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Pharmacology II > Exam 1: Cholinergics > Flashcards

Exam 1: Cholinergics Flashcards

1
Q

What are the 2 basic classes of cholinergic agents?

A

cholinomimetics

anticholinergics

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2
Q

Cholinomimetics include which drug classes?

A

direct agonists

AChE inhibitors

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3
Q

Anticholinergics include which drug classes?

A

cholinergic antagonists

NMJ Blockers

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4
Q

This receptor is a ligand gated sodium channel that responds to acetylcholine and what other substance?

A

Nicotinic receptor

nicotine

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5
Q

A patient had an initial muscle twitch followed by a depolarizing blockade and paralysis. This occured after nicotine administration. What just happened?

A

desensitization

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6
Q

These receptors have the following characteristics:

GCPR
Located on PNS effectors
Resond to ACh

A

Muscarinic receptors

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7
Q

Stimulation of muscarinic receptors on the eye have what 3 effects?

A

miosis

blurred vision

decreased intraocular pressure

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8
Q

What is responsible for the miosis when eyes are stimulated by a muscarinic agonist?

A

contraction of the circular muscle

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9
Q

What is responsible for the blurred vision that occurs during stimulation by a muscarinic agonist?

A

contractin of the ciliary muscle leading to a round lens

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10
Q

Muscarinic agonists will have what effect on glands?

A

increased secretion

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11
Q

What happens to the GI system with muscarinic stimulation?

A

increased motility, secretion, peristalsis and relaxed sphincters

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12
Q

When a muscarinic agonist is administered, will the bladder favor physiologic conditions for filling or voiding?

A

voiding (i.e. detrusor contraction, sphincter relaxation)

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13
Q

What is responsible for the bradycardia induced by muscarinic stimulation?

A

slowing of the SA node

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14
Q

what effects should be expected on injection of ACh?

A

decreased HR and BP

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15
Q

What causes the decreased BP from ACh injection since the vessels generally don’t directly respond to PNS stimulation?

A

endothelial M3 release of NO

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16
Q

What happens in the respiratory system with muscarinic stimulation?

A

increased secretions

bronchoconstriction

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17
Q

Muscarinic agonists have what effects on the brain?

A

increased memory, cognition, alertness, arousal

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18
Q

What drug class has the following adverse effects?

N/V
bladder tightness
sweating
salivation
bronchoconstriction
constricted pupils
blurred vision
A

muscarinic agonists

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19
Q

What drugs are considered direct muscarinic agonists?

A

ACh, bethanechol, pilocarpine

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20
Q

What conditions are contraindicated for muscarinic agonists?

A

Asthma/COPD
Peptic Ulcer
Bowel Obstruction
CAD/Heart Disease

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21
Q

SLUDGE is an acronym that describes muscarinic agonist toxicity. what does it stand for?

A 
salivation
lacrimation
urination
defecation
GI distress
Emesis
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22
Q

In addition to SLUDGE, what adverse effects can be seen in muscarinic agonist toxicity?

A 
HA
visual disturbance
bronchospasm
bradycardia
shock
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23
Q

describe the half life and clinical use of acetylcholine

A

no clinical use due to short half life

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24
Q

What two major effects will be seen on acetylcholine administration?

A

decreased BP, decreased HR

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25
Q

these two drugs are nonspecific muscarinic agonists

A

bethanechol and pilocarpine

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26
Q

What therapeutic effects does bethanechol have?

A

increased GI motility

decreased urinary retention

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27
Q

Can bethanechol cross the BBB?

A

no

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28
Q

Why doesn’t bethanechol have CNS activity?

A

quaternary ammonium salt, charged

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29
Q

which ammonium salts can cross the BBB?

A

tertiary ammonium salts

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30
Q

Pilocarpine is used as a drug of last resort for which condition?

A

acute angle closure glaucoma

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31
Q

Pilocarpine is useful for treating what conditions via what routes?

A

topical for glaucoma

PO for xerostomia

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32
Q

What is an adverse effect for pilocarpine when administered PO?

