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Pharmacology 2 > E1- Cholinergic Agents > Flashcards

E1- Cholinergic Agents Flashcards

1
Q

What are the effects of muscarinic agonist/cholinomimetics?

A 
Bradycardia
A lot of secretions
Near vision accommodation
Defecation
Decreased intraocular pressure
Urination
Miosis
Bronchoconstriction 
Vasodilation
"BAND DUMB V"
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2
Q

What are the effects of muscarinic antagonist/cholinergic blockers?

A 
Far vision accommodation/cycloplegia
Increased intraocular pressure
Tachycardia
Mydriasis
Bronchodilation
Absent secretions
"FIT MBA"
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3
Q

What is the main effect of neuromuscular blocking agents?

A

Paralysis of skeletal muscle

DO NOT produce unconsciousness or anesthesia because they do not enter the brain

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4
Q

How do depolarizing neuromuscular blocking agents work?

A

Initially depolarize the NMJ
If the depolarizing action is prolonged, the receptors desensitize, so that subsequent release of ACh does not have any effect and the muscle is paralyzed

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5
Q

What are the direct acting muscarinic agonist? (3)

A

Acetylcholine
Bethanechol (Urecholine)
Pilocarpine (IsoptoCarpine)

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6
Q

Why does ACh have no clinical use?

A

Very short half-life, rapidly hydrolyzed by AChE

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7
Q

The IV infusion of acetylcholine is similar to parasympathetic stimulation except the decreased BP is caused by what?

A

Production of NO and cGMP by endothelial cells in the blood vessels

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8
Q

What is the MOA of Bethanechol (Urecholine)?

A

Non-specific muscarinic agonist with highest effects in urinary bladder and GI tract
Resistant to AChE

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9
Q

What is DOC for increasing GI motility and tx of urinary retention?

A

Bethanechol (Urecholine)

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10
Q

Does Bethanechol (Urecholine) cross the BBB?

A

No, charged ammonia ion prevents it from crossing BBB

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11
Q

What is the MOA of Pilocarpine (IsoptoCarpine)?

A

Non-specific muscarinic agonist

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12
Q

What can Pilocarpine (IsoptoCarpine) be used for?

A

Topical: closed angle glaucoma (not a DOC)
Oral: xerostomia

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13
Q

Why is Pilocarpine (IsoptoCarpine) not a DOC for tx of glaucoma?

A

Side effects (blurred vision)

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14
Q

What are side effects of Pilocarpine (IsoptoCarpine)?

A

Topical: blurred vision
Oral: sweating
Both: HA

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15
Q

What are contraindications of the direct acting muscarinic agonist? (Acetylcholine, Bethanechol, Pilocarpine)

A

Asthma/COPD
Peptic ulcer
Bowel obstruction

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16
Q

What are side effects of the direct acting muscarinic agonist? (Acetylcholine, Bethanechol, Pilocarpine)

A 
Diarrhea
Abdominal cramps
Salvation
Sweating
Bronchoconstriction
Blurred vision
Miosis
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17
Q

Besides overdose, what else can cause muscarinic toxicity?

A

Mushroom poisoning

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18
Q

How does muscarinic toxicity present?

A

“SLUDGE”

  • Salvation
  • Lacrimation
  • Urination
  • Defecation
  • Gastric distress
  • Emesis
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19
Q

How is muscarinic toxicity treated?

A

Atropine (antagonist) and albuterol (beta agonist)

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20
Q

What are the direct acting nicotinic agonist? (2)

A

Nicotine

Varenicline

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21
Q

Does nicotine activate sympathetic or parasympathetic neurons?

A

Both

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22
Q

What is the effect of nicotinic on sympathetic neurons?

A

HTN, tachycardia alternating with vagal bradycardia

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23
Q

What is the effect of nicotinic on parasympathetic neurons?

A

N/V, diarrhea, urination

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24
Q

What are the effects of nicotine at low doses?

A

Increases alertness and attention

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25
Q

What are the effects of nicotine at high doses?

A

Tremor, N/V, increased respiration

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26
Q

What are the effects of nicotine at toxic doses?

A

Convulsions, seizures

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27
Q

How does nicotine toxicity present?

