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Cholinesterase Inhibitors
Pharmacology Drugs for Exam 2
11
Pharmacology
Graduate
10/09/2010

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Term
edrophonium (Tensilon)
Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
short acting (< 10 minutes) and is used in diagnosing myasthenia gravis (Tensilon test)
Term
physostigmine (Eserine, Antilirium)
Definition
Reversible Cholinesterase Inhibitors
nonquaternary, so it can get into the CNS
used in treating poisoning with atropine or other antimuscarinic agents
Term
neostigmine (Prostigmin)
Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
longer acting and are used in the treatment of myasthenia gravis
Term
pyridostigmine (Mestinon)
Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
longer acting and are used in the treatment of myasthenia gravis
used by the military to protect troops against nerve agents used in chemical warfare
Term
rivastigmine (Exelon)
Definition
Reversible Cholinesterase Inhibitors
Term
donepezil (Aricept)
Definition
Reversible Cholinesterase Inhibitors
Term
carbamate insecticides (e.g. *Carbaryl)
Definition
Reversible Cholinesterase Inhibitors
widely used insecticide
Not absorbed through the skin as much as parathion and malathion
Signs and symptoms of poisoning are similar to those of other cholinesterase inhibitors.
Treat poisoning with atropineand other symptomatic support. Pralidoxime is not useful in treating poisoning with carbaryl or other carbamate insecticides!
Term
organophosphate insecticides (*parathion, malathion, diazinon and others)
Definition
Irreversible Cholinesterase Inhibitors
must be oxidized to active metabolites (paroxone and malaoxone). The conversion occurs more rapidly in insects than humans
can be absorbed through the skin
Signs and symptoms of poisoning are typical
Treat poisoning with *atropine, *pralidoxime, and other symptomatic support
Term
DFP/diisopropylfurophosphate/Isoflurophate and echothiophate
Definition
Irreversible Cholinesterase Inhibitors
Very potent and toxic, irreversible cholinesterase inhibitors
Signs and symptoms are typical for cholinesterase inhibitors
Treat poisoning with atropine and pralidoxime
DFP/Isoflurophate has been used in ophthalmology for the treatment of glaucoma
Term
nerve gases (*Sarin and others)
Definition
Irreversible Cholinesterase Inhibitors
Very potent and toxic, irreversible cholinesterase inhibitors
Signs and symptoms are typical for cholinesterase inhibitors
Treat poisoning with atropine and pralidoxime
Term
pralidoxime/2-PAM (Protopam)
Definition
Cholinesterase Reactivator
chemically binds to the phosphate group that inhibits the enzyme and thereby regenerates the enzyme
antidote for organophosphate poisoning
must be used within 2 hours following exposure
does not work with carbamate insecticides (e.g. carbaryl)
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