Anticholinesterase Flashcards

1
Q

Name the anticholinesterase drug that is a tertiary amine:

A

Physostigmine

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2
Q

Name the anticholinesterase drugs that are Quaternary ammonium:

A
  • Edrophonium
  • Neostigmine
  • Pyridostigmine
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3
Q

Anticholinesterase enzyme inhibition does:

A
  • inhibit acetylcholinesterase

- Result in increased availability of acetylcoline.

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4
Q

What happens when actylcholinesterase and Neostigmine/Pyridostigmine come together:

A
  • Hydrolyzed by acetylcholinesterase
  • Carbamylates the enzyme in the process
  • Block enzyme’s ability to hydrolyze Ach
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5
Q

What happens when actylcholinesterase and edrophonium come together:

A

Forms a reversible electrostatic attachment

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6
Q

The absence of neuromuscular blockers, acetylcholinesterase inhibitors may produce fasiculations: (What is this called)

A

Presynaptic Effect

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7
Q

At doses greater than usual clinical doses, anticholinesterase drugs have been reported to produce some form of neuromuscular blockade: (What is this called)

A

Direct Effect

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8
Q

_________ inhibition electrostatic attachment to the anionic site (Edrophonium)

A

Reversible

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9
Q

_________ of _______ _______ are reversible formation of carbamyl ester complexes at the esteratic site (Neostigmine, pyridostigmine, physostigmine)

A

Formation, Carbamyl, Esters

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10
Q

___________ inhibition is when Organophosphates combine with the esteratic site to form a stable inactive complex

A

Irreversible

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11
Q

T/F: Anticholinesterase drugs have no significant differences in patients with normal renal function.

A

True

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12
Q

What is the onset of action for edrophonium:

A

1-2 minutes

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13
Q

What is the onset of action for neostigmine:

A

7-11 minutes

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14
Q

What is the onset of action for pyridostigmine:

A

up to 16 minutes

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15
Q

What is the duration for action of anticholinesterase drugs

A

All are the same (60-120 minutes)

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16
Q

What kind of pharmacological effects will be seen with anticholinesterase:

A
  • Bradycardia
  • Salivation,
  • Bronchoconstriction
  • Miosis,
  • Hyperperistalsis
  • PONV
17
Q

What kind of pharmacological effects will be seen with nicotinic:

A

-Act at the neuromuscular junction and autonomic ganglia

18
Q

T/F: Neostigmine and pyridostigmine, but not edrophonium, produce marked and prolonged inhibition of plasma cholinesterase.

A

TRUE

19
Q

What clinical use does anticholinesterase drugs have:

A

-Reversal of neuromuscular (antagonist)
-Treatment of mysthenia gravis
(Increases ACh at the neuromuscular junction)
-Treatment of glaucome (cause miosis)
-post op analgesia
-post op shivering

20
Q

Antagonist-assisted reversal of NMB:

A
  • Increase the availability of ACh at the NMJ
  • Acts presynaptic and postsynaptic
  • Administered during the time of spontaneous recovery from NMB
21
Q

What is the dosage for Edrophonium:

A

0.5 mg/kg

22
Q

What is the dosage for neostigmine:

A

0.043 mg/kg

23
Q

What is the dosage for pyridostigmine:

A

0.21 mg/kg

24
Q

What does potency depend on for anticholinesterase drugs:

A
  • NMB being antagonized
  • Speed of spontaneous recovery
  • Depth of NMB when the reversal is initiated
  • End point selected
25
Q

Mixture with a anticholinergic and anticholinesterase will have what effect:

A
  • Reversal requires only nicotinic effects
  • Muscarinic effects blocked with an anticholinergic drug
  • Administer anticholinergic with a faster onset than anticholinesterase to minimize bradycardia
26
Q

T/F: Once acetylcholinesterase is maximally inhibited, additional anticholinesterase does not further antagonize the neuromuscular blockade.

A

True

27
Q

What must be seen before administration of anticholinesterase drug:

A

Twitch height has recovered to > 10 %

28
Q

What factors can/will influence reversal of neuromuscular blockade:

A
  • Nondepolarizing neuromuscular blocking drug
  • Intensity of NMB
  • Antibiotic
  • hypothermia
  • respiratory acidosis (PaCO2 > 50%)
  • hypokalemia
  • metabolic acidosis
29
Q

What are some basic on Physostigmine:

A
  • Tertiary amine that crosses the BBB

- Antagonizes adverse CNS effeccts of certain drugs

30
Q

What is the dose for Physostigmine:

A

0.015 to 0.06 mg/kg IV

31
Q

Acute overdose of physostigmine will have what type of effects on muscarinic:

A
  • Miosis and difficulty focusing
  • Salivation
  • Bronchoconstriction
  • Bradycardia
  • Abdominal cramps
  • Loss of bowel and bladder control
32
Q

Acute overdose of physostigmine will have what type of effects on nicotinic:

A

Skeletal muscle weakness to paralysis and apnea

33
Q

What type of CNS effects will be seen with physostigmine acute overdoes:

A
  • Confusion
  • Ataxia
  • Seizures
  • Coma
  • Depressed ventilation
34
Q

What would be organophsphate anticholinesterases:

A
  • insecticides

- nerve agents

35
Q

T/F: Organophosphates are lipid soluble and can cross the BBB.

A

True

36
Q

What is the reversal for anticholinesterase overdose:

A
  • Atropine (Antimuscarinic effect)
  • Pralidoxime (Acetylchoinesterase reactivator)
  • Supportive measures