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.
Surface here is educational only; do not use without medical supervision. Our editorial verdict is SKIP-PERMANENT — risk:benefit fails for the canonical archetype.
Adrafinil
Modafinil prodrug from the 1980s, withdrawn from French market 2011 for an unfavorable risk-benefit ratio (hepatotoxicity, including…
Aliases (4)
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
▸Brand options3 known
StatusUnscheduled in US (FDA "unapproved drug" — not legal for commercial distribution but not DEA-controlled); withdrawn from prescription markets in France 2011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.
Peptide Interactions
once converted to modafinil, the synergy profile is modafinil's (l-theanine, citicoline, rhodiola, bromantane, selegiline). But there is no reason to stack o…
alcohol (any amount), high-dose acetaminophen, statins, methotrexate, isoniazid, kava, comfrey, high-dose niacin. The additive hepatic load is the major issue.
that would slow conversion — paradoxically would reduce adrafinil → modafinil conversion AND extend exposure to the unconverted parent compound. Worst of bot…
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 1PK-driven acute peak per administration. Verify dose tolerated.
- Week 1Steady-state reached for most daily-dosed pharma.
- Week 2-4Therapeutic effect established; titration window if needed.
- Long-termPeriodic monitoring per drug class (labs, BP, ECG as applicable).
Side Effects & Safety 12
Side Effects
- 1Elevated ALT/AST — most consistent and clinically relevant. Often asymptomatic but detectable on routine LFT. Chronic dose users frequently see 1.5-3× ULN.
- 2Elevated GGT and alkaline phosphatase — co-occurring with transaminase rise.
- 3Stomach pain / GI upset — more common than with modafinil.
- 4Headache — similar to modafinil (~30%).
- 5Skin irritation / pruritus — more common than with modafinil.
- 6Insomnia / shifted sleep onset — same as modafinil mechanism.
- 7Anxiety, nervousness (more frequent than with modafinil per French surveillance)
- 8Dry mouth, increased thirst
- 9Tachycardia, palpitations
- 10Reduced appetite
- 11Dizziness
- 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
primary reference; Lafon developmental history, 1985 narcolepsy approval in France, 2011 voluntary withdrawal due to "unfavorable risk-benefit ratio."
View StudyAdrafinil — DrugBank DB08925
pharmacology, mechanism of action, prodrug-to-modafinil conversion pathway.
View StudyModafinil/Armodafinil — LiverTox NCBI Bookshelf NBK548274
modafinil hepatic safety baseline (likelihood E, "unlikely cause of clinically apparent liver injury") — the comparator that makes adrafinil's signal stand out.
View StudyAdrafinil — PsychonautWiki
community pharmacology summary, dose ranges, subjective effects.
View StudyAdrafinil — American Journal of Psychiatry Residents' Journal 2021
review of adrafinil pharmacology and the prodrug rationale, with discussion of hepatotoxicity.
View StudyIdentification of adrafinil and its main metabolite modafinil — PMC7782130
analytical-chemistry confirmation of metabolic pathway and metabolite formation.
View StudySousa & Dinis-Oliveira 2020 — Modafinil PK/PD review
pharmacokinetic and pharmacodynamic synthesis covering adrafinil's prodrug profile.
View StudyFDA enforcement: Arizona vendor $2.4M fine for adrafinil distribution
2023 case confirming FDA's "unapproved drug" enforcement posture toward US adrafinil distribution.
View StudyAdrafinil PubChem CID 3033226
chemical structure, CAS 63547-13-7, molecular reference.
View StudyHow was your experience with this compound?
Anonymous · one vote per session · results below at 5+ votes.
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