A

profuse sweating

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33
Q

What is an adverse effect for pilocarpine when administered topically in the eye?

A

blurred vision

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34
Q

Nicotine causes IPSPs/EPSPs

A

EPSPs

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35
Q

The central effects of low doses of nicotine include…

A

increased alertness and attention

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36
Q

What are the effects on the central body with high dose nicotine?

A

tremor, vomiting, tachypnea

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37
Q

What cardiac sxs can occur with nicotine poisoning?

A

HTN, tachycardia with alternating vagal bradycardia

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38
Q

What are the GI/GU side effects of nicotine?

A

vomiting, diarrhea, urination

39
Q

at the NMJ, overdose of nicotine can have what effects?

A

convulsions leading to receptor desensitization and flaccid paralysis

40
Q

How do you treat nicotine toxicity?

A

anticonvulsants and assisted respiration

41
Q

This drug is a partial nicotinic receptor agonist that stimulates dopamine release, and stimulates the reward center.

A

Varenicline

42
Q

What therapeutic effect does varenicline have?

A

Tx for smoking cessation

43
Q

Describe the adverse effects of varenicline…

A

N/V, constipation, flatulence

nightmares, psychosis, suicidal ideation

44
Q

What six drugs are considered cholinesterase inhibitors?

A

neostigmine, pyridostigmine, physostigmine, edrophonium, donepezil, organophosphates

45
Q

What is the common suffix for AChE inhibitors, and what are two exceptions?

A

“stigmine” suffix

edrophonium, donepezil exceptions

46
Q

What is the general mechanism of cholinesterase inhibitors?

A

inhibit ACh breadown leading to increased time in the cleft and increased receptor activation

47
Q

Are AChE inhibitors depolarizing or non-depolarizing blockers?

A

non-depolarizing

48
Q

Muscle Twitch and Fasciculation

NMJ Blockade

Paralysis

These are signs of poisoning via high-dose _____

A

cholinesterase inhibitors

49
Q

What are three clinical uses for low dose cholinesterase inhibitors?

A

Tx of Myasthenia Gravis

Reverse NMJ Blockade

Nicontine antagonism

50
Q

What are three severe, serious side effects of cholinesterase overdose/toxicity?

A

SLUDGE sxs

Respiratory Arrest

Death

51
Q

These Cholinesterase inhibitors have the following indications…

Tx of ileus

Tx of bladder atony

Tx of Myasthenia

Overcome Post-op NMJ Block

A

Neostigmine & Pyridostigmine

52
Q

Which cholinesterase inhibitors form covalent bonds with AChE?

A

Neostigmine and pyridostigmine

53
Q

Do Neostigmine and pyridostigmine cross the BBB? why or why not?

A

no… quaternary ammonium compound

54
Q

Neostigmine and Pyridostigmine dosing needs to be titrated. What happens if the dose is too high?

A

receptor desensitization, patient weakness

55
Q

Which Cholinesterase Inhibitor is a tertiary ammonium compound and can therefor cross the BBB?

A

Physostigmine, Donepizil

56
Q

What is physostigmine used for?

A

treat atropine (m antagonist) poisoning

57
Q

Edrophonium is useful for what two processes

A

diagnosis and dose determination for myasthenia

58
Q

Donepizil is useful in treating what?

A

alzheimers

59
Q

How do you treat organophosphate poisoning?

A

atropine, +/- 2-PAM, diazepime, ABCs

60
Q

In OP poisoning, describe the dosing regime for atropine

A

titrate atropine until pupils dilate

only use if known OP poisoning

61
Q

When can 2-PAM be administered with OP poisoning?

A

if < 3-4 hours of exposure

62
Q

Why can you only use atropine if confirmed OP poisoning?

A

atropine is an AChE inhibitor itself, but is more attracted to OP

63
Q

Describe the “aging”process of OP and AChE

A

occurs within 4 hours

covalent phosphorylation that breaks O-P bond from drug to make AChE bond irreversible

64
Q

The following are SFx of what drug class?

