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Pharmacology - Exam 2 > Cholinergic Antagonists > Flashcards

Cholinergic Antagonists Flashcards

1
Q

Review: effect of cholinergic agonists - eye

A
  • miosis

- accomodation

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2
Q

Review: effect of cholinergic agonists - lungs

A
  • bronchiolar constriction

- increased secretion

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3
Q

Review: effect of cholinergic agonists - GI tract

A
  • increased motility

- increased secretions

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4
Q

Review: effect of cholinergic agonists - GU tract

A
  • bladder emptying
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5
Q

Review: effect of cholinergic agonists - CV system

A
  • decreased vascular resistance

- bradycardia

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6
Q

Review: effect of cholinergic agonists - sweat glands

A
  • diaphoresis (sweating)
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7
Q

Review: effect of cholinergic agonists - CNS

A
  • stimulation
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8
Q

Review: effect of cholinergic agonists - NMJ

A
  • muscle contrction
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9
Q

What is the response seen when a receptor binds an agonist?

A
  • same as the endogenous compound for which the receptor was designated
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10
Q

What is the response seen when a receptor binds an antagonist?

A
  • often the opposite as the agonist
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11
Q

What other names are muscarinic antagonists known as?

A
  • parasympatholtyics

- antimuscarinic

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12
Q

What is the effect of a muscarinic antagonist?

A
  • blocks effect of parasympathetic autonomic dischange
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13
Q

What are examples of muscarinic antagonists?

A
  • atropine, scopolamine
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14
Q

What is the effect of nicotinic antagonists in the ANS and NMJ?

A
  • ganglionic blockers (ANS)

- neuromuscular blockers (NMJ)

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15
Q

What is the effect of atropine on the eye?

A
  • mydriasis (pupil dilation), opposite of miosis
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16
Q

What is the action of atropine?

A
  • reversibly blocks muscarinic receptors
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17
Q

What is the mechanism of atropine’s action?

A
  • prevents ACh from binding to muscarinic receptors
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18
Q

T/F: Atropine typically blocks actions of endogenous acetylcholine better than it blocks exogenously administered cholinergics.

A

False, exogenous > endogenous

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19
Q

What are the most sensitive areas to atropine?

A
  • salivary
  • bronchial
  • sweat glands
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20
Q

What are the effects of anticholinergics on the CNS?

A
  • atropine has minimal effect/use

- scopolamine can produce drowsiness and amnesia which is useful as an antiemetic

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21
Q

What can scopolamine toxicity in the CNS cause?

A
  • CNS excitement
  • agitation
  • hallucinations
  • coma
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22
Q

What are the clinical uses & drugs of anticholinergics on the CNS?

A
  • adjuncts to treat Parkinson’s tremors (Benxtropine)

- prevention of motion sickness (scopolamine injx, oral, or patch)

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23
Q

What are the effects of anticholinergics on the eye?

A
  • block cholinergic stimulation of pupillary constrictor muscles, result in unopposed sympathetic dilation (mydriasis)
  • prevents contraction of ciliary muscle, results in loss of accommodation (cycloplegia)
  • decreases lacrimal secretions (dry eyes)
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24
Q

What is a contraindication of anticholinergic use and why?

A
  • glaucoma

- decreases outflow of aqueous humor

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25
Q

What clinical use do anticholinergics have?

A
  • mydriasis and cycloplegia are useful to ophthos to view retina
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26
Q

What are the effects of low dose antimuscarinics on the CV system?

A
  • blocks M1 receptors only: bradycardia

- because ACh still binds to M3 on sinus node that results in slowed HR

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27
Q

What are the effects of moderate to high doses of antimuscarinics on the CV system?

A
  • blocks M1 & M2: tachycardia 2ndary to blockade of vagal slowing
  • inhibiting the brakes on HR
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28
Q

What is a clinical use of moderate to high doses of antimuscarinics on the CV system?

A
  • tx bradycardia in ACLS

- atropine

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29
Q

What are the effects of toxic doses of antimuscarinics on the CV system?

A
  • intraventricular conduction block (cessation of HR)

- little effect on BP

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30
Q

What are the effects of anticholinergics on the respiratory system?

A
  • bronchodilation

- reduce/dry up secretions

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31
Q

What are the therapeutic uses and drugs of anticholinergics on the respiratory system?

A
  • asthma/COPD (ipatropium, titropium)

- prior to surgery or in vented patients (atropine, scopolamine)

32
Q

What are the effects of antimuscarinics on the GI tract?

A
  • decrease motility via decrease GI smooth M. contraction

- decrease salivary and GI secretions (xerostomia)

33
Q

What are the therapeutic uses of antimuscarinics on the GI tract?

A
  • tx: diarrhea (atropine, inotecan) via decrease GI secretions
34
Q

T/F: Antimuscarinics do not affect acid secretions in the stomach.

A
  • True
35
Q

T/F: Anticolinergic agents cannot cause significant constipation.

A
  • False
36
Q

What is the effect of antimuscarinics on the GU tract?

A
  • relaxation of bladder smooth muscle, leads to reduced voiding
37
Q

What group of patients can atnimuscarinics worsen urinary retention in?

A
  • men with BPH (benign prostatic hyperplasia)
38
Q

What are the clinical indications of antimuscarinics in treating urinary disorders?

