Anticholinesterases

Question 0

NEOSTIGMINE

Answer 0

Reversible AChE inhibitor
Carbamate (competitive substrate)

Used for Paralytic loss of tone bladder or GI tract
Standard for myasthenia gravis
Short duration if action (0.5-2 hrs)

Question 1

PHYSOSTIGMINE

Answer 1

Reversible AChE inhibitor
Carbamate

Tx for Wide angle glaucoma
Can enter CNS and reverse effects of atropine and other anti muscarinic drugs

Adverse: can facilitate cataract formation, dec. night vision

Question 2

PYRIDOSTIGMINE

Answer 2

Reversible AChE inhibitor
Long acting: 3-6hrs

Choice for myasthenia gravis
Nerve gas prophylactic

Question 3

EDROPHONIUM

Answer 3

Reversible AChE Inhibitor
Simple competitive at anionic site

Test for myasthenia gravis
Brief duration of action (1-5 mins)

Question 4

DONEPEZIL

Answer 4

Reversible AChE Inhibitor

First choice for Alzheimer’s

Question 5

Rivastigmine

Answer 5

Reversible AChE inhibitor

Alzheimer’s

Question 6

Galantamine

Answer 6

Weak AChE inhibitor
nAChR enhancer

Alzheimer’s

Question 7

ECHOTHIOPHATE

Answer 7

Organophosphate AChE Inhibitor
Irreversible; covalent attachment, can undergo “aging”

Used in Glaucoma

Question 8

Malathion

Parathion

Answer 8

Organophosphate AChE inhibitor
Pro-drugs

Insecticides often involved in farm poisonings

Malathion undergoes detox in mammals via plasma esterases
Parathion responsible for most poisoning ad death cases

Question 9

Cholinergic toxidrome

Answer 9

SLUDGE-BAM

Salivation/Sweating
Lacrimation
Urination
Defecation
GI upset
Emesis

Bradycardia/Bronchoconstriction/BM
Abdominal cramps/Anorexia
Miosis

Question 10

Death from cholinesterase inhibitor poisoning usually due to…

Answer 10

Respiratory failure

Bronchoconstriction, bronchochorrhea, central respiratory depression,weakness of paralysis of resp muscles

Question 11

Treatment for toxicity of cholinesterase inhibitors

Answer 11

Atropine
Praladoxime

Supportive measures for respiratory distress
Diazepam to prevent or alleviate convulsions