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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
Q

What are the major uses for Cholinergic Agonists?

A
  • Glaucoma
  • Accommodative Estropia
  • GIGU disorders
26
Q

Symptoms of Muscarinic Stimulant Toxicity?

A

N/V, diarrhea, salivation, sweating, urinary urgency, bronchial constriction

27
Q

What are contraindications to take Muscarinic stimulant medications?

A

Asthma, hyperthyroidism, etc.

28
Q

What are examples of Nicotinic Stimulant toxicity agents?

A

Nicotine – tobacco and insecticides

29
Q

What does Nicotinic Stimulant Toxicity cause?

A

CNS stimulation
Skeletal muscle end plate depolarization
HTN
Cardiac Arrhythmias

30
Q

What does Nicotinic Stimulant Toxicity cause?

A

CNS stimulation
Skeletal muscle end plate depolarization
HTN
Cardiac Arrhythmias

31
Q

What is the treatment for Nicotinic Stimulant Toxicity?

A

Atropine and Diazepam

32
Q

Convulsions, coma, respiratory paralysis and neuromuscular blockade are symptoms seen with _______ toxicity

A

Nicotinic Stimulant Toxicity

33
Q

What are 3 types of Cholinesterase (-) ?

AchE (-)

A
  1. Alcohols
  2. Carbamic Acid Esters
  3. Organophosphates
34
Q

What are 2 charged and poorly absorbed AchE (-)?

A
  1. Alcohols

2. Carbamic Acid Esters

35
Q

What is 1 uncharged and highly absorbed AchE (-)?

A

Organophosphates

36
Q

Alcohols and Carbamic Acid Esters are Cholinesterase (-)’s that are _____

A

Reversible

37
Q

Organophosphates are Cholinesterase (-)’s that are _____

A

Irreversible

38
Q

What are the major clinical uses for Cholinesterase Inhibitors?

A

Dementia

Myasthenia Gravis

39
Q

What can be used to reverse neuromuscular paralysis and anticholinergic poisoning?

A

Cholinesterase (-)’s

40
Q

Where will AchE (-)’s toxicity effects be seen?

41
Q

What is a prototypical Cholinergic Antagonist?

42
Q

Cholinergic Antagonists will block what autonomic activity?

A

Parasympathetic

43
Q

With Anesthesia, what does Atropine do?

A

Blocks responses to vagal reflexes induced by surgical manipulation

44
Q

What 2 drugs can treat Asthma and COPD?

A

Cholinergic Antagonists

= Ipratropium and Tiotropium

45
Q

Classification of Ipratropium and Tiotropium?

A

Cholinergic Antagonists

46
Q

Ipratropium and Tiotropium can treat?

A

Asthma and COPD

47
Q

Which acetylcholine receptors are Ipratropium and Tiotropium Antagonists at?

A

Muscarinic

48
Q

Ipratropium and Tiotropium - which has the longer action and what is their action?

A

Longer action - Tiotropium

= Bronchodilators

49
Q

What muscarinic receptor should Cholinergic Antagonists work at to treat urinary urgency?

50
Q

What are 4 Cholinergic Antagonists that can treat Urinary Urgency at M3?

A
  1. Oxybutynin
  2. Darifenacin
  3. Solifenacin
  4. Tolterodine
51
Q

What are 4 Cholinergic Antagonists that can treat Urinary urgency by blocking M3 receptors?

A
  1. Oxybutynin
  2. Darifenacin
  3. Solifenacin
  4. Tolterodine
52
Q

Darifenacin, Solifenacin and Tolterodine have LESS _______ than Oxybutynin

A

Xerostomia

Constipation

53
Q

What are 3 contraindications for Cholinergic Antagonists?

A

Glaucoma
Prostatic Hyperplasia
Acid-peptic Disease

2 - CPR (cardio) (44 decks)

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