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UNMC PA Pharmacology > Anticholinesterases > Flashcards

Anticholinesterases Flashcards

1
Q

MOA of anticholinesterases

A

Blocks hydrolytic inactivation of ACh in synapse to enhance and prolong stimulation of cholinergic receptors

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2
Q

Anticholinesterase sites of action

A

ANS- muscarinic, nicotinic, and NMJ nicotinic receptors
CNS- cholinergic neurons (especially for cognition)

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3
Q

Anticholinesterases cause _____ paralysis

A

Flaccid

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4
Q

Reversible (non-covalent) anticholinesterase

A

Donepezil

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5
Q

Donepezil can/can’t cross BBB

A

Can

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6
Q

Donepezil clinical use

A

Treatment of Alzheimer’s

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7
Q

Donepezil Alzheimer’s MOA

A

Deficiency of cerebral ACh counteracted by central inhibition of ACh degradation
Doesn’t affect disease progression

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8
Q

Donepezil adverse effects

A

Diarrhea
N/V
Bradycardia

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9
Q

Prototype reversible covalent anticholinesterase

A

Neostigmine

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10
Q

Low (therapeutic) doses of neostigmine increase/decrease contractile force

A

Increase

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11
Q

High (toxic) doses of neostigmine increase/decrease contractile force

A

Decrease (N receptor desensitization)

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12
Q

Neostigmine MOA

A

Direct agonist at Nm receptors; induce muscle contraction without ACh release

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13
Q

Duration of neostigmine action

A

2 hours

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14
Q

Circulating neostigmine is cleared by ____

A

Butylcholinesterase

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15
Q

Neostigmine does/doesn’t cross the BBB

A

Doesn’t

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16
Q

Clinical uses of neostigmine

A

Reverses effect of competitive neuromuscular blockers (paralyzing drugs) after surgery
Myasthenia gravis

17
Q

How does neostigmine help with myasthenia gravis?

A

Increases response of myasthenic muscle to repetitive somatic nerve impulses (auto-antibodies destroy Nm receptors)

18
Q

Adverse effects of neostigmine

A

Excess muscarinic stimulation
Paralysis of diaphragm at toxic doses

19
Q

What drug fixes excessive muscarinic stimulation?

A

Atropine

20
Q

Physostigmine is the antidote for _____ poisoning

A

Atropine

21
Q

Difference between physostigmine and neostigmine

A

Physostigmine can cross the BBB

22
Q

Malathion is commonly used as an _____

A

Insecticide

23
Q

Malathion has a very long/short duration of action

A

Long (>50 hours)

24
Q

Malathion is a _____ that is converted to its highly toxic metabolite

A

Prodrug

25
Q

Clinical use of malathion

A

Topical lotion for head lice

26
Q

Diagnostic test for anticholinesterase poisoning

A

Decreased plasma cholinesterase (butylcholinesterase) activity

27
Q

Symptoms of anticholinesterase poisoning (cholinergic crisis)

A

Muscarinic: sweating, salivation, mitosis, bronchospasm, involuntary urination and defecation
Nicotinic: muscle weakness
CNS: confusion, ataxia, coma, respiratory depression

28
Q

Antidotes of anticholinesterase poisoning

A

Atropine
Pralidoxime

29
Q

Proalidoxime reactivates AChE only at the ___

A

NMJ

UNMC PA Pharmacology (23 decks)

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