Exelon: Advanced Cognitive Support for Dementia Symptoms
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Synonyms | |||
Exelon (rivastigmine) is a prescription medication specifically formulated for the treatment of mild to moderate dementia associated with Alzheimer’s disease and Parkinson’s disease. As a reversible cholinesterase inhibitor, it works by increasing the levels of acetylcholine, a crucial neurotransmitter involved in memory, thinking, and reasoning. By enhancing cholinergic function in the brain, Exelon helps mitigate the cognitive decline characteristic of these neurodegenerative conditions, offering patients a chance to maintain functional abilities for a longer period. This medication is available in multiple formulations, including capsules, oral solution, and transdermal patches, providing flexibility to accommodate individual patient needs and preferences. It is an evidence-based therapeutic option supported by extensive clinical research demonstrating efficacy in improving cognitive and global function.
Features
- Active ingredient: Rivastigmine
- Available formulations: Capsules (1.5 mg, 3 mg, 4.5 mg, 6 mg), oral solution (2 mg/mL), transdermal patch (4.6 mg/24h, 9.5 mg/24h, 13.3 mg/24h)
- Pharmacologic class: Reversible cholinesterase inhibitor
- Mechanism of action: Inhibits acetylcholinesterase and butyrylcholinesterase
- Half-life: Approximately 1.5 hours (oral), with steady-state inhibition of cholinesterase for 10 hours
- Administration: Twice daily with food (oral forms); once-daily application (transdermal patch)
- FDA-approved indications: Mild to moderate dementia of the Alzheimer’s type; mild to moderate dementia associated with Parkinson’s disease
Benefits
- Helps slow the progression of cognitive decline in Alzheimer’s and Parkinson’s disease dementia
- Improves or maintains memory, attention, and reasoning abilities
- Supports enhanced performance in activities of daily living, promoting greater independence
- Offers flexible dosing options to improve tolerability and adherence
- Transdermal formulation reduces gastrointestinal side effects compared to oral administration
- May positively impact behavioral symptoms such as apathy and agitation in some patients
Common use
Exelon is primarily prescribed for the management of cognitive symptoms in patients diagnosed with mild to moderate Alzheimer’s disease or Parkinson’s disease dementia. In clinical practice, it is often initiated when patients begin experiencing noticeable decline in memory, problem-solving abilities, or functional independence. The transdermal patch formulation is particularly beneficial for patients who have difficulty swallowing or experience significant gastrointestinal discomfort with oral medications. Treatment is typically long-term, as discontinuation may lead to a return to pretreatment cognitive levels. Regular assessment of cognitive function, through tools such as the Mini-Mental State Examination (MMSE) or Alzheimer’s Disease Assessment Scale-cognitive subscale (ADAS-cog), helps clinicians monitor therapeutic response and adjust treatment as needed.
Dosage and direction
Initial dosing: For oral capsules or solution, the recommended starting dose is 1.5 mg twice daily with meals. After a minimum of two weeks, and if well tolerated, the dose may be increased to 3 mg twice daily. Subsequent increases to 4.5 mg and 6 mg twice daily should follow with a minimum of two-week intervals. The maximum recommended dose is 6 mg twice daily (12 mg total daily dose).
For the transdermal patch, therapy should be initiated with the 4.6 mg/24h patch applied once daily. After a minimum of four weeks, if well tolerated, the dose may be increased to the 9.5 mg/24h patch. The 13.3 mg/24h patch is reserved for patients who have been on the 9.5 mg/24h patch for at least four weeks and require further dose escalation.
Administration guidelines: Oral formulations must be taken with food to enhance tolerability. The transdermal patch should be applied to clean, dry, intact skin on the upper or lower back, upper arm, or chest, avoiding areas that might be rubbed by tight clothing. The application site should be rotated daily, with no reapplication to the same site within 14 days. Patches must be replaced every 24 hours.
Precautions
Patients and caregivers should be advised that Exelon may cause dizziness or somnolence, potentially affecting the ability to drive or operate machinery. Gastrointestinal effects, including nausea, vomiting, and diarrhea, are common, particularly during dose escalation. Adequate hydration should be maintained to prevent dehydration, especially in elderly patients. Those with underlying cardiac conduction abnormalities should be monitored closely, as cholinesterase inhibitors may have vagotonic effects. Exelon should be used with caution in patients with a history of peptic ulcer disease or those taking NSAIDs concurrently due to increased risk of gastrointestinal bleeding. Pulmonary conditions such as asthma or COPD warrant careful observation, as increased bronchial secretions may occur. Weight should be monitored regularly, as decreased appetite and weight loss are possible.
