10 replies to this topic

[nootropi]

Heh, I thought you guys might want to see this:

Aricept available w/o a prescription

That is pretty darn expensive. Just thought you guys would like to see. But, as I have mentioned before, it has few side effects and is very effective.

Can anybody find a better deal?

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Donepezil hydrochloride is a specific and reversible inhibitor of acetylcholinesterase, the predominant cholinesterase in the brain. Donepezil hydrochloride is over 1000 times more potent an inhibitor of this enzyme than of butyrylcholinesterase, an enzyme which is present mainly outside the central nervous system.

In patients with Alzheimer's dementia participating in clinical trials, administration of single daily doses of 5 mg or 10 mg of donepezil hydrochloride produced steady-state inhibition of acetylcholinesterase activity (measured in erythrocyte membranes) of 63.6% and 77.3%, respectively when measured post dose. The inhibition of acetylcholinesterase (AChE) in red blood cells by donepezil hydrochloride has been shown to correlate to changes in ADAS-cog, a sensitive scale which examines selected aspects of cognition. The potential for donepezil hydrochloride to alter the course of the underlying neuropathology has not been studied.

In the clinical trials, an analysis was done at the conclusion of 6 months of donepezil treatment using a combination of three efficacy criteria: the ADAS-Cog (a measure of cognitive performance), the Clinician Interview Based Impression of Change with Caregiver Input (a measure of global function) and the Combined Activities of Daily Living Domains of the Clinical Dementia Rating Scale (a measure of capabilities in community affairs, home and hobbies and personal care).

The 10 mg tabs can be split into two, which makes each month cost about $62.50.

'Smart drugs' boost pilot memory

Neurology. 2002 Jul 9;59(1):123-5.  Related Articles, Links


Comment in:
Neurology. 2003 Sep 9;61(5):721; author reply 721.

Donepezil and flight simulator performance: effects on retention of complex skills.

Yesavage JA, Mumenthaler MS, Taylor JL, Friedman L, O'Hara R, Sheikh J, Tinklenberg J, Whitehouse PJ.

Palo Alto Veterans Affairs Health Care System, Stanford University School of Medicine, Stanford, CA 94305-5550, USA. yesavage@stanford.edu

We report a randomized, double-blind, parallel group, placebo-controlled study to test the effects of the acetylcholinesterase inhibitor, donepezil (5 mg/d for 30 days), on aircraft pilot performance in 18 licensed pilots with mean age of 52 years. After 30 days of treatment, the donepezil group showed greater ability to retain the capacity to perform a set of complex simulator tasks than the placebo group, p < 0.05. Donepezil appears to have beneficial effects on retention of training on complex aviation tasks in nondemented older adults.

Publication Types:
Clinical Trial
Randomized Controlled Trial

PMID: 12105320 [PubMed - indexed for MEDLINE]

An article about memory

Can a pill boost your brain’s ability to hold information?

'Smart pills' make headway

Limiting doctors' prescribing power

Smart pill, anyone?

Enjoy! [thumb]

[lynx]

This is the first study on Aricept not done by the manufacturer. The results are anything but stellar. The upshot: Aricept is not worth it.

Compare this with Namenda and Aricept is a total bust.


Lancet. 2004 Jun 26;363(9427):2105-15.

Comment in:
Lancet. 2004 Jun 26;363(9427):2100-1.

Long-term donepezil treatment in 565 patients with Alzheimer's disease (AD2000): randomised double-blind trial.

Courtney C, Farrell D, Gray R, Hills R, Lynch L, Sellwood E, Edwards S, Hardyman W, Raftery J, Crome P, Lendon C, Shaw H, Bentham P; AD2000 Collaborative Group.

Trials Unit, University of Birmingham, Birmingham, UK.

