BACKGROUND AND PURPOSE: The one-day rivastigmine patch is reportedly well tolerated and has minimal side effects. However, Asian patients show more side effects than those in Western countries. We evaluated tolerability of the rivastigmine patch in South Korean patients with Alzheimer's disease (AD) and the specific factors affecting adverse events of the skin. METHODS: A 6-month, open labeled, multi-centered, observational study was carried out in 440 patients with probable AD from July 2009 to September 2010 (NCT01312363). RESULTS: A total of 25.9% of the patients experienced adverse skin events at the rivastigmine patch application site and 17.0% discontinued treatment due to adverse events at the skin application site. The most common adverse events were itching and erythema. Patients with an allergic history and users of electric heating appliances reported skin discomfort. Older age was associated with discontinuing treatment. CONCLUSION: These results suggest that the rivastigmine patch induced some adverse skin events and may contribute to understanding and improving skin tolerability to the rivastigmine patch.
Alzheimer Disease* ; Asian Continental Ancestry Group ; Erythema ; Heating ; Hot Temperature ; Humans ; Observational Study ; Pruritus ; Skin* ; Rivastigmine

Alcohol-induced cognitive disorder is a very severe problem in problem alcohol drinker and alcohol itself seems to be one of the main causalities in the development of senile dementia. However, the spectrum of alcohol induced cognitive disorder is quite broad, for example, it covered from alcohol-induced persistent amnestic disorder to Wernicke-Korsakoff syndrome and alcohol-induced persistent dementia. By that reason, broad spectrum of cognitive impairment by excessive alcohol drinking is regarded as alcohol related dementia. The pharmacological treatment is not well established yet in alcohol related dementia, except Wernicke-Korsakoff syndrome which is definitely related to thiamine deficiency. Therefore we introduced that some reports about the clinical efficacies by rivastigmine or donepezil trial and recent outcomes of memantine trial by authors in this review.
Alcohol Drinking ; Alzheimer Disease ; Dementia ; Indans ; Korsakoff Syndrome ; Memantine ; Phenylcarbamates ; Piperidines ; Rivastigmine ; Thiamine ; Thiamine Deficiency

BACKGROUND AND PURPOSE: This study was designed to evaluate the effect on sleep of rivastigmine transdermal patch in patients with probable Alzheimer's disease (AD). METHODS: Patients with probable AD underwent a sleep questionnaire, overnight polysomnography and neuropsychological tests before and after rivastigmine transdermal patch treatment. We analyzed the data from enrolled patients with AD. RESULTS: Fourteen patients with probable AD were finally enrolled in this study. The respiratory disturbance index after the rivastigmine patch treatment was improved in patients with probable AD and sleep breathing disorder, compared with that of before treatment (p<0.05). CONCLUSIONS: Rivastigmine transdermal patch application are expected to improve the symptoms of sleep disordered breathing in patients with probable AD. Further placebo controlled studies are needed to confirm these results.
Alzheimer Disease* ; Humans ; Neuropsychological Tests ; Polysomnography ; Respiration ; Rivastigmine* ; Sleep Apnea Syndromes* ; Transdermal Patch*

OBJECTIVES: Despite the fact that delirium is a frequent neuropsychiatric disorder in cancer patients, there are, in Korea, no guidelines for the pharmacological treatment of such delirium. This systematic review evaluated the efficacy and safety of some pharmacological interventions and summarized the results. METHODS: We searched PubMed, Embase, CINAHL, the Cochrane Library, and the KMbase, targeting from January 1990 to October 2008, using key words. Moreover, we included systematic reviews, meta-analyses, and randomized controlled trial literature in the search. Then, we stratified the trials based on their evidence levels. RESULTS AND CONCLUSION: We identified 13 randomized, controlled studies and 2 case-control studies that met our inclusion criteria. These showed that haloperidol was the medication of choice to treat delirium. In addition, they revealed that atypical antipsychotics have not shown clear superiority with regard to effectiveness as compared to haloperidol. Neither donepezil nor rivastigmine were shown to be effective in preventing or treating delirium.
Antipsychotic Agents ; Case-Control Studies ; Delirium ; Haloperidol ; Humans ; Indans ; Korea ; Phenylcarbamates ; Piperidines ; Rivastigmine

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
Acetylcholinesterase ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Proline ; analogs & derivatives ; Rivastigmine ; chemistry ; Structure-Activity Relationship

OBJECTIVETo optimize the synthetic procedure of S-(+)-rivastigmine hydrogentartrate which was known as an agent for the treatment of Alzheimer disease.

METHODSS-(+)-rivastigmine hydrogentartrate was synthesized by using 1-(3-hydroxyphenyl)ethanone as the starting material via oximation, reduction and N-methylation to produce the key intermediate 3-1-dimethylaminoethylphenol, which finally reacted with N-ethyl-N-methylcarbamoyl chloride. The enantiomers were resolved with di-(+)-p-toluoyl-D-tartaric acid, and the title compound was prepared by mixing S-rivastigmine base with L-(+)-tartrate.

