Rivastigmine is a reversible, non-competitive, brain-selective, dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), used for the symptomatic treatment of mild to moderate dementia of the Alzheimer's type and dementia associated with Parkinson's disease. The 3mg strength is typically the starting dose for oral capsules.
Adult: Start with 1.5 mg twice daily. After a minimum of 2 weeks, if tolerated, increase to 3 mg twice daily (the dose represented by this monograph). Further increases to 4.5 mg and 6 mg twice daily can be made at minimum 2-week intervals based on tolerability. Target therapeutic range: 3-6 mg twice daily.
Note: Administer twice daily, morning and evening, with food to improve tolerability. Swallow capsule whole with water. Do not crush or chew. If switching from capsules to transdermal patch, omit oral dose on the day of switch and apply the first patch.
Rivastigmine exerts its therapeutic effect by enhancing cholinergic function in the cerebral cortex and hippocampus, brain regions critically involved in memory, attention, and learning, which are deficient in Alzheimer's and Parkinson's disease dementia. It does this by inhibiting the enzymes that break down acetylcholine.
Pregnancy: Category B (US FDA). Animal studies show no risk, but no adequate, well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus.
Driving: May cause dizziness, somnolence, and blurred vision. Patients should be cautioned about operating machinery or driving until they know how rivastigmine affects them.
| Metoclopramide | Increased risk of extrapyramidal symptoms | Major |
| Beta-blockers (e.g., Propranolol, Atenolol) | Additive bradycardic effect; risk of syncope | Major |
| Other Cholinesterase Inhibitors (e.g., Donepezil, Galantamine) | Additive cholinergic effects and toxicity | Major |
| Anticholinergic drugs (e.g., Atropine, Oxybutynin, Tricyclic Antidepressants) | Pharmacodynamic antagonism; may reduce rivastigmine efficacy | Moderate |
| Cholinergic agonists (e.g., Bethanechol) | Additive cholinergic effects and toxicity | Moderate |
| Succinylcholine-type muscle relaxants | Prolonged neuromuscular blockade | Moderate |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of gastrointestinal bleeding | Moderate |