Dimebon

Known by the brand name Dimebon, Dimebolin hydrochloride is an antihistamine drug. It has been used clinically in Russia since 1983.[1] Research is continuing in both Russia and western nations into possible applications as a potential nootropic and neuroprotective.(2). The drug is an orally active small molecule that has been shown to trim down brain cell death in preclinical studies of Alzheimer's disease and Huntington's disease, making it a probable treatment for these and other neurodegenerative diseases. Research recommends that it may also have cognition-enhancing effects in healthy individuals, in the absence of neurodegenerative disease pathology.

Medications and Prescriptions

Generic name: dimebolin

Product Brand Name: Dimebon (to be marketed in USA as Latrepirdine)

Product Manufacturer: made in Russia

Alzheimer's disease
After being shown to have positive effects on persons suffering from AlzheimerЎЇs disease, dimebolin has attracted renewed interest in recent times. Animal studies showing probable beneficial effects on Alzheimer's disease models were shown in Russian research in 2000.[4] Beginning results from human trials have also been promising. Results have shown that at 12 months there was significant improvement over placebo in an initial six-month phase II trial.[5] Dimebolin showed promising results in a Phase III-equivalent double blind trial in Russia with mildЁCmoderate stage patients.[6][7] Apr 2009 Pfizer and Medivation initiate a phase III trial (CONCERT study) aiming for FDA approval. [8] On July 2009 Pfizer and Medivation announced that latrepirdine will be the proposed international nonproprietary name for Dimebon for the treatment of Alzheimer's.[9]


Pharmacology:
Dimebolin appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels,[10] modulating the action of AMPA and NMDA glutamate receptors,[11] and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores,[12] which are supposed to play a function in the cell death that is related with neurodegenerative diseases and the aging procedure.[13] It also blocks a number of other receptors including alpha-Adrenergic receptors and the serotonin receptor subtypes 5-HT2C, 5-HT5A and 5-HT6.[14]
Usage: 20 mg orally three times every day.

Interpretation: With mild-to-moderate Alzheimer's disease, Dimebon was well tolerated, and considerably improved the clinical course of patients.
Additional analyses of the dimebon essential study data presented at medical conferences showed that:

Dimebon is impact extended to caregivers, reducing caregiver distress and time spent caring for patients each day.

The drug had medical advantage continued through 18 months. These results were based on data from a six-month, open-label extension of the 12-month placebo-controlled study of dimebon in patients with mild-to-moderate Alzheimer's disease.


Dimebon notes:
Chemically known as dimebolin, Dimebon is an older Russian antihistamine drug that has recently been discovered to be most useful in treating patients with Alzheimer’s disease. Currently the medicine is in clinical trials in the United States under Medivation pharmaceutical company. As a cognitive enhancer, it has shown competence in all measures of cognition and behavior in mild-to-moderate Alzheimer disease patients.

Dimebon mechanism of action includes inhibiting L-type calcium channels and blocking the action of neurotoxic beta-amyloid proteins. At present, Medivation together owns a patent application for the use of Dimebon for the treatment of Alzheimer’s disease. The proposed generic name for Dimebon is Latrepirdine.
The predicted side effects of the drug incorporate dry mouth, drowsiness and depression or depressed mood. It has been reported that customers in USA will be capable to purchase Dimebon by 2011. In Russia, Dimebon was known by the generic name dimebonum.