RESULTSThe total yield of S-(+)-rivastigmine hydrogentartrate was 4.17%.

CONCLUSIONThe materials in this procedure are all commercially available. The reaction conditions are mild and total yield is high.

Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Models, Chemical ; Molecular Structure ; Phenylcarbamates ; chemical synthesis ; chemistry ; Rivastigmine ; Stereoisomerism

OBJECTIVE: D-galactose has been commonly used in rodent models to induce accelerated effects of aging, including those on learning, memory, and muscular tone and coordination. This is normally seen on chronic administration of D-galactose. However, there is minimal suggestive evidence on the short-term effects of the same. The aim of the study was to study the acute and chronic effects of D-galactose on learning and memory in Wistar rats. METHODS: Twenty four male Wistar rats were randomly assigned to the control, standard (rivastigmine), oral D-galactose (200 mg/kg/day) and subcutaneous D-galactose (200 mg/kg/day) for a total duration of 8 weeks. Effects on learning and memory were assessed at 2 weeks, 4 weeks and 8 weeks by Morris water maze model and passive avoidance testing. RESULTS: Both oral and subcutaneous D-galactose showed positive effects on learning and memory on acute dosing, whereas this beneficial effect was lost during chronic dosing. CONCLUSION: Short-term administration of D-galactose showed positive effects, while long-term administration nullified these effects.
Aging ; Alzheimer Disease ; Galactose* ; Humans ; Learning* ; Male ; Memory* ; Rats, Wistar* ; Rivastigmine ; Rodentia ; Water

Despite epidemiological studies reporting no negative effects of mild to moderate alcohol drinking on cognitive functioning, a recent well-controlled study showed that chronic mild drinking diminished the volume of the brain and was associated with cognitive decline that worsened as a function of the amount of alcohol consumed. Animal studies have demonstrated that neural cell damage follows chronic alcohol intake and withdrawal. In addition, acute excessive alcohol intake has been shown to result in temporary impairment of memory, and chronic alcohol drinking is often related to neuronal damage and cognitive disorders. Even though a diverse spectrum of cognitive disorders can develop after sustained alcohol drinking, no definite diagnostic criteria existed before those proposed by Oslin; the availability of these criteria will provide more structured clinical and academic approaches to alcohol-related cognitive decline, including dementia. In general, diminished cognitive functioning has been related to excessive alcohol consumption, with cognitive functioning gradually recovering over time. With the exception of the administration of thiamine in Wernicke-Korsakoff syndrome, only supportive pharmacotherapies have been provided for patients with alcohol-related cognitive disorders. However, experimental trials with rivastigmine or donepezil have been conducted for special populations with persistent cognitive impairments, and these studies reported favorable outcomes. We administered memantine for alcohol-related dementia and observed improvements in verbal memory and scores on the mini-mental status exam. We anticipate that novel and appropriate therapeutic agents for various conditions in this domain will be developed based on systematic diagnostic criteria and the accumulation of neurobiological evidence about alcohol-related cognitive decline.
Alcohol Drinking ; Alcoholism ; Animals ; Brain ; Dementia ; Drinking ; Humans ; Indans ; Korsakoff Syndrome ; Memantine ; Memory ; Neurons ; Phenylcarbamates ; Piperidines ; Thiamine ; Rivastigmine

Parkinson's disease dementia (PDD) is notorious for its debilitating clinical course and high mortality rates. Consequently, various attempts to investigate predictors of cognitive decline in Parkinson's disease (PD) have been made. Here we report a case of a 75-year-old female patient with PD who visited the clinic with complaints of recurrent visual hallucinations and cognitive decline, whose symptoms were ameliorated by the titration of rivastigmine. Imaging results showed pronounced diffuse cortical amyloid deposition evidenced by 18F-florbetaben amyloid positron emission tomography (PET) imaging. This observation suggests that pronounced amyloid deposition and visual hallucinations in PD patients could be clinically significant predictors of cognitive decline in PD patients. Future research should concentrate on accumulating more evidence for possible predictors of cognitive decline and their association with PD pathology that can enable an early intervention and standardized treatment in PDD patients.
Aged ; Amyloid* ; Dementia* ; Early Intervention (Education) ; Female ; Hallucinations* ; Humans ; Mortality ; Parkinson Disease* ; Pathology ; Plaque, Amyloid* ; Positron-Emission Tomography ; Rivastigmine

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Acetylcholinesterase ; metabolism ; Benzimidazoles ; chemical synthesis ; chemistry ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Drug Design ; Phenylcarbamates ; chemistry ; Rivastigmine ; Structure-Activity Relationship