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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTI-DEMENTIA DRUGS › Anticholinesterases
rivastigmine
N06DA03
Forms & Strengths
- Oral capsule: 1.5 mg, 3 mg, 4.5 mg, 6 mg
- Oral solution: 2 mg/mL
- Transdermal patch: 4.6 mg/24 hr, 9.5 mg/24 hr, 13.3 mg/24 hr
Adult Dosing
- Alzheimer's disease (Capsules/Solution): Initial 1.5 mg twice daily; titrate by 1.5 mg twice daily every 2 weeks as tolerated to maintenance 3-6 mg twice daily; max 6 mg twice daily.
- Alzheimer's disease (Patch): Initial 4.6 mg/24 hr patch; increase after minimum 4 weeks to 9.5 mg/24 hr; may further increase to 13.3 mg/24 hr if needed.
- Parkinson's disease dementia (Capsules/Solution): Initial 1.5 mg twice daily; titrate by 1.5 mg twice daily every 2 weeks to target 3-6 mg twice daily; max 6 mg twice daily.
- Parkinson's disease dementia (Patch): Initial 4.6 mg/24 hr patch; increase after minimum 4 weeks to 9.5 mg/24 hr; max 13.3 mg/24 hr.
Pediatric Dosing
- Safety and efficacy not established in pediatric patients.
Indications
- Treatment of mild-to-moderate dementia of the Alzheimer's type
- Treatment of mild-to-moderate dementia associated with Parkinson's disease
Mechanism of Action
- Dual inhibitor of both acetylcholinesterase and butyrylcholinesterase
- Slows the degradation of acetylcholine released by functionally intact cholinergic neurons, enhancing cholinergic neurotransmission in the central nervous system
Contraindications
- Known hypersensitivity to rivastigmine, other carbamate derivatives, or any component of the formulation
- Previous history of application-site contact dermatitis with rivastigmine transdermal patch when allergic contact dermatitis is suspected
Adverse Reactions
- Gastrointestinal: Nausea, vomiting, diarrhea, anorexia, abdominal pain, weight loss
- Neurological: Dizziness, headache, somnolence, tremor, syncope
- Psychiatric: Insomnia, anxiety, agitation, depression
- Dermatological (Patch): Application site erythema, pruritus, edema
- Cardiovascular: Bradycardia, hypertension
Drug Interactions
- Cholinesterase inhibitors: May exert synergistic toxicity; concurrent use with other cholinomimetics should be avoided.
- Neuromuscular blocking agents: Rivastigmine may exaggerate succinylcholine-type muscle relaxation during anesthesia.
- Beta-blockers: Risk of additive bradycardia and heart block.
- Metoclopramide: May increase extrapyramidal symptoms or antagonize therapeutic effects.
Curated Content: Needs Vetting Before Put to Clinical Use