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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Exelon
Generic Name
Rivastigmine
Active Ingredient
RivastigmineCategory
Cholinesterase Inhibitor [EPC]
Salt Form
Tartrate
Variants
6
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Exelon, you must consult a qualified healthcare professional.
| 13.3 mg/24h | PATCH, EXTENDED RELEASE | TRANSDERMAL | 0078-0503 |
| 9.5 mg/24h | PATCH, EXTENDED RELEASE | TRANSDERMAL | 66758-143 |
| 9.5 mg/24h | PATCH, EXTENDED RELEASE | TRANSDERMAL | 0078-0502 |
Detailed information about Exelon
Rivastigmine is a cholinesterase inhibitor used to treat dementia associated with Alzheimer's and Parkinson's disease. It works by increasing levels of acetylcholine in the brain to improve cognitive function.
The dosage of rivastigmine must be individualized and carefully titrated (gradually increased) to minimize side effects, particularly gastrointestinal distress.
Rivastigmine is not approved for use in pediatric patients. The safety and efficacy of this medication in children and adolescents under the age of 18 have not been established. Because the conditions rivastigmine treats (Alzheimer's and Parkinson's dementia) are almost exclusively diseases of aging, there is no clinical data to support its use in younger populations.
In patients with mild to moderate kidney disease, dosage adjustments are generally not necessary. However, for those with severe renal impairment, the titration should be performed with extreme caution, and the maintenance dose may need to be lower based on individual tolerance.
Patients with mild to moderate liver impairment (Child-Pugh score 5-9) may have higher drug exposure. Healthcare providers typically limit the maximum dose in these patients. For the transdermal patch, the maximum recommended dose for those with hepatic impairment is often the 4.6 mg/24-hour patch.
While rivastigmine is primarily used in the elderly, this population is more susceptible to side effects like weight loss and dehydration. Dosage increases should be slow, and monitoring for adverse effects should be frequent.
If you miss a dose of the oral medication, take it as soon as you remember, unless it is almost time for your next dose. Do not double the dose. For the patch, apply a new one as soon as you remember.
CRITICAL: If you have missed doses for more than three days, do not take the next dose until you have spoken with your doctor. You may need to restart the medication at the lowest dose to avoid severe side effects.
An overdose of rivastigmine can cause a 'cholinergic crisis.' Symptoms include severe nausea, vomiting, salivation, sweating, bradycardia (slow heart rate), hypotension (low blood pressure), respiratory depression, and seizures. If an overdose is suspected, contact emergency services or a poison control center immediately.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking the medication without medical guidance, as this can cause symptoms to return or worsen.
Side effects are most common during the titration phase (when the dose is being increased). The most frequently reported adverse effects are gastrointestinal in nature.
Rivastigmine is a powerful medication that affects the central and autonomic nervous systems. It is vital that caregivers and patients understand that this drug is not a cure for dementia but a treatment for symptoms. Safety depends heavily on correct administration, particularly for the transdermal patch system. Medication errors involving the patch have resulted in serious hospitalizations and, in some cases, death.
No FDA black box warnings for Rivastigmine. However, clinicians emphasize the 'Warning' section of the label regarding gastrointestinal reactions and the potential for severe skin reactions with the patch.
While few drugs are strictly 'contraindicated' for use with rivastigmine, certain combinations are avoided due to direct pharmacological antagonism:
Rivastigmine must NEVER be used in the following circumstances:
These are conditions where the risk may outweigh the benefit, and the drug should only be used with extreme caution and frequent monitoring:
Rivastigmine is classified by the FDA as Pregnancy Category B (under the old system). This means that animal reproduction studies have failed to demonstrate a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women.
It is not known whether rivastigmine is excreted in human milk. In animal studies, rivastigmine and its metabolites were found in the milk of lactating rats. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants (such as excessive cholinergic stimulation), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Rivastigmine is a carbamate-type, pseudo-irreversible inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). In the brain, these enzymes are responsible for the hydrolysis of the neurotransmitter acetylcholine. By inhibiting these enzymes, rivastigmine increases the concentration of acetylcholine available for synaptic transmission.
The 'pseudo-irreversible' nature refers to the fact that rivastigmine binds to the esteratic site of the enzyme and forms a carbamylated complex. This complex is much more stable than the acetylated complex formed by the natural substrate, acetylcholine. While the drug is cleared from the blood quickly, the enzyme remains inhibited for up to 10 hours because the carbamyl group dissociates very slowly from the enzyme's active site.
The pharmacodynamic effect of rivastigmine is directly related to the degree of cholinesterase inhibition. In clinical studies, a 6 mg oral dose has been shown to inhibit AChE in the cerebrospinal fluid (CSF) by approximately 40% within the first few hours. This inhibition correlates with improvements in cognitive subscales of the ADAS-cog (Alzheimer's Disease Assessment Scale). The duration of effect is significantly longer than the plasma half-life would suggest, allowing for twice-daily oral dosing or once-daily patch application.
