Autonomics: Acetylcholinesterase Inhibitors

Question 1

What are Indirect Cholinomimetics?

Answer 1

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

Question 2

What is the effect of acetylcholinesterase inhibitors?

Answer 2

They degrade acetylcholinesterase, thus increasing synaptic concentrations of Ach

Question 3

What is the common suffix for Ach inhibitors?

Answer 3

“-stigmine”

the stigma graffiti

Question 4

What does acetylcholinesterase normally affect?

Answer 4

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)

Question 5

What is Myasthenia Gravis?

Answer 5

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

Question 6

What are the effects of MG?

Answer 6

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

(graffiti covering motor end plate outlets)

Question 7

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

Answer 7

Pyridostigmine

community PRIDE girl

Question 8

What is the goal of treatment for MG?

Answer 8

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

(removing MG graffiti on end plates)

Question 9

Aside from pyridostigmine, what is another MG treatment?

Answer 9

Neostigmine

neon STIGMA sign

Question 10

What is the MOA of edrophonium?

Answer 10

Acetylcholinesterase inhibitor that transiently reverses symptoms of MG

(phone booth)

Question 11

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

Answer 11

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)

Question 12

Describe the Tensilon Test

Answer 12

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

Question 13

What is the MOA of Curare?

Answer 13

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

Question 14

What is the role of neostigmine post-op?

Answer 14

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

Question 15

What is the MOA of Succinlycholine?

Answer 15

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)

Question 16

Which Ach inhibitor has central effects?

Answer 16

Physostigmine - tertiary amine

phys ed center

Question 17

What are some CNS effects of Atropine?

Answer 17

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

Atropine in Wonderland

Question 18

What is physostigmine used for?

Answer 18

Atropine overdose, nightshade poisoning, jimson weed poisoning

Question 19

What does DUMBBELS stand for?

Answer 19

Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Lacrimation
Salivation
Sweating

Question 20

What is seen in Ach inhibitor toxicity?

Answer 20

Flaccid Paralysis

weak nicotine kid

Question 21

What are organophosphates?

Answer 21

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

Question 22

What is used to reverse organophosphate toxicity?

Answer 22

Pralidoxime

Reverses organophosphate toxicity by hydrolyzing the covalent bond

(closing LID on toxic waste)

Question 23

What is the MOA of pralidoxime?

Answer 23

Regenerates acetylcholinesterase at muscarinic and nictonic receptors

(brand new toxic waste dumpster)

Question 24

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

Answer 24

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

Question 25

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

Answer 25

Irreversible Binding - Pralidoxime is ineffective at this point

(old pest control man next to a corroded dumpster)

Question 26

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

Answer 26

Galantamine, Rivastigmine, Donepezil

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

Question 27

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

Answer 27

The three Alzheimer’s drugs penetrate the CNS