Exelon

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Exelon is the brand name for rivastigmine, a cholinesterase inhibitor prescribed for the symptomatic treatment of mild to moderate dementia associated with Alzheimer's disease and Parkinson's disease.

Rivastigmine works by inhibiting the enzymes that break down acetylcholine, a neurotransmitter essential for memory, learning, and cognitive function.

By increasing acetylcholine availability in the brain, Exelon helps to maintain cognitive abilities and support daily functioning for as long as possible.

Exelon is a prescription-only medicine (POM) in the United Kingdom, available as capsules, oral solution, and transdermal patches.

It is manufactured by Novartis and has been in clinical use since 1998.

Dementia is one of the most significant health challenges in the UK, affecting approximately 900,000 people, with this number projected to rise above one million by 2025.

Alzheimer's disease accounts for roughly 60 to 70% of all dementia cases, while dementia associated with Parkinson's disease affects up to 80% of Parkinson's patients over the course of their illness.

Both conditions involve progressive loss of cholinergic neurones in the brain, leading to declining memory, reasoning, language, and the ability to perform everyday tasks.

This page provides a comprehensive clinical guide to Exelon, covering how it works, who it is suitable for, dosing, side effects, important safety information, and how to obtain a prescription in the United Kingdom.

Important safety information about Exelon

Before reading further, note the following essential safety points. Exelon must be prescribed and supervised by a specialist experienced in dementia care.

• Exelon must be initiated by a specialist (psychiatrist, neurologist, or geriatrician) experienced in diagnosing and managing dementia.
• Dose titration must be gradual. Increasing the dose too quickly significantly raises the risk of severe nausea, vomiting, and potentially dangerous gastrointestinal complications.
• If treatment is interrupted for more than 3 days, it must be restarted from the lowest dose. Do not resume at the previous dose without specialist advice.
• Only one transdermal patch should be worn at a time. Used patches still contain active drug and must be disposed of safely, out of reach of children and pets.
• Report any suspected adverse reactions to the MHRA via the Yellow Card scheme at yellowcard.mhra.gov.uk.

Understanding Alzheimer's disease and the cholinergic deficit

Alzheimer's disease is a progressive neurodegenerative condition characterised by the accumulation of amyloid plaques and neurofibrillary tangles in the brain.

These pathological changes lead to widespread neuronal loss, with particularly severe damage to cholinergic neurones in the basal forebrain (the nucleus basalis of Meynert).

The resulting reduction in acetylcholine levels in the cerebral cortex and hippocampus is closely correlated with the severity of cognitive decline.

Cholinesterase inhibitors such as rivastigmine are designed to counteract this deficit by preventing the enzymatic breakdown of the remaining acetylcholine, thereby prolonging its action at synaptic cleft receptors.

In Parkinson's disease dementia, a similar cholinergic deficit develops alongside the well-known dopaminergic dysfunction that causes motor symptoms.

The degeneration of cholinergic pathways in Parkinson's disease contributes to cognitive impairment, visual hallucinations, attentional deficits, and executive dysfunction.

Rivastigmine is the only cholinesterase inhibitor with specific licensing for Parkinson's disease dementia in the UK, based on the results of the EXPRESS trial.

How Exelon works: mechanism of action

Rivastigmine is a carbamate-type reversible inhibitor of two key cholinergic enzymes: acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE).

AChE is the primary enzyme responsible for hydrolysing acetylcholine at cholinergic synapses throughout the central nervous system.

BuChE, while less abundant in the healthy brain, becomes increasingly important in advanced stages of Alzheimer's disease as AChE-producing neurones degenerate and BuChE activity proportionally increases in plaques and tangles.

By inhibiting both enzymes, rivastigmine may maintain its efficacy further into the disease course compared with agents that target only AChE.

Rivastigmine binds to the esteratic site of these enzymes, forming a carbamoylated complex that inactivates the enzyme for approximately 10 hours.

This pseudo-irreversible mechanism means the enzyme is effectively blocked until the carbamate moiety is hydrolysed and the enzyme regenerates.

This contrasts with donepezil and galantamine, which are rapidly reversible competitive inhibitors of AChE only.

In clinical trials (the IDEAL and EXPRESS studies), rivastigmine demonstrated statistically significant improvements in ADAS-cog scores (a standard measure of cognitive function in dementia research), Clinician's Interview-Based Impression of Change (CIBIC-plus), and the Alzheimer's Disease Cooperative Study activities of daily living scale (ADCS-ADL).

While the magnitude of benefit is modest, measured as a slowing of cognitive decline rather than absolute improvement, these gains translate into meaningful preservation of daily independence for many patients and their families.

Clinical evidence and UK prescribing guidance

Rivastigmine is recommended by NICE Technology Appraisal TA217 as a treatment option for mild to moderate Alzheimer's disease.

The guideline stipulates that treatment should only be initiated by a specialist in secondary care (old age psychiatrists, neurologists, or physicians with a special interest in dementia), although prescribing may subsequently be transferred to primary care under shared-care protocols.

Treatment should be continued only if it is considered to be having a worthwhile effect on cognitive, global, functional, or behavioural symptoms, assessed at regular review intervals (typically every 6 to 12 months).

