- Rivastigmine (Exelon) is one of five drugs the FDA approves for the treatment of Alzheimer’s disease.
- It works by boosting a neurotransmitter called acetylcholine.
- It comes in capsule form, as a solution, and also as a patch.
- Research has shown notable benefits from Rivastigmine on memory and cognitive function.
- Tolerable side effects can include nausea, dizziness, weakness and possible diarrhea.
- More severe potential side effects can include abdominal pain, tremors, and fainting.
- Signs of overdose include blue skin, chronic vomiting, and chest pain.
- Exelon interacts with hundreds of drugs, though only a dozen seriously.
- Final thoughts: medications can help provide temporarily relief.
Rivastigmine, the generic form of Exelon, is a drug used principally for the treatment of Alzheimer’s disease and Parkinson’s disease, although it is also used to mitigate particular symptoms that present in other types of dementia. Rivastigmine is in a class of medications called cholinesterase inhibitors. These medications work by stopping the breakdown of acetylcholine, thus enhancing synaptic transmissions in the brain, essentially those brain connections associated with memory and other cognitive functions. People with Alzheimer’s, Parkinson’s, and some other types of dementia are known to typically have diminished levels of the acetylcholine chemical in the brain.
Alzheimer’s is a degenerative disease of the brain that gradually impacts a person’s memory, causing confusion, disorientation, other altered thought processes, and problems with communicating. Alzheimer’s is a progressive disease that over time spreads to all areas of the brain. There are currently nearly 50 million people with Alzheimer’s worldwide, a number that is expected to increase drastically in upcoming decades.
Parkinson’s is a brain and nervous system disease that causes memory loss, muffled speech, difficulties interpreting visual information, rapid eye movement (REM) sleep disorder, shaking, visual hallucinations, and various other symptoms. In Parkinson’s, the brain damage is located in the region of the brain that plays a key role in a person’s ability to move. These symptoms arise from microscopic deposits of Lewy Bodies in the brain. Parkinson’s currently affects 2 percent of those age 65 and over, with the number of Americans with Parkinson’s thought to be nearing the one million mark.
Dementia is an umbrella term for many different diseases, each of them brain disorders that disrupt individuals’ daily lives and impact their abilities to perform activities of daily living (ADLs). Dementia occurs when nerve cells in one or more parts of the brain are damaged, and people with dementia experience several different symptoms, depending on the location and severity of the damage in the brain. The cognitive symptoms of dementia typically include memory loss, confusion, loss of visual and spatial skills, and difficulties articulating thoughts, while behavioral symptoms include crankiness, mood changes, agitation, lack of self-control, poor judgment, hallucinations, and wandering.
Rivastigmine is a reversible inhibitor of both the acetylcholinesterase and butyrylcholinesterase enzymes. A reversible inhibitor is a molecule that attaches to an enzyme and inhibits its functions. In so doing, a reversible enzyme can destroy a pathogen, which is something that carries a disease, or it can redress a metabolic imbalance, which is to bring back to functioning status that life-sustaining chemical activity that, for example, turns sugar into energy.
Because of those abilities, there is a profusion of drugs that are enzyme inhibitors, and Rivastgmine is one of them. Most of the other enzyme inhibitors are not usually prescribed for the treatment of Alzheimer’s.
The acetylcholinesterase that Rivastgmine inhibits is an enzyme that acts as a neurotransmitter to the brain; neurotransmitters are stored in nerve cells in the brain and nervous system, and this neurotransmitter serves to end synaptic (inter-neuron) communications. The butyrylcholinesterase that it inhibits is an enzyme that is manufactured in the liver and found in blood plasma (the liquid part of blood), and it also indicates the presence of a pathogen.
With those two actions, Rivastigmine works by stopping the breakdown of acetylcholine. It thus enhances synaptic transmissions in the brain, particularly those associated with memory and other cognitive functions.
Exelon, the brand name of Rivastigmine, can therefore be prescribed for patients to treat mild to moderate dementia caused by Alzheimer’s or Parkinson’s disease. The generic Rivastigmine system is used in any of its forms (oral or transdermal) in the treatment of confusion and other cognitive disorders associated with both Alzheimer’s disease and Parkinson’s disease. It does not cure those diseases (both Alzheimer’s and Parkinson’s are degenerative and incurable diseases). However, it may provide some relief and decrease or delay symptoms for some period of time.
Exelon is commonly taken twice daily, either for oral treatment with capsules or liquid solutions to be taken by mouth, or for transdermal treatment with patches.
Doctors commonly start individuals with low dosages, twice a day, to be taken morning and evening and preferably with food, as it may cause nausea, vomiting, loss of appetite, and other side effects when taken on an empty stomach. The dosage that your physician may start you off with will depend on your specific condition and other factors that the physician will ascertain after examining you and taking measure of your medical history, family history, age and mental condition.