A
  • Vomiting
  • CNS stimulation (seizures, coma, respiratory arrest)
  • Skeletal muscle depolarization (initial muscle twitch followed by depolarizing blockade and paralysis)
  • HTN
  • Arrhythmia
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28
Q

What is the MOA of Varenicline (Chantix)?

A

Partial agonist on the nicotinic receptor subtype that stimulates reward system in the brain by releasing DA

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29
Q

What is Varenicline (Chantix) used for?

A

Smoking cessation

  • Provides some nicotinic stimulation to decrease cravings as it releases a small amount of DA
  • Also blocks effect of nicotine if they do smoke
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30
Q

What are some adverse effects of Varenicline (Chantix)?

A 
N/V
Constipation, flatulence
Nightmares
Mania, psychosis
Anxiety, suicidal ideation
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31
Q

What are the indirect acting/cholinesterase inhibitors? (6)

A 
Neostigmine
Pyridostigmine
Physostigmine
Edrophonium
Donepezil
Organophosphates
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32
Q

What is the MOA of Neostigmine and Pyridostigmine?

A

Form covalent bond with AChE

Effects last 30min-6hours

33
Q

What are Neostigmine and Pyridostigmine used for?

A
  • Myasthenia gravis
  • Reverse neuromuscular blockade following surgery
  • Postop/neurogenic ileus or atony of urinary bladder
34
Q

Can Neostigmine or Pyridostigmine cross the BBB?

A

No, quaternary ammonia ions

35
Q

What can be used to tx muscarinic antagonist (atropine) poisoning?

A

Physostigmine

36
Q

Can Physostigmine cross the BBB?

A

Yes, tertiary ammonia ion

37
Q

What is the MOA of Edrophonium?

A

An alcohol that binds briefly to AChE

Reversible, very short acting (5-10min)
Injection only

38
Q

What is Edrophonium used for?

A
  • Dx and determine treatment dose for myasthenia gravis

- Reverse neuromuscular blockade in surgery

39
Q

Can Edrophonium cross the BBB?

A

No, quaternary ammonia ion

40
Q

What is the MOA of Donepezil?

A

Binds with AChE

Well absorbed orally

41
Q

What is Donepezil used for?

A

Alzheimer’s disease

42
Q

What is the MOA of organophosphates (Di-isopropyl flurophosphate)?

A

Phosphorylate and form covalent bond with AChE, producing long lasting and irreversible effect
“Aging”

43
Q

What is aging?

A

When one of the phosphorus-oxygen bonds on the drug breaks, making the bond to AChE irreversible

44
Q

How does cholinesterase inhibitor toxicity present?

A

“SLUDGE”

  • Salvation
  • Lacrimation
  • Urination
  • Defecation
  • Gastric distress
  • Emesis

Miosis, sweating, bronchoconstriction, N/V, diarrhea
Bradycardia and hypotension
CNS effects
Neuromuscular stimulation followed by blockade –> respiratory paralysis –> death

45
Q

How do you tx cholinesterase inhibitor toxicity?

A
  • Atropine until pupils dilate
  • Administer 2-PAM (Pralidoxime) if less than 3-4 hours since exposure
  • Maintain respiration
  • Diazepam (Valium) for convulsions
46
Q

What precautions should you take when precribing 2-PAM (Pralidoxime) for tx of cholinesterase inhibitor toxicity?

A

Only prescribe if less than 3-4 hrs since exposure as only works before “aging occurs”

DO NOT use if unsure if the poisoning is from an organophosphate

47
Q

What is atropine used for?

A
  • Decrease bradycardia due to excessive vagal stimulation
  • Reverse heart block
  • Block muscarinic effects of organophosphate or mushroom poisoning
  • Diarrhea when combined with an opioid
48
Q

What are contraindications of atropine?

A

Closed-angle glaucoma

Benign prostate hyperplasia

49
Q

How is scopolamine administered?

A

Transdermal patch

50
Q

What is scopolamine used for?

A

Motion sickness

51
Q

What are some adverse effects of scopolamine?

A

Crosses BBB and can cause:

  • Drowsiness, short-term memory loss
  • Toxicity: hallucinations, agitation, coma
52
Q

What is Tropicamide (Mydriacil) used for?

A

Used to dilate pupils for eye exam (topical)

53
Q

What is Ipratropium (Atrovent) used for?