For Parkinson's disease dementia, NICE TA217 also recommends rivastigmine as a treatment option.

The EXPRESS trial, a large randomised controlled study of rivastigmine in Parkinson's disease dementia, showed significant improvements in cognitive function and activities of daily living compared with placebo.

Rivastigmine is the only cholinesterase inhibitor with a specific UK licence for this indication.

The British National Formulary (BNF) lists rivastigmine under anticholinesterase drugs used in dementia.

It provides detailed dosing guidance for both oral and transdermal formulations, along with cautions, contraindications, and monitoring requirements.

The Summary of Product Characteristics (SmPC) for Exelon is available on the Electronic Medicines Compendium (EMC) and should be consulted for full prescribing information.

Exelon compared with other cholinesterase inhibitors

Three cholinesterase inhibitors are available in the UK for Alzheimer's disease: donepezil, galantamine, and rivastigmine.

All three have similar overall efficacy in mild to moderate disease, and NICE does not recommend one over another as first-line treatment.

The choice between them is typically based on individual patient factors, tolerability, formulation preference, and comorbidities.

Rivastigmine is distinguished by its dual inhibition of AChE and BuChE, its carbamate mechanism, and the availability of a transdermal patch formulation.

The patch may be preferred for patients who have difficulty swallowing, who experience significant gastrointestinal side effects with oral cholinesterase inhibitors, or whose carers find once-daily patch application more practical than twice-daily oral dosing.

The Exelon patch was shown in the IDEAL study to provide comparable efficacy to the highest oral dose with significantly fewer gastrointestinal side effects.

For Parkinson's disease dementia, rivastigmine is the only licensed cholinesterase inhibitor and is therefore the standard pharmacological treatment for cognitive symptoms in this population.

Dosage and administration of Exelon

Oral capsules and solution

Exelon capsules are available in 1.5 mg, 3 mg, 4.5 mg, and 6 mg strengths. Treatment begins at 1.5 mg twice daily with food.

The dose is increased by 1.5 mg per dose (3 mg daily increase) at intervals of at least two weeks, provided each dose level is well tolerated.

The recommended maintenance dose is 3 to 6 mg twice daily. The oral solution (2 mg/mL) may be used as an alternative for patients who cannot swallow capsules.

Doses should be taken with morning and evening meals to improve absorption and reduce nausea.

Transdermal patches

Exelon patches deliver rivastigmine continuously through the skin over 24 hours.

Treatment starts with the 4.6 mg/24 hours patch, progressing to 9.5 mg/24 hours after at least four weeks, and to 13.3 mg/24 hours after a further four weeks if clinically indicated and tolerated.

Each patch should be applied to clean, dry, hairless skin on the upper back, chest, or upper arm.

The application site should be rotated daily to prevent skin irritation.

Only one patch should be worn at any time, and the previous patch must be removed before applying a new one.

Switching between oral and patch formulations

Patients currently taking oral rivastigmine may be switched to the patch formulation.

Patients on 3 to 6 mg per day orally should start on the 4.6 mg/24 hours patch.

Patients on 6 to 9 mg per day orally should start on the 9.5 mg/24 hours patch.

Patients on 9 to 12 mg per day orally should start on the 9.5 mg/24 hours patch and may progress to 13.3 mg/24 hours after four weeks.

The first patch should be applied the day after the last oral dose.

Side effects of Exelon

Common gastrointestinal side effects

Nausea, vomiting, diarrhoea, abdominal pain, and decreased appetite are the most frequently reported adverse effects.

These are caused by the cholinomimetic action of rivastigmine on the gastrointestinal tract and are most common during dose titration.

Taking oral doses with food and following the recommended titration schedule minimises the risk.

The transdermal patch formulation produces significantly fewer gastrointestinal side effects because it avoids the peak plasma levels associated with oral dosing.

Weight loss is a recognised consequence of persistent gastrointestinal symptoms and reduced appetite; regular weight monitoring is recommended.

Nervous system and psychiatric side effects

Dizziness, headache, somnolence, and tremor are common.

Agitation, confusion, insomnia, and depression may occur, though these symptoms overlap substantially with the underlying dementia and may not always be drug-related.

Falls are a significant concern in elderly patients with dementia, and the dizziness and postural instability associated with rivastigmine may increase fall risk.

Carers should be advised to supervise mobility, particularly at the start of treatment and after dose changes.

Cardiovascular side effects

Cholinesterase inhibitors increase vagal tone, which can reduce heart rate. Bradycardia and, rarely, syncope have been reported with rivastigmine.

These effects are particularly relevant in patients with pre-existing cardiac conduction abnormalities, sick sinus syndrome, or concurrent use of beta-blockers, digoxin, or other heart-rate-lowering medicines.

An ECG should be considered before starting treatment in patients with known cardiac disease.

Skin reactions with patches

Application site reactions including erythema (redness), itching, swelling, and dermatitis are common with transdermal patches. These are usually mild and resolve within 48 hours of patch removal.

Rotating the application site daily and avoiding the same area for at least 14 days reduces the incidence and severity.

