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Methyprylon

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Title: Methyprylon  
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Subject: Piperidione, Alcoholic beverage, Propylbarbital, SL-164, Spirobarbital
Collection: Gabaa Receptor Positive Allosteric Modulators, Ketones, Lactams, Piperidines
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Methyprylon

Methyprylon
Systematic (IUPAC) name
(RS)-3,3-diethyl-5-methylpiperidine-2,4-dione
Clinical data
Trade names Dimerin, Methyprylone, Noctan, Noludar
Legal status
Routes of
administration
oral
Pharmacokinetic data
Protein binding 60%
Biological half-life 6-16 hours
Identifiers
CAS Registry Number  YesY
ATC code N05
PubChem CID:
IUPHAR/BPS
DrugBank  YesY
ChemSpider  YesY
UNII  YesY
KEGG  N
ChEMBL  N
Chemical data
Formula C10H17NO2
Molecular mass 183.248 g/mol
 N   

Methyprylon (Noludar) is a sedative of the piperidinedione derivative family developed by Hoffmann-La Roche.[1] This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.[2] Methyprylon was withdrawn from the US market in June 1989 and the Canadian market in September 1990. Some other trade names are Noctan and Dimerin.

Contents

  • Adverse effects 1
  • Pharmacokinetics 2
  • See also 3
  • References 4

Adverse effects

Side effects can include skin rash, fever, depression, ulcers or sores in mouth or throat, unusual bleeding or bruising, confusion, fast heartbeat, respiratory depression, swelling of feet or lower legs, dizziness, drowsiness, headache, double vision, clumsiness, constipation, diarrhea, nausea, vomiting, unusual weakness.

Pharmacokinetics

A study of single oral doses of 300 mg in healthy volunteers found that the zero-order absorption model fit the data best. Mean (+/- SD) values for the half-life (9.2 +/- 2.2 h), apparent clearance, (11.91 +/- 4.42 mL/h/kg) and apparent steady-state volume of distribution, (0.97 +/- 0.33 L/kg) were found.[3]

A case report found that the pharmacokinetics of methyprylon were not concentration dependent in an overdose case; explanations included saturation or inhibition of metabolic pathways. The generally accepted half-life for a therapeutic dose was not found appropriate in intoxicated patients and would underestimate the time required to reach a safe concentration of the drug.[4]

See also

References

  1. ^ US patent 2680116, Frick, H. & Lutz, A. H., "Piperidiones and Process for the Manufacture thereof", issued 1954-06-01, assigned to Hoffmann-La Roche 
  2. ^
  3. ^
  4. ^
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