rivastigmines

Rivastigmine is a carbamate acetylcholinesterase inhibitor with activity against both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). It is approved for the treatment of symptoms of mild to moderate Alzheimer’s disease and Parkinson’s disease dementia. The medication is available in oral capsule form and as a transdermal patch, marketed under various brand names such as Exelon.

Mechanism of action and use: Rivastigmine increases brain acetylcholine levels by inhibiting AChE and BuChE, which may help improve cognitive symptoms and daily functioning in some individuals. It is considered a symptomatic treatment and is not believed to modify the underlying disease process.

Administration and formulations: Oral rivastigmine is typically started at 1.5 mg twice daily and titrated by 1.5 mg twice daily every two weeks to a maximum of 6 mg twice daily (12 mg/day). The transdermal patch delivers 4.6 mg/24 hours or 9.5 mg/24 hours and is applied once daily, with site rotation. Converting between oral and patch forms follows dose equivalence guidelines.

Pharmacokinetics, safety, and adverse effects: Rivastigmine is primarily metabolized by hydrolysis and is largely excreted renally, with limited involvement of hepatic enzymes. Common adverse effects include nausea, vomiting, diarrhea, anorexia, weight loss, dizziness, and headache. The patch can cause skin irritation. Cautions include liver impairment, potential bradycardia, and interactions with agents with anticholinergic effects, which can reduce efficacy.

Contraindications and notes: Do not use in known hypersensitivity to rivastigmine or to patch adhesives. Use with caution in severe hepatic impairment and during pregnancy or lactation, with decisions based on clinical judgment. Generic rivastigmine formulations are available in many regions.