Autonomics: Acetylcholinesterase Inhibitors Flashcards

1
Q

What are Indirect Cholinomimetics?

A

They upregulate the actions of acetylcholine “indirectly”, for example by inhibiting acetylcholinesterase.

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2
Q

What is the effect of acetylcholinesterase inhibitors?

A

They degrade acetylcholinesterase, thus increasing synaptic concentrations of Ach

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3
Q

What is the common suffix for Ach inhibitors?

A

“-stigmine”

the stigma graffiti

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4
Q

What does acetylcholinesterase normally affect?

A

It inhibits effects of Ach at the NMJ, increased activity of nictoinic ach receptors, leading to increased strength of contractions

(noted by the skeletal muscle brick wall)

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5
Q

What is Myasthenia Gravis?

A

caused by antibodies against nicotinic Ach receptors at the motor end plate

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6
Q

What are the effects of MG?

A

Progressive muscle weakness, ptosis, diplopia, caused by inactivated nicotinic receptors at motor end plate

(graffiti covering motor end plate outlets)

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7
Q

What drug is used as a long term treatment for MG?

A

Pyridostigmine

community PRIDE girl

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8
Q

What is the goal of treatment for MG?

A

Give Ach inhibitors in order to increase Ach at NMJ endplate to outcompete MG antibodies

(removing MG graffiti on end plates)

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9
Q

Aside from pyridostigmine, what is another MG treatment?

A

Neostigmine

neon STIGMA sign

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10
Q

What is the MOA of edrophonium?

A

Acetylcholinesterase inhibitor that transiently reverses symptoms of MG

(phone booth)

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11
Q

Why do the MG drugs not penetrate the CNS? what is the result?

A

They are quaternary amines, and thus do not penetrate into the CNS. The result is that they only relieve symptoms for 5-15 minutes

(“quarters only” in the telephone booth)

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12
Q

Describe the Tensilon Test

A

Edrophonium reverses muscle weakness in undertreated MG patients. If it fails to reverse muscle weakness, MG not the issue (probably cholinergic crisis)

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13
Q

What is the MOA of Curare?

A

A non-depolarizing neuromuscular blocking agent that inhibits nictonic Ach receptors at the NMJ endplate

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14
Q

What is the role of neostigmine post-op?

A

Acetylcholinesterase inhibitors such as neostigmine/edrophonium can be used to reverse the effects of curare-like compounds in anesthesia.

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15
Q

What is the MOA of Succinlycholine?

A

It is a depolarizing neuromuscular blocking agent that overstimulates the NMJ, causing muscles to remain depolarized and unable to respond to stimulus

(dude unable to clean the SUCKS graffiti)

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16
Q

Which Ach inhibitor has central effects?

A

Physostigmine - tertiary amine

phys ed center

17
Q

What are some CNS effects of Atropine?

A

Mad as a hatter, Hot as a hare, Blind as a bat

Atropine in Wonderland

18
Q

What is physostigmine used for?

A

Atropine overdose, nightshade poisoning, jimson weed poisoning

19
Q

What does DUMBBELS stand for?

A
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Lacrimation
Salivation
Sweating
20
Q

What is seen in Ach inhibitor toxicity?

A

Flaccid Paralysis

weak nicotine kid

21
Q

What are organophosphates?

A

The -thiols. Insecticides are organophosphates, a type of acetylcholinesterase inhibitor

22
Q

What is used to reverse organophosphate toxicity?

A

Pralidoxime

Reverses organophosphate toxicity by hydrolyzing the covalent bond

(closing LID on toxic waste)

23
Q

What is the MOA of pralidoxime?

A

Regenerates acetylcholinesterase at muscarinic and nictonic receptors

(brand new toxic waste dumpster)

24
Q

What is the difference between Atropine and Pralidoxime when used for organophosphate poisioning?

A

Atropine reverses both peripheral and central muscarinic toxicity, whereas pralidoxime is peripheral only

25
Q

What is the effect of aging on the organophosphate-cholinesterase complex?

A

Irreversible Binding - Pralidoxime is ineffective at this point

(old pest control man next to a corroded dumpster)

26
Q

What are the three acetylcholinesterase inhibitors used to treat Alzheimer’s Disease?

A

Galantamine, Rivastigmine, Donepezil

alzheimer’s GALA, “reverse the stigma”, done with puzzle

27
Q

What is the significance of the brain puzzle the two oldies are completing?

A

The three Alzheimer’s drugs penetrate the CNS