DONEPEZIL

brands

Class

• Neuroscience-based Nomenclature: acetylcholine enzyme inhibitor (ACh-EI)
• Cholinesterase inhibitor (selective acetylcholinesterase inhibitor); cognitive enhancer

DONEPEZIL commonly prescribed for

(Bold for FDA approved)

How DONEPEZIL works

• Reversibly but noncompetitively inhibits centrally active acetylcholinesterase, making more acetylcholine available</br>

• Increased availability of acetylcholine compensates in part for degenerating cholinergic neurons in neocortex that regulate memory</br>

• Does not inhibit butyrylcholinesterase</br>

• May release growth factors or interfere with amyloid deposition

How long until DONEPEZIL 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, increased gastric acid secretion, weight loss

• Insomnia, dizziness

• Muscle cramps, fatigue, depression, abnormal dreams

• Application-site reactions (transdermal system)

• Nausea, diarrhea, vomiting, appetite loss, increased gastric acid secretion, weight loss

• Insomnia, dizziness

• Muscle cramps, fatigue, depression, abnormal dreams

• Application-site reactions (transdermal system)

Life Threatening Side Effects

• Rare seizures

• Rare syncope

• Allergic contact dermatitis (transdermal system)

weight gain

unusual

sedation

unusual

What to do about DONEPEZIL side effects

• Wait

• Wait

• Wait

• Take in daytime to reduce insomnia

• Use slower dose titration

• Consider lowering dose, switching to a different agent, or adding an appropriate augmenting agent

usual dosage range

• 5–10 mg at night

Dosage Forms

• Tablet 5 mg, 10 mg, 23 mg

• Orally disintegrating tablet 5 mg, 10 mg

• Namzaric extended-release (combination memantine/donepezil) 7 mg/10 mg, 14 mg/10 mg, 21 mg/10 mg, 28 mg/10 mg

• Adlarity transdermal system 5 mg, 10 mg

long term use

• Drug may lose effectiveness in slowing degenerative course of Alzheimer disease after 6 months

• Can be effective in some patients for several years

habit forming

• No

Renal Impairment

• Few data available but dose adjustment is most likely unnecessary

• For Namzaric, for patients with severe renal impairment, the recommended maintenance dose is 14 mg/10 mg once daily in the evening

Hepatic Impairment

• Few data available; may need to lower dose

Cardiac Impairment

• Should be used with caution

• Syncopal episodes have been reported with the use of donepezil

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

• Preliminary reports of efficacy as an adjunct in attention deficit hyperactivity disorder (ADHD) (ages 8–17)

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Not recommended for use in pregnant women or women of childbearing potential

Breast Feeding

• Unknown if donepezil is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or formula feed

• Donepezil is not recommended for use in nursing women