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Exelon is a selective acetyl- and butyrylcholinesterase inhibitor of the brain used to treat Alzheimer's disease and dementia in Parkinson's disease.
Rivastigmine slows down the destruction of the acetylcholine mediator produced by functionally intact neurons. While rivastigmine selectively increases the content of acetylcholine in the cerebral cortex and the hippocampus, and, thus, helps to improve cholinergic nervous transmission.
Ekselon may have a positive effect on reducing cognitive functions associated with acetylcholine deficiency, particularly in dementia associated with Alzheimer's disease and Parkinson's disease.
In addition, there is evidence that inhibition of cholinesterase can slow down the formation of fragments of the protein precursor of beta-amyloid, which is involved in amyloidogenesis, and thus slow down the formation of amyloid plaques, which is one of the main pathological signs of Alzheimer's disease.
Rivastigmine interacts with the target enzyme to form a covalent bond, which leads to a temporary inactivation of the enzyme. It was shown that in young healthy men after taking Ekselon at a dose of 3 mg, acetylcholinesterase activity in the cerebrospinal fluid (CSF) decreases by approximately 40% during the first 1.5 hours. After reaching the maximum inhibitory effect, the enzyme activity returns to its original level after about 9 hours. It was shown that the activity of butyrylcholinesterase in CSF in young healthy volunteers is inhibited reversibly and is restored to the original after 3-6 hours. In patients with Alzheimer's disease, rivastigmine inhibition of acetylcholinesterase activity in CSF is dose-dependent in the studied dose range (up to the highest dose of 6 mg twice a day). AND
The inhibition of butyrylcholinesterase is also dose-dependent: a dose of 6 mg 2 times a day causes a decrease in enzyme activity by more than 60% compared to the original. This effect of Ekselon remained for 12 months of therapy (the maximum studied period). Statistically significant correlations between the degree of rivastigmine inhibition of both enzymes in CSF and changes in cognitive functions in patients with Alzheimer's disease were shown; at the same time, it is precisely inhibition of butyrylcholinesterase in CSF that reliably and stably correlates with an improvement in the results of tests of memory, attention and speed of reaction.
The efficacy of treatment with Exelon in Alzheimer's disease has been shown in patients with mild to moderate dementia (10–24 points on the short scale for assessing mental status, Mini Mental State Examination, MMSE). According to clinical studies, Exelon therapy leads to a significant improvement in cognitive functions (attention, memory, speech, etc.), functional status and activity in everyday life, as well as a decrease in the severity of the disease and severity of mental and behavioral manifestations (such as agitation, tearfulness, illusions, hallucinations, etc.).
Studies have shown that the effect of treatment with Ekselon is observed at about the 12th week and lasts for 6 months of therapy, while during the control period in the group of patients who received placebo, the deterioration of the corresponding indicators was observed.
In dementia associated with Parkinson's disease, the efficacy of Exelon has been demonstrated in a 24-week placebo-controlled study in patients with mild and moderate dementia (10 - 24 points for MMSE). In patients treated with Exelon, there was a statistically significant improvement in cognitive functions (attention, memory, speech, etc.), while in patients treated with placebo, similar indicators worsened.
Mild or moderately severe Alzheimer's-type dementia:
- Probable Alzheimer's disease.
- Alzheimer's disease.
1 TTS contains:
Active substances: rivastigmine 13.3 mg.
Excipients: D, L-α-tocopherol, poly (butyl methacrylate, methyl methacrylate), acrylic copolymer.
The composition of the adhesive layer: silicone copolymer, dimethicone (silicone oil 12.500 cSt), D, L-α-tocopherol.
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