Rivamer

FDA‑Approved Indications:

• Mild to Moderate Alzheimer's Disease (AD): Oral and transdermal patch forms for symptomatic treatment to improve cognition and function.
• Mild to Moderate Parkinson’s Disease Dementia (PDD): Symptomatic treatment of dementia associated with Parkinson’s disease.

Off‑Label / Clinically Accepted Uses:

• Lewy Body Dementia (LBD): Used to manage cognition and behavioral symptoms.
• Vascular Cognitive Impairment: Limited data suggest potential benefit.
• Postoperative Delirium Prevention: Emerging off-label use in elderly hospitalized patients.

Route: Oral capsules/tablets or transdermal patch.

Adults & Elderly:

• Oral:
• Start with 1.5 mg twice daily.
• Increase by 1.5 mg every two weeks up to 6 mg twice daily, tolerated.
• Transdermal Patch:
• Start at 4.6 mg/24 h.
• After four weeks, increase to 9.5 mg/24 h if well tolerated.
• Can escalate to 13.3 mg/24 h patch for severe symptoms.

Pediatric Use: Not established.

Renal Impairment:

• Mild–moderate: No adjustment.
• Severe: Use lower starting oral dose (1.5 mg BID). Monitor closely.

Hepatic Impairment:

• Mild–moderate: No adjustment.
• Severe: No clinical data; use with prudence.

Administration Notes:

• Oral doses with food to reduce GI upset.
• Apply patch to clean, dry, non‑hairy skin; rotate sites daily.

Rivastigmine is a dual inhibitor of acetylcholinesterase and butyrylcholinesterase, increasing acetylcholine levels within the brain. By enhancing cholinergic transmission in hippocampal and cortical neurons, it helps improve memory, attention, and other cognitive functions. The reversible binding of rivastigmine leads to prolonged elevation of acetylcholine, offering symptomatic relief in neurodegenerative dementias.

• Absorption:
• Oral—peak plasma level in ~1 hour.
• Transdermal—steady absorption over 24 hours.
• Bioavailability (Oral): ~36% due to first-pass metabolism.
• Distribution: Volume of distribution ~5 L/kg; ~40% protein-bound.
• Metabolism: Enzymatically hydrolyzed via brain esterases to inactive metabolites (no CYP involvement).
• Half-life: ~1.5 hours (oral); sustained release from patch materials.
• Elimination: Primarily renal as metabolites; <1% excreted unchanged.
• Onset: Steady state reached in 1–2 days with oral; 2–3 days with patch.

• Pregnancy: Category C. Animal studies show adverse effects at high doses. Use only if benefit outweighs risk.
• Lactation: Likely excreted in breast milk due to molecular size—use with caution. Breastfeeding is generally not recommended during therapy.
• Data: Limited human data; use only if necessary and with clinical monitoring.

• Primary Class: Cholinesterase Inhibitor
• Subclass: Dual BuChE and AChE inhibitor

• Known hypersensitivity to rivastigmine, carbamate derivatives, or excipients
• History of severe allergic reaction to cholinesterase inhibitors
• Skin conditions preventing patch use (e.g., atopic dermatitis at application sites)

• Gastrointestinal Disturbances: Start low, titrate slowly.
• Cardiac Issues: Avoid in sick sinus syndrome, bradyarrhythmias, or conduction blocks unless pacemaker-inserted.
• Pulmonary Disease: Caution in asthma or COPD due to possible bronchospasm.
• Genitourinary Disorders: May exacerbate urinary obstruction.
• Neurologic Risks: Syncope or seizures possible; monitor neurological status.
• Topical Site Reactions: With patch use; monitor skin regularly.
• Weight Loss: Especially in elderly—monitor body weight weekly.

Common:

• GI: Nausea, vomiting, diarrhea, decreased appetite
• Neurologic: Headache, dizziness, insomnia
• CV: Bradycardia, syncope (more likely at higher doses)
• Dermatologic: Skin irritation at patch site

Serious (Rare):

• Severe bradyarrhythmias, AV block, seizures
• Extrapyramidal or neuroleptic malignant syndrome-like symptoms
• Severe weight loss and malnutrition
• Syncope-related injuries

Timing & Dose Dependence:

• GI side effects appear early and taper with dose stability.
• Bradycardia and syncope may emerge at higher doses or in predisposed individuals.

• Anticholinergics (e.g., benztropine): May negate effect
• Cholinomimetics (e.g., bethanechol): Additive effects
• Ketoconazole: May increase oral rivastigmine levels—use with caution
• Bradycardic Agents (beta-blockers, digoxin): Increased risk of bradycardia/syncope
• NSAIDs/Ulcerogenic Drugs: GI bleeding risk due to potential mucosal irritation

• International dementia guidelines: Include rivastigmine patch as alternative to oral formulation for improved tolerability.
• NICE: Recommends patch for patients intolerant to oral therapy or with swallowing issues.
• ADA: Highlights use in Parkinson’s disease dementia.
• New evidence: Supports earlier initiation in dementia for optimal functional benefit; patch form may reduce GI side effects and improve adherence.

• Temperature: 20°C–25°C (68°F–77°F); excursions up to 30°C permitted
• Humidity/Light: Keep in original foil pouch; store in dry place away from direct sunlight
• Handling:
• Capsules/Tablets: Keep in blister until use
• Patch: Remove backing just before application; discard used patch and fold adhesive to prevent accidental exposure
• Refrigeration: Not required
• Disposal: Fold used patch and discard securely out of reach of children and pets