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Pemoline
Pemoline is a central nervous system stimulant1 of the 4-oxazolidinone class2 that was used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy.2 It was first synthesized in 1913, and its stimulant activity was identified in the 1930s. It has relatively little cardiovascular activity compared with many other stimulants. Rare cases of severe liver damage have been reported during medical use, sometimes requiring transplantation or resulting in death.3
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Pemoline is described as a selective dopamine reuptake inhibitor,4 although its precise mechanism has not been definitively established.5 In animal studies, it appears to inhibit dopamine reuptake and weakly promote dopamine release, increasing brain dopamine levels and indirectly activating dopamine receptors. It appears to have no significant central or peripheral noradrenergic activity.6
Pharmacokinetics
Pemoline is rapidly absorbed from the gastrointestinal tract,5 and food does not significantly affect absorption. After oral administration, peak blood levels occur within 2-4 hours,5 and multiple-dose studies in adults at several dose levels indicate that steady state is reached in approximately 2-3 days.5 Plasma protein binding is reported as either insignificant or approximately 50%. Pemoline undergoes hepatic metabolism,5 including conjugation, and is eliminated primarily through the kidneys, with approximately 50% excreted unchanged and minor amounts excreted as metabolites.5 Its elimination half-life is 7-12 hours, approximately 7 hours in children and potentially increasing to 11-12 hours with age. Conventional tablets and chewable tablets, whether swallowed or chewed, showed no differences in pharmacokinetics.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
Addiction & Dependence
Psychological
Pemoline can be habit-forming.7
Toxicity
Pemoline can rarely cause severe liver injury progressing to liver failure, transplantation, or death, including in children and adolescents. Injury is idiosyncratic and unpredictable, may develop after months or years of treatment, and has no clear relationship to exposure.
History & Culture
Pemoline was first synthesized in 1913, and its stimulant activity was identified in the 1930s. It was approved for the treatment of attention deficit hyperactivity disorder (ADHD) in the United States in 1975.10 It was also used to treat narcolepsy and excessive daytime…
Legality
International
Controlled internationally under the UN Convention on Psychotropic Substances 1971.
References
Source Pages
Citations
Article Status
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