BACKGROUND: Cholinesterase inhibitors produce small improvements in cognitive and global assessments in Alzheimer's disease. We aimed to determine whether donepezil produces worthwhile improvements in disability, dependency, behavioural and psychological symptoms, carers' psychological wellbeing, or delay in institutionalisation. If so, which patients benefit, from what dose, and for how long? METHODS: 565 community-resident patients with mild to moderate Alzheimer's disease entered a 12-week run-in period in which they were randomly allocated donepezil (5 mg/day) or placebo. 486 who completed this period were rerandomised to either donepezil (5 or 10 mg/day) or placebo, with double-blind treatment continuing as long as judged appropriate. Primary endpoints were entry to institutional care and progression of disability, defined by loss of either two of four basic, or six of 11 instrumental, activities on the Bristol activities of daily living scale (BADLS). Outcome assessments were sought for all patients and analysed by logrank and multilevel models. FINDINGS: Cognition averaged 0.8 MMSE (mini-mental state examination) points better (95% CI 0.5-1.2; p<0.0001) and functionality 1.0 BADLS points better (0.5-1.6; p<0.0001) with donepezil over the first 2 years. No significant benefits were seen with donepezil compared with placebo in institutionalisation (42% vs 44% at 3 years; p=0.4) or progression of disability (58% vs 59% at 3 years; p=0.4). The relative risk of entering institutional care in the donepezil group compared with placebo was 0.97 (95% CI 0.72-1.30; p=0.8); the relative risk of progression of disability or entering institutional care was 0.96 (95% CI 0.74-1.24; p=0.7). Similarly, no significant differences were seen between donepezil and placebo in behavioural and psychological symptoms, carer psychopathology, formal care costs, unpaid caregiver time, adverse events or deaths, or between 5 mg and 10 mg donepezil.
INTERPRETATION: Donepezil is not cost effective, with benefits below minimally relevant thresholds. More effective treatments than cholinesterase inhibitors are needed for Alzheimer's disease.

[nootropi]

Dement Geriatr Cogn Disord. 2004;18(1):50-4. Epub 2004 Apr 06. Related Articles, Links


Effects of cholinergic drugs and cognitive training on dementia.

Requena C, Lopez Ibor MI, Maestu F, Campo P, Lopez Ibor JJ, Ortiz T.

Universidad de Leon (Area de Psicologia), Leon, Spain.

A study was performed on patients with Alzheimer's disease (AD) in order to evaluate the efficacy of a combined treatment (donepezil plus cognitive training) in both cognitive processes and affective states. Eighty-six subjects, 25 men and 61 women, with an average age of 75.58 years, were studied. Almost all the subjects had a basic educational level. Donezepil was administered at a dose of 10 mg daily along with cognitive treatment involving images of everyday life and reminiscent music; the sessions took place on Monday to Friday and lasted three quarters of an hour. The study lasted 12 months. Subjects underwent test-retest with the following tests: Mini-Mental State Examination (MMSE), the cognitive subscale of the Alzheimer's Disease Assessment Scale (ADAS-cog); the Geriatric Depression Scale (GDS) and the overall deterioration scale (FAST). The results showed that subjects receiving the combined treatment had a better response than those who did not receive any cognitive training. These subjects' MMSE score decreased by 3.24 on average. The affective symptomatology of those receiving only drug treatment improved whereas the cognitive processes did not. Copyright 2004 S. Karger AG, Basel

PMID: 15084794 [PubMed - in process]

[nootropi]

Cholinergic enhancement of frontal lobe activity in mild cognitive impairment.

Saykin AJ, Wishart HA, Rabin LA, Flashman LA, McHugh TL, Mamourian AC, Santulli RB.

Brain Imaging Laboratory, Department of Psychiatry, Dartmouth Medical School, Lebanon, NH 03756, USA. Andrew.J.Saykin@dartmouth.edu

Cholinesterase inhibitors positively affect cognition in Alzheimer's disease (AD) and other conditions, but no controlled functional MRI studies have examined where their effects occur in the brain. We examined the effects of donepezil hydrochloride (Aricept) on cognition and brain activity in patients with amnestic mild cognitive impairment (MCI), a diagnosis associated with a high risk of developing AD. Nine older adults with MCI were compared with nine healthy, demographically matched controls. At baseline, patients showed reduced activation of frontoparietal regions relative to controls during a working memory task. After stabilization on donepezil (5.7 +/- 1.7 weeks at 10 mg) patients showed increased frontal activity relative to unmedicated controls, which was positively correlated with improvement in task performance (r = 0.49, P = 0.05) as well as baseline hippocampal volume (r = 0.62, P < 0.05). The patients' overall cognitive function was stable or improved throughout the study. Short-term treatment with a cholinesterase inhibitor appears to enhance the activity of frontal circuitry in patients with MCI, and this increase appears to be related to improved cognition and to baseline integrity of the hippocampus. These relationships have implications for understanding the mechanisms by which cognition-enhancing medications exert their effects on brain function and for the use of functional MRI in early detection and treatment monitoring of AD and MCI. Copyright 2004 Guarantors of Brain

[nootropi]

Effects of acute acetylcholinesterase inhibition on the cerebral cholinergic neuronal system and cognitive function: Functional imaging of the conscious monkey brain using animal PET in combination with microdialysis.

Tsukada H, Nishiyama S, Fukumoto D, Ohba H, Sato K, Kakiuchi T.

