic agonists?
It is non-specific and acts in both nicotinic and muscarinic receptors --> occur at all physiological sites of action
62
What is the consequence of the boost of cholinergic activity?
The drugs have a wide range of effects that depend on their pharmacological properties (half life, solubility etc.)
63
What is the chemical class of Edrophonium?
Alcohol
64
What is the duration cation of Edrophonium?
Short (10 to 20 minutes)
65
What is the lipid solubility of Edrophonium?
Poor
66
Which anticholinesterase agent is no longer clinically used?
Edrophonium
67
What is the chemical class of Physostigmine?
Carbamic acid ester
68
What is the duration of Physostigmine?
Intermediate (30 minutes to 2 hours)
69
What is the lipid solubility of Physostigmine?
Good
70
What is the clinical use of Physostigmine?
Increases intestinal and bladder motility Reverses the effects of atropine
71
What is the chemical class of Neostigmine?
Carbamic acid ester
72
What is the duration of Neostigmine?
Intermediate (30 minutes to 2 hours)
73
What is the lipid solubility of Neostigmine?
Poor
74
What are the clinical uses of Neostigmine?
Prevents urinary retention Management of myasthenia gravis Antidote for competitive neuromuscular-blocking gents
75
What is the chemical class of Pyridostigmine?
Carbamic acid ester
76
What is the duration of action of Pyridostigmine?
Long (3 to 6 hours)
77
What is the lipid solubility of Pyridostigmine?
Poor
78
What are the clinical uses of Pyridostigmine?
Management of myasthenia gravis
79
Which drugs are used as treatment for Alzheimer's disease?
Donepezil & Rivastigmine
80
Why were anticholinesterase agents developed?
By the military as nerve agents
81
What are the related compounds of anticholinesterase agents that are used as insecticides?
Parathion and Malathion
82
What is the MOA of anticholinesterase agents?
Once bound to AChE, they phosphorylate the esteratic site on AChE --> permanently inactivates the enzyme
83
What are the actions of Echothiophate?
Cholinergic stimulation, paralysis of motor function --> breathing difficulties
84
What is the antidote of Echothiophate?
Atropine in high doses
85
What is therapeutic use of Echothiophate?
Open angle glaucoma, especially after cataract surgery.
86
Which drug should NOT be used for narrow angle glaucoma?
Echothiophate
87
What is the main reason of death when it comes to anticholinesterase agents?
Respiratory failure due to respiratory depression, respiratory muscle weakness and direct pulmonary effects
88
What are the different management methods of anticholinesterase agents toxicity?
Pralidoxime Atropine Diazepam
89
Where is acetyl-coa synthesised?
Mitochondria
90
How is choline transported into the presynaptic nerve?
Sodium dependent choline transporter (CHT)
91
What drug is the CHT transporter inhibited by?
Hemicholinium
92
How is ACh transported form the cytoplasm into the synaptic vesicles?
Vesicle-associated transporter (VAT)
93
What drug inhibits VAT?
Vesamicol
94
Which toxin interacts with the synaptobrevin and other proteins to prevent ACh release?
Botulinum toxin
95
When does the release of transmitters occurs?
When voltage sensitive calcium channels in terminal membrane are opened
96
What is Botox?
Botulinum toxin
97
How does Botox work?
Blocks ACh release by nerve impulses
98
How long after the Botox will the muscles start regaining function?
Six months after treatment

Immunology Drugs (7 decks)

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