Pemoline is a stimulant drug of the oxazoline class. It was first synthesized in 1913 but its activity was not discovered until the 1930s. Under the names Betanamin, Cylert, Tradon, and Ceractiv it was used as a medication to treat attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Under the Convention on Psychotropic Substances, it is a Schedule IV drug. It is no longer generally available in the United States because pemoline magnesium, a chelate between pemoline and magnesium, displays certain pharmacological advantages over pemoline. The compound is the monohydrate of an equimolar mixture between pemoline and magnesium hydroxide. The absorption of pemoline magnesium is more rapid and the duration of action is extended, and the effect is more reliable.
Pemoline is generally considered dopaminergic, but its precise method of action hasn't yet been definitively determined. Pemoline passes the blood–brain barrier and acts as a surrogate for dopamine, not affecting endogenous intracellular dopamine. For this reason, and the fact that it has little or no affinity for adrenaline receptors, pemoline has minimal sympathomimetic side effects such as: dry mouth, reduction in appetite, high blood pressure, increased heart rate, constriction of smooth muscle, cardiac stress, dilated pupils and insomnia. There is some data to suggest that pemoline is a nootropic acting as a catalyst conductor in the synapses of the brain's memory centers, raising the efficiency of memory and assisting RNA formation in the brain. While drugs like dexamphetamine and methylphenidate are classified as Schedule II, pemoline is listed as Schedule IV (non-narcotic). In studies conducted on primates, pemoline fails to demonstrate a potential for self-administration.
In some patients pemoline is suspected of causing hepatotoxicity, so the FDA recommended that regular liver tests should be performed on those treated with it. Since receiving FDA approval in 1975, it has been linked with 21 cases of liver failure, of which 13 resulted in liver replacement or death.
In March 2005 Abbott Laboratories and generic manufacturers withdrew pemoline from the market due to concerns about the liver toxicity risk.
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