What is the use of Rivastigmine (Cholinesterase inhibitor)?

From the Guidelines

Rivastigmine should be used to treat mild to moderate dementia associated with Alzheimer's disease and Parkinson's disease, as it can result in clinically important improvements in global assessment, despite not significantly improving cognition or quality of life, as evidenced by studies such as 1.

Key Points

• Rivastigmine works by inhibiting the enzyme acetylcholinesterase, increasing acetylcholine levels in the brain, which can temporarily improve cognitive function or slow cognitive decline in some patients 1.
• Typical dosing starts at 1.5 mg twice daily and gradually increases every 2-4 weeks as tolerated to a target dose of 3-6 mg twice daily, with the medication available in oral capsules, oral solution, and transdermal patches 1.
• Common side effects include nausea, vomiting, decreased appetite, and dizziness, which often improve with continued use or dose adjustment, and can be minimized by taking the medication with food 1.
• Treatment response should be evaluated after 3-6 months, and the medication may need to be continued long-term if beneficial, with patients and caregivers aware that abrupt discontinuation can lead to worsening symptoms, so any dose changes should be done gradually under medical supervision 1.

Considerations

• The long-term effects of treatment with rivastigmine are not known, as the duration of trials was less than 7 months 1.
• The frequency of adverse events between treatment and control groups did not differ, but 2 studies showed a dose–response relationship for adverse events, with the types of adverse events consistent with those related to cholinesterase inhibitor use, including dizziness, nausea, vomiting, eating disorder/weight loss, and headache 1.
• The harm with the greatest effect size was vomiting, with a relative risk of 6.06, and the smallest effect size was dizziness, with a relative risk of 2.24 1.

From the FDA Drug Label

INDICATIONS AND USAGE Rivastigmine tartrate is an acetylcholinesterase inhibitor indicated for treatment of: • Mild-to-moderate dementia of the Alzheimer's type (AD) (1.1) • Mild-to-moderate dementia associated with Parkinson's disease (PD) (1.2)

The indications for Rivastigmine are:

• Mild-to-moderate dementia of the Alzheimer's type (AD)
• Mild-to-moderate dementia associated with Parkinson's disease (PD) 2

From the Research

Rivastigmine Overview

• Rivastigmine is a powerful slow-reversible, noncompetitive carbamate cholinesterase inhibitor used for the treatment of mild-to-moderate Alzheimer's disease 3.
• It has been shown to have beneficial effects on cognition and global functioning in patients with Alzheimer's disease, with effects lasting up to 5 years 3.
• Rivastigmine is also used to treat cognitive and behavioral symptoms in Alzheimer's disease associated with vascular risk factors, dementia with Lewy bodies, and Parkinson's disease dementia 3.

Rivastigmine in Parkinson's Disease Dementia

• A study published in The New England Journal of Medicine found that rivastigmine was associated with moderate improvements in dementia associated with Parkinson's disease, but also with higher rates of nausea, vomiting, and tremor 4.
• The study found that rivastigmine-treated patients had a mean improvement of 2.1 points in the score for the 70-point ADAS-cog, compared to a 0.7-point worsening in the placebo group 4.

Dual Inhibition of Acetylcholinesterase and Butyrylcholinesterase

• Rivastigmine has a unique dual inhibition of acetylcholinesterase and butyrylcholinesterase, which may afford additional therapeutic potential in subcortical dementias such as vascular dementia and Parkinson's disease dementia 5.
• The dual inhibition of AChE and BuChE may specifically benefit executive dysfunction frequently observed in subcortical dementias 5.

Comparison with Other Treatments

• A study published in Cureus compared the effects of acetylcholinesterase inhibitors, including rivastigmine, with the new treatment aducanumab, and found that conventional treatment was more cost-effective and had fewer adverse effects 6.
• Another study published in Clinical Interventions in Aging found that rivastigmine was effective in improving cognition, activities of daily living, and global function in patients with mild to moderate Alzheimer's disease 7.