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 Number 125-64-4 YesY
ATC code N05CE02
PubChem CID 4162
IUPHAR/BPS 7238
DrugBank DB01107 YesY
ChemSpider 4018 YesY
UNII CUT48I42ON YesY
KEGG D01150 N
ChEMBL CHEMBL1200790 N
Chemical data
Formula C10H17NO2
Molar mass 183.248 g/mol
Chirality 1 : 1 mixture (racemate)
 NYesY (what is this?)  (verify)

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developed by Hoffmann-La Roche.[1] This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.[2] Methyprylon was withdrawn from the US market in June 1989 and the Canadian market in September 1990.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.

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. ↑ Lomen, P.; Linet, O. I. (1976). "Hypnotic efficacy of triazolam and methyprylon in insomniac in-patients". The Journal of international medical research 4 (1): 55–58. PMID 16792.
  3. ↑ Gwilt, P. R.; Pankaskie, M. C.; Thornburg, J. E.; Zustiak, R.; Shoenthal, D. R. (1985). "Pharmacokinetics of methyprylon following a single oral dose". Journal of pharmaceutical sciences 74 (9): 1001–1003. doi:10.1002/jps.2600740920. PMID 2866242.
  4. ↑ Contos, D. A.; Dixon, K. F.; Guthrie, R. M.; Gerber, N.; Mays, D. C. (1991). "Nonlinear elimination of methyprylon (noludar) in an overdosed patient: Correlation of clinical effects with plasma concentration". Journal of pharmaceutical sciences 80 (8): 768–771. doi:10.1002/jps.2600800813. PMID 1686463.
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