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Cholinergic Agonists and Antagonists Flashcards

1
Q

What are the functions of the M1 muscarinic receptor?

A

Activates myenteric plexus

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2
Q

What are the functions of the M2 muscarinic receptor?

A

Decreases HR and contraction via opening of the K channels

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3
Q

What are the functions of the M3 muscarinic receptor?

A

Pupillary constriction
Bronchoconstriction
Increase GI motility
Contract bladder detrusor
Stimulate salivary secretion

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4
Q

What are the muscarinic receptors?

A

M1
M2
M3

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5
Q

What are the nicotinic receptors?

A

Nn
Nm

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6
Q

What is the Nn receptor?

A

Neuronal nicotinic receptor

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7
Q

What is the Nm receptor?

A

Muscle cell nicotinic receptor

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8
Q

What receptor does nicotine bind?

A

Nn

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9
Q

What is the effect of nicotine?

A

Diffuse activation of central and peripheral nicotinic receptors

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10
Q

Nicotine indication

A

Limited to preparations for smoking cessation often in a transdermal patch

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11
Q

Nicotine Toxicity

A

Effects include irritation at site of administration and dyspepsia

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12
Q

What does succinylcholine stimulate?

A

Succinylcholine sticks on the Nm receptor for a
long period of time and that leads to prevention
of action potential conduction by blocking the Nm receptor

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13
Q

Succinylcholine indication

A

Used clinically as a muscle relaxant during intubation or electro convulsive shock therapy

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14
Q

Succinylcholine Contraindications

A

Familial hyperthermia
Skeletal muscle myopathies

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15
Q

What are the types of muscarinic agonists?

A

Quaternary nitrogen analogs
Tertiary amine alkaloids
Synthetic analogs

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16
Q

What does ACh stimulate?

A

Binds to both nicotinic and muscarinic receptors of the autonomic nervous system, the CNS and the neuromuscular junction.

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17
Q

ACh indication

A

It is rapidly hydrolyzed by acetyl- and plasma cholinesterases. Therefore, it has no therapeutic use.

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18
Q

What does methacholine stimulate?

A

Primarily muscarinic effects on smooth muscle, glands and heart

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19
Q

Methacholine indication

A

Used to diagnose bronchial hyperactivity in patients suspected of having asthma

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20
Q

Methacholine Toxicity

A

Bronchiolar constriction

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21
Q

Methacholine Contraindications

A

Contraindicated in pts given β-blockers since antidote to overdose is β-agonist.

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22
Q

What does carbachol stimulate?

A

Muscarinic and nicotinic activity

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23
Q

Is carbochol easily hydrolyzed by AChE?

