Exelon

Exelon is used for treating mild to moderate dementia (eg, impairment of memory or judgement, abstract thinking, changes in personality) in patients with Alzheimer disease or Parkinson disease.

Product dosage: 3mg
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Product dosage: 6mg
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Synonyms Prometax Remizeral Rivadem Rivamer Rivasmine Rivastigmin Rivastigmina Rivastigminum

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 cholinesterase inhibitor, it works by increasing the levels of certain chemicals in the brain involved in memory, thinking, and reasoning. This medication is a cornerstone of pharmacological management for cognitive decline, aiming to slow symptom progression and improve daily functioning. It is available in multiple formulations, including capsules, oral solution, and transdermal patches, to accommodate individual patient needs and preferences.

Features

• Active pharmaceutical ingredient: Rivastigmine
• Pharmacological class: Reversible cholinesterase inhibitor
• 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)
• Mechanism of Action: Inhibits both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the brain
• Dosing schedule: Typically administered twice daily (oral forms) or once daily (transdermal patch)

Benefits

• Enhances Cognitive Function: Works to improve memory, attention, and the ability to reason.
• Supports Daily Activities: Can help patients maintain independence for a longer period by improving performance of everyday tasks.
• Slows Symptom Progression: Aims to delay the worsening of dementia symptoms associated with Alzheimer’s and Parkinson’s diseases.
• Flexible Administration: The availability of a transdermal patch option can improve compliance and minimize gastrointestinal side effects.
• Dual Enzyme Inhibition: Its unique action on both AChE and BuChE may provide a broader therapeutic effect for some patients.

Common use

Exelon is primarily indicated for the treatment of mild to moderate dementia of the Alzheimer’s type. It is also approved for the treatment of mild to moderate dementia associated with Parkinson’s disease. It is used as a symptomatic treatment to address the core cognitive, functional, and behavioral manifestations of these conditions. It is not a cure for these diseases but is a key component of a comprehensive management plan that often includes non-pharmacological interventions.

Dosage and direction

Dosing must be individualized under the strict supervision of a healthcare professional.

• Oral Capsules/Solution: Treatment is initiated at a low dose (e.g., 1.5 mg twice daily) and titrated upward at intervals of at least two weeks, based on tolerability. The recommended dosage range is 3 to 6 mg twice daily. The solution should be administered directly from the syringe provided into the mouth or mixed with a small glass of water, cold fruit juice, or soda.
• Transdermal Patch: Treatment is initiated with the 4.6 mg/24h patch once daily. After a minimum of four weeks, if well tolerated, the dose may be increased to the 9.5 mg/24h patch, which is the effective maintenance dose. A 13.3 mg/24h patch is available for patients with severe dementia who have been on the 9.5 mg/24h dose for at least six months and who tolerate it well.
• The patch should be applied to clean, dry, intact, and hairless skin on the upper or lower back, upper arm, or chest, avoiding areas that will be rubbed by tight clothing. The application site should be rotated daily.
• The patch must be replaced with a new one every 24 hours.
• Crucial: Always follow the specific titration schedule and instructions provided by the prescribing physician.

Precautions

• Exelon can cause significant weight loss. Patient weight should be monitored during therapy.
• The transdermal patch can cause skin reactions (redness, itching, rash) at the application site. Rotating the site helps minimize this.
• Use with caution in patients with a history of asthma, chronic obstructive pulmonary disease (COPD), or other types of lung disease.
• May cause nausea, vomiting, and diarrhea, especially during the dose titration phase. The transdermal patch formulation is associated with a lower incidence of these gastrointestinal effects.
• Can potentially slow heart rate (bradycardia) and cause syncope (fainting). Caution is advised in patients with underlying cardiac conduction disorders (e.g., ‘sick sinus syndrome’).
• May increase gastric acid secretion. Use with caution in patients at risk for ulcers or gastrointestinal bleeding.
• Can cause bladder outflow obstruction. Use with caution in patients with urinary retention.

Contraindications

Exelon is contraindicated in patients with:

• A known hypersensitivity to rivastigmine, other carbamate derivatives, or any other components of the formulation.
• A history of application site reactions with the transdermal patch that were consistent with allergic contact dermatitis.

Possible side effect

The most common side effects are often related to the cholinergic action of the drug and are typically dose-dependent and most frequent during the titration phase.

• Very Common (≥1/10): Nausea, vomiting, diarrhea, loss of appetite, dizziness, headache.
• Common (≥1/100 to <1/10): Abdominal pain, dyspepsia, fatigue, asthenia, malaise, increased sweating, weight decreased, agitation, insomnia, depression, anxiety, tremor, fall, bradycardia.
• Uncommon (≥1/1,000 to <1/100): Syncope (fainting), dehydration (secondary to vomiting/diarrhea), gastric and duodenal ulcers, rash (including application site reactions for the patch).
• Rare (≥1/10,000 to <1/1,000): Seizures, pancreatitis, hepatitis, hallucinations, aggression, skin hypersensitivity reactions.

Drug interaction

Concomitant use of Exelon with other drugs can lead to interactions.

• Other Cholinesterase Inhibitors: Concurrent use with drugs of a similar class (e.g., donepezil, galantamine) is not recommended due to additive cholinergic effects and increased risk of side effects.
• Cholinergic Agonists (e.g., bethanechol): Additive effects are expected, increasing the risk of side effects.
• Anticholinergic Medications (e.g., oxybutynin, tolterodine, some antihistamines, tricyclic antidepressants): These drugs oppose the pharmacological effect of Exelon and may reduce its efficacy.
• Depolarizing Neuromuscular Blocking Agents (e.g., succinylcholine): Rivastigmine may exaggerate the muscle relaxation effect of these agents used during anesthesia.
• Beta-Blockers: May have an additive effect on heart rate, increasing the risk of bradycardia.

Missed dose

• For oral formulations (capsules/solution): If a dose is missed, it should be skipped and the next dose taken at the regularly scheduled time. Do not double the dose to make up for the missed one.
• For the transdermal patch: If a patch is forgotten, a new patch should be applied as soon as it is remembered. The next patch should be applied at the regular time the following day. Only one patch should be worn at any given time.

Overdose

An overdose of Exelon can lead to a severe cholinergic crisis characterized by severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, syncope, and convulsions. Due to its long duration of action, supportive measures may need to be prolonged. Muscle weakness can occur, potentially leading to respiratory failure. Death has been reported following overdose. General supportive measures should be instituted. Tertiary anticholinergics such as atropine can be used as an antidote, with an initial intravenous dose of 1 to 2 mg, with subsequent dosing based on clinical response. It is critical to seek immediate emergency medical attention in case of a suspected overdose.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F).
• Oral Solution: Use within one month of first opening the bottle.
• Transdermal Patches: Keep in the sealed pouch until immediately before application.
• Keep all medications out of the reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided may not cover all possible uses, directions, precautions, drug interactions, or adverse effects.

Reviews

“After starting my father on the Exelon patch, we noticed a stabilization in his confusion. The twice-daily pill was a constant battle, but the patch has made administration much simpler for our family. We did have some initial skin redness, but rotating sites solved the issue.” – Caregiver D.S.

“As a neurologist, I find Exelon to be a valuable tool, particularly the transdermal formulation. It allows for a smoother delivery of the drug, which significantly improves gastrointestinal tolerability in my patients and supports better long-term adherence to therapy.” – Dr. A.L., Neurologist

“The titration process was rough with significant nausea, but once we reached a stable maintenance dose on the capsules, my husband’s memory recall seemed sharper. His ability to follow conversations improved, which has been a welcome change.” – Spouse J.K.