A
  • COPD to reverse bronchoconstriction

- Occasionally used in acute asthma attacks

54
Q

Does Ipratropium cross the BBB?

A

No, quaternary ammonia ion

55
Q

What are Tolterodnine, Fesoterodine, Darifenacin, and Solifenacin used for?

A

Overactive bladder (greater M3 selectivity)

56
Q

What drugs have greater M3 selectivity? (4)

A

Tolerodnine, Fesoterodine, Darifenacin, and Solifenacin

57
Q

What is Oxybutynin used for?

A

To decrease bladder spasms

58
Q

What is Dicyclomine (Bentyl) used for?

A

GI antispasmodic agent to decrease abdominal cramping and tx diarrhea-predominant IBS

59
Q

What is the MOA of OnabotuliniumtoxinA (Botox)?

A

Blocks release of ACh

Injection only

60
Q

What is OnabotuliniumtoxinA (Botox) used for?

A
  • Urinary incontinence in pts who are refractory to antimuscarinic drugs
  • Chronic migraine prophylaxis
  • Wrinkles
61
Q

What is an adverse effect of OnabotuliniumtoxinA (Botox)?

A

Asthenia (difficulties with speech, swallowing, numbness, ptosis)

62
Q

What is an example of a depolarizing neuromuscular blocker?

A

Succinylcholine

63
Q

What is the MOA of Succinylcholine?

A

Initial stimulation and contraction

Longer lasting than ACh –> receptor desensitization and blockade –> muscle paralysis

64
Q

How is succinylcholine administered?

A

IV only
Rapid onset: <90 sec
Rapid recovery: 5-10min

65
Q

What is succinylcholine used for?

A

Used to paralyze muscles for procedures where a rapid and short-acting effect is needed

  • Tracheotomy
  • Intubation
66
Q

What are contraindications of succinylcholine?

A

Hx of malignant hyperthermia

Extensive soft tissue damage/burns

67
Q

What are adverse effects of succinylcholine?

A

Hyperkalemia

Malignant hyperthermia

68
Q

How is malignant hyperthermia treated?

A

Dantrolene

69
Q

What are adverse effects of the muscarinic antagonists? (Atropine, Scopolamine, Tropicamide, Ipratropium, Tolterodine, Fesoterodine, Darifenacin, Solifenacin, Oxybutynin, Dicyclomine, OnabotuliniumtoxinA)

A 
Mydriasis
Cycloplegia
Photophobia
Tachycardia
Dry mouth
Dry eyes
Decreased GI motility
Urinary retention
Little effect on CNS at low doses, but can cause hallucinations, delirium, and coma at toxic/high doses
70
Q

What are the muscarinic antagonists? (11)

A 
"F SODAS DITTO"
Fesoterodine
Scopolamine
Oxybutynin
Darifenacin
Atropine
Solifenacin
Dicyclomine
Ipratropium
Tropicamide
Tolterodine
OnabotuliniumtoxinA
71
Q

How does muscarinic antagonists overdose present?

A
  • Hot, dry
  • Constipated, urinary retention
  • Dilated pupils, poor vision
  • Tachycardia
  • Agitation, delirium, dementia
  • Cardiovascular and respiratory collapse

“Hot as a hare, dry as a bone, blind as a bat, red as a beet, mad as a hatter”

72
Q

How is muscarinic antagonists overdose treated?

A

Supportive

Physostigmine to increase ACh levels in the brain

73
Q

Does Succinylcholine cross the BBB?

A

Does not cross BBB

Do NOT produce unconsciousness

74
Q

Because Succinylcholine is hydrolyzed by plasma pseudocholinesterase, the addition of a ____ will delay recovery.

A

Cholinesterase inhibitor

75
Q

____ in pseudocholinesterase activity can prolong effects (last for hrs instead of min.)

A

Genetic variations

76
Q

How is Nicotine toxicity treated?

A

Anticonvulsants and assisted respiration (there is no antidote and have to just stabilize until nicotine wears away)

77
Q

What are the cardiovascular effects of AChE inhibitors?

A

While both sympathetic and parasympathetic nerves will be stimulated, parasympathetic dominates on the heart and will cause bradycardia and decreased cardiac output

78
Q

How can a non-depolarizing blockade be reversed?

A

By the addition of AChE to increased ACh

Pharmacology 2 (12 decks)

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