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Pemoline
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Pemoline
Pemoline, formerly sold under the brand name Cylert among others, is a stimulant medication which was used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It has since been discontinued in most countries due to rare but serious liver toxicity. The medication was taken by mouth.
Common side effects include insomnia, decreased appetite, abdominal pain, irritability, and headaches, while rare cases of serious liver damage requiring liver transplantation or causing death have been reported. As a stimulant, pemoline acts as a selective dopamine reuptake inhibitor and releasing agent via indirect agonism of dopamine receptors. In addition, it shows little activity with respect to norepinephrine, thus minimal to no cardiovascular or sympathomimetic effects in comparison to many other stimulants.
Pemoline was first synthesized in 1913, but its stimulant activity was not discovered until the 1930s, nor used for ADHD until 1975. Between 1997 and 2005, many countries, including the United States, withdrew the drug due to liver toxicity. However, it remains available in Japan for the treatment of narcolepsy at lower doses than those used for ADHD. Pemoline is a schedule IV controlled substance in the United States due to structural and functional similarity to other stimulants, and potential for misuse. but is noted to have less misuse potential than other stimulant drugs.
Pemoline has been used in the treatment of ADHD and narcolepsy. It has also been used in the treatment of excessive daytime sleepiness. The medication was typically used at doses of 18.75 to 112.5 mg once per day in the treatment of ADHD, with the effective dose for most people being in the range of 56.25 to 75 mg. The onset of action of pemoline is gradual and therapeutic benefits may not occur until the third or fourth weeks of use. This may be due to a cautious low initial starting dose of 37.5 mg and gradual titration in dose upwards over several weeks.
Pemoline was available in the form of 18.75, 37.5, and 75 mg oral immediate-release tablets (Cylert) as well as 37.5 mg oral immediate-release chewable tablets. It was provided mainly in the form of the free base but also as the magnesium salt.
Side effects of pemoline include insomnia, decreased appetite, abdominal pain, irritability, and headaches. It has minimal cardiovascular or sympathomimetic side effects. Pemoline is described as a lower-efficacy/milder stimulant than classical stimulants like amphetamines and methylphenidate and is said to have fewer side effects than them.
Rarely, pemoline is implicated in causing hepatotoxicity. Because of this, the FDA recommended that regular liver tests be performed in those treated with it. Since being introduced, it has been linked with at least 21 cases of liver failure, of which 13 resulted in liver replacement or death. Approximately 1–2% of patients taking the drug show elevated levels of liver transaminase enzymes, a marker for liver toxicity, though serious cases are rare. Over 200,000 children with ADHD were prescribed pemoline in the United States and Canada alone during the approximate 25 years that it was available, plus a smaller number of adults prescribed it for other indications (and not including prescriptions in the rest of the world). As such, the number of liver failure cases was statistically not that large. However the reactions proved idiosyncratic and unpredictable, with patients sometimes taking the drug with no issue for months or even years, before suddenly developing severe liver toxicity. There was no clear exposure–toxicity relationship, and no characteristic liver pathology findings. Some patients showed as little as one week between first appearance of jaundice and complete liver failure, and some of the patients that developed liver failure had not showed elevated liver transaminase levels when tested previously. On the other hand, there are no cases of liver failure associated with pemoline in Japan, although it is used at lower doses and is only prescribed for the niche indication of narcolepsy in this country.
Overdose of pemoline may present with choreoathetosis symptoms.
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Pemoline
Pemoline, formerly sold under the brand name Cylert among others, is a stimulant medication which was used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It has since been discontinued in most countries due to rare but serious liver toxicity. The medication was taken by mouth.
Common side effects include insomnia, decreased appetite, abdominal pain, irritability, and headaches, while rare cases of serious liver damage requiring liver transplantation or causing death have been reported. As a stimulant, pemoline acts as a selective dopamine reuptake inhibitor and releasing agent via indirect agonism of dopamine receptors. In addition, it shows little activity with respect to norepinephrine, thus minimal to no cardiovascular or sympathomimetic effects in comparison to many other stimulants.
Pemoline was first synthesized in 1913, but its stimulant activity was not discovered until the 1930s, nor used for ADHD until 1975. Between 1997 and 2005, many countries, including the United States, withdrew the drug due to liver toxicity. However, it remains available in Japan for the treatment of narcolepsy at lower doses than those used for ADHD. Pemoline is a schedule IV controlled substance in the United States due to structural and functional similarity to other stimulants, and potential for misuse. but is noted to have less misuse potential than other stimulant drugs.
Pemoline has been used in the treatment of ADHD and narcolepsy. It has also been used in the treatment of excessive daytime sleepiness. The medication was typically used at doses of 18.75 to 112.5 mg once per day in the treatment of ADHD, with the effective dose for most people being in the range of 56.25 to 75 mg. The onset of action of pemoline is gradual and therapeutic benefits may not occur until the third or fourth weeks of use. This may be due to a cautious low initial starting dose of 37.5 mg and gradual titration in dose upwards over several weeks.
Pemoline was available in the form of 18.75, 37.5, and 75 mg oral immediate-release tablets (Cylert) as well as 37.5 mg oral immediate-release chewable tablets. It was provided mainly in the form of the free base but also as the magnesium salt.
Side effects of pemoline include insomnia, decreased appetite, abdominal pain, irritability, and headaches. It has minimal cardiovascular or sympathomimetic side effects. Pemoline is described as a lower-efficacy/milder stimulant than classical stimulants like amphetamines and methylphenidate and is said to have fewer side effects than them.
Rarely, pemoline is implicated in causing hepatotoxicity. Because of this, the FDA recommended that regular liver tests be performed in those treated with it. Since being introduced, it has been linked with at least 21 cases of liver failure, of which 13 resulted in liver replacement or death. Approximately 1–2% of patients taking the drug show elevated levels of liver transaminase enzymes, a marker for liver toxicity, though serious cases are rare. Over 200,000 children with ADHD were prescribed pemoline in the United States and Canada alone during the approximate 25 years that it was available, plus a smaller number of adults prescribed it for other indications (and not including prescriptions in the rest of the world). As such, the number of liver failure cases was statistically not that large. However the reactions proved idiosyncratic and unpredictable, with patients sometimes taking the drug with no issue for months or even years, before suddenly developing severe liver toxicity. There was no clear exposure–toxicity relationship, and no characteristic liver pathology findings. Some patients showed as little as one week between first appearance of jaundice and complete liver failure, and some of the patients that developed liver failure had not showed elevated liver transaminase levels when tested previously. On the other hand, there are no cases of liver failure associated with pemoline in Japan, although it is used at lower doses and is only prescribed for the niche indication of narcolepsy in this country.
Overdose of pemoline may present with choreoathetosis symptoms.
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