Rarely, severe allergic contact dermatitis may develop, requiring discontinuation of the patch formulation.

When to seek urgent medical advice

Contact your GP, specialist team, or NHS 111 if you experience persistent vomiting, signs of dehydration, unexplained weight loss, significant dizziness, fainting, unusually slow heart rate, or worsening neurological symptoms.

Seek emergency care (call 999 or attend A&E) if you observe signs of severe allergic reaction, severe gastrointestinal bleeding (vomiting blood or passing black stools), or seizures.

Report any suspected adverse reactions to the MHRA via the Yellow Card scheme at yellowcard.mhra.gov.uk .

Warnings and precautions for Exelon

Specialist initiation and monitoring

Exelon must be initiated by a specialist experienced in dementia diagnosis and management.

Ongoing treatment should be regularly reviewed, typically every 6 to 12 months, to assess continued clinical benefit.

Treatment should be discontinued when it is no longer considered to provide a meaningful benefit or when the patient progresses to severe dementia (unless other factors support continuation).

Dose re-titration after interruption

If treatment with Exelon is interrupted for more than 3 days, it is essential to re-titrate from the lowest starting dose.

Restarting at the previous maintenance dose without re-titration can cause severe nausea, vomiting, and potentially oesophageal rupture.

This is one of the most important safety messages for patients and carers.

Cardiac cautions

Rivastigmine increases vagal tone and can cause bradycardia, which may be relevant for patients with sick sinus syndrome, sinoatrial or atrioventricular block, or those taking concurrent cardiac medications that reduce heart rate.

Electrocardiographic monitoring should be considered before and during treatment in at-risk patients.

Gastrointestinal cautions

Cholinesterase inhibitors increase gastric acid secretion. Patients with a history of peptic ulcer disease, gastrointestinal bleeding, or concurrent NSAID use should be monitored closely. Active or recent peptic ulceration is a relative contraindication.

Respiratory cautions

Rivastigmine may cause bronchoconstriction through its cholinomimetic effects. Caution is advised in patients with asthma or chronic obstructive pulmonary disease. If respiratory symptoms develop or worsen during treatment, the prescriber should reassess the risk-benefit balance.

Seizure risk

Cholinergic agents may provoke or worsen seizures. While this risk is low, caution is advised in patients with a known seizure disorder or a history of epilepsy.

Use in Parkinson's disease

Patients with Parkinson's disease dementia may experience worsening of extrapyramidal symptoms (tremor, rigidity, bradykinesia) during rivastigmine treatment. The prescriber should carefully balance the cognitive benefits against any deterioration in motor function and adjust treatment accordingly.

How to get Exelon in the UK

Exelon is available on the NHS in the United Kingdom.

Treatment must be initiated by a specialist in secondary care, typically following a formal cognitive assessment using standardised tools such as the Mini-Mental State Examination (MMSE) or the Addenbrooke's Cognitive Examination (ACE-III).

Once treatment is established and stable, prescribing may be transferred to the patient's GP under a shared-care agreement.

If you or a family member is experiencing memory problems, changes in thinking, or difficulties with daily tasks, the first step is to visit your GP.

Your GP can perform an initial assessment and, if appropriate, refer you to a memory assessment service or specialist clinic.

The NHS prescription charge in England is currently 9.90 pounds per item; prescriptions are free in Scotland, Wales, and Northern Ireland.

Many patients with dementia are eligible for free prescriptions through the NHS medical exemption certificate system.

Authorised online prescribers cannot typically initiate cholinesterase inhibitors, as specialist assessment and diagnosis are required first.

However, once treatment has been established by a specialist, ongoing supplies may in some cases be facilitated through registered online pharmacies with appropriate clinical oversight.

Living with dementia: practical advice for patients and carers

Medication is one component of dementia care. NICE recommends a comprehensive approach including cognitive stimulation therapy, structured group activities, regular physical exercise, social engagement, and carer support.

The Alzheimer's Society and Parkinson's UK provide extensive resources, support groups, and helplines for people living with dementia and their carers across the United Kingdom.

Carers play a central role in medication management.

Practical tips include using a dosette box or medication organiser for oral capsules, setting reminders for patch application, keeping a diary of observed effects and side effects, and attending review appointments to provide input on the patient's response to treatment.

If you are a carer, ensure you are aware of your rights to a carer's assessment from your local authority, which can identify support services available to you.

When to seek further medical advice

Contact the specialist team, your GP, or NHS 111 if you notice a sudden worsening of cognitive function, significant behavioural changes, persistent vomiting, unexplained weight loss, or any new symptoms that concern you.

If the patient shows signs of a medical emergency such as seizures, loss of consciousness, severe allergic reaction, or gastrointestinal bleeding, call 999 immediately.

Sources

• Exelon Capsules, Summary of Product Characteristics (EMC)
• Exelon Transdermal Patches, Summary of Product Characteristics (EMC)
• Rivastigmine, British National Formulary (BNF)
• NICE TA217: Donepezil, galantamine, rivastigmine and memantine for Alzheimer's disease
• Alzheimer's disease, NHS
• Parkinson's disease treatment, NHS
• MHRA Yellow Card Scheme