Pemoline
Pemoline (Cylert) was an oxazolidinone CNS stimulant used for ADHD from the 1970s until it was withdrawn from most markets in the 2000s over fatal hepatotoxicity. It has substantial historical clinical data but is now largely obsolete because of the liver-failure risk.
01 Overview
Pemoline was valued as a long-acting, once-daily stimulant with weaker sympathomimetic effects than amphetamine. It demonstrated efficacy in ADHD across multiple trials.
Reports of idiosyncratic, sometimes fatal acute hepatic failure led the FDA to conclude the risks outweighed benefits; it was withdrawn in the US (2005), UK, Canada and elsewhere. It remains a Schedule IV controlled substance where still listed.
02 Mechanism
Central dopaminergic stimulant thought to act primarily by increasing dopamine release/transmission, with comparatively little peripheral sympathomimetic activity.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Starting | 37.5 mg/day | Oral | Historical: start 37.5 mg each morning. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Improved attentionReduced inattention and hyperactivity in ADHD, historically demonstrated. | n/a | Clinical | |
| Long durationOnce-daily dosing due to gradual onset and long action. | n/a | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| HepatotoxicityIdiosyncratic acute hepatic failure, sometimes fatal, that prompted withdrawal. | Life-threatening | Rare but fatal | Clinical | |
| InsomniaDifficulty sleeping. | Mild | Common | Clinical | |
| Appetite suppressionReduced appetite. | Mild | Common | Clinical |