Question

Comment on the potential clinical utility for these inhibitors?Comment on the potential clinical utility for these inhibitors, Tacrine and Neostigmine?

Answer 1

Ans- Tacrine- There is an area in brain called basal nucleus of maynert where acetycholine are concentrated which is required for retaining memory. Degeneration of this area leads to loss of memory or dementia in a disease called alzeihmers disease. Tacrine is a cholinesterase inhibitor that elevates acetylcholine in the cerebral cortex by slowing the degradation of acetylcholine. It is a mixed type reversible inhibitor of cholinesterase that binds to closely active serine in its active site. Therefore it is the first drug approved for the treatment of Alzheimer's disease. However, due to the adverse effects it is not preferred but alternatives are used.

Neostigmine- Neostigmine is inhibitor of enzyme acetycholinestrase, which hydrolyses acetylcholine. This is a competitive reversible antagonist of cholinesterase which degrades acetylcholine and ends the cholinergic termination. This action is used in treatment of disorders of neuromuscular junction like myasthenia gravis and antagonist of nondepolarising neuromuscular blockade.