Donepezil HCl CAS #: 120011-70-3
Donepezil HCl was first approved in the US by the FDA in 1983. It’s since seen tremendous success with the branded version of the API (Aricept) becoming the number-one selling medication for treatment of Alzheimer’s since 2011. According to current data, the brand is still very strong, worth close to $300 million in revenues in the US market, where generic formulations have been available since November 2010, and around $1.2 billion worldwide. It has been considered for a number of other cognitive conditions, including schizophrenia, Down’s Syndrome, and ADD. However, while researchers have good reason to continue testing for additional indications, it has not yet been approved for any of these disorders.
Donepezil HCl can be used to prevent the breakdown of brain tissue in patients suffering from dementia. It works by protecting the neurotransmitters in the brain, blocking the enzymes that would threaten its natural healthy structure. This drug may not be able to cure or even slow the effects of dementia but it can mediate its symptoms by increasing the patient’s cognitive and physical functions. It may help patients maintain their independence by increasing their memory, awareness, and ability to complete simple tasks.
Donepezil HCl has proved effective at delaying the progression of symptoms in those with dementia, even if it typically cannot sustain the improvement over long periods of time. In a three-year study conducted at the National Institutes of Health, researchers found that those with mild cognitive impairment (MCI), a precursor to Alzheimer’s disease, were less likely to be diagnosed with Alzheimer’s after taking Donepezil for a year. 16 of 253 patients on the API were diagnosed as opposed to 38 of 259 patients who took the placebo.
After three years of the study though, the API and placebo showed no statistical difference in terms of diagnoses. 63 of 253 patients taking Donepezil were diagnosed with Alzheimer’s as opposed to 73 of 259 patients who were taking the placebo. In similar studies conducted by the NIH, a small subgroup with the apolipoprotein E4 genotype saw sustained progress, indicating that the drug may be effective at delaying the progress of dementia in certain patients. However, the evidence is not conclusive enough to confirm the API can effectively slow the disease’s effects on a long term basis.
In addition to helping those with dementia regain their cognitive function, Donepezil also helps people improve their sleep and motor functions. Donepezil HCl is a type of cholinesterase inhibitor and works by increasing the amount of acetylcholine in the brain. It has been recommended for those with even the severest forms of Alzheimer’s, though all patients will need to be heavily monitored when on this API. If the patient isn’t showing any signs of improvement, their treatment will either need to be modified or stopped entirely.
Donepezil HCl is an oral medication that can be taken with or without food, and doctors will start patients at the 10 mg dose. If the patient doesn’t respond to the lower dose, they may be given a higher dose (23 mg) by their doctor. In 2018, a study performed in South Korea found that patients who received the API in dose titration in their first four weeks experienced milder side effects than those who were taking the straight dose. Because the safety profile of the higher dose has not been solidified, this study may give patients a new way to take their medication while reducing their general discomfort.
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