Dry mouth

Dry eyes
Midriasis
Cycloplegia
Tachycardia

Reduced GI motility
Urinary Retention

A

Cholinergic antagonists

65
Q

Rank PNS tone/antimuscarinic affinity of the following tissue types

salivary/sweat/bronchioles

heart/eye

GI/GU

CNS

A

Salivary, Sweat, Bronchioles > Heart, Eye > GI/GU > CNS

66
Q

Rank the following tissue types from most-sensitive to least-sensitive to cholinergic antagonists…

salivary/sweat/bronchioles

heart/eye

GI/GU

CNS

A

Salivary, Sweat, Bronchioles > Heart, Eye > GI/GU > CNS

67
Q

What mnemonic is helpful for remembering the adverse effects of atropine?

A

“hot as a hare, dry as a bone, blind as a bat, red as a beat, mad as a hatter”

68
Q

In the eye, atropine has what three effects?

A

mydriasis
cycloplegia
increased IOP

69
Q

In the CV system, atropine has what effects, particularly on what patient population?

A

healthy young adults

increased vagal tone
Tachygardia

70
Q

Atropine has what three effects on the glads?

A

xerostomia
dry eyes
increased skin temperature

71
Q

What effect does atropine have on the lungs?

A

bronchodilation

72
Q

What effect does atropine have on GI/GU?

A

GI: decreased motility and secretion

GU: decreased motility/activity

73
Q

What adverse effects of atropine occur in the CV system?

A

tachycardia

cardiopulm collapse

74
Q

In the heart, where does atropine exert its effects?

A

the atria

75
Q

What are the mechanisms by which atropine can increase HR?

A

Block post-synaptic M2 receptors, decrease PNS, increase HR

Block pre-synaptic SNS M2 receptors, increased NE, increased Beta 1 stimulation, increased HR

76
Q

Atropine exerts what therapeutic effects on the heart?

A

tx for bradycardia

tx for heart block

post-MI therapy

77
Q

Which cholinergic antagonist is used to dilate the eyes for eye exam?

A

topicamide

78
Q

This cholinergic antagonist is delivered transdermally to treat motion sickness…

A

scopalamine

79
Q

Which cholinergic antaagonist acts as a bronchodilator, and therefor is useful in treating COPD and Acute Asthma Attack?

A

ipratropium

80
Q

how is ipratropium administered?

A

inhalation

81
Q

Which four cholinergic antagonists are M3 selective, and what are they used to treat?

A

Tolderodine, Fesoterodine, Darifenacin, Solifenacin

Tx of overactive bladder

82
Q

This drug is a cholinergic antagonist that is useful in treating bladder spasm…

A

oxybutynin

83
Q

Which cholinergic antagonist decreases GI spasm/cramping making it a tx for diarrhea predominant IBS?

A

dicycloamine

84
Q

What is an adverse effect of onabotulinumtoxinA?

A

asthenia

85
Q

What are three indications for IM injection of onabotulinumtoxin A?

A

urinary incontinence

migraine prophylaxis

wrinkles

86
Q

______ blocks the release of ACh to the synaptic cleft,

A

botox

87
Q

This drug causes a depolarization, which causes initial contraction, then receptor desensitization and NMJ block…

A

succinylcholine

88
Q

Which NMJ blocker is useful as a paralytic for short surgical procedures and ET intubation?

A

succinylcholine

89
Q

What are the two major adverse effects of succinylcholine?

A

cardiac arrest secondary to hyperkalemia in burn patients

malignant hyperthermia

90
Q

how do you treat malignant hyperthermia?

A

dantrolene

91
Q

What are the 3 contraindications of succinylcholine?

A

burns

hx of malignant hyperthermia

soft tissue damage

92
Q

Rank the order of effects felt by non-depolarizing NMJ blockers…

A

small muscles > large muscles > diaphragm

93
Q

If strength improves after edrophomium administration, what do you need to do to the daily dose of neostigmine/pyridostigmine?

A

increase it

94
Q

If strength is worsened with edrophonium administration, what do you need to do to the daily dose of neostigmine/pyridostigmine and why?

A

decrease it, causing desensitization

Pharmacology II (23 decks)

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