Yellow Donepezil Hydrochloride Raw Powder CAS 120014-06-4 For Alzheimer's Disease

Yellow Raw Powder CAS 120014-06-4 Donepezil Hydrochloride For Alzheimer′S Disease Treatment

Description

Donepezil is a oxide and is a second-generation specific reversible central acetylcholinesterase (AChE) inhibitor with little effect on peripheral AChE. This product slows down the decomposition of acetylcholine (ACh) in the synaptic cleft by inhibiting the activity of AChE, thereby increasing the content of ACh and improving the cognitive function of Alzheimer's disease (AD) patients. The intensity of inhibiting the activity of acetylcholinesterase is 570 times that of inhibiting butyrylcholinesterase, and has higher selectivity. Oral administration of 10 mg/kg can inhibit cholinesterase in the brain, and there is a dose-effect relationship.

Donepezil is a centrally acting reversible acetylcholinesterase inhibitor. Its primary therapeutic use is in the palliative care of Alzheimer's disease. Common side effects include gastrointestinal upset. It has 100% oral bioavailability and readily crosses the blood-brain barrier. Because of its biological half-life of approximately 70 hours, it can be taken once a day.

Donepezil has been tested in other cognitive disorders (sometimes used off-label), including dementia with Lewy bodies and vascular dementia, but is not currently approved for these indications. Donepezil has been found to improve sleep apnea in people with Alzheimer's disease. Donepezil has also been used in patients with mild cognitive impairment, schizophrenia, attention deficit disorder, cognitive impairment after coronary artery bypass grafting, cognitive impairment associated with multiple sclerosis, CADASIL, and Down syndrome.

A 3-year NIH trial in patients with mild cognitive impairment reported that donepezil was superior to placebo in slowing the rate of dementia progression during the first 18 months of the study, but not at 36 months continued. In secondary analyses, a subgroup of individuals with the apolipoprotein E4 genotype showed sustained benefits of donepezil throughout the study. However, donepezil is not currently used to prevent dementia. Recent research has shown that donepezil can improve language skills in children with autism. The study found that the language skills of mildly to moderately affected children with autism appeared to improve after using donepezil.

Application

1. Donepezil reversibly binds and inactivates cholinesterase, thereby inhibiting the hydrolysis of acetylcholine. This results in increased concentrations of acetylcholine at cholinergic synapses.

2. Donepezil has a very good effect on Alzheimer's disease. Of course, Alzheimer's disease involves a massive loss of elements of the cholinergic system, and it is widely believed that the symptoms of Alzheimer's disease are related to this cholinergic deficit, particularly in the cerebral cortex and other regions of the brain.

3. We noticed that the formation of the hippocampus plays an important role in the control process of attention, memory and learning. The severity of loss of central nervous system (CNS) cholinergic neurons alone has been found to correlate with the severity of cognitive impairment.