This page describes pharmacological agents that may have legal restrictions, side effects, and drug interactions in your jurisdiction. Information is for educational research only — consult a clinician before considering any compound.

High-risk compound

Surface here is educational only; do not use without medical supervision. Our editorial verdict is SKIP-PERMANENT — risk:benefit fails for the canonical archetype.

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Adrafinil

Extensively Studied

Modafinil prodrug from the 1980s, withdrawn from French market 2011 for an unfavorable risk-benefit ratio (hepatotoxicity, including…

Aliases (4)
Olmifon · CRL-40028 · (±)-2-[(diphenylmethyl)sulfinyl]-N-hydroxyacetamide · ADRAFINIL
TYPICAL DOSE
600-900 mg
Daily
ROUTE
Oral (tablet)
Oral
CYCLE
Same as modafinil
As prescribed
STORAGE
Room temp; original container
Room temp

Overview

What is Adrafinil?

Adrafinil is a prodrug of modafinil, formerly marketed in France as Olmifon for narcolepsy. It is sold OTC in many jurisdictions as a non-scheduled wakefulness-promoting agent, metabolized hepatically to modafinil after oral dosing.

Key Benefits

Promotes wakefulness and sustained attention with effects similar to modafinil but slower onset (1-2 hr); reduces fatigue and supports cognitive endurance during long work sessions or sleep deprivation.

Mechanism of Action

Prodrug — hepatic conversion to modafinil and modafinilic acid. Downstream effects mirror modafinil: dopamine reuptake inhibition (DAT), elevated histaminergic and orexinergic tone, with minimal classical sympathomimetic activity.

Pharmacokinetics

·
PeakHalf-life
Approximate curve — visual aid only, not data-precise PK
Brand options3 known
OlmifonCRL-40028ADRAFINIL

StatusUnscheduled in US (FDA "unapproved drug" — not legal for commercial distribution but not DEA-controlled); withdrawn from prescription markets in France 2011

Research Protocols

Disclaimer: These are commonly discussed research protocols and not medical advice.

Goal:Cycled use only
Dose:
Frequency:
Solo:
Cycle:

Peptide Interactions

N/A
Synergistic

once converted to modafinil, the synergy profile is modafinil's (l-theanine, citicoline, rhodiola, bromantane, selegiline). But there is no reason to stack o…

Other hepatotoxic compounds
Avoid

alcohol (any amount), high-dose acetaminophen, statins, methotrexate, isoniazid, kava, comfrey, high-dose niacin. The additive hepatic load is the major issue.

CYP3A4 inhibitors
Avoid

that would slow conversion — paradoxically would reduce adrafinil → modafinil conversion AND extend exposure to the unconverted parent compound. Worst of bot…

Hormonal contraceptives
Avoid

same CYP3A4 induction issue as modafinil; reduced contraceptive efficacy during use and 1 month after.

Quality Indicators

Pharmacy-dispensed, intact packaging

Prescription tablets in original sealed packaging from a licensed pharmacy.

!

Generic vs branded

Generics are usually fine but bioavailability can vary slightly; track if you switch.

Unbranded blister or counterfeit risk

Counterfeit pharmaceuticals are a known issue; verify pharmacy and lot if buying internationally.

What to Expect

  • Day 1
    PK-driven acute peak per administration. Verify dose tolerated.
  • Week 1
    Steady-state reached for most daily-dosed pharma.
  • Week 2-4
    Therapeutic effect established; titration window if needed.
  • Long-term
    Periodic monitoring per drug class (labs, BP, ECG as applicable).

Side Effects & Safety 12

Side Effects

  1. 1Elevated ALT/AST — most consistent and clinically relevant. Often asymptomatic but detectable on routine LFT. Chronic dose users frequently see 1.5-3× ULN.
  2. 2Elevated GGT and alkaline phosphatase — co-occurring with transaminase rise.
  3. 3Stomach pain / GI upset — more common than with modafinil.
  4. 4Headache — similar to modafinil (~30%).
  5. 5Skin irritation / pruritus — more common than with modafinil.
  6. 6Insomnia / shifted sleep onset — same as modafinil mechanism.
  7. 7Anxiety, nervousness (more frequent than with modafinil per French surveillance)
  8. 8Dry mouth, increased thirst
  9. 9Tachycardia, palpitations
  10. 10Reduced appetite
  11. 11Dizziness
  12. 12Orofacial dyskinesia (case reports in elderly Olmifon population — likely a population-specific effect)

When to Stop

  • Clinical hepatitis — case reports in French post-marketing data, including a small number requiring discontinuation and clinical workup. This is the smoking gun that withdrew Olmifon from the French market in 2011.
  • Stevens-Johnson Syndrome / DRESS / TEN — inherited risk via modafinil pathway; same 1-8 week watch period applies. Possibly *higher* baseline risk than pure modafinil because of additional reactive intermediate exposure during hepatic conversion.
  • Psychiatric — psychosis, mania, suicidal ideation (rare, inherited from modafinil).
  • Cardiovascular — PVCs, BP elevation (inherited from modafinil).
  • Weeks 1-8: SJS rash watch (inherited from modafinil; possibly elevated baseline risk).
  • Weeks 4-12: liver enzyme elevation watch — mandatory ALT/AST/GGT/bilirubin panel at 4 weeks and 12 weeks if used at all. Stop drug immediately on >3× ULN.
  • Indefinite: hepatic surveillance — chronic users need quarterly LFTs minimum.

References

Adrafinil — Wikipedia 2026

en.wikipedia.org · 2026

primary reference; Lafon developmental history, 1985 narcolepsy approval in France, 2011 voluntary withdrawal due to "unfavorable risk-benefit ratio."

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Adrafinil — DrugBank DB08925

go.drugbank.com

pharmacology, mechanism of action, prodrug-to-modafinil conversion pathway.

View Study

Modafinil/Armodafinil — LiverTox NCBI Bookshelf NBK548274

ncbi.nlm.nih.gov

modafinil hepatic safety baseline (likelihood E, "unlikely cause of clinically apparent liver injury") — the comparator that makes adrafinil's signal stand out.

View Study

Adrafinil — PsychonautWiki

psychonautwiki.org

community pharmacology summary, dose ranges, subjective effects.

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Adrafinil — American Journal of Psychiatry Residents' Journal 2021

psychiatryonline.org · 2021

review of adrafinil pharmacology and the prodrug rationale, with discussion of hepatotoxicity.

View Study
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