Common questions about Exelon
Rivastigmine is primarily used to treat the symptoms of mild to moderate dementia associated with Alzheimer's disease and Parkinson's disease. It belongs to a class of drugs called cholinesterase inhibitors, which work by increasing the levels of a natural substance called acetylcholine in the brain. This neurotransmitter is essential for learning, memory, and overall cognitive function. While the drug cannot cure these progressive neurological diseases, it can help improve or stabilize memory and the ability to perform daily tasks. Healthcare providers may also occasionally use it off-label for other forms of dementia, such as Lewy Body Dementia.
The most common side effects of rivastigmine are gastrointestinal, including nausea, vomiting, loss of appetite, and diarrhea. These symptoms are most likely to occur when you first start the medication or when your doctor increases your dose. Many patients also report feeling dizzy, tired, or having a headache during the initial weeks of treatment. To minimize these effects, the oral version should always be taken with food, and the dose should be increased very slowly over several months. Using the transdermal patch form instead of capsules can also significantly reduce the severity of stomach-related side effects.
It is generally recommended that you avoid or significantly limit alcohol consumption while taking rivastigmine. Alcohol can worsen many of the drug's side effects, such as dizziness, drowsiness, and confusion, which are already concerns for individuals with dementia. Furthermore, alcohol increases the production of stomach acid, which, when combined with rivastigmine, significantly raises the risk of developing stomach ulcers or gastrointestinal bleeding. Because alcohol can also impair cognitive function and balance, it increases the risk of falls in the elderly population for whom this drug is typically prescribed. Always consult your doctor before consuming alcohol with this medication.
Rivastigmine is considered a Pregnancy Category B medication, meaning animal studies haven't shown harm, but there isn't enough data from human studies to guarantee safety. Since Alzheimer's and Parkinson's dementia almost exclusively affect older adults, there is very little clinical experience with rivastigmine in pregnant women. If a woman of childbearing age needs this medication, she should discuss the potential risks and benefits with her healthcare provider. It is also unknown if the drug passes into breast milk, so breastfeeding is generally not recommended while using rivastigmine. Your doctor will help you weigh the necessity of the drug against the potential risks to a developing fetus or infant.
Rivastigmine does not provide immediate results; it typically takes several weeks or even months to notice a significant difference in cognitive function. Because the medication must be started at a low dose and gradually increased every four weeks to prevent side effects, most patients do not reach an effective maintenance dose for at least two to three months. Some people may notice improvements in their attention and ability to perform daily chores within the first month, while for others, the benefit may simply be that their symptoms stop getting worse as quickly. It is important to continue taking the medication exactly as prescribed, even if you do not feel an immediate change.
You should never stop taking rivastigmine suddenly without first consulting your healthcare provider. If you stop the medication abruptly, your dementia symptoms may worsen more quickly as the levels of acetylcholine in your brain drop. Furthermore, if you stop taking the medication for more than three days and then try to restart at your usual high dose, you may experience severe and dangerous vomiting or other cholinergic side effects. If a break in treatment is necessary, your doctor will provide a plan to slowly restart the medication from the lowest possible dose to allow your body to readjust safely.
If you miss a dose of the oral capsules or solution, take it as soon as you remember with food, unless it is almost time for your next scheduled dose. Never take two doses at once to make up for a missed one. For the transdermal patch, apply a new patch as soon as you realize you've missed a day, and then resume your normal 24-hour schedule. Most importantly, if you miss your doses for more than three consecutive days, do not take any more medication and call your doctor immediately. You will likely need to restart at the lowest dose and begin the titration process over again to avoid severe toxicity.
No, rivastigmine is actually more likely to cause weight loss rather than weight gain. One of the primary side effects of the medication is a decrease in appetite, which, combined with potential nausea or diarrhea, can lead to significant weight reduction over time. Clinical trials have shown that a notable percentage of patients lose 5% or more of their body weight while on the drug. Because of this, healthcare providers usually monitor a patient's weight closely during follow-up appointments. If weight loss becomes excessive, your doctor may suggest nutritional supplements, a dose reduction, or switching to the transdermal patch to improve your appetite.
Rivastigmine can interact with several types of medications, so it is crucial to provide your doctor with a complete list of everything you take. It should not be taken with anticholinergic drugs (like certain allergy or bladder medications) because they work in opposite ways and will cancel each other out. Caution is also needed if you take beta-blockers for your heart, as the combination can cause a dangerously slow heart rate. Additionally, taking rivastigmine with NSAIDs like ibuprofen increases your risk of stomach ulcers. Because rivastigmine is not processed by the liver's CYP450 enzymes, it often has fewer interactions than other dementia drugs, but professional medical review is still required.
Yes, rivastigmine is available in generic form for both the oral capsules and the transdermal patches. The brand name for rivastigmine is Exelon. Generic versions are typically much more affordable than the brand-name product and are required by the FDA to have the same active ingredient, strength, and effectiveness. If you are concerned about the cost of your medication, ask your pharmacist or healthcare provider if a generic version is appropriate for you. Most insurance plans and Medicare Part D cover the generic version of rivastigmine for the treatment of Alzheimer's and Parkinson's dementia.
