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2 - CPR (cardio) > Cholinergic Agonists and Antagonists > Flashcards

Cholinergic Agonists and Antagonists Flashcards

1
Q

Cholinergic Agonists will mimic the action of what neurotransmitter?

A

Acetylcholine

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2
Q

What are the 2 types of Cholinergic Agonists?

A 
Direct  = Receptor Stimulants
Indirect = Cholinesterase (-)
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3
Q

What are the 2 types of Acetylcholine receptors?

A

Muscarinic

Nicotinic

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4
Q

M1 receptors are located where and have what GPCR?

A

Nerves

- Gq/11 = IP3/DAG cascade

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5
Q

M2 receptors are located where and have what GPCR?

A

Heart, nerves and smooth muscle

- Gi/o = (-) cAMP

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6
Q

M3 receptors are located where and have what GPCR?

A

Glands and smooth muscle

- Gq/11 = IP3/DAG cascade

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7
Q

M4 receptors are located where and have what GPCR?

A

CNS

- Gi/o = (-) cAMP

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8
Q

M5 receptors are located where and have what GPCR?

A

CNS

- Gq/11 = IP3/DAG cascade

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9
Q

Nicotinic type N receptors are found where and have what types/effects?

A

CNS
- Alpha and Beta types
= K+/Na+ depolarizing channel

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10
Q

What type of Muscarinic receptor predominates in most tissues?

A

M3

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11
Q

What are 3 charged and poorly absorbed Cholinergic Agonists?

A
  1. Carbachol
  2. Methacholine
  3. Bethanechol
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12
Q

Carbachol classification and what it treats?

A

Charged and poorly absorbed Cholinergic Agonist

= Glaucoma and decreases pupil size

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13
Q

What Acetylcholine receptor type do Methacholine and Bethanechol act on?

A

Muscarinic

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14
Q

Methacholine classification and what it treats?

A

Muscarinic charged and poorly absorbed Cholinergic Agonist

= Bronchospasm

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15
Q

Bethanechol classification and what it treats?

A

Muscarinic charged and poorly absorbed Cholinergic Agonist

= Treats urinary retention, heartburn and post-op Ileus

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16
Q

What are 3 Uncharged and Highly Absorbed Cholinergic Agonists?

A
  1. Cevimeline
  2. Pilocarpine
  3. Varenicline
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17
Q

Cevimeline classification and what it treats?

A

Uncharged and highly absorbed Cholinergic Agonist

= Treats Xerostomia (dry eye) in Sjogrens Syndrome

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18
Q

What metabolizes Cevimeline?

A

CYP450

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19
Q

Pilocarpine classification and what it treats?

A

Muscarinic Uncharged and Highly absorbed Cholinergic Agonist

= Treats Xerostomia (dry eye), Glaucoma and decreases pupil size

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20
Q

What Cholinergic Agonists that are Uncharged and Highly absorbed can treat Xerostomia?

A

Cevimeline

Pilocarpine

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21
Q

Varenicline classification and what specific receptor it is a Cholinergic Agonist for?

A

Uncharged and Highly absorbed

- Alpha4 Beta2 nAchR partial agonist

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22
Q

MOA for Varenicline

A

(+) alpha4 beta 2 nAchR receptors

= Releases mesolimbic dopamine

23
Q

What does Varenicline treat?

A

Smoking cessation – decreases withdrawal symptoms

24
Q

What are the possible adverse effects of Varenicline and what should the patient do if they experience them?

A

Nausea and Neuropsych (depression/suicide)

– STOP meds and contact doctor

25
What are the major uses for Cholinergic Agonists?
- Glaucoma - Accommodative Estropia - GIGU disorders
26
Symptoms of Muscarinic Stimulant Toxicity?
N/V, diarrhea, salivation, sweating, urinary urgency, bronchial constriction
27
What are contraindications to take Muscarinic stimulant medications?
Asthma, hyperthyroidism, etc.
28
What are examples of Nicotinic Stimulant toxicity agents?
Nicotine -- tobacco and insecticides
29
What does Nicotinic Stimulant Toxicity cause?
CNS stimulation Skeletal muscle end plate depolarization HTN Cardiac Arrhythmias
30
What does Nicotinic Stimulant Toxicity cause?
CNS stimulation Skeletal muscle end plate depolarization HTN Cardiac Arrhythmias
31
What is the treatment for Nicotinic Stimulant Toxicity?
Atropine and Diazepam
32
Convulsions, coma, respiratory paralysis and neuromuscular blockade are symptoms seen with _______ toxicity
Nicotinic Stimulant Toxicity
33
What are 3 types of Cholinesterase (-) ? | AchE (-)
1. Alcohols 2. Carbamic Acid Esters 3. Organophosphates
34
What are 2 charged and poorly absorbed AchE (-)?
1. Alcohols | 2. Carbamic Acid Esters
35
What is 1 uncharged and highly absorbed AchE (-)?
Organophosphates
36
Alcohols and Carbamic Acid Esters are Cholinesterase (-)'s that are _____
Reversible
37
Organophosphates are Cholinesterase (-)'s that are _____
Irreversible
38
What are the major clinical uses for Cholinesterase Inhibitors?
Dementia | Myasthenia Gravis
39
What can be used to reverse neuromuscular paralysis and anticholinergic poisoning?
Cholinesterase (-)'s
40
Where will AchE (-)'s toxicity effects be seen?
NMJ
41
What is a prototypical Cholinergic Antagonist?
Atropine
42
Cholinergic Antagonists will block what autonomic activity?
Parasympathetic
43
With Anesthesia, what does Atropine do?
Blocks responses to vagal reflexes induced by surgical manipulation
44
What 2 drugs can treat Asthma and COPD?
Cholinergic Antagonists | = Ipratropium and Tiotropium
45
Classification of Ipratropium and Tiotropium?
Cholinergic Antagonists
46
Ipratropium and Tiotropium can treat?
Asthma and COPD
47
Which acetylcholine receptors are Ipratropium and Tiotropium Antagonists at?
Muscarinic
48
Ipratropium and Tiotropium - which has the longer action and what is their action?
Longer action - Tiotropium | = Bronchodilators
49
What muscarinic receptor should Cholinergic Antagonists work at to treat urinary urgency?
M3
50
What are 4 Cholinergic Antagonists that can treat Urinary Urgency at M3?
1. Oxybutynin 2. Darifenacin 3. Solifenacin 4. Tolterodine
51
What are 4 Cholinergic Antagonists that can treat Urinary urgency by blocking M3 receptors?
1. Oxybutynin 2. Darifenacin 3. Solifenacin 4. Tolterodine
52
Darifenacin, Solifenacin and Tolterodine have LESS _______ than Oxybutynin
Xerostomia | Constipation
53
What are 3 contraindications for Cholinergic Antagonists?
Glaucoma Prostatic Hyperplasia Acid-peptic Disease

2 - CPR (cardio) (44 decks)

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