Anticholinesterases

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Chapter: Essential pharmacology : Cholinergic System And Drugs

Anticholinesterases (antiChEs) are agents which inhibit ChE, protect ACh from hydrolysis—produce cholinergic effects in vivo and potentiate ACh both in vivo and in vitro. Some anti ChEs have additional direct action on cholinergic receptors.


ANTICHOLINESTERASES

 

Anticholinesterases (antiChEs) are agents which inhibit ChE, protect ACh from hydrolysis—produce cholinergic effects in vivo and potentiate ACh both in vivo and in vitro. Some anti ChEs have additional direct action on cholinergic receptors.

 

            Reversible

 

Carbamates            Acridine

 

Physostigmine (Eserine) Tacrine

 

Neostigmine

 

Pyridostigmine

 

Edrophonium

 

Rivastigmine, Donepezil

 

Galantamine

 

             Irreversible

 

Organophosphates

Carbamates

Dyflos (DFP)

Carbaryl* (SEVIN)

Echothiophate

Propoxur* (BAYGON)

Parathion*, Malathion*

*Insecticides

 

Diazinon* (TIK20)

£Nerve gases for

 

Tabun£, Sarin£, Soman£

chemical warfare

 

 

Chemistry

 

AntiChEs are either esters of carbamic acid or derivatives of phosphoric acid.

The generic formula of carbamates and organophosphates is shown below:

 

In carbamates R1 may have a nonpolar tertiary amino N, e.g. in physostigmine, rendering the compound lipid soluble. In others, e.g. neostigmine, R1 has a quaternary N+—rendering it lipid insoluble. All organophosphates are highly lipid soluble except echothiophate which is water soluble.

 

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