Pemoline

PemoUne is an oxazolidinone derivative that is not structurally similar to amphetamine or methylphenidate. It has fewer stimulating properties than other stimulants and may have less abuse potential. Unlike most other stimulants, pemoline is a Schedule IV agent and does not require a triplicate prescription. However, there are numerous reports of hepatotoxicity in patients taking pemoline (see review by Safer et al. 2001), and it is no longer available in the United States. 

Modafinil is a stimulant medication used to improve wakefulness in patients with narcolepsy, obstructive sleep apnea/hypopnea syndrome (as adjunct to standard treatments for the underlying disorder), and shift work sleep disorder. Controlled and open trials provided data on the efficacy and safety of modafinil in patients with narcolepsy (Besset et al. 1996 Billiard et al. 1994 Broughton et al. 1997 Mitler et al. 2000 U.S. Modafinil in Narcolepsy Multicenter Study Group 1998, 2000). Modafinil has a long duration of action and low potential for dependence and may be a reasonable first choice in the treatment of mild to moderate narcolepsy (Silber 2001). There is also considerable interest in the potential use of modafinil in the treatment of ADHD, and studies are in progress. 

Modafinil is a Schedule IV medication and does not require a triplicate prescription. Its mechanism of action is unclear but is thought to differ from those of conventional stimulants. Modafinil is metabolized by the liver and excreted by the kidneys. Its half-life is approximately 15 hours. It is available in 100- and 200-mg tablets. The typical daily dose is 200 00 mg every morning this dose should be reduced in elderly or hepatically impaired patients. 

Modafinil is contraindicated in patients with a known hypersensitivity to it, and the drug should be used cautiously in patients with a history of psychosis or cardiovascular disease. 

Side effects are similar to those of other stimulants. Additionally, some patients may experience confusion, ataxia, hyperglycemia, gingival ulcers, urinary retention, paresthesias, neck and joint discomfort, amblyopia, pharyngitis, or dyspnea. 

MacKenzie, J.S. and Morgan, C.S. Jr. U.S. Patent 2,820,046 January 14,1958 assigned to Celanese Corp, of America 

Chemical Name 2-imino-5-phenyl-4-oxazolidinone Common Name Phenoxazole phenylisohydantoin Structural Formula  

Trade Name Manufacturer Country Year Introduced 

Trada Nama Manufacturar Country Year Introduced 

It is preferably prepared by reacting mandelic acid ethyl ester with guanidine in boiling alcoholic solution whereby it is obtained as difficultly soluble precipitate with a yield of 90%. 

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However, clinical results with compounds enhancing cholinergic function have not been overly convincing (272). In the case of tacriae, however, the beneficial therapeutic iadex was sufficient to justify regulatory approval ia several countries. Psychostimulants such as pemoline, amphetamine, procaine, and methylphenidate have failed to show cognitive enhancing effects ia patients with dementia, except possibly as iadirect consequences of mood elevation. 

Pemoline [2152-34-3] (24), stmcturally dissimilar to amphetamine or methylphenidate, appears to share the CNS-stimulating properties. As a consequence, pemoline is employed in the treatment of ADHD and of narcolepsy. There are several other compounds that are stmcturally related to amphetamines, although not as potent and, presumably, without as much abuse potential. These compounds also have anorexic effects and are used to treat obesity. Some of the compounds available are phentermine [122-09-8] fenfluramine [458-24-2] and an agent that is available over-the-counter, phenylpropanolamine [1483815-4] (26). 

Pemoline pem -oh-leen Cylert ADHD Insomnia, nervousness, headache, tachycardia, anorexia, dizziness, excitement 37.5-112.5 mg/d PO... 

CH5N3 113-00-8) see Abacavir Amiloride Folic acid Guanfacine Pemoline Pyrimethamine Sulfamerazine Tetroxoprim... 

Methylphenidate (Ritalin), dextroamphetamine (Dexedrine), and pemoline (Cylert) are currently available in the United States. Methylphenidate has been the most widely used and is usually the first choice. Pemoline sometimes impairs liver function and is rarely used today due to the potential for toxicity. 

Pemoline (Cylert). Pemoline was introduced as an alternative stimulant. Its two key advantages are that it can be taken once a day, though with the extended-release versions of methylphenidate and Adderall this is less of an issue, and it may be less prone to abuse. It was generally believed that pemoline has a gradual onset of action, taking several weeks to reach full therapeutic benefit, but some researchers discount this assumption. 

Pemoline is less potent than the other available stimulants. It is started at 18.75 mg each morning and is increased in increments of 18.75 mg every week or two. The maximum dose is 112.5mg/day, though some patients do require higher doses. Because pemoline is less potent than other stimulants, it is more likely to be ineffective even at its higher doses. When pemoline does not relieve the symptoms of ADHD, patients should be changed to a different stimulant. 

One benefit of pemoline s milder effects and slower onset of action is that it appears to possess less abuse potential than other stimulants. The abuse potential, however, is usually a concern not for patients who are prescribed the stimulant, but for others who may want to buy it on the street or steal the pills from someone else. Although pemoline does have some potential for abuse, it is limited. 

The side effects of pemoline are similar to other stimulants but milder. The most common side effects are loss of appetite, nausea, and insomnia. Infrequent side effects include headache, dizziness, changes in mood, increases in blood pressure or pulse, and psychosis. 

The greatest concern is that pemoline on rare occasions causes a chemical hepatitis (liver malfunction). For this reason, patients with known liver disease should never take pemoline. Patients should have a baseline laboratory assessment of liver... 

Close to 70% of children with ADHD will respond to a stimulant. When the child is not helped by the first stimulant that is prescribed, there is still a good chance of responding to a different one. If an initial trial of methylphenidate isn t successful, then switching to dextroamphetamine or Adderall is a reasonable strategy. If dextroamphetamine or Adderall was used first and did not work well, then we recommend switching to methylphenidate. Because dextroamphetamine and Adderall are more similar, it makes less sense to switch between these two. We do not recommend pemoline as a first-line treatment. 

Monoamine oxidase inhibitors Paroxetine Protriptyline Sertraline Venlafaxine Stimulants Atomoxetine Dextroamphetamine Methylphenidate Modaflnil Pemoline... 

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