A

Resistant to hydrolysis by AchE

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24
Q

Carbachol indication

A

Miotic agent for ocular surgery and glaucoma

Used as an intraocular injection to reduce pressure after cataract surgery

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25
Carbachol Toxicity
Side effects are related to excessive muscarinic and nicotinic receptor activation i.e., bronchoconstriction, reduced cardiac conduction
26
Bethanechol targets
Muscarinic selectivity
27
Bethanechol hydrolysis
It is resistant to hydrolysis by cholinesterases
28
What is the effect of bethanechol?
It has selective action on muscarinic receptors of GI tract and urinary bladder and minimizes the cardiac effects.
29
Bethanechol indication
Post-op urinary retention Neurogenic bladder atony
30
Bethanechol Toxicity
Bradycardia Bronchoconstriction
31
Bethanechol Contraindications
Asthma Peptic ulcer Bradycardia
32
What are the quaternary nitrogen analogs?
Methacholine Carbachol Bethanechol
33
Muscarine targets
Pure muscarinic activity
34
Muscarine hydrolysis
Resistant to hydrolysis (no ester moiety)
35
Muscarine indication
No therapeutic use
36
What is muscarine poisoning treated with?
Muscarinic poisoning causes profound parasympathetic activation, and is treated with atropine, a muscarinic receptor antagonist
37
Pilocarpine targets
Pure muscarinic activity
38
Pilocarpine and BBB
Crosses the BBB and has CNS effects
39
Pilocarpine indication
Dry mouth due to head and neck radiotherapy Sjogren’s syndrome Open angle glaucoma Acute and chronic angle-closure glaucoma
40
Pilocarpine Toxicity
Excess muscarnic activation (slowed AV conduction), Hypotension Excessive salivation Bronchoconstriction
41
Pilocarpine Contraindications
Administer with care to patients taking β-blockers due to exacerbation of conduction slowing.
42
Acetylcholinesterase
Acetylcholinesterase catalyzes the hydrolysis of acetylcholine
43
What are indirect cholinergic agonists?
Inhibition of cholinesterase protects acetylcholine from hydrolysis, and leads to the accumulation of endogenous acetylcholine and increased cholinergic activity. Thus, cholinesterase inhibitors act indirectly as cholinergic agonists.
44
What is regional function of acetylcholinesterase?
Hydrolysis of acetylcholine liberated in synaptic cleft or in neuroeffector transmission.
45
What is the regional function of butyl cholinesterase?
Plasma, non-specific esterase. Does hydrolyze certain exogenous drugs, e.g., succinylcholine.
46
Neostigmine and BBB
Contains a quaternary nitrogen, and thus poorly penetrates blood brain barrier.
47
What is the effect of neostigmine?
Inhibits acetylcholinesterase and has direct stimulatory effect on nicotinic receptors at the skeletal muscle endplate
48
Neostigmine indication
Myasthenia graves Used to reverse neuromuscular blockade
49
Neostigmine Toxicity
Side effects due to excessive Ach action at peripheral muscarinic and nicotinic receptors
50
Neostigmine Contraindications
Intestinal obstruction
51
Edrophonium targets
Inhibits cholinesterases and stimulates nicotinic receptors
52
Edrophonium onset and duration of effect
Has a very rapid onset of action, and a very short duration of action (10-15 min)
53
Edrophonium indication
Diagnosis of myasthenia gravis Differential diagnosis of too little or too much AchE inhibitor in myasthenia gravis
54
Edrophonium Toxicity
Bradycardia
55
Edrophonium Contraindications
Intestinal blockade Urinary obstruction
56
How does treatment with edrophonium allow for differential diagnosis in myasthenia gravis?
Treatment with short acting cholinesterase inhibitor reduces symptoms if muscle weakness is due to disease progression. It will worsen symptoms if due to cholinesterase toxicity.
57
Physostigmine and BBB
Readily crosses the BBB
58
Physostigmine onset and duration
Inactivated by plasma cholinesterases but takes a long time with duration of action up to 2 hours
59
Physostigmine indication
Antidote for muscarinic antagonist poisoning
60
Physostigmine Toxicity
Side effects related to increased Ach at muscarinic or nicotinic receptors. Convulsions, respiratory and CV depression
61
Physostigmine Contraindications
Asthma Cardiac insufficiency Gut obstruction
62
Donezipil indication
Alzheimer's Disease
63
Donezipil target
Inhibits only acetylcholinesterase and is reversible inhibitor in the CNS
64
What are the irreversible cholinesterase inhibitors?
Organophosphates phosphorylate cholinesterases which exhibits severe toxicity.
65
What are the signs of organophosphate toxicity? (DUMBBELS)
D Diarrhea U Urination M miosis B bradycardia B bronchorrea E emesis L lacrimation S Salivation
66
How is atropine used in the treatment of organophosphates?
It protects from systemic muscarinic effects
67
How does pralidoximine treat organophosphate poisoning?
Reactivation of the alkylphosphorylated acetylcholinesterase with Pralidoxime Chloride (2-PAM)
68
Echothiophate targets
Irreversible acetycholinesterase inhibitor
69
Echothiophate indication
Produce long term miosis in the treatment of open angle glaucoma
70
Echothiophate Toxicity
Blurred vision Brow ache
71
Echothiophate duration
Long half life and once a day administration is enough
72
What are the competitive muscarinic antagonists?
Atropine Scopolamine Glycopyrrolate
73
Atropine target
Muscarinic antagonist
74
Atropine indication
Organophosphate poisoning Induction of mydriasis and cycloplegia (though long duration of action) Reverse bradycardia of vagal origin Reverse gastrointestinal hypermotility Bladder spasms (urgency) associated with cystitis
75
Scopolamine target
Muscarinic antagonist
76
Scopolamine indication
Used in preparation for surgical anesthesia to minimize secretion To treat nausea and vomiting associated with motion sickness and chemotherapy induced nausea
77
Scopolamine Toxicity
Anti-muscarinic actions
78
Scopolamine Contraindications
Narrow angle glaucoma
79
Glycopyrrolate target
Muscarinic antagonist
80
Glycopyrrolate indication
Its antimuscarinic activity is used to prevent overstimulation of the gut during reversal of neuromuscular blockade
81
Glycopyrrolate Toxicity
Heat stroke due to inability to sweat in heat
82
What are the signs of atropine poisoning?
Dry mouth Hot Dilated pupils Tachycardia Increased BP Nervousness

Pharmacology (5 decks)

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