Contraindications
Exelon is contraindicated in patients with known hypersensitivity to rivastigmine, other carbamate derivatives, or any component of the formulation. The transdermal patch should not be used in patients with known latex allergy, as the backing film contains latex. Patients with a history of application site reactions with similar transdermal systems should avoid the patch formulation. Those with severe liver impairment should not use Exelon, as pharmacokinetic studies indicate significantly increased exposure. Concomitant use with other cholinergic drugs is not recommended due to additive effects.
Possible side effect
The most frequently reported adverse reactions are gastrointestinal in nature, including nausea (47% with oral form, 7% with patch), vomiting (31% oral, 6% patch), and diarrhea (19% oral, 5% patch). Other common side effects include decreased appetite, weight loss, dizziness, headache, and abdominal pain. The transdermal formulation demonstrates a significantly improved gastrointestinal tolerability profile compared to oral administration. Application site reactions may occur with the patch, including erythema, pruritus, and rash. Less common but clinically significant effects include bradycardia, syncope, tremors, and urinary tract infections. Psychiatric symptoms such as agitation, insomnia, depression, and hallucinations have been reported, though these may also be related to the underlying dementia.
Drug interaction
Concomitant use with other cholinergic agents (e.g., bethanechol) or anticholinesterase agents may result in additive effects and increased toxicity. Anticholinergic medications (e.g., oxybutynin, tolterodine) may reduce the efficacy of Exelon. Metoclopramide may exacerbate extrapyramidal symptoms when used with rivastigmine. Beta-blockers may potentiate bradycardic effects, requiring close cardiac monitoring. Cholinesterase inhibitors may interfere with the action of neuromuscular blocking agents during anesthesia. NSAIDs may increase the risk of gastrointestinal bleeding when used concurrently. Rivastigmine is metabolized primarily through hydrolysis by esterases, with minimal cytochrome P450 involvement, reducing the potential for many pharmacokinetic interactions.
Missed dose
If a dose of oral Exelon is missed, it should be skipped and the next dose taken at the regular time. Patients should not double the dose to make up for a missed one. For the transdermal patch, if a dose is missed, a new patch should be applied as soon as possible, and the next patch applied at the regular time the following day. Multiple patches should never be applied simultaneously. Caregivers should maintain a consistent medication schedule and use reminder systems to support adherence.
Overdose
Symptoms of overdose are primarily related to exaggerated cholinergic effects and may include severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, syncope, and convulsions. Increasing muscle weakness may occur, potentially leading to death if respiratory muscles are involved. Management involves general supportive measures, with particular attention to maintaining adequate hydration and cardiovascular stability. Atropine sulfate is recommended as an antidote, with an initial intravenous dose of 0.03 mg/kg, titrated to effect. Due to the short half-life of rivastigmine, symptomatic treatment is typically sufficient, but patients should be observed for at least 24 hours due to the potential for recurrent symptoms.
Storage
Exelon capsules and oral solution should be stored at room temperature (15-30°C or 59-86°F) in their original container, tightly closed and protected from moisture. The oral solution should be used within 30 days after first opening the bottle. Transdermal patches must be kept in their sealed pouch until time of use and stored at room temperature. All formulations should be kept out of reach of children and pets. Unused medication should be disposed of properly according to local regulations, with particular care taken to fold used patches so that the adhesive side sticks to itself before disposal.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Exelon is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to treatment may vary, and not all patients will experience the same benefits or side effects. Proper diagnosis and treatment planning require comprehensive evaluation by a physician. Patients should not initiate, discontinue, or modify their dosage without consulting their healthcare provider. The complete prescribing information should be reviewed before initiating therapy.
Reviews
Clinical trials have demonstrated that Exelon provides statistically significant improvements in cognitive function, activities of daily living, and global functioning compared to placebo. In a 26-week study of patients with Alzheimer’s disease, those receiving 6-12 mg/day of oral rivastigmine showed significantly better performance on the ADAS-cog and CIBIC-Plus scales. Research in Parkinson’s disease dementia has similarly shown benefits in attention, memory, and executive function. The transdermal formulation has been shown to provide comparable efficacy to the highest doses of oral rivastigmine with significantly improved tolerability. Many clinicians report that patients who tolerate dose escalation often maintain cognitive benefits for extended periods, though the progressive nature of neurodegenerative diseases means continued decline is expected despite treatment. Caregivers frequently note improvements in engagement and functional independence, particularly when treatment is initiated early in the disease course.