A
  • tx: urinary spasms (oxybutinin, a selective M3 antagonist)
39
Q

What is an effective treatment for muscarinic toxicity?

A
  • atropine
40
Q

What is the treatment for rapid onset mushroom poisoning?

A
  • atropine
41
Q

What is the treatment for delayed onset mushroom poisoning?

A
  • supportive care

- atropine ineffective

42
Q

What is a treatment for hyperhidrosis?

A
  • anticholinergics
43
Q

T/F: anticholinergics are always effective on sweat glands.

A
  • False, different types of sweat glands

- eccrine > apocrine

44
Q

What are the adverse effects of anticholinergics?

A
  • dry mouth (dry as a bone)
  • mydriasis (blind as a bat)
  • tachycardia
  • hot, flushed skin (red as a beet)
  • agitation (mad as a hatter)
  • urinary retention (can’t pee)
  • visual changes (can’t see)
  • dry mouth (can’t spit)
  • constipation (can’t shit)
45
Q

What are the contraindications of anticholinergic use?

A
  • glaucoma
  • BPH
  • gastric ulcers (due to slowed gastric emptying)
46
Q

What happens during presynaptic inhibition of cholinergic actions?

A
  • presynaptic proteins block the release of ACh
47
Q

What is the result of presynaptic inhibition of cholinergic actions?

A
  • paralysis of skeletal m.
  • decreased activity at parasympathetic and sympathetic synapses
  • inhibition lasts weeks to months
48
Q

What are the drugs used for presynaptic inhibition of cholinergic actions?

A
  • Clostridum botulinum: onabotulinum, abobotulinum, rimabotulinum
49
Q

What is the MOA of ganglionic blocking agents?

A
  • block ACh and its agonists at nicotinic receptors of para and sympathetic ganglia
50
Q

What are ganglionic blocking agents also known as?

A
  • nondepolarizing competitive antagonists
51
Q

What is the overall result of ganglionic blocking agents?

A
  • blocking all autonomic outflow

- mixed sympathetic and para effects

52
Q

What are the effects of ganglionic blockers at the CNS?

A
  • sedation
  • tremor
  • choreiform (abnormal) movements
  • mental aberrations
53
Q

What are the effects of ganglionic blockers at the eye?

A
  • cycloplegia
  • loss of accommodation
  • moderate dilation of pupil
54
Q

What are the effects of ganglionic blockers at the CV system?

A
  • tachycardia
55
Q

What are the effects of ganglionic blockers at the GI tract?

A
  • decreased secretions

- decreased motility

56
Q

What is the major use of therapeutic ganglionic blockers?

A
  • pharmacological research
57
Q

What is the action of neuromuscular blockers?

A
  • block transmission b/t neuron and nicotinic receptor on skeletal m.
58
Q

What are the two groups of neuromuscular blockers?

A
  • nondepolarizing (antagonists)

- depolarizing (agonists)

59
Q

Describe the action of nondepolarizing neuromuscular blockers

A
  • block ACh from binding nicotinic receptors
  • competitive binding
  • prevents depolarization of muscle fibers and inhibits contraction
60
Q

What is the result of a nondepolarizing neuromuscular blockers?

A
  • very relaxed/paralyzed muscle
61
Q

What can terminate the action of nondepolarizing neuromuscular blockers?

A
  • AChE inhibitors (neostigmine)
62
Q

What is the clinical use of nondepolarizing neuromuscular blockers?

A
  • adjuncts to anesthesia to produce muscle paralysis/relaxation
63
Q

What are the groups of nondepolarizing neuromuscular blockers drugs?

A

suffixes:

  • curarine
  • curium
  • curonium
64
Q

How do the different nondepolarizing neuromuscular blockers drugs differ?

A
  • onset of action
  • 1/2 life
  • means of elimination
65
Q

Describe the action of depolarizing neuromuscular blockers

A
  • binds to nicotinic receptors on skeletal m. and acts like ACh
66
Q

What is the initial effect of depolarizing neuromuscular blockers?

A
  • facilitates muscle contraction
67
Q

What is the effect of prolonged depolarizing neuromuscular blockers?

A
  • muscle paralysis
68
Q

What is a drug used as a depolarizing neuromuscular blockers?

A
  • succinylcholine
69
Q

What are the clinical uses of depolarizing neuromuscular blockers?

A
  • facilitate intubation

- during electroconvulsive shock therapty

70
Q

Give some therapeutic uses of anticholinergics

A
  • diarrhea
  • bradycardia
  • asthma/COPD
71
Q

depolarizing or nondepolarizing neuromuscular blocker: tubocurarine

A
  • non
72
Q

depolarizing or nondepolarizing neuromuscular blocker: atracurium

A
  • non
73
Q

depolarizing or nondepolarizing neuromuscular blocker: succinylcholine

A
  • depolarizing
74
Q

depolarizing or nondepolarizing neuromuscular blocker: rocuronium

A
  • non
75
Q

depolarizing or nondepolarizing neuromuscular blocker: doxacurium

A
  • non
76
Q

depolarizing or nondepolarizing neuromuscular blocker: vecuronium

A
  • non

Pharmacology - Exam 2 (4 decks)

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