|( R ) -Pemoline (top) and ( S ) -Pemoline (bottom)|
( RS ) -2-Amino-5-phenyl-1,3-oxazol-4-one ( IUPAC )
|Molecular formula||C 9 H 8 N 2 O 2|
|External identifiers / databases|
|Molar mass||176.17 g · mol -1|
256-257 ° C
practically insoluble in water, soluble in hot ethanol
|As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .|
Pemoline was on the market in Germany for over 50 years. Initially used to treat poor performance and drive, e.g. For example, during menopause, depression, epileptic seizures and other diseases of the nervous system, pemoline was recently only approved as a reserve drug for the treatment of ADHD .
After the risk of hepatotoxicity became known, the British authorities withdrew the approval in 1997. The FDA initially restricted the indication and the BfArM reassessed the risk profile. After repeated occurrences of acute liver failure, the manufacturers took the substance off the market under pressure from the authorities (FDA Alert). The manufacturer Abbott Laboratories ( Cylert ) stopped production in 2005. Finally, Lilly took the last product ( Tradon ) from the German market in 2006. Finished medicinal products are no longer on the market worldwide.
Pemoline is regulated by narcotics law.
The dosage is 20 to max. 100 mg. The half-life is about 8 to 12 hours.
The drug works by selectively inhibiting the presynaptic dopamine and noradrenaline transporters. By preventing resumption, the concentration of these neurotransmitters increases. However, the exact mechanism of action is not known. The therapeutic effect only sets in after a latency period of four to six weeks after the first dose.
In comparison with other stimulants, the rebound phenomenon is absent or only weakly pronounced. The half-life is significantly longer than z. B. that of methylphenidate.
Typical common side effects are insomnia, insomnia, loss of appetite, and weight loss. Internet sources also mention drowsiness, dizziness and headaches. During the use of pemoline, increased liver enzyme values and the occurrence of hepatotoxic reactions were observed, which prompted the Drug Commission of the German Medical Association to issue a prescription restriction: Pemoline could only be prescribed if other treatment measures (therapy with other psychostimulants such as methylphenidate or amphetamine ) were unsuccessful or not on their own were sufficient and with special monitoring of liver function. Since pemoline was approved by the FDA in 1975, 21 cases of liver failure have been reported, 13 of which resulted in liver transplant or death. According to the FDA, this is up to 25 times more common than would be expected without the drug. Therefore, the FDA first issued a warning and withdrew US marketing approval in 2005.
In Germany, pemoline falls under the Narcotics Act. The exception to this is the tablet form with a dose of up to 20 mg per piece, for which no BTM prescription is required. In the US, the FDA lists pemoline as a Schedule IV drug under the Controlled Substances Act .
Cylert (USA, supra ), Abbott Laboratories; Tradon (D, A.H.), Lilly; Stimul (CH, a. H.)
- psychotropicon.info Information about Cylert
- psychotropicon.info Information about pemoline
- drugs.com American precautionary statements
- drugs.com American product information on Cylert
- Entry on pemoline. In: Römpp Online . Georg Thieme Verlag, accessed on October 1, 2014.
- harmonized classification for this substance . A labeling of pemoline in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), retrieved on July 10, 2020, is reproduced from a self-classification by the distributor . There is not yet a
- Fatal liver damage from the psychostimulant pemoline (Tradon®) | Good pills, bad pills. Retrieved July 10, 2020 .
- ABDA database (as of December 6, 2009).
- Tradon | ADHD medication. Retrieved July 10, 2020 .
- Medicines Commission of the German Medical Association: Prescription restrictions for pemoline (Tradon®) due to the risk of liver damage , Deutsches Ärzteblatt 97, issue 6, February 11, 2000.
- Cylert (pemoline): Uses, Dosage, Side Effects, Interactions, Warning. Retrieved July 10, 2020 .