A wide range of evidence shows that cholinesterase (ChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The earliest known ChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of AD patients. However, clinical studies show that physostigmine has poor oral activity, brain penetration and pharmacokinetic parameters, whi...

OBJECTIVE To study the safety and efficacy of a cholinesterase inhibitor, donepezil hydrochloride, for the treatment of dementia in Parkinson's disease (PD). METHODS This was a randomised double blind, placebo controlled, crossover study in 22 subjects with PD and dementia. Participants were randomised to receive either donepezil followed by identical placebo, or placebo followed by donepezil...

A liquid chromatography/tandem mass spectrometry (LC/MS/MS) method was developed and validated for the determination of donepezil in human plasma samples. Diphenhydramine was used as the internal standard. The collision-induced transition m/z 380 --> 91 was used to analyze donepezil in selected reaction monitoring mode. The signal intensity of the m/z 380 --> 91 transition was found to relate l...

OBJECTIVE The only approved pharmacological approach for the symptomatic treatment of Alzheimer's disease in Japan is the use of a cholinesterase inhibitor, donepezil hydrochloride. Recent in vivo and in vitro studies raise the possibility that cholinesterase inhibitors can slow the progression of Alzheimer's disease. The purpose of the present study was to determine whether donepezil has a neu...

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, name...

Delayed encephalopathy following carbon monoxide poisoning is a serious complication. Here, we report a patient with delayed encephalopathy who suffered from cognitive disorders and urinary incontinence after a temporal normal period of 15 days after acute intoxication, and his cognitive function recovered gradually following donepezil hydrochloride treatment. Now, he can undertake slight farmi...

OBJECTIVE The pharmacological effects of generic (GE) donepezil are the same as Aricept, its brand-name counterpart. However, little is known as to whether these two drugs provide the same quality of life (QOL). The study subjects were patients with Alzheimer's disease who were taking donepezil hydrochloride tablets, and were selected by visiting either the local pharmacies or the patients' hom...

Donepezil hydrochloride (Aricept) is a drug for the treatment of Alzheimer's disease. The absorption, distribution, metabolism, and excretion of donepezil were investigated in male Sprague-Dawley rats after a single oral administration. Orally administered (14)C-labeled donepezil was absorbed rapidly. The plasma level of unchanged donepezil declined more rapidly than that of radioactivity, and ...

In this study, new fumarate compounds (I-IV) containing some natural phenols (eugenol, guaiacol, isoeugenol and vanillin) were synthesized characterized. The single crystal X-ray diffraction technique was used to determine the structures of all compounds. All evaluated as acetylcholinesterase (AChE) inhibitory, especially compound IV (IC50 =5.25±0.51 µg/mL), can be identified a promising anti-a...

Objective: To explore the effect of donepezil hydrochloride on the cognitive function recovery of the rats with Alzheimer’s disease and the positive expression of nitric oxide synthase and acetylcholinesterase (NOS and AchE) in brain tissues of rats with Alzheimer's disease (AD). Methods: Forty SD (Sprague Dawley) rats were randomly classified into model group, treatment group, control group an...