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Cholinerneric Drugs


Synthesis of acetyl choline

  1. Choline is actively taken up by the axonal membrane by a Na+: choline cotransporter and acetylated with the help of ATP and coenzyme-A by the enzyme choline acetyl transferase present in the axoplasm.
  2. Hemicholinium blocks choline uptake (the rate limiting step in ACh synthesis) and depletes ACh. Most of the ACh is stored in ionic solution within small synaptic vesicles, but some free ACh is also present in the cytoplasm of cholinergic terminals.
  3. Active transport of ACh into synaptic vesicles is effected by another carrier which is blocked by Vesamicol.
  4. Two toxins interfere with cholinergic transmission by affecting release: Botulinum Toxin inhibits release, while Blackwidow Spider toxin induces massive release and depletion. Immediately after release, ACh is hydrolyzed by the enzyme cholinesterase and choline is recycled.
  5. A specific (Acetylcholinesterase-AChE or true cholinesterase) and a nonspecific (Butyrylcholinesterase-BuChE or pseudocholinesterase) type of enzyme occur in the body.

              AcetylCholinesterase (True)


a.  Main                 
b.  Fast acting           
c.  RBC/Neurons  
d.  No deficiency                                     
e.  Metabolize only Ach

a.  minor(major route of drug elimination)                    
b.  slow acting                      
c.  Gut/plasma, liver, placenta, neuroglial cells             
d.  Deficiency leads to apnoea
e.  Drugs metabolized are succinylcholine, remifentanil, procaine

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