AIM The aim of this study was to examine the pharmacokinetics of donepezil HCl and ketoconazole separately, and in combination, following administration of single and multiple oral doses. METHODS This was an open-label, randomized, three-period crossover study in healthy volunteers (n=21). During each treatment period, subjects received single daily doses of either donepezil HCl (5 mg), ketoc...

AIMS The primary objective of this study was to characterize the pharmacokinetics and pharmacodynamics of single daily doses of donepezil (5 and 10 mg) each evening for 28 consecutive days. A secondary objective was to measure the plasma protein binding of donepezil at steady state. METHODS This was a double-blind, randomized, multiple-dose study in healthy male (n=13) and female (n=3) volunt...

AIM The aim of this study was to characterize the pharmacokinetics and pharmacodynamics of donepezil HCl, a new, chemically distinct and specific acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease, following multiple-dose administration. METHODS This was a double-blind, randomized, placebo-controlled, multiple-dose study in healthy male volunteers (n=27). Three dos...

BACKGROUND Alzheimer's disease is a progressive neurodegenerative disease. Although some of the current treatments offer some symptomatic relief, this disease cannot be cured at present. Electroacupuncture may be effective for Alzheimer's disease for cognitive function, but the evidence for its effectiveness is still limited. The aim of this study is to evaluate the add-on effect of electroacup...

Donepezil is used worldwide for the treatment of Alzheimer’s disease, where it is used to increase cortical acetylcholine. We present a simple liquid chromatography-tandem mass spectrometry (LC-MS/MS) method developed and validated for the quantification of Donepezil in Human Plasma. Quetiapine was used as the internal standard. The simple and cost effective Liquid-Liquid Extraction method is a...

Clinical reports indicate that cardiotoxicity due to donepezil can occur after coadministration with cilostazol. We speculated that the concentration of donepezil in heart tissue might be increased as a result of interaction with cilostazol at efflux transporters such as P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2), which are expressed in many tissues includin...

BACKGROUND Findings from observational studies have suggested a delay in nursing home placement with dementia drug treatment, but findings from a previous randomised trial of patients with mild-to-moderate Alzheimer's disease showed no effect. We investigated the effects of continuation or discontinuation of donepezil and starting of memantine on subsequent nursing home placement in patients wi...

The acetylcholinesterase (AChE) inhibitor donepezil is also a sigma1 receptor agonist. We examined whether donepezil binds to sigma1 receptors in the living human brain after a single oral administration. Dynamic positron emission tomography (PET) data acquisition using the selective sigma1 receptor ligand [11C]SA4503 was performed to evaluate quantitatively the binding of [11C]SA4503 to sigma1...

INTRODUCTION Donepezil is indicated for the symptomatic treatment of mild to moderate Alzheimer's disease. It is a specific and reversible inhibitor of acetylcholinesterase (AChE); by increasing levels of available acetylcholine, donepezil may compensate for the loss of functioning cholinergic brain cells. AIMS This review evaluates the clinical impact of donepezil by assessing randomized con...