Central Research Laboratory, Hamamatsu Photonics K. K., Hamakita, Shizuoka 434-8601, Japan. tsukada@crl.hpk.co.jp

This study demonstrated the effects of acute acetylcholinesterase (AChE) inhibition by donepezil (Aricept) on the cerebral cholinergic neuronal system in the brains of young (5.2 +/- 1.1 years old) and aged (20.3 +/- 2.6 years old) monkeys (Macaca mulatta) in the conscious state. Donepezil at doses of 50 and 250 microg/kg suppressed AChE activity, analyzed by metabolic rate (k(3)) of N-[(11)C]methyl-4-piperidyl acetate ([(11)C]MP4A), in all cortical regions in a dose-dependent manner in both age groups. However, the suppression degree was more marked in young than in aged monkeys. AChE inhibition by donepezil resulted in a dose-dependent increase in acetylcholine levels in the prefrontal cortex of young animals as measured by microdialysis. Binding of (+)N-[(11)C]propyl-3-piperidyl benzilate ([(11)C](+)3-PPB) to cortical muscarinic receptors was reduced by donepezil, probably in a competitive inhibition manner. Aged monkeys showed less reduction of [(11)C](+)3-PPB binding than young animals. As evaluated by an oculomotor delayed response task, aged monkeys showed impaired working memory performance compared to young monkeys, and the impaired performance was partly improved by the administration of donepezil, due to the facilitation of the cholinergic neuronal system by AChE inhibition. These results demonstrate that the PET imaging technique with specific labeled compounds in combination with microdialysis and a behavioral cognition task could be a useful method to clarify the mechanism of drugs in the living brains of experimental animals. Copyright 2004 Wiley-Liss, Inc.

[nootropi]

1: Int J Geriatr Psychiatry. 2004 Jan;19(1):1-8. Related Articles, Links


Randomized placebo-controlled trial of donepezil in cognitive impairment in Parkinson's disease.

Leroi I, Brandt J, Reich SG, Lyketsos CG, Grill S, Thompson R, Marsh L.

Department of Psychiatry, North Manchester General Hospital, Manchester, UK. wendy.heap@mail.manhhc-tr.nwest.nhs.uk

OBJECTIVE: To evaluate the efficacy and safety of donepezil, an acetylcholinesterase inhibitor, as a treatment for cognitive impairment and dementia in patients with Parkinson' s disease (PD). METHODS: Using a randomized, double-blind, placebo-controlled design, nine patients received placebo and seven patients received donepezil (2.5-10 mg/day) for a mean (SD) duration of 15.2 (3.4) weeks. The primary efficacy outcomes were derived from a neuropsychological battery that assessed global cognitive status as well as memory, attention, psychomotor speed, and visuospatial and executive functions. Secondary efficacy outcomes were psychiatric symptom and activities of daily living ratings. Primary safety measures were motor signs and assessments of adverse effects. RESULTS: Patients on donepezil showed selective and significant (p<0.05) improvement on the memory subscale of the Dementia Rating Scale. There was also a trend toward improvement on a measure of psychomotor speed and attention. There were no group differences in psychiatric status, motor function, or activities of daily living as measured at baseline or end-point. Adverse effects resulted in premature withdrawal of four patients on donepezil, two for peripheral cholinergic effects and one for increased parkinsonism. Side effects were associated with dosage increases. CONCLUSION: Donepezil has a beneficial effect on memory and may improve other cognitive deficits in patients with PD and cognitive impairment. However, variable tolerability in our sample underscores the need for careful monitoring when prescribing donepezil to patients with PD, especially with dosage increases. Copyright 2004 John Wiley & Sons, Ltd.

[nootropi]

Donepezil in a chronic drug user--a potential treatment?

Jovanovski D, Zakzanis KK.

Department of Life Sciences, University of Toronto, Ontario, Canada.

