Chemical Compound

Centrophenoxine

Meclofenoxate

Evidence TierDWADA PROHIBITED

tuneTypical Dose

2 g/day reported in one 8-week dementia trial. 200 mg single-dose PK data available.

watchEffect Window

Weeks to ~3 months in legacy trials

lockCompliance

WADA PROHIBITED

Overview

Clinical Summary

Centrophenoxine is a synthetic cholinergic compound with mostly legacy cognition data in older adults and little contemporary replication.

Older dementia and aging trials reported some improvement in alertness, memory consolidation, and psychometric outcomes, and preclinical work linked meclofenoxate to reduced lipofuscin accumulation and oxidative stress. Those details still matter, but the evidence is legacy-era, methodologically dated, and not a basis for broad anti-aging or high-confidence modern cognition claims.

Meclofenoxate is a prodrug with DMAE-related cholinergic plausibility and preclinical anti-oxidative/lipofuscin-related signals. Translational support remains limited and inconsistent.

Outcomes

What This Is Expected To Influence

Primary Outcomes

  • Fit elderly trial signals improved memory consolidation and alertness vs placebo in specific domains.
  • Dementia RCTs report improved psychometric and psychogeriatric outcomes in some participants.

Secondary Outcomes

  • Preclinical animal models suggest reduced age-related neuronal pigment markers under specific dosing conditions.
  • No consistent evidence for broad anti-aging prevention endpoints in humans.

Safety

Contraindications and Interactions

Contraindications

  • Pregnancy/lactation (DMAE metabolite neural tube defect risk)
  • Severe hypertension
  • Seizure history
  • Major psychiatric instability
  • Severe hepatic/renal disease

Side effects

  • Headache
  • Nausea/GI upset
  • Insomnia
  • Irritability
  • Jaw tension (anecdotal)

Interactions

  • Anticholinergics (opposes mechanism)
  • Cholinesterase inhibitors (additive cholinergic load)
  • Alpha-GPC/CDP-choline/DMAE/huperzine A (overlapping choline pathways)

Avoid if

  • Active mania/psychosis
  • Uncontrolled cardiovascular disease
  • Label-uncertain OTC products
  • Women of childbearing age without reliable contraception

Evidence

Study-level References

centrophenoxine-SRC-001Double-blind controlled clinical trial (human)
Sourceopen_in_new

Marcer, D. and Hopkins, S.M. "The differential effects of meclofenoxate on memory loss in the elderly." Age Ageing. 1977;6(2):123-31. DOI: 10.1093/ageing/6.2.123. PMID: 329662.

Population: Fit elderly adults

Dose protocol: Meclofenoxate versus placebo. Memory performance battery and alertness outcomes (dose not fully specified in abstract).

Key findings: Reported improved consolidation of new information into long-term memory and greater alertness. No benefit across all memory domains.

Notes: Effect appears endpoint-specific. Limited sample-era detail.

Paper content

Reported improved consolidation of new information into long-term memory and greater alertness; no benefit across all memory domains.

centrophenoxine-SRC-002Randomized double-blind placebo trial
Sourceopen_in_new

Fülöp Jr, T. et al. "Effects of centrophenoxine on body composition and some biochemical parameters of demented elderly people as revealed in a double-blind clinical trial." Arch Gerontol Geriatr. 1990;10(3):239-51. DOI: 10.1016/0167-4943(90)90025-2. PMID: 15374499.

Population: Older adults with dementia (n=50, average age 77)

Dose protocol: 2 g/day meclofenoxine for 8 weeks, after 2-week placebo lead-in control period

Key findings: Reported psychometric improvements and intracellular water increase with meclofenoxine treatment.

Notes: Legacy trial. Endpoints include biochemical and cognitive metrics. Full adverse-event detail limited in abstract.

Paper content

Reported psychometric improvements and intracellular water increase with meclofenoxine treatment.

centrophenoxine-SRC-003Randomized comparative clinical trial
Sourceopen_in_new

Popa, R. et al. "Antagonic-stress superiority versus meclofenoxate in gerontopsychiatry (alzheimer type dementia)." Arch Gerontol Geriatr. 1994;19 Suppl 1:197-206. DOI: 10.1016/S0167-4943(05)80065-2. PMID: 18649860.

Population: Older adults with SDAT (n=63)

Dose protocol: meclofenoxate versus comparator over 3 months

Key findings: Reported reduced psychogeriatric scores and improved cognitive performance, with comparator superiority over monotherapy.

