Methyprylon
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| Trade names | Noludar, Dimerin, Noctan, Methyprylone, Noctan |
| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Protein binding | 60% |
| Elimination half-life | 6-16 hours |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.004.315 |
| Chemical and physical data | |
| Formula | C10H17NO2 |
| Molar mass | 183.251 g·mol−1 |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
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Methyprylon, or Noludar, is a sedative/tranquilizer and hypnotic central nervous system depressant of the piperidinedione derivative chemical class, first developed in the 1940s by Hoffmann-La Roche.[2] This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.[3]
Methyprylon was withdrawn from the US market in June 1975 and the Canadian market in September 1990. Some other trade names are Noctan and Dimerin.
Adverse effects
[edit]Side effects can include
- skin rash
- fever
- depression
- ulcers or sores in mouth or throat
- unusual bleeding or bruising
- fast heartbeat
- CNS depressant effects, including mental depression and confusion, clumsiness, lack of coordination, respiratory depression, confusion, drowsiness, lethargy, swelling of feet or lower legs, dizziness
- headache
- double vision
- constipation, diarrhea,
- nausea and/or vomiting
- ataxia, unusual weakness, clumsiness
Pharmacokinetics
[edit]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.[4]
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.[5]
See also
[edit]References
[edit]- ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
- ^ US granted 2680116, Frick H, Lutz AH, "Piperidiones and Process for the Manufacture thereof", issued 1954-06-01, assigned to Hoffmann-La Roche
- ^ Lomen P, Linet OI (1976). "Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients". The Journal of International Medical Research. 4 (1): 55–8. doi:10.1177/030006057600400108. PMID 16792. S2CID 12500779.
- ^ Gwilt PR, Pankaskie MC, Thornburg JE, Zustiak R, Shoenthal DR (September 1985). "Pharmacokinetics