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Pemoline
Systematic (IUPAC) name
(RS)-2-amino-5-phenyl-1,3-oxazol-4(5H)-one
Identifiers
CAS number 2152-34-3
ATC code N06BA05
PubChem 4723
DrugBank APRD01169
Chemical data
Formula C9H8N2O2 
Mol. mass 176.172 g/mol
Pharmacokinetic data
Bioavailability 50% bound to plasma proteins
Metabolism Hepatic
Half life 12 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat. B U.S.
Legal status Schedule IV (United States)
Schedule IV (Canada)
Lista II (Argentina)
Routes Oral

Pemoline (Cylert, Tradon) was a medication used to treat attention-deficit hyperactivity disorder (ADHD) and narcolepsy. It is no longer available in the United States.

Under the Convention on Psychotropic Substances, it is a Schedule IV drug.[1]

Pemoline has some advantages over other stimulants in that it does not reduce the appetite or cause dry mouth.

Dependence has only rarely been reported.[2]

Contents

Mechanism of action

Similar to methylphenidate, the mechanism of action of pemoline is to inhibit the reuptake of dopamine and to increase the release of dopamine and norepinephrine in the central nervous system.

Interactions

Methylphenidate may enhance the liver toxicity of pemoline.[3]

Hepatotoxicity and discontinuation

In some patients pemoline is suspected of causing hepatotoxicity,[3] so the FDA recommended that regular liver tests should be performed on those treated with it.[4] Since receiving FDA approval in 1975,[5] it has been linked with 21 cases of liver failure, of which 13 resulted in liver replacement or death.

In 2005, the Food and Drug Administration (FDA) withdrew approval for pemoline due to pressure from certain public advocacy groups, including Public Citizen. The medication was used by an estimated 10,000 Americans afflicted with narcolepsy.

A more potent analogue of pemoline, 4-methylaminorex has appeared as a black market drug with abuse potential similar to methamphetamine.

In March 2005, Abbott Laboratories (Cylert marketer) had discontinued the production of Cylert arguing economic reasons.

Overdose

Overdose of pemoline may present with choreoathetosis symptoms.[6]

See also

References

  1. ^ Annual Estimates Of Requirements Of Narcotic Drugs, Manufacture Of Synthetic Drugs, Opium Production And Cultivation Of The
  2. ^ Bonnet U, Davids E (September 2006). "A rare case of dependence on pemoline". Prog. Neuropsychopharmacol. Biol. Psychiatry 30 (7): 1340–1. doi:10.1016/j.pnpbp.2006.02.017. PMID 16600453. http://linkinghub.elsevier.com/retrieve/pii/S0278-5846(06)00078-9. 
  3. ^ a b Marotta PJ, Roberts EA (May 1998). "Pemoline hepatotoxicity in children". J. Pediatr. 132 (5): 894–7. PMID 9602211. http://linkinghub.elsevier.com/retrieve/pii/S002234769800208X. 
  4. ^ Willy ME, Manda B, Shatin D, Drinkard CR, Graham DJ (July 2002). "A study of compliance with FDA recommendations for pemoline (Cylert)". J Am Acad Child Adolesc Psychiatry 41 (7): 785–90. PMID 12108802. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0890-8567&volume=41&issue=7&spage=785. 
  5. ^ Etwel FA, Rieder MJ, Bend JR, Koren G (2008). "A surveillance method for the early identification of idiosyncratic adverse drug reactions". Drug Saf 31 (2): 169–80. PMID 18217792. 
  6. ^ Stork CM, Cantor R (1997). "Pemoline induced acute choreoathetosis: case report and review of the literature". J. Toxicol. Clin. Toxicol. 35 (1): 105–8. PMID 9022662. 

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