Pemoline is classified as a central nervous system (CNS) stimulant. It is sold in the United States under the brand names Cylert and PemADD and is also available under its generic name.
Pemoline is a central nervous system stimulant that derives at least some of its effects by increasing levels of dopamine in the brain. Dopamine is one of several neurotransmitters in the brain. Neurotransmitters are naturally occurring chemicals that regulate the transmission of nerve impulses from one cell to another. Mental and physical well-being are partially dependent on maintaining the proper balance among the various neurotransmitters in the brain.
Pemoline is similar in its effects to dextroamphetamine and methylphenidate, two other drugs used to treat ADHD, although it is not chemically related to these drugs. The mechanism of action of CNS stimulants in the treatment of ADHD is not totally clear, but probably includes increased mental alertness, decreased mental fatigue, and an increased sense of well-being.
Pemoline should not be used as a substitute for psychological, educational, and social support in treating ADHD. Because pemoline may be associated with liver toxicity (poisoning causing liver damage), it should be used only after other drugs to treat ADHD have been tried. Patients should try dextroamphetamine or methylphenidate first.
Pemoline is available in 18.75-mg, 37.5-mg, and 75-mg oral tablets and in 37.5-mg chewable tablets.
The dose of pemoline should be carefully adjusted to patient need. The initial dose of pemoline in children six years of age or older is 37.5 mg each morning. The dose may be increased by 18.75 mg each week to as much as 75 mg daily. Most people respond to doses ranging from 56.25 mg to 75 mg daily, although some people may require as much as 112.5 mg daily.
There is no need to continue pemoline indefinitely. Rather, patients should be evaluated both during therapy and during periods in which the medication is voluntarily stopped. In many situations, the drug may be safely discontinued altogether when the child reaches adolescence.
Pemoline is associated with liver toxicity. Symptoms range from mild reversible changes in liver function tests to acute liver failure. The risk of liver damage should be weighed against any therapeutic benefit derived from treatment with pemoline. Therefore, if no therapeutic benefit is observed within three to four weeks of starting the drug, pemoline should be discontinued. In order to detect the early signs of liver damage, liver function tests should be performed before starting the drug and every two weeks while taking pemoline.
Because pemoline is a central nervous stimulant, physical or psychological addiction is possible in people who are emotionally unstable.
Loss of appetite accompanied by weight loss generally occurs during the first few weeks after starting pemoline. With continued treatment, appetite and body weight usually stabilize.
Because it is a central nervous system stimulant, insomnia is a common side effect of pemoline.
The most serious side effect is liver toxicity. Liver toxicity is usually characterized by changes in liver function tests without obvious liver damage, but in rare cases, liver failure resulting in death or requiring a liver transplant has occurred.
There are no scientific data concerning drugs that negatively interact with pemoline. However, because pemoline is considered a stimulant, other drugs with stimulant properties (caffeine, over-the-counter decongestants, amphetamines, antidepressants) may theoretically and inappropriately increase CNS stimulation.
American Society of Health-System Pharmacists. AHFS Drug Information 2002. Bethesda: American Society of Health-System Pharmacists, 2002.
O'Brien, Charles P. "Drug Addiction and Drug Abuse." In Goodman & Gillman's The Pharmacological Basis of Therapeutics, edited by Joel G. Hardman, Ph.D. and Lee E. Limbird, Ph.D. Tenth Edition. New York: McGraw-Hill, 2001.
Jack Raber, Pharm.D.