Rivastigmine Anticholinesterases

Anticholinesterase A drug that inhibits the enzyme acetylcholinesterase, which normally inactivates acetylcholine at the synapse. The effect of an anticholinesterase (or cholinesterase inhibitor) is thus to prolong the duration of action of the neurotransmitter. An example is rivastigmine, used in the treatment of Alzheimer s disease. 

Rivastigmine An anticholinesterase used to treat Alzheimer s disease. 

Figure 5. Cartoon of a cholinergic synapse showing major steps in the synthesis of acetylcholine. The two major receptor types, the ionotropic nicotinic receptor and the metabotropic muscarinic receptor, are shown (see also Chapter 1). Presynaptic muscarinic (M2) and nicotinic receptors are also depicted. Drugs which have been widely used to manipulate the cholinergic systems, and which are mentioned in the text, include the muscarinic receptor antagonists scopolamine and atropine and the nicotinic receptor agonist nicotine. Anticholinesterases (discussed elsewhere in this volume) include drugs such as physostigmine, rivastigmine, donepezil, and galanthamine.

Anticholinesterases E.g. physostigmine, tacrine, donepezil, metrifonate, huperzine A, eptastigmine, velnacrine, galantamine, rivastigmine Efficacy in early stages of AD... 

A more recent use of anticholinesterase drugs has been to improve cognitive function in patients with Alzheimer s disease, where both the degree of dementia and amyloid plaque density correlate with the impairment of brain cholinergic function. Donepezil and rivastigmine are licensed in the UK for this indication. Both are orally active and cross the blood-brain barrier readily (see p. 408). 

Funding/implementation issues led to variable availability in the UK. Subject of national guideline from National Institute for Clinical Excellence (NICE) requiring availability of licensed anticholinesterases (donepezil, rivastigmine, galantamine) subject to specific requirements ... 

---