Donepezil 23 mg: A Brief Insight on Efficacy and Safety Concerns

Abstract

As life expectancy increases, it is imperative that health care providers recognize the importance of safe medication use within an aging geriatric population. Dealing with a cohort that has different biological and medical demands requires pharmacists to pay particular attention to details when treating this subset of individuals. In particular, this manuscript will focus on Alzheimer's disease (AD) and considerations when dealing with new treatment options. The Food and Drug Administration's recent approval of the increased dosage strength, donepezil 23 mg, previously only available in 5 mg and 10 mg strengths, has raised efficacy and safety concerns. Reservations stem from unproven superiority along with an increased incidence of adverse events. The purpose of the manuscript is to provide a brief insight into these concerns and provide readers the knowledge necessary to make a clinically sound decision when treating patients with moderate-to-severe AD.

Procognitive effect of AC-3933 in aged mice, and synergistic effect of combination with donepezil in scopolamine-treated mice

“…Although AChE inhibitors, such as donepezil are widely used for treatment of patients with Alzheimer's disease, dosing with high-doses of an AChE inhibitor frequently induces gastrointestinal adverse effects, such as nausea, vomiting, diarrhea, and anorexia (Nguyen and Salbu, 2013). Therefore, in the case of donepezil, treatment is usually initiated at a low dose (5 mg) and is maintained for at least one month to acclimate the patient to treatment and avoid adverse effects.…”

“…In line with this hypothesis, a number of drug development approaches, based on cholinergic replacement strategy, have been pursued, leading to the discovery and launch of a series of acetylcholinesterase (AChE) inhibitors, including donepezil, as therapeutic agents for Alzheimer's disease (Whitehead et al, 2004). However, these agents have limited efficacy and produce undesirable side effects, including nausea, vomiting, diarrhea, and anorexia (Nguyen and Salbu, 2013). Therefore, new therapeutic agents with sufficient efficacy and better safety profiles have long been desired.…”

Chronic Administration of Donepezil in Inhibitory and Spatial Learning and Memory in Male Rats

“…Alzheimer's disease is a progressive disorder caused by the lack of acetylcholine in the brain [6]. To date, AChE inhibitors such as donepezil hydrochloride prevent the reduction of acetylcholine in the brain in Alzheimer's disease [7,8,9]. Donepezil (Aricept) is an AChE inhibitor that is approved for the treatment of Alzheimer's disease with once-daily dosing [9,10].…”

“…To date, AChE inhibitors such as donepezil hydrochloride prevent the reduction of acetylcholine in the brain in Alzheimer's disease [7,8,9]. Donepezil (Aricept) is an AChE inhibitor that is approved for the treatment of Alzheimer's disease with once-daily dosing [9,10]. The clinical efficacy of donepezil is based on the AChE inhibition that elevates the acetylcholine level at synapses and leads to the improvement of memory and learning impairments [11].…”

“…The high doses of donepezil have been used for the treatment of patients with Alzheimer's disease [19]. Using a low dose of donepezil reduces the side effects of the drug such as nausea, vomiting, diarrhea, and anorexia [9]. However, the chronic high doses of donepezil modulate cognitive behavior in the treatment of rats [20,21].…”