Notes: Context includes combined regimen comparison. Magnitude relative to placebo unclear from abstract summary.

Paper content

Reported reduced psychogeriatric scores and improved cognitive performance, with comparator superiority over monotherapy.

centrophenoxine-SRC-004Animal cognitive aging model
Sourceopen_in_new

Nandy, K. J. "Centrophenoxine: effects on aging mammalian brain" (animal preclinical component; same publication as above). PMID: 342588.

Population: Aged female mice

Dose protocol: 3 months meclofenoxate exposure

Key findings: Meclofenoxine-treated mice improved in maze learning and reduced neuronal lipofuscin markers.

Notes: Preclinical support only. Not sufficient for human anti-aging efficacy claims.

Paper content

Reduced lipofuscin-associated changes plus behavioral learning improvement in treated old mice.

centrophenoxine-SRC-005Animal cognitive aging model
Sourceopen_in_new

Nandy, K. J. "Centrophenoxine: effects on aging mammalian brain" (animal preclinical component; same publication as above). PMID: 342588.

Population: Aged female mice

Dose protocol: repeated dosing for 3 months

Key findings: Reduced lipofuscin-associated changes plus behavioral learning improvement in treated old mice.

Notes: This source confirms preclinical mechanism signal but should not be interpreted as clinical proof.

Paper content

Reduced lipofuscin-associated changes plus behavioral learning improvement in treated old mice.

centrophenoxine-SRC-006Product-content and regulatory-risk analysis (public health)
Sourceopen_in_new

Cohen, P.A. et al. "The unapproved drug centrophenoxine (meclofenoxate) in cognitive enhancement dietary supplements." Clin Toxicol (Phila). 2022;60(10):1156-1158. DOI: 10.1080/15563650.2022.2109485. PMID: 35959800.

Population: OTC supplement products sold in US market

Dose protocol: 7-product product assay

Key findings: Centrophenoxine detected in all sampled products, with 79-251 mg per serving and high label-label mismatch.

Notes: Strong product-quality signal for dosing uncertainty. Not a clinical efficacy trial.

Paper content

Centrophenoxine detected in all sampled products, with 79–251 mg per serving and high label-label mismatch.

centrophenoxine-SRC-007PK crossover trial
Sourceopen_in_new

Zou, J-J. et al. "Bioequivalence and pharmacokinetic comparison of a single 200-mg dose of meclofenoxate hydrochloride capsule and tablet formulations in healthy Chinese adult male volunteers." Clin Ther. 2008;30(9):1651-7. DOI: 10.1016/j.clinthera.2008.09.013. PMID: 18840370.

Population: Healthy adult male volunteers (n=24)

Dose protocol: Single 200 mg oral dose, crossover capsule vs tablet

Key findings: Bioequivalence of two formulations. No adverse events reported in the single-dose setting.

Notes: Supports formulation-level PK, not clinical efficacy.

Paper content

Bioequivalence of two formulations; no adverse events reported in the single-dose setting.

centrophenoxine-SRC-008Clinical trial
Sourceopen_in_new

Fisman, M. et al. "Double-blind trial of 2-dimethylaminoethanol in Alzheimer's disease." Am J Psychiatry. 1981;138(7):970-972. DOI: 10.1176/ajp.138.7.970. PMID: 7020434.

Population: People with moderate-to-severe Alzheimer disease

Dose protocol: DMAE trial. Active component relevance for mechanistic/safety context.

Key findings: High withdrawal due to side effects (drowsiness/retardation/confusion/mild BP elevation), with no significant benefit.

Notes: Component-level safety signal only. Not a direct equivalence to meclofenoxine trials.

Paper content

High withdrawal due to side effects (drowsiness/retardation/confusion/mild BP elevation), with no significant benefit.

centrophenoxine-SRC-009Regulatory/athlete education summary
Sourceopen_in_new

U.S. Anti-Doping Agency. "What Do Athletes Need to Know About Meclofenoxate?" USADA, Feb 2026 update. URL: https://www.usada.org/spirit-of-sport/athletes-need-know-meclofenoxate/

Population: Athletes/supplement regulation context

Dose protocol: Product classification and supplement-market context

Key findings: Classifies meclofenoxate as prohibited stimulant context. Notes USFDA non-approval for medical indications and likely non-legitimate DS status.

Notes: Policy/regulatory source. Not primary clinical efficacy evidence.

Paper content

Classifies meclofenoxate as prohibited stimulant context; notes USFDA non-approval for medical indications and likely non-legitimate DS status.