Donepezil: Difference between revisions

| generic           = Donepezil

| brand             = Aricept (oral), Adlarity (transdermal patch)

| structure         =

| classes           = [[:Category:Anti-dementia medicines|Anti-dementia medicine]], [[:Category:Acetylcholinesterase inhibitors|Acetylcholinesterase inhibitor]]

| uses             = <vote slug="alzheimer-mild-moderate-use">Alzheimer disease dementia, mild to moderate (FDA)</vote>, <vote slug="alzheimer-severe-use">Alzheimer disease dementia, severe (FDA, 23 mg/day formulation)</vote>, <vote slug="lewy-body-dementia-use">Lewy body dementia (off-label)</vote>, <vote slug="parkinson-disease-dementia-use">Parkinson disease dementia (off-label)</vote>

| starting_dose     = 5 mg PO once daily at bedtime; titrate to 10 mg/day after 4-6 weeks. Severe Alzheimer disease: may escalate to 23 mg/day. Adlarity patch: 5 or 10 mg/day applied weekly

| preparations     = Oral tablets 5, 10, 23 mg; ODT 5, 10 mg; Adlarity transdermal patch 5, 10 mg/day (weekly application)

| fda_max           = 23 mg/day

| pill_id           =

| routes           = Oral, transdermal

| onset             = Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose

| duration         = 24 hours (once-daily dosing)

| halflife          = ~70 hours (long, supports once-daily dosing without peak-trough variation)<ref name="aricept-label">FDA Prescribing Information, Aricept (donepezil hydrochloride), Eisai/Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020690s039lbl.pdf</ref>

| bioavailability   = ~100% (oral)<ref name="aricept-label" />

| pregnancy        = Limited human data; rarely indicated in pregnancy given the patient population.{{citation needed}}

| legal             = [[USLegal:Prescription only|Rx-only]] in US

| mechanism         = <vote slug="donepezil-mech-claim">Selective, reversible acetylcholinesterase inhibitor with central nervous system penetration. Increases synaptic acetylcholine in cortical and hippocampal circuits, partially compensating for the characteristic cholinergic deficit of Alzheimer disease.</vote> The effect is symptomatic only: donepezil does '''not''' alter the underlying neurodegenerative trajectory. CYP3A4 and CYP2D6 metabolism. '''Cholinergic adverse effects''' (nausea, diarrhea, vomiting, vivid dreams, bradycardia, syncope) are dose-limiting; bradyarrhythmia and syncope are clinically important, with risk elevated by concurrent β-blockers or non-dihydropyridine calcium channel blockers. The bedtime dosing convention minimizes nausea and vivid-dream burden<ref name="aricept-label" />.

 

[[Category:Anti-dementia medicines]]

[[Category:Acetylcholinesterase inhibitors]]