Autonomic Parasympathetic Drugs: Acetylcholinesterase Inhibitors Flashcards

1
Q

Indirect cholinomimetics inhibit

A

acetylcholinesterase

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2
Q

Acetylcholinesterase degrades

A

acetylcholine (ACh)

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3
Q

Acetylcholinesterase inhibitors increase

A

synaptic concentrations of ACh

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4
Q

drug suffix of acetylcholinesterase inhibitors

A

“-stigmine”

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5
Q

Acetylcholinesterase inhibitors enhance effects of

A

ACh at the NMJ (increase activity of NICOTINIC ACh receptors)

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6
Q

Myasthenia gravis (MG)

A

myasthenia gravis (MG) → antibodies against nicotinic ACh receptors at motor endplate (skeletal muscle NMJ)

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7
Q

Myasthenia gravis (MG) causes

A

progressive proximal weakness, ptosis, diplopia (inactivated nicotinic ACh receptors at motor endplate)

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8
Q

Pyridostigmine

A

acetylcholinesterase inhibitor used as long-term treatment for MG

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9
Q

Acetylcholinesterase inhibitors for the treatment of Myasthenia Gravis

A

acetylcholinesterase inhibitors increase ACh at NMJ endplate to outcompete MG antibodies

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10
Q

Neostigmine

A

acetylcholinesterase inhibitor used as treatment for MG

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11
Q

Edrophonium

A

acetylcholinesterase inhibitor that transiently reverses symptoms of MG

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12
Q

Pyridostigmine, Neostigmine and Edrophonium are

A

quaternary amines and do not penetrate the CNS

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13
Q

Edrophonium REVERSES

A

edrophonium REVERSES muscle weakness in undertreated MG patients (POSITIVE tensilon test)

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14
Q

Tensilon test

A

Tensilon test → edrophonium reverses (positive) or fails to reverse (negative) muscle weakness

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15
Q

Edrophonium FAILS to reverse muscle weakness during

A

edrophonium FAILS to reverse muscle weakness during cholinergic crisis (NEGATIVE tensilon test)

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16
Q

Nondepolarizing neuromuscular blocking agents (e.g. tubocurarine, pancuronium, cisatracurium) inhibit

A

nicotinic ACh receptors at NMJ endplate

17
Q

Nondepolarizing neuromuscular blocking agents include

A
  1. Tubocruraine
  2. Pancuronium
  3. Cisatracurium
18
Q

Acetylcholinesterase inhibitors (e.g neostigmine) reverse

A

nondepolarizing neuromuscular blockade

19
Q

Succinylcholine is a

A

depolarizing neuromuscular blocking agent (nicotinic ACh receptor AGONIST)

20
Q

Initial PHASE-1 of depolarizing blockade is

A

initial PHASE-1 of depolarizing blockade is IRREVERSIBLE (acetylcholinesterase inhibitors potentiate blockade)

21
Q

Acetylcholinesterase inhibitors can be used to treat

A

urinary retention (muscarinic activation)

22
Q

Physostigmine is an

A

acetylcholinesterase inhibitor with CENTRAL effects

23
Q

Atropine overdose

A

atropine overdose → “mad as a hatter, hot as a hare, blind as a bat” (reversed by physostigmine)

24
Q

Atropine overdose is revered by

A

physostigmine

25
Q

______ is a naturally occurring form of atropine

A
  1. Belladonna flower

2. Jimson weed

26
Q

Physostigmine reverses

A

atropine overdose (peripheral and CENTRAL effects)

27
Q

Physostigmine (and organophosphates) enters CNS to

A

cause central cholinergic effects

28
Q

Acetylcholinesterase inhibitor toxicity

A

Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Lacrimation, Salivation

29
Q

Acetylcholinesterase inhibitor toxicity includes

A

flaccid paralysis (NMJ nicotinic ACh receptor over-activation)

30
Q

Insecticides

A

insecticides (parathion, malathion, echothiophate) are organophosphates, a type of acetylcholinesterase inhibitor (also includes nerve agents and herbicides)

31
Q

Organophosphates are a major cause of

A

acute cholinergic toxicity (DUMBBELS)

32
Q

Pralidoxime reverses

A

organophosphate toxicity (DUMBBELS)

33
Q

Pralidoxime

A

pralidoxime regenerates acetylcholinesterase at muscarinic and NICOTINIC receptors (reverses cholinergic toxicity INCLUDING FLACCID PARALYSIS)

34
Q

Atropine reverses

A

atropine reverses both peripheral and CENTRAL muscarinic toxicity from organophosphate poisoning (pralidoxime is peripheral only)

35
Q

“Aging” of the organophosphate-cholinesterase complex leads to

A

irreversible binding

36
Q

______ is ineffective once aging of organophosphate- cholinesterase complex has occurred

A

pralidoxime

37
Q

________ is a acetylcholinesterase inhibitor used to treat Alzheimer’s disease

A
  1. Galantamine
  2. Rivastigmine
  3. Donepezil
38
Q

Galantamine, Rivastigmine, and Donepezil penetrate the

A

CNS