Galantamine and behavior in Alzheimer disease: analysis of four trials

Abstract

Galantamine reduces behavioral symptoms in patients with mild to moderate AD, leading to reduced caregiver burden. The reductions were greatest in patients with moderate or advanced moderate disease.

The Effects of an Uninterrupted Switch from Donepezil to Galantamine without Dose Titration on Behavioral and Psychological Symptoms of Dementia in Alzheimer's Disease

“…According to an analysis of four trials on galantamine and behavior in AD, 5-6 months of galantamine treatment reduced behavioral symptoms of AD and the associated caregiver burden; the beneficial effects on the NPI were reported for galantamine versus a placebo [9,19,20,21]. Moreover, several clinical trials involving galantamine in patients with mild to moderate AD showed improvement of neuropsychiatric symptoms and the associated caregiver distress [19,22,23].…”

“…Galantamine has allosteric modulating activity at the nicotinic acetylcholine receptors (nAChRs) in addition to acting as an acetylcholinesterase inhibitor (AChEI) [8], and shows improvement of behavioral and neuropsychiatric symptoms [9]. In this study, the efficacy of galantamine on the symptoms of cognition and BPSD was evaluated by an uninterrupted switch from donepezil to galantamine with no washout period or dose titration in amnestic mild cognitive impairment (MCI) and AD patients, whose BPSD were unresponsive to donepezil, or whose caregivers were not satisfied with donepezil treatment.…”

Synthesis and anticholinesterase activities of novel 1,3,4-thiadiazole based compounds

“…Compound 2 with the heptyl substituent is one of the most active derivatives. From the group of compounds with two 1,3,4-thiadiazole rings (5,6,7) compound 7 with benzene as a link shows the highest affinity for AChE. Derivative 9 with the 2,4-dichlorophenoxymethyl substituent is the most active against AChE of all compounds of 1,3,4-thiadiazole series.…”

“…A common method for the treatment of cognitive and behavioral symptoms of AD is the use of structurally diverse group of cholinesterase inhibitors (ChEIs) with an amine moiety and distinct modes of action. Available ChEI drugs are tacrine (Cognex 3 ), donepezil (Aricept 4 ) galanthamine (Reminyl) -reversible inhibitors 5 and rivastigmine (Exelon 6 ) which acts as a pseudo-irreversible ChEI, and differs in selectivity toward AChE and butyrylcholinesterase (BuChE).…”

Synthesis and <i>in Vitro</i> Evaluation of 1,3,4-Thiadiazol-2-yl Urea Derivatives as Novel AChE Inhibitors

“…[3][4][5][6] One of the oldest AD hypotheses, 7) the cholinergic hypothesis, has led to the development of acetylcholinesterase inhibitors (AChEIs) that increase levels of acetylcholine (ACh) through inhibition of acetylcholinesterase (AChE). 8) Several antiacetylcholinesterase agents such as donepezil, 9) tacrine, 10) galantamine, 11) and ensaculin 12) have shown to induce modest improvement in memory and cognitive functions. Unfortunately, the potential effectiveness offered by these inhibitors is often limited by the appearance of central and peripheral side effects.…”