RIVASTIGMINE
THERAPEUTICS
Class
- Neuroscience-based Nomenclature: acetylcholine enzyme inhibitor (ACh-EI)
- Cholinesterase inhibitor (acetylcholinesterase inhibitor and butyrylcholinesterase inhibitor); cognitive enhancer
RIVASTIGMINE commonly prescribed for
(Bold for FDA approved)
How RIVASTIGMINE works
• Pseudoirreversibly inhibits centrally active acetylcholinesterase, making more acetylcholine available
• Increased availability of acetylcholine compensates in part for degenerating cholinergic neurons in neocortex that regulate memory
• Inhibits butyrylcholinesterase
• May release growth factors or interfere with amyloid deposition
How long until RIVASTIGMINE works
• May take up to 6 weeks before any improvement in baseline memory or behavior is evident
• May take months before any stabilization in degenerative course is evident
SIDE EFFECTS
Notable Side Effects
• Nausea, diarrhea, vomiting, appetite loss, weight loss, dyspepsia, increased gastric acid secretion
• Headache, dizziness
• Fatigue, asthenia, sweating
Life Threatening Side Effects
• Rare seizures
• Rare syncope
weight gain

unusual
sedation

unusual
What to do about RIVASTIGMINE side effects
• Wait
• Wait
• Wait
• Use slower dose titration
• Consider lowering dose, switching to a different agent or adding an appropriate augmenting agent
DOSING AND USE
usual dosage range
• Oral: 6–12 mg/day in 2 doses
• Transdermal: 9.5 mg/24 hours once daily
Dosage Forms
• Capsule 1.5 mg, 3 mg, 4.5 mg, 6 mg
• Transdermal 9 mg/5 cm2 (4.6 mg/24 hours), 18 mg/10 cm2 (9.5 mg/24 hours), 27 mg/15 cm2 (13.3 mg/24 hours)
long term use
• Drug may lose effectiveness in slowing degenerative course of Alzheimer disease after 6 months
• Can be effective in many patients for several years
habit forming
• No
SPECIAL POPULATIONS
Renal Impairment
• Dose adjustment not necessary; titrate to point of tolerability
Hepatic Impairment
• Dose adjustment not necessary; titrate to point of tolerability
Cardiac Impairment
• Should be used with caution
• Syncopal episodes have been reported with the use of rivastigmine
Elderly
• Some patients may tolerate lower doses better
• Use of cholinesterase inhibitors may be associated with increased rates of syncope, bradycardia, pacemaker insertion, and hip fracture in older adults with dementia
Children and Adolescents
• Safety and efficacy have not been established
Pregnancy
• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001
• Controlled studies have not been conducted in pregnant women
• Animal studies do not show adverse effects
• Not recommended for use in pregnant women or women of childbearing potential
Breast Feeding
• Unknown if rivastigmine is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk
• Recommended either to discontinue drug or bottle feed
• Rivastigmine is not recommended for use in nursing women
Based on data Published online by Cambridge University Press
Compiled by Dr. Jash Ajmera