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by Sugimoto H, Iimura Y, Kawakami Y, Yamanishi Y. Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki, 300-2635, Japan.
March 24, 2000
SUMMARY:
The benefits of taking acetylcholinesterase (AChE) inhibitors for Alzheimer's disease is well known and clinically proven. AChE inhibitors have the potential to delay the decline in cognitive and mental functions in Alzheimer patients. AChE inhibitors used in the past, namely, physostigmine and tacrine, brought their own host of problems along with their mild benefits. Studies in search of a better inhibitor have proven fruitful; researchers have discovered donepezil hydrochloride, an AChE inhibitor with a longer and more selective action (therefore offering greater benefits) with manageable adverse side effects. Huperzine A is a drug free AChE inhibitor. Like donepezil hydrochloride, Huperzine A has been proven to have a powerful and lasting effect on the brain while keeping side effects to a minimum. In addition, recent news reports Huperzine A can lower neuronal cell death attributed to glutamate. The multiple benefits Alzheimer patients experience as a result of including AChE inhibitors in their treatment program make them an excellent Alzheimer's treatment.
ABSTRACT:
A wide range of evidence shows that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of Alzheimer's patients. However, clinical studies show that physostigmine has poor oral activity, brain penetration and pharmacokinetic parameters while tacrine has hepatotoxic liability. Studies were then focused on finding a new type of acetylcholinesterase inhibitor that would overcome the disadvantages of these two compounds. Donepezil hydrochloride inaugurates a new class of AChE inhibitors with longer and more selective action with manageable adverse effects. Currently, there are about 19 new Alzheimer's drugs in various phases of clinical development.
Editor's note: Huperzine A is a drug free AChE inhibitor that has been proven to have a powerful and lasting protective effect on the brain while keeping side effects to a minimum.
Source: Curr Med Chem 2000 Mar;7(3):303-39
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