Dimebolin has shown to inhibit brain cell death in clinical studies of Alzheimer's disease and Huntington's disease.
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Dimebolin: Medications and Prescriptions
Generic name: dimebolin Product Brand Name: Dimebon (Russia), Latrepirdine (USA) Product Manufacturer: made in Russia
Dimebolin description
This new drug for Alzheimer works by blocking mitochondrial pores, which are believed to play a role in the cell death that, is associated with neurodegenerative diseases and the aging process. Customers can buy dimebolin online from the trustworthy and reliable pharmaceutical sites.
Currently Medivation jointly owns a patent application for the use of Dimebon for the treatment of Alzheimer’s disease which will expire in 2021. According to Medivation studies, the first pivotal trial of Dimebon had shown behavioral symptoms stability in patients with mild-to-moderate Alzheimer's disease, resulting in decreased caregiver distress.
Dimebolin does have a number of predicted side effects such as dry mouth as do most of the older non-specific antihistamines have.
Dimebolin hydrochloride (Dimebon™) is an orally-available, small-molecule agent that is in clinical testing for the treatment of Alzheimer's and Huntington's diseases-two progressive, devastating conditions with limited treatment options. Based on clinical and preclinical data generated to date, developer Medivation believes that dimebolin operates via a novel mechanism of action and may exert a neuroprotective effect in multiple areas of the central nervous system. Dimebolin appears to block a new target that involves mitochondrial pores, which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process. Dimebolin also blocks both cholinesterase and the NMDA receptor simultaneously. These two targets provide the mechanism of action for all FDA-approved drugs for Alzheimer's disease, although no marketed drug is known to have an effect on both pathways.
In July, the Huntington Study Group (HSG) reported that recruitment of participating sites for the DIMOND phase II trial (ClinicalTrials.gov identifier: NCT00497159), which will evaluate dimebolin in subjects with mild to moderate Huntington's disease (HD), is currently in progress. The randomized, double-blind, placebo-controlled phase II trial will enroll up to 90 patients at some 15 research centers in the U.S. and U.K. It is designed to evaluate the safety and tolerability of dimebolin during three months of treatment, as well as its effects on cognition, motor signs and overall functioning of HD patients aged 18 years or older.
In June, the company reported that benefits of dimebolin hydrochloride over placebo in a double-blind, placebo-controlled phase II study in mild to moderate Alzheimer's disease (AD) were statistically significant on all five study endpoints at 12 months. In the multicenter, double-blind trial, 183 patients with mild to moderate AD were randomized to oral dimebolin (60 mg/day) or placebo for six months. Of these patients, 134 subsequently consented to continue treatment for up 12 months in their same treatment group. On the primary endpoint, the ADAS-cog, dimebolin caused an improvement over placebo of 6.9 points at one year. On the global function endpoint used in this study, the CIBIC-plus, dimebolin's benefit over placebo was 0.8 points at 12 months. Global function improved or remained stable in 69% of treated Alzheimer's disease patients after one year of dimebolin therapy. Dimebolin produced an aggregate benefit over placebo in this study that was larger at 12 months than at six. After a year of treatment, dimebolin's benefit over placebo was greater than six-month levels on the ADAS-cog (6.9 points vs. 4.0 points), CIBIC-plus (0.8 points vs. 0.6 points), and ADCS-ADL (5.2 points vs. 2.9 points) scales; however, only the ADAS-cog difference reached statistical significance. Dimebolin's benefit over placebo on the other two endpoints (the Mini Mental State Exam, [MMSE] and the Neuropsychiatric Inventory [NPI]) at six months was maintained at one year. Dimebolin-treated patients experienced significantly fewer serious adverse events than placebo-treated patients (3.4% vs. 11.7%). The most frequent adverse events associated with treatment were dry mouth, depressed mood/depression and sweating. Six-month phase III studies of dimebolin in AD will begin next year.
Dimebolin hydrochloride, which also acts as an antihistamine, is marketed in Russia by the Russian Academy of Sciences for the treatment of skin allergy and allergic rhinitis.
Dimebon notes:
"Understanding Dimebon As A Cure For Alzheimer’s Disease"
Alzheimer’s disease is perhaps one of the most feared conditions of old age, affecting, as it does, the very essence of a person as it gradually destroys the mind. This neurodegenerative disease not only causes memory loss but also gradually reduces the ability of sufferers to perform even the most mundane of everyday tasks. Although, this most common form of dementia generally affects those in the over 65-age group, younger people have been diagnosed with the disease. Until recently treatment for this disease has been main symptomatic. Now, however research has proved that a drug named Dimebon may help in retarding the progress of the disease.
