Rivastigmine in the treatment of Alzheimer's disease: an update

Abstract

Alzheimer’s disease is the most common form of dementia in industrialized countries. In the European Union, about 54% of dementia cases are believed to be due to Alzheimer’s disease. The condition is an age-related neurodegenerative disorder characterized by multiple cognitive deficiencies, including loss of memory, judgment, and comprehension. These manifestations are accompanied by behavioral and mood disturbances. Although no cure has yet been discovered for Alzheimer’s disease, symptomatic therapies are now widely available and offer significant relief to patients and benefits to caregivers in terms of reduced care burden. At the start of the 21st century, health technology assessments recommended three agents for the symptomatic treatment of mild to moderate Alzheimer disease: rivastigmine, donepezil, and galantamine. Rivastigmine (Exelon®, Novartis Basel—Switzerland) is a slowly reversible inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), while donepezil (Aricept®, Pfizer, New York, USA) and galantamine (Reminyl®, Janssen, New Jersey,USA) show no functional inhibition of BuChE, and are considered AChE-selective, rapidly-reversible inhibitors. The efficacy of all three agents has been evaluated in large, double-blind, placebo-controlled clinical trials of up to 6 months’ duration. Rivastigmine treatment in mild to moderate Alzheimer’s disease improves cognition, activities of daily living, and global function.

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

“…Alzheimer's disease is characterized, among other neuropathological features, by the degeneration of cholinergic neurons in the cortex and hippocampus, resulting in lower levels of acetylcholine and altered cholinergic transmission [33]. Barnes et al showed that the overall hippocampal atrophy rate is 1.4% in healthy patients from 69 to 83 years; this rate increased to 4.6% for subjects with Alzheimer's disease [34].…”

“…Until 2007, AChE inhibitors were only available as oral formulations taken once or twice daily in order to achieve adequate and consistent inhibition of cholinesterase [33]. Recently, a once-a-day rivastigmine patch received approval in the US.…”

Protection of PMS777, a New AChE Inhibitor with PAF Antagonism, Against Amyloid-β-Induced Neuronal Apoptosis and Neuroinflammation

“…Indeed, the application of AChE inhibitors has been proved to be effective approach in symptomatic treatment of AD patients. However, AChE inhibitors temporally aim to palliatively alleviate the cognition impairment and behavior disabilities but do not stop the disease progression (Onor et al 2007; Raina et al 2008). On the other hand, anti-inflammatory agents are likely to reduce the risk and delay the onset to develop AD (Etminan et al 2003;Hoozemans et al 2003) and may represent one of the disease-modifying strategies for AD therapy.…”

Drug Repositioning for Parkinson�s Disease Based on Adverse Drug Reactions Detected from Social Media (Preprint)

“…A double-blind placebo-controlled clinical study showed that a global rating of cognition, health status, and anxiety severity were improved by using rivastigmine, as well as the cognitive abilities according to a performance-based measure [29].…”