indirect cholinomimetics/acetylcholinesterase inhibitors/anticholinesterases

epdrophonium

• diagnosis of myasthensia gravis

• shortest acting (onset 10-30 sec; duration 10 mins)

• quaternary amine

pyridostigmine

• treatment of myasthenia gravis

• longest acting

• quaternary amine

• do NOT cross the BBB

• only act on peripheral nervous system

neostigmine

• reverse the anesthesia post op

• treatment of myasthenia gravis

• quaternary amine

• do NOT cross BBB

• only act on peripheral nervous system

donepezil

• use to treat alzheimers 

• tertiary amine

rivastigmine

• used to treat alzheimers

• tertiary amine

galantamine

• used to treat alzheimers

• tertiary amine

physostigmine

• treat glaucoma and anticholinergic toxicity (antidote of atropine)

VX

• novichok nerve toxin

• OP compounds

VR

• novichok nerve toxin

• OP compound

A-230

• nerve gas agent

• no antidote; CANNOT be reversed by treatment with 2-PAM to allow for regen of active enzyme b/c of increased stability of phosphonate esters

A-232

• nerve gas agent

• no antidote; CANNOT be reversed by treatment with 2-PAM to allow for regen of active enzyme b/c of increased stability of phosphonate esters

A-234

• nerve gas agent

• no antidote; CANNOT be reversed by treatment with 2-PAM to allow for regen of active enzyme b/c of increased stability of phosphonate esters

malathion

• irreversible inhibitor of ACHE

• insecticide

parathion

• irreversible inhibitor of ACHE

• insecticide

schradan

• irreversible inhibitor of ACHE

• insecticide

dichlofenthion

• irreversible inhibitor of ACHE

• insecticide

chlorpyrifos

• irreversible inhibitor of ACHE

• insecticide 

carbaryl

• slowly reversible inhibitor of ACHE 

• insecticide (carbamate)

pralidoxime (2-PAM)

• antidote for OP poisoning

• competes with ACHE for phosphorus group of inhibitor → enzyme restored

dichlorvos (DDVP)

• organophosphate

• insecticide

• antidotes = atropine + 2-PAM

sarin