Anticholinesterase

Question 1

Name the anticholinesterase drug that is a tertiary amine:

Answer 1

Physostigmine

Question 2

Name the anticholinesterase drugs that are Quaternary ammonium:

Answer 2

• Edrophonium
• Neostigmine
• Pyridostigmine

Question 3

Anticholinesterase enzyme inhibition does:

Answer 3

• inhibit acetylcholinesterase

- Result in increased availability of acetylcoline.

Question 4

What happens when actylcholinesterase and Neostigmine/Pyridostigmine come together:

Answer 4

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

Question 5

What happens when actylcholinesterase and edrophonium come together:

Answer 5

Forms a reversible electrostatic attachment

Question 6

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

Answer 6

Presynaptic Effect

Question 7

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

Answer 7

Direct Effect

Question 8

_________ inhibition electrostatic attachment to the anionic site (Edrophonium)

Answer 8

Reversible

Question 9

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

Answer 9

Formation, Carbamyl, Esters

Question 10

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

Answer 10

Irreversible

Question 11

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

Answer 11

True

Question 12

What is the onset of action for edrophonium:

Answer 12

1-2 minutes

Question 13

What is the onset of action for neostigmine:

Answer 13

7-11 minutes

Question 14

What is the onset of action for pyridostigmine:

Answer 14

up to 16 minutes

Question 15

What is the duration for action of anticholinesterase drugs

Answer 15

All are the same (60-120 minutes)

Question 16

What kind of pharmacological effects will be seen with anticholinesterase:

Answer 16

• Bradycardia
• Salivation,
• Bronchoconstriction
• Miosis,
• Hyperperistalsis
• PONV

Question 17

What kind of pharmacological effects will be seen with nicotinic:

Answer 17

-Act at the neuromuscular junction and autonomic ganglia

Question 18

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

Answer 18

TRUE

Question 19

What clinical use does anticholinesterase drugs have:

Answer 19

-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

Question 20

Antagonist-assisted reversal of NMB:

Answer 20

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

Question 21

What is the dosage for Edrophonium:

Answer 21

0.5 mg/kg

Question 22

What is the dosage for neostigmine:

Answer 22

0.043 mg/kg

Question 23

What is the dosage for pyridostigmine:

Answer 23

0.21 mg/kg

Question 24

What does potency depend on for anticholinesterase drugs:

Answer 24

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

Question 25

Mixture with a anticholinergic and anticholinesterase will have what effect:

Answer 25

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

Question 26

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

Answer 26

True

Question 27

What must be seen before administration of anticholinesterase drug:

Answer 27

Twitch height has recovered to > 10 %

Question 28

What factors can/will influence reversal of neuromuscular blockade:

Answer 28

- Nondepolarizing neuromuscular blocking drug - Intensity of NMB - Antibiotic - hypothermia - respiratory acidosis (PaCO2 > 50%) - hypokalemia - metabolic acidosis

Question 29

What are some basic on Physostigmine:

Answer 29

- Tertiary amine that crosses the BBB | - Antagonizes adverse CNS effeccts of certain drugs

Question 30

What is the dose for Physostigmine:

Answer 30

0.015 to 0.06 mg/kg IV

Question 31

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

Answer 31

- Miosis and difficulty focusing - Salivation - Bronchoconstriction - Bradycardia - Abdominal cramps - Loss of bowel and bladder control

Question 32

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

Answer 32

Skeletal muscle weakness to paralysis and apnea

Question 33

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

Answer 33

- Confusion - Ataxia - Seizures - Coma - Depressed ventilation

Question 34

What would be organophsphate anticholinesterases:

Answer 34

- insecticides | - nerve agents

Question 35

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

Answer 35

True

Question 36

What is the reversal for anticholinesterase overdose:

Answer 36

- Atropine (Antimuscarinic effect) - Pralidoxime (Acetylchoinesterase reactivator) - Supportive measures