Pharmacology of Carbamyl Inhibitors of Acetylcholinesterase

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Presentation transcript:

Pharmacology of Carbamyl Inhibitors of Acetylcholinesterase Eye Exocrine glands Cardiac muscle Smooth muscles Skeletal muscle Toxicity 1

Therapeutic Uses of Inhibitors of Acetylcholinesterase Glaucoma (wide angle) Atony of the bladder Atony of the gastrointestinal tract Intoxication by antimuscarinic agents (use physostigmine) Intoxication by tricyclic antidepressants (TCA’s) or phenothiazines (use physostigmine) Recovery of neuromuscular function after competitive blockade of NN receptor of skeletal muscle fibers Myasthenia gravis 2

Therapeutic Uses of Edrophonium Diagnosis of myasthenia gravis In conjunction with chosen therapeutic agent to determine proper dose of agent 3

Determining Proper Dose of AChE Inhibitor

Inhibitors of AChE Are Used for Therapy of Alzheimer’s Disease Tacrine Donepezil Rivastigmine Galantamine 5

Organophosphate Inhibitors of AChE 6

Some Organophosphate Inhibitors of Acetylcholinesterase Tetraethylpyrophosphate Echothiophate (N+) Diisopropylflurophosphate (DFP) Sarin Soman Tabun Malathion Parathion Diazinon Chlorpyrifos Many others 7

Organophosphate Inhibitors - 2 Diisopropylfluorophosphate (DFP) Soman Tabun Sarin 8

Therapeutic use - local application to the eye for wide angle glaucoma Echothiophate Therapeutic use - local application to the eye for wide angle glaucoma 9

Conversion of Parathion to Paraoxon 10

Conversion of Malathion to Malaoxon 11