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Cholinesterase and Cholinesterase Inhibitors
Pharmacology
27
Medical
Professional
09/05/2011

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Cards

Term
3 classes of cholinesterase inhibitors
Definition
reversible Noncovalent inhibitors
reversible carbamate inhibitors
Irreversible organophosphates
Term
Noncovalent AChE inhibitors
Definition
Edrophonium- quatnernary (do NOT cross BBB)
Tacrine, donepezil- tertiary (cross BBB)
Term
4 carbamates
Definition
neostigmine, pyridostigmine, physostigmine, rivastigmine
Term
Carbamate mech of action
Definition
react w/serine in the active site to form carbamoylated AChE
Term
PCKN of Carbamates
Definition
neo and pyri (poor absorption in GI)do NOT cross BBB.

phys and riva enter BBB

undergo non-enzymatic hydrolysis
Term
Organophosphates
Definition
DFP, echothiophate, parathion, malathion
Term
Organophosphates PCKN
Definition
All enter CNS except Echothiophate
Term
Organophosphate mech of action
Definition
react w/serine in catalytic triad- phosphorylated intermediate
Term
Pharm effects on cholinergic nerve stimulation
Definition
stimulation of musc. receptors
stimu then depress of ganglia (nicotinic)
Term
AChE block effect on Eye
Definition
conjunctivial hyperemia, miosis
blurred vision
reduced intraocular pressure w/wide-angle glaucoma
Term
AChE block effect on GI tract
Definition
PS action
Term
AChE block effect on resp. tract
Definition
PS
Term
AChE block effect on CNS
Definition
anxiety, restlessness
resp depression, convulsions
Term
How is MG treated?
Definition
neostigmine, pyridostigmine, ambenonium- enhance ACh in the cleft

Corticosteroids and cyclosporine
Term
Close-angle glaucoma
Definition
acetazolamide, mannitol, and pilocarpine
Term
Open angle glaucoma
Definition
Pilocarpine (miotic)
Timolo (beta blocker) decr aqueous humor
Demecarium,
echothiophate
Term
First inhibitor approved for AD
Definition
Tacrine
short half life; very hepatoxic!
Term
AD drug HIGHLY selective for CNS AChE
Definition
Donepzil
Longest half-life
Very LITTLE hepatoxicity
Term
AD drug- once daily transdermal patch
Definition
Rivastigmine
Term
Adynamic Ileus of bladder after surgery
Definition
Neostigmine
Term
Antimuscarinic toxicity
Definition
PHysostigmine reverses it
Term
Side effects of AChE Inhibitor
Definition
Increase PS effects
occasional cataracts, lenticiular opacities
Term
AChE inhibitor poisoning
Definition
Insecticides- parathion/malathion
80% of hospital admissions
Term
Symptoms of poisoning
Definition
SLUDGE and DUMBELS- muscarinic
Nicotinic- respiratory difficult, arrest. muscle weakness
CNS: malaise, memory loss, confusion, delirium, seizures and coma
Term
Treatment of poisoning
Definition
Atropine + pralidoxime
Term
Prophylaxis
Definition
pyridostigmine administered to soldiers in case of nerve gas
Term
Cholinesterase regenerator
Definition
2-PAM
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