Exelon (rivastigmine tartrate)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Indicated for the treatment of mild to moderate dementia of the Alzheimer's type
Exelon has been approved in oral solution and capsule
form for the treatment of mild to moderate Alzheimer's disease.
This drug belongs to the class of drugs called cholinesterase
inhibitors. Cholinesterase breaks down acetylcholine, a
neurotransmitter which assists in human memory and cognition
processes. By inhibiting cholinesterase, more acetylcholine
available to the patient for memory and cognitive functioning. This
is effective in treatment of Alzheimer's disease, since
acetylcholine is at significantly lower levels in Alzheimer's
patients than in normally functioning people.
Exelon has been shown to improve patients' performance in
the three major domains of assessment of Alzheimer's: global
functioning (such as activities of daily living), behavior, and
Another long term advantage to the drug is that it could treat
symptoms early on in the deterioration process. Delaying the onset
of the disease by five years in patients could save up to $50
billion in U.S. healthcare costs annually (half of the current
Currently, 70 countries have approved Exelon for marketing.
Alzheimer's Disease is a neurodegenerative
disease affecting up to 4 million adults in the U.S. and 10 million
worldwide. Memory loss and other cognitive and behavior
deteriorations are symptoms of the disease. As there is no current
cure, Alzheimer's Disease is fatal.
The safety and efficacy of Exelon was investigated in two
placebo-controlled investigations. Participants, all
Alzheimer's patients, were evaluated in terms of their
cognitive performance using the Alzheimer's Disease Assessment
Scale (ADAS-cog) and the Clinician's Interview Based Impression
of Change (CIBIC-Plus). The ADAS-cog considers elements of memory,
orientation, attention, reasoning, language and praxis. Improvement
in global functioning was measured by the CIBIC-Plus. This
instrument of evaluation considers overall patient cognition,
behavior and functioning. The patient population for this study
reflected a real world population, since most of the patients used
concomitant medications to treat other conditions during the
In a 26-week, U.S. study, patients were divided into three
groups, each receiving 1-4 mg/day of Exelon, 6-12 mg/day of Exelon,
or placebo. At the end of the treatment period, both ADAS-cog
scores and CIBIC-Plus ratings for those treated in either
dose-group of Exelon were significantly superior than scores of
those who took placebo. Furthermore, the higher-dosage group had
better ADAS-cog scores and CIBIC-Plus ratings than the lower-dosage
group. Better scores in these assessments indicate greater
improvement and less worsening in cognitive function (such as
memory, recognition, ability to speak, and other symptoms of
dementia) than the average placebo-treated patient.
In a 26-week, global study, patients were divided into similar
groups. Results of this study also indicated that the 6-12 mg/day
group showed significantly better ratings for CIBIC-Plus than
placebo, and significantly better scores on the ADAS-cog scale,
compared to placebo and the 1-4 mg/day group. However, the
1-4 mg/day treatment group did not improve significantly over
placebo with either assessment tool.
To date, 5,300 patients have received Exelon in clinical
research studies. This is considered the largest phase III program
of an Alzheimer's treatment.
The following are the most common side effects of Exelon, as
experienced by patients in clinical studies:
- Weight loss*
*26% of women, and 18% of men in the high-dose group
The above effects were experienced with greater frequency
earlier in the treatment.
Mechanism of Action
Pathological changes in Dementia of the Alzheimer's type
involve cholinergic neuronal pathways that project from the basal
forebrain to the cerebral cortex and hippocampus. These pathways
are thought to be intricately involved in memory, attention,
learning, and other cognitive processes. While the precise
mechanism of rivastigmine's action unknown, it is postulated to
exert its therapeutic effect by enhancing cholinergic function.
This is accomplished by increasing the concentration of
acetylcholine through reversible inhibition of its hydrolysis by
cholinesterase. If this proposed mechanism is correct, Exelon's
effect may lessen as the disease process advances and fewer
cholinergic neurons remain functionally intact. There is no
evidence that rivastigmine alters the course of the underlying
dementing process. After a 6 mg dose of rivastigmine,
anticholinesterase activity is present in CSF for about 10 hours,
with a maximum inhibition of about 60% five hours after
(From FDA Label)
Visit the Novartis
Pharmaceuticals U.S. web site to learn more about Exelon and
about other products, research, and services provided by the
company that developed this drug.
For more information about Alzheimer's Disease, visit
Novartis's Alzheimer's Disease site:
http://www.alzheimersdisease.com, designed to educate and support
Alzheimer's patients' caregivers.
or visit the
Alzheimer's Association web
site, which provides information for patients, families,
physicians, as well as recent research and glossary about