Other drugs with the same active ingredient (Rivastigmine)
> Warning: Stop taking Rivastigmine and call your doctor or seek emergency care immediately if you experience any of the following:
With prolonged use, the most significant concern is continued weight loss. According to clinical studies, a significant percentage of patients may lose 5% or more of their body weight over the course of a year. Long-term use also requires monitoring for cardiac issues, as the drug's effect on the vagus nerve can lead to persistent slow heart rates in susceptible individuals. Additionally, some patients may develop a tolerance to the cognitive benefits over several years, as the underlying neurodegeneration continues to progress.
There are currently no FDA black box warnings for rivastigmine. However, the FDA has issued several safety communications regarding the risk of medication errors with the transdermal patch (e.g., patients applying multiple patches at once), which can lead to fatal overdoses. It is imperative that only one patch is worn at a time and the old one is removed before a new one is applied.
Report any unusual symptoms or persistent side effects to your healthcare provider immediately. They may need to adjust your dose or switch your formulation to improve tolerance.
There are no specific 'therapeutic drug monitoring' blood tests for rivastigmine levels, but patients should undergo the following regular evaluations:
Dementia itself typically impairs the ability to drive. Furthermore, rivastigmine can cause dizziness, somnolence (sleepiness), and confusion. Patients should not drive or operate dangerous machinery until they and their caregivers are certain the medication does not adversely affect their coordination or alertness.
Alcohol should be avoided or strictly limited while taking rivastigmine. Alcohol can increase the sedative effects of the medication and may also increase the risk of gastrointestinal irritation and stomach ulcers. Combining alcohol with the cognitive impairment of dementia also increases the risk of falls and accidents.
If rivastigmine treatment is interrupted for more than three days, it must not be restarted at the previous maintenance dose. The risk of severe, intractable vomiting is high. Treatment must be restarted at the lowest dose (1.5 mg BID or the 4.6 mg/24h patch) and re-titrated. Abruptly stopping the drug does not typically cause a withdrawal syndrome, but the patient's cognitive function may decline rapidly to the level it would have been without treatment.
> Important: Discuss all your medical conditions, especially heart, lung, or stomach issues, with your healthcare provider before starting Rivastigmine.
Rivastigmine does not have many known interactions with common laboratory tests. However, because it affects the autonomic nervous system, it may occasionally influence results of tests that measure heart rate variability or certain sweat tests used in neurology.
For each major interaction, the primary mechanism is usually pharmacodynamic (how the drugs affect the body) rather than pharmacokinetic (how the body processes the drug). Because rivastigmine bypasses the CYP450 system, it is often a preferred choice for patients who are on multiple other medications for blood pressure, cholesterol, or depression.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. Keep a current list of your medications to share with all healthcare providers, especially before any surgical procedures.
There is a potential for cross-sensitivity between rivastigmine and other carbamate medications. Carbamates are used not only in medicine (like neostigmine or pyridostigmine) but also in some pesticides. If a patient has had a severe reaction to these substances, healthcare providers will use rivastigmine with caution. There is no known cross-sensitivity between rivastigmine and non-carbamate cholinesterase inhibitors like donepezil (Aricept) or galantamine (Razadyne), though patients who cannot tolerate the side effects of one may still struggle with the side effects of another.
> Important: Your healthcare provider will evaluate your complete medical history, including any past skin reactions to bandages or tapes, before prescribing Rivastigmine.
As previously noted, rivastigmine is not approved for pediatric use. The safety and effectiveness in children have not been established. There is no evidence to suggest that cholinesterase inhibitors are beneficial for cognitive issues in children, such as those associated with ADHD or developmental delays, and the risk of gastrointestinal toxicity is high in smaller bodies.
The majority of patients taking rivastigmine are over the age of 65.
While the kidneys are the primary route of elimination for rivastigmine metabolites, the parent drug is rapidly metabolized by esterases. Studies show that patients with moderate renal impairment do not require specific dose adjustments. However, for those with End-Stage Renal Disease (ESRD) or those on dialysis, clearance may be altered. These patients should be monitored closely for signs of toxicity, and doses should be kept at the lowest effective level.
In patients with mild to moderate hepatic impairment (Child-Pugh score 5-9), the mean clearance of rivastigmine is significantly lower (about 60% lower). This leads to higher concentrations of the drug in the blood.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you have liver or kidney issues or if you are caring for an elderly patient with multiple health conditions.
| Parameter | Value |
|---|---|
| Bioavailability | 36% (Oral, 3mg dose) |
| Protein Binding | ~40% |
| Half-life | 1.5 hours (Oral); 3 hours (Patch, after removal) |
| Tmax | 1 hour (Oral); 8-16 hours (Patch) |
| Metabolism | Non-CYP; via esterase-mediated hydrolysis |
| Excretion | Renal 97%, Fecal <1% |
Rivastigmine is classified as a Cholinesterase Inhibitor [EPC]. It belongs to the therapeutic category of anti-dementia agents. Within this class, it is grouped with other medications such as donepezil and galantamine. However, rivastigmine is unique as the only carbamate in this group and the only one with significant inhibitory activity against both AChE and BuChE.