Huperzine A

Cholinergicoral · inferred

Naturally derived reversible acetylcholinesterase inhibitor from Chinese club moss (Huperzia serrata). Highly selective for AChE over BuChE. Biphasic pharmacokinetics: rapid distribution (alpha ~21 min) followed by slower elimination (beta half-life up to 12h). Do NOT combine with other cholinesterase inhibitors (donepezil, rivastigmine, galantamine).

Projected serum levels — 200 mcg (≈ 0.20 mg), once daily

Huperzine A
Huperzine A modeled serum levels, 200 mcg (≈ 0.20 mg) once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 0.25 0.50 0.75 1 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1
Huperzine A modeled serum levels with a loading dose of 257 mcg, then 200 mcg (≈ 0.20 mg) once daily The first dose is larger so levels approach steady state faster. 0 0.25 0.50 0.75 1 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 200 mcg (≈ 0.20 mg) once daily (oral).

Loading schedule: 257 mcg on day 1, then 200 mcg (≈ 0.20 mg) once daily — reaching therapeutic levels sooner.

Modeled steady state after ~1 days: peak ≈ 0.23 mg, trough ≈ 0.056 mg body load. Population-based estimate over 15 days for a reference dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Cholinergic
Route modeled
Oral
Model confidence
inferred
Half-life
11 h
Common dose
200 mcg (≈ 0.20 mg)
Suggested maximum
400 mcg/day
Reference dose range
100–400 mcg (single dose)
Suggested cadence
once daily
Validated against
0.40 mg oral — Cmax 0.001 mg/L at 1.3 h

Documented interactions

  • danger
    Carbamazepine (Tegretol) + Huperzine A CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Huperzine A AUC by ~0.43x

  • danger
    Efavirenz (Sustiva) + Huperzine A CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Huperzine A AUC by ~0.30x

  • danger
    Rifampin + Huperzine A CYP induction

    Rifampin inducer of CYP3A4 predicted to change Huperzine A AUC by ~0.30x

  • danger
    St. John's Wort (Hypericum perforatum) + Huperzine A CYP induction

    St. John's Wort (Hypericum perforatum) inducer of CYP3A4 predicted to change Huperzine A AUC by ~0.50x

  • moderate
    Amlodipine (Norvasc) + Huperzine A CYP inhibition

    Amlodipine (Norvasc) reversible_inhibitor of CYP3A4 predicted to change Huperzine A AUC by ~1.30x

  • moderate
    Apigenin + Huperzine A CYP inhibition

    Apigenin reversible_inhibitor of CYP1A2 predicted to change Huperzine A AUC by ~1.87x

Serum checks 84 modeled interaction pairings for huperzine a across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Huperzine A for Alzheimer's disease: a systematic review and meta-analysis of randomized clinical trials Yang G et al. · PLOS ONE, 2013 DOI

    Meta-analysis of 20 RCTs (1823 participants) found Huperzine A significantly improved MMSE scores at 8, 12, and 16 weeks in Alzheimer patients with no severe adverse events.

  2. A phase II trial of huperzine A in mild to moderate Alzheimer disease Rafii MS et al. · Neurology, 2011 DOI

    ADCS Phase II RCT in 210 mild-to-moderate AD patients found 200 mcg BID huperzine A did not demonstrate cognitive benefit over 16 weeks, though 400 mcg BID showed trends for improvement.

  3. Pharmacokinetics of huperzine A following oral administration to human volunteers Li YX et al. · European Journal of Drug Metabolism and Pharmacokinetics, 2007 DOI

    Human PK study established two-compartment open model: Tmax ~58 min, Cmax 2.59 ng/mL, absorption half-life 12.6 min, and elimination half-life ~4.8 hours.

  4. A phase II trial of huperzine A in mild to moderate Alzheimer disease. Rafii MS, Walsh S, Little JT, Behan K, Reynolds B, Ward C, Jin S, Thomas R, Aisen PS, Alzheimer's Disease Cooperative Study · Neurology, 2011 DOI

    This citation reports a human clinical study involving Huperzine A. It does not by itself establish a qualified dose, safety profile, efficacy claim, or pharmacokinetic route for this record.

4 published studies referenced in the app, each with a plain-language summary.