The objective of the current study was to explore the potential cognitive benefits of an anticholinesterase inhibitor, donepezil, in a former chronic drug user. A neuropsychological test battery composed of the vocabulary and matrix reasoning subtests of the Wechsler adult intelligence scale-III, measures of everyday executive functioning (behavioural assessment of the dysexecutive syndrome [BADS]), and verbal learning and memory tasks (California verbal learning test-II; Rivermead behavioural memory test) was completed at baseline, at 3 months after introducing donepezil, and at 3 months after donepezil was discontinued. After donepezil treatment, substantial improvements were found on tasks of nonverbal fluid reasoning (i.e. matrix reasoning) and other executive functioning tests (i.e. BADS). At entry into the study, poor academic performance and subjective problems with memory and concentration were reported, particularly after amphetamine use (i.e. MDMA and crystal methamphetamine); after donepezil treatment, dramatic increases in memory, concentration and academic achievement were observed. The finding of improvements in tests of executive functioning and in academic performance in this case study, together with the minimal adverse side effects of donepezil, warrants the investigation of controlled studies of cholinergic enhancement in chronic amphetamine and other drug users. Copyright 2003 John Wiley & Sons, Ltd

[nootropi]

Augmenting atypical antipsychotics with a cognitive enhancer (donepezil) improves regional brain activity in schizophrenia patients: a pilot double-blind placebo controlled BOLD fMRI study.

Nahas Z, George MS, Horner MD, Markowitz JS, Li X, Lorberbaum JP, Owens SD, McGurk S, DeVane L, Risch SC.

Brain Stimulation Laboratory, Center for Advanced Imaging Research, Department of Psychiatry, Medical University of South Carolina, Charleston, SC 29425, USA. nahasz@musc.edu

Cognitive impairments are cardinal features of schizophrenia and predictors of poor vocational and social outcome. Imaging studies with verbal fluency tasks (VFT) lead some to suggest that in schizophrenia, the combination of a failure to deactivate the left temporal lobe and a hypoactive frontal lobe reflects a functional disconnectivity between the left prefrontal cortex and temporal lobe. Others have theorized that an abnormal cingulate gyrus modulates such fronto-temporal connectivity. Thus addition of a cognitive enhancing medication to current antipsychotic therapy might improve functionality of networks necessary in working memory and internal concept generation. To test this hypothesis, we serially measured brain activity in 6 subjects on stable atypical antipsychotics performing a VFT, using BOLD fMRI. Measurements were made at baseline and again after groups were randomized to receive 12 weeks of donepezil (an acetylcholinesterase inhibitor) and placebo in a blind cross-over design. Donepezil addition provided a functional normalization with an increase in left frontal lobe and cingulate activity when compared to placebo and from baseline scans. This pilot study supports the cingulate's role in modulating cognition and neuronal connectivity in schizophrenia.

[nootropi]

Effectiveness of donepezil on several cognitive functions in patients with Alzheimer's disease over 12 months]

[Article in Spanish]

Lopez-Pousa S, Vilalta-Franch J, Garre-Olmo J, Turon-Estrada A, Lozano-Gallego M, Hernandez-Ferrandiz M, Fajardo-Tibau C, Cruz-Reina MM.

Unitat de Valoracio de la Memoria i les Demencies, Hospital Santa Caterina, Institut d'Assistencia Sanitaria, Girona. uvamid@yahoo.es

OBJECTIVES: The efficacy of donepezil for the treatment of cognitive dysfuntion in Alzheimer's disease has been demonstrated. The objetive of this study was to evaluate the effectiveness of donepezil in different neuropsychological areas of mild or moderate AD patients over a period of twelve months compared with data from untreated patients (historical control). METHODS: This was an open-label study where 100 patients received donepezil 5mg or 10 mg/day for twelve months. Because the study was uncontrolled, data were compared with historical data from 81 patients who had not received anticholinesterase inhibitors. The CAMCOG neuropsychological battery was used in both groups at baseline and at month 12. RESULTS: A hundred patients (30% male and 70% female) were enrolled in the study receiving donepezil 5 or 10 mg/day (average age: 74.3 6.1 years). The historical control group consisted of 81 people (average age 72.9 6.5 years), 29.6% of whom were men. There were no significant differences with respect to age, sex and CAMCOG score at baseline. The differences within the groups were significant in the following neuropsychological areas: recent, remote and learning memory, attention, calculation and abstract verbal thinking. Differences in expressive language and learning memory between both groups were confirmed by the multivariative analysis of baseline. CONCLUSION: The rate of cognitive deterioration observed in mild to moderate AD patients receiving open-label donepezil treatment was less than expected if this cohort had not been treated. The cognitive beneficial effects observed during one year treatment with donepezil were mainly focused on memory and verbal expression.

[wis]

[montana2012]

I bought this genuine product  from a pharmacy overseas over the counter for $9-10, if I remember correctly. Mine was the 10mg version.

 

http://static1.frama...donecept5mg.jpg

 

It doesn't do much for me though, except for making me extremely sleepy and sleep 14h/day.

Edited by montana2012, 10 June 2014 - 02:08 AM.

[John Katz]

Aricept Evess, 10 mg, 28 tablets Pfizer - 75$ box