It is important that you follow your doctor’s prescribed dosage and daily repetitions carefully, and to never deviate from what the doctor prescribed. If you have any questions about the medication, for example in regard to how to measure the drug for the solution, or in regard to its interactions with other medications or foods you may have started ingesting since your last visit to your doctor, you can ask your pharmacist or physician. In addition, never stop taking Exelon, even if you are feeling better, without first checking with your physician. Finally, to help you remember taking your medication, take it regularly at the same time of day.
It is common for physicians to start treatment with a low dosage that can then be increased once every 2 weeks to reach the desired long-term maintenance level. The maximum recommended dose is 6 milligrams twice a day for adults. Exelon oral solution may be swallowed directly from the syringe or mixed with a liquid prior to use. It can be taken plain or mixed with a small glass of water, cold fruit juice, or soda; when mixing it, stir the mixture well and, once mixed, take the solution within 4 hours.
Exelon oral solution is a clear yellow liquid comprising 2 mgs of the drug per milliliter. The capsule comes in doses of:
The transdermal patch comes in doses of:
The transdermal patch is used once a day since its effect lasts for 24 hours. In order to avoid skin irritation, it should be applied daily on different spots of the body, and never on reddish skin, or skin that is already irritated or cut. By way of transdermal absorption, the patch provides steady plasma absorption of Rivastigmine, avoiding it being metabolized and neutralized in the liver and intestine. Physicians like it also because it produces considerably fewer gastrointestinal complications while providing patients with higher therapeutic doses.
Studies have repeatedly shown some benefits in cognitive function accruing to individuals with Alzheimer’s taking Rivastigmine versus others who don’t. To cite one study that compared patients with mild to moderate Alzheimer’s taking a daily dose that ranged in strength with others who were not given the drug, it was demonstrated that those who did not take Rivastigmine showed no abnormal change, whereas those who took Rivastigmine capsules showed some dose-associated benefits, particularly on general function such as with ADLs (activities of daily living).
Other studies in Europe showed demonstrably similar outcomes with Rivastigmine. The skin patch formulation was evaluated in a study of 1,195 patients with mild to moderate Alzheimer’s and, once again, participants who were given a daily dose of the Rivastigmine patch outperformed those who did not, with a majority of caregivers who attended to the patients proclaiming that the 13.3mg/24-hour patch was not only more effective than taking the drug orally, but it also produced far fewer gastrointestinal issues.
The typical dosage of Exelon to treat Alzheimer’s disease is 6-12 mg/day, given twice daily with food. The dosage of Exelon to treat Parkinson’s disease is 3-12 mg/day, given twice daily with food.
Five drugs are currently FDA-approved for the treatment of Alzheimer’s; they are also used to treat Parkinson’s disease and other conditions, although they are specifically approved for the treatment of AD. These are:
- Rivastigmine (Exelon and Exelon patch)
- Memantime (Namenda and Namenda XR)
- Donepezil (Aricept and Aricept dissolvable tablet)
- Galantamine (Razadyne and Razadyne ER)
- Tacrine (Cognex)
Although various other medications are continually being prescribed in attempts to treat dementia symptoms, these are the only ones that have, under the appropriate testing standards, demonstrated to be effective in delaying the onset of Alzheimer’s, or slowing the progression of some symptoms of the disease.
Some other drugs prescribed might include anti-inflammatory medications such as Advil, Motrin and Celebrex, Eldepryl (Selegiline) for Parkinson’s, and statins that are prescribed to lower cholesterol levels.
Many of the side effects are mild and do not require medical attention. They are of the type that people taking Rivastigmine get used to over a short period of time before they disappear altogether. It is nevertheless important to keep a check of what your loved one is feeling, just in case one or more of the more severe side effects crop up, in which eventuality it would be critically important to consult with his or her physician.
