Pharmacology of Carbamyl Inhibitors of Acetylcholinesterase

1
Pharmacology of Carbamyl Inhibitors of
Acetylcholinesterase

• Eye
• Exocrine glands
• Cardiac muscle
• Smooth muscles
• Skeletal muscle
• Toxicity

2
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 (TCAs)
  or phenothiazines (use physostigmine)
• Recovery of neuromuscular function after
  competitive blockade of NN receptor of skeletal
  muscle fibers
• Myasthenia gravis

3
Therapeutic Uses of Edrophonium

• Diagnosis of myasthenia gravis
• In conjunction with chosen therapeutic agent to
  determine proper dose of agent

4
Determining Proper Dose of AChE Inhibitor
5
Inhibitors of AChE Are Used for Therapy of
Alzheimers Disease

• Tacrine
• Donepezil
• Rivastigmine
• Galantamine

6
Organophosphate Inhibitors of AChE
7
Some Organophosphate Inhibitors of
Acetylcholinesterase

• Tetraethylpyrophosphate
• Echothiophate (N)
• Diisopropylflurophosphate (DFP)
• Sarin
• Soman
• Tabun
• Malathion
• Parathion
• Diazinon
• Chlorpyrifos
• Many others

8
Organophosphate Inhibitors - 2
Diisopropylfluorophosphate (DFP)
Soman
Tabun
Sarin
9
Echothiophate
Therapeutic use - local application to the eye
for wide angle glaucoma
10
Conversion of Parathion to Paraoxon
11
Conversion of Malathion to Malaoxon