RIVASTIGMINE

brands

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

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

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

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