Pemoline

Pemoline is a stimulant drug of the oxazoline class that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. Pemoline acts as a dopamine agonist, specifically at the D1 and D2 receptors. It is distinguished from other psychostimulants by its mode of action, primarily affecting dopaminergic neurotransmission without significant effects on norepinephrine or serotonin pathways. This unique mechanism contributes to its therapeutic effects and side effect profile.

Medical Uses

Pemoline is primarily indicated for the treatment of ADHD in children and adults. It has also been used to manage symptoms of narcolepsy, a sleep disorder characterized by excessive daytime sleepiness and sudden sleep attacks. The medication aims to increase alertness, attention span, and overall cognitive performance by stimulating the central nervous system.

Side Effects

The use of pemoline can be associated with several side effects, ranging from mild to severe. Common adverse effects include insomnia, irritability, increased heart rate, and headache. Less frequently, pemoline has been linked to more serious conditions such as liver toxicity, which can be potentially life-threatening. Due to the risk of liver damage, pemoline is considered a second-line treatment and requires regular monitoring of liver function tests during therapy.

Pharmacology

Pemoline exhibits its stimulant effects primarily through the modulation of dopaminergic activity in the brain. Unlike other stimulants that increase dopamine release, pemoline is thought to act by enhancing dopamine receptor sensitivity. This action results in improved neurotransmission in areas of the brain responsible for regulating attention and behavior.

History

Pemoline was first synthesized in the early 20th century and was introduced for medical use in the United States in the 1970s. Its use has declined over the years due to concerns about its hepatotoxicity and the availability of other ADHD medications with safer profiles. In some countries, pemoline has been withdrawn from the market or its use has been severely restricted.

Legal Status

The legal status of pemoline varies by country. In the United States, it is classified as a Schedule IV controlled substance under the Controlled Substances Act, indicating a lower potential for abuse compared to more potent stimulants. However, due to safety concerns, the production and prescription of pemoline have been discontinued in the U.S. since 2005.

See Also

• Stimulant
• Dopamine agonist
• Attention deficit hyperactivity disorder
• Narcolepsy

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  Structural diagram of Pemoline

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  Ball-and-stick model of Pemoline

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  UC Irvine Medical Center