First produced in Russia more than 20 years ago, Dimebon is an antihistamine that can help improve the memory, thought process, and overall performance of patients suffering from Alzheimer’s disease. In fact, until recently this drug could be purchased over-the-counter, in Russia, where it was known by the generic name Dimebonum. However, as new antihistamine drugs came to the market, the popularity of Dimebon decreased. Eventually it was withdrawn from sale and its commercial production ceased. Recently however, interest in the drug was revived as it was realised that it had some positive effect in slowing down the progress of Alzheimer’s disease.
Now the drug is undergoing clinical tests in both the United States and Russia because of its ability to obstruct the receptor indicating route of N-methyl-D-aspartate and cholinesterase, which play a vital part in neurodegenerative ailments. Dimebon is a tiny molecule, which pre-clinical examinations have shown, can slow down the death of brain cells in Alzheimer's disease. Further research has indicated that the drug can improve mental awareness, perception, reasoning, and judgment in people who are otherwise healthy.
Although, the exact mechanism of how Dimebon works, is, as yet, unknown, it is speculated that it might actually protect the mitochondria inside the cells from injury, which can be vital in preventing the death of the cell. The medicine seems to follow varied methods of action including causing hindrance to the working of some specific proteins and slowing down the L-type calcium channels that transform the action of some other elements present in the brain.
In a clinical trial aimed at finding the effects of the drug on patients suffering from Alzheimer’s disease, a study was conducted on 183 patients who were at different stages of the disease. The patients were randomly chosen to receive an oral dose of 20 mg Dimebon three times daily while others in the trial were given an equivalent dose of placebo. Evaluation of the ability of the mental process of perception, awareness reasoning etc., was measured as well as any alteration of original behaviour compared to behaviour observed after 26 weeks of treatment.
This study was carried out for an extended period of six months, with neither the patients nor the observers aware of which patients were receiving actual treatment and which were receiving the placebo. The trial included 155 patients of which, 78 patients had been put on Dimebon treatment while 77 were given a placebo. The patients who were treated with Dimebon showed considerable improvement over the 26 week trial period with significant improvement in memory, performing everyday activities, personal behaviour, and overall function.
The patients were also examined for any side effects that might have been caused by Dimebon but in general the drug was well tolerated. Side effects observed were moderate and included drowsiness, dryness of the mouth and depression. It was also found that the caregivers of the patients who were also given Dimebon felt relaxed as they faced much lower stress levels along with the decreased time required to care for patients.
The positive results of this initial trial have raised even more interest in the use of Dimebon as a drug for hindering the progress of Alzheimer’s disease. New clinical trials are being planned with a new set of patients known to be suffering from mild-to-moderate Alzheimer’s disease. In the latest trials, patients who are already taking other Alzheimer’s disease medications like donepezil have also been included. Additional medical trials for patients suffering from moderate-to-severe Alzheimer’s disease are also being planned.
The initial success of Dimebon in treating Alzheimer’s disease has brought a ray of hope to millions of people who are suffering from this disease as well as hope to their caregivers. Even although the drug has shown great improvement in patients with mild-to-moderate Alzheimer’s disease, its effect on people with moderate-to-severe Alzheimer’s disease is still a matter of speculation. Additional medical trials are essential for ascertaining the benefits of Dimebon in addition to ascertaining the response rates at various stages of the disease.
If further trials prove successful, it will revolutionise the approach to treating this disease. It has also been announced that by 2011, Dimebon will be launched in the US markets.
Cassels, C., (2008) Dimebon Improves Clinical Course of Alzheimer's Disease retrieved on 5th November 2009 from: Medscape Medical News
Van Marum MD, PhD (2009) Do Amyloid-lowering Strategies Work Clinically? Therapeutic Advances in Neurological Disorders published 30/01/09 Therapeutic Advances in Neurological Disorders
DeArment, A., (2009) Pfizer, Medivation to commence phase 3 trials for Alzheimer's disease treatment retrieved on 5th November 2009 from: http://drugstorenews.com/(S(wu0mlefyo5d2uoqa0tb3m455))/story.aspx?id=121133&menuid=335
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