The less serious and more common side effects of Rivastigmine Tartrate include:
- Dizziness and weakness, i.e. a diminished strength in muscles and muscle groups, and loss of muscle function
- Diarrhea, nausea and vomiting, these being symptoms of underlying gastrointestinal issues and upset stomach or indigestion
- Weight loss and loss of appetite, medically called anorexia, and frequently of a reversible nature
- Swelling in hands and feet, and joint pain
- Coughing, runny nose, and increased sweating
- Headache and shakiness or tremors
- Insomnia and sleep disturbance
More serious and far less common side effects of Rivastigmine tartrate can include:
- Trouble urinating, possible constipation, bloating and full feeling
- Black or tarry stool, and vomit that looks like coffee grounds, which may indicate there is considerable internal bleeding
- Slow or irregular heartbeat, lightheadedness, and fainting (syncope), which is a temporary partial or complete loss of consciousness with reflexive recovery
- Considerable stomach or abdominal pain, constipation, and unusual fatigue
- Chest pain, discomfort and seizures (convulsions)
- Loss of balance control, shuffling walk, twisting movements of the body, difficulty with speech, and drooling
- Uncontrolled movements, particularly of the face, back, and neck
- Aggression, confusion, depression
- Hallucinating, i.e. seeing, hearing, or sensing things or people that are not there
Dan’s Mom, the story of a person with Alzheimer’s
Dan’s 77-year old mom was diagnosed with mild Alzheimer’s roughly two years ago. Since then, and having stocked up on some reading material on Alzheimer’s, Dan thought that she had progressed to the “mild to moderate” stage. Her doctor recently started her on 1.5 mg capsules of Exelon that Dan made sure she took mornings and evenings, and always just after a meal. Three weeks later, the doctor increased the dosage to 3 mgs, and then three more weeks later to 4.5 mgs He explained that this method would get her gradually to the desired long-term dose of 4.5 mgs, which he estimated to be the appropriate maintenance level given her age and other physical health. “Any faster way of getting her up there might well produce undesirable side effects,” he told Dan.
She did not take well to the higher dosage however. Dan’s mom at first showed signs of nausea and constipation, and a few days later, she started vomiting two or three times a day, alarming enough for Dan to take her back to the doctor. The doctor promptly took her off of the capsules and put her instead on the Exelon patch, starting again with the low dosage of 4.6mg/24-hour, and taking it up to 9.5mg/24-hour four weeks later.
This time, the patch worked well. Not only did Dan’s mom stop showing signs of gastrointestinal stress but, over the three or four months that followed, she began to do a better job of dressing herself and even brushing her hair. She also brightened up a little, although Dan confessed to himself that he may have imagined that kind of improvement. There were nevertheless other clear signs that her cognitive faculties, and particularly her memory, had improved a little. Dan now continues to give her the patch, each day on a different spot on her skin so as not to irritate the skin.
The use of more than one Exelon patch at a time may cause an overdose. The patch itself may cause redness or other skin irritation; this does not indicate that you have an allergy to Exelon for it is a temporary reaction to the materials of the patch itself and not to Rivastigmine. If, on the other hand, you do have a reaction to Rivastigmine, your physician may merely replace the patch with an oral solution.
One or more of the following symptoms may additionally indicate an overdose and will necessitate medical emergency treatment:
- Pale or discolored (bluish) skin, lips, and fingernails
- Shortness of breath, trouble breathing, and slow or irregular heartbeat
- Chest pain or significant discomfort
- Severe or chronic vomiting and severe nausea
- Increased sweating and increased watering of the mouth or drooling
- Lightheadedness, dizziness or unconscious spells (fainting)
- Extreme fatigue
People who weigh less than 110 lbs should be monitored closely by their physician when they are prescribed Rivastigmine in any of its forms. Pregnant women should also check with their physicians as it has not been ascertained whether Rivastigmine can pass to infants by way of breast milk. Anyone suffering from the following conditions should also check with their doctor:
- COPD or serious lung issues
- Enlarged prostate
- Heart, bladder, liver or kidney problems
- Severe gastrointestinal issues
- History of stomach ulcers
- Seizure disorders or chronic tremors
- Slow heart rate
More generally, there are literally hundreds of drugs that interact with Rivastigmine, 12 in a major way, over 400 in a moderate way, and the rest in a minor way (check with your physician for interactions with ALL categories of drugs). The 12 drugs that interact with Rivastigmine in a major way are:
So, if you are taking any of these drugs, be sure to tell your doctor, as they may be able to find an alternative that won’t be hazardous to your health.
Caregivers of individuals with Alzheimer’s and other types of dementia may also consider other medications for their loved one, including antidepressants or antipsychotics, or drugs that can help mitigate anxiety, agitation, aggression, or other behavioral challenges. When used thoughtfully, these can help manage some of the more difficult symptoms of dementia.
Medications, including Rivastigmine, are only one piece of puzzle when it comes to caring for someone with Alzheimer’s. A good treatment plan typically involves the active participation of caregivers, the individual’s medical history and relevant information, and a knowledgeable dementia specialist.
It is important to remember that radical improvements are not likely to occur, and that current medications only provide a temporary solution, as opposed to a cure. Hopefully, increased funding for dementia research will lead to new information and better treatments, and hopefully one day, a cure.
Caregivers should be diligent when it comes to managing dementia with medication. Not only is it easy to make mistakes, but mistakes can also go unnoticed, as side effects can be perceived as symptoms dementia. Work with your loved one’s doctors to distinguish between disease symptoms and medication side effects. Appropriate measures can then be taken to improve the quality of life for both the caregiver and person with dementia. Treatments may not offer a cure, but they does offer some hope and maybe a greater number of “good days” with your loved one.