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(J2) Pharm > Cholinesterase Inhibitors (indirect acting cholinergics) > Flashcards

Cholinesterase Inhibitors (indirect acting cholinergics) Flashcards

1
Q

What is a common suffix for cholinesterase inhibitors?

A

“-stigmine”

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2
Q

What are the effects of AChE inhibitors?

A

CNS (if able to cross BBB):

-CNS stimulation (possible convulsions and respiratory arrest)

Eye:

-miosis

Lung:

-bronchoconstriction

GI (and salivary glands):

-increased motility and secretion

GU:

-facilitates urination

Heart:

-bradycardia and increased blood pressure

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3
Q

What is neostigmine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

quaternary/charged, unable to cross BBB

*Myasthenia gravis

*reverse non-depolarizing neuromuscular blockade

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4
Q

What is pyridostigmine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

quaternary/charged; unable to cross BBB

*myasthenia gravis

*reverse non-depolarizing neuromuscular blockade

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5
Q

What is edrophonium?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

quaternary/charged, unable to cross BBB

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6
Q

What is physostigmine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

tertiary/uncharged, able to cross BBB

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7
Q

What is galantamine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

tertiary/uncharged, able to cross BBB

*dementia

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8
Q

What is rivastigmine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

tertiary/uncharged, able to cross BBB

*dementia

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9
Q

What is donepezil?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE inhibitor

tertiary/uncharged, able to cross BBB

*dementia

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10
Q

What AChE inhibitors are quarternary amines and therefore unable to cross the BBB due to charge?

A
  • neostigmine
  • pyridostigmine
  • edrophonium
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11
Q

What AChE inhibitors are tertiary amines and therefore able to cross the BBB due to charge?

A
  • physostigmine
  • donepezil
  • rivastigmine
  • galantamine
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12
Q

What are organophosphates?

Which receptors it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

IRREVERSIBLE AChE inhibitor

frequently have “-thio-“ in the name

able to cross BBB

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13
Q

What are the side effects of AChE inhibitor toxicity?

A

BM SLUDGE (from muscarinic effect) + CNS effects and flaccid paralysis (from nicotinic effects)

  • bronchoconstriction
  • miosis
  • salivation
  • lacrimation
  • urination
  • diarrhea
  • GI pain
  • emesis
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14
Q

What AChE inhibitors would be most effective treating myasthenia gravis?

A
  • neostigmine
  • edrophonium
  • pyridostigmine

*all unable to cross BBB and act at the neuromuscular junction

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15
Q

What AChE inhibitors would be most effective treating demetia/Alzheimer’s?

A
  • donepizil
  • rivastigmine
  • galantimine
  • physostigmine

*all able to cross BBB and effect CNS

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16
Q

What AChE inhibitors would be most effective reversing pharmacologic paralysis?

A
  • neostigmine
  • edrophonium

*all unable to cross BBB and act at the neuromuscular junction

17
Q

What AChE inhibitors would be most effective treating anticholinergic toxicity?

A

-physotigmine

*able to cross BBB and treat central effect

*unable to

18
Q

What is pralidoxime?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

AChE regnerator

*removes covalently bound organophosphates from AChE, restoring function

Unable to cross BBB, only treats peripheral effects

19
Q

What drugs would be most effective reversing organophosphate toxicity?

A
  • pralidoximine (PNS effects, restoring AChE)
  • atropine (CNS/PNS effects, mAChR antagonist)
  • benzodiazepine (anticonvulsant)
20
Q

What interactions occur with AChE inhibitors and nondepolarizing neuromuscular blocking agents?

A

diminishes blockade

21
Q

What interactions occur with AChE inhibitors and succinylcholine?

A
  • enhances phase 1 block
  • antagonizes phase 2 block
22
Q

What interactions occur with AChE inhibitors and direct acting cholinergics?

A

enhanced cholinergic effects

23
Q

What interactions occur with AChE inhibitors and beta-blockers?

A

enhanced bradycardia

24
Q

What interactions occur with AChE inhibitors and corticosteroids?

A

enhance muscle weakness in myasthenia gravis

(J2) Pharm (9 decks)

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