Pemoline
 |
|
 |
|
| Clinical data | |
|---|---|
| Trade names | Cylert |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Pregnancy category |
|
| Routes of administration |
Oral |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 50% bound to plasma proteins |
| Metabolism | Hepatic |
| Biological half-life | 12 hours |
| Excretion | ? |
| Identifiers | |
|
|
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| ECHA InfoCard | 100.016.763 |
| Chemical and physical data | |
| Formula | C9H8N2O2 |
| Molar mass | 176.172 g/mol |
| 3D model (Jmol) | |
| Chirality | Racemic mixture |
|
|
|
|
  (what is this?)
|
|
Pemoline is a stimulant drug of the 4-oxazolidinone class. It was first synthesized in 1913 but its activity was not discovered until the 1930s. Under the names Betanamin, Cylert, Tradon, and Ceractiv it was used as a medication to treat attention-deficit hyperactivity disorder (ADHD) and narcolepsy. Under the Convention on Psychotropic Substances, it is a Schedule IV drug. It is no longer generally available in the United States as a result of the FDA withdrawing approval of pemoline as an indicated treatment for ADHD, due to its implication in liver failures among children who were receiving the medication. An FDA Alert warned against prescribing pemoline for ADHD. This spurred Abbott Laboratories, the patent owner of Cylert, to cease manufacturing Cylert. Manufacturers of the generic equivalents followed suit.
Pemoline is generally considered dopaminergic, but its precise method of action hasn't yet been definitively determined. Pemoline passes the blood–brain barrier and acts as a surrogate for dopamine, not affecting endogenous intracellular dopamine. For this reason, and the fact that it has little or no affinity for adrenaline receptors, pemoline has minimal sympathomimetic side effects such as: dry mouth, reduction in appetite, high blood pressure, increased heart rate, constriction of smooth muscle, cardiac stress, dilated pupils and insomnia. There is some data to suggest that pemoline is a nootropic acting as a catalyst conductor in the synapses of the brain's memory centers, raising the efficiency of memory and assisting RNA formation in the brain. While drugs like dexamphetamine and methylphenidate are classified as Schedule II, pemoline is listed as Schedule IV (non-narcotic). In studies conducted on primates, pemoline fails to demonstrate a potential for self-administration.
...
Wikipedia