Huperzine A

Class

Reversible acetylcholinesterase inhibitor / NMDA receptor antagonist (natural alkaloid supplement)

Mechanism

Inhibits acetylcholinesterase to increase acetylcholine levels; also exhibits neuroprotective and NMDA receptor antagonism properties

FDA-Approved Use

None (supplement, not FDA-approved)

Off-Label Use

Cognitive enhancement, Alzheimer’s disease (AD), vascular dementia, mild cognitive impairment (MCI)

Formulation

Oral capsules/tablets, typically OTC supplements

Titration

100–400 mcg/day divided BID; dosing varies by product

Dose Range

100–400 mcg/day

Kinetics

Limited formal pharmacokinetic data; oral absorption variable

Common AEs

Nausea, diarrhea, insomnia, bradycardia, dizziness

Serious/Rare AEs

Unknown; long-term safety data lacking

Monitoring

Monitor for bradycardia and additive cholinergic effects, especially if combined with other cholinergic drugs

Black Box Warning

None

Considerations

May offer modest cognitive benefit in AD, vascular dementia, and post-stroke cognitive decline. Limited evidence supports use in younger adults with attention or memory complaints. Use caution in patients with cardiac conduction abnormalities or when combined with other cholinergic agents due to potential additive effects. Not FDA-approved and lacks long-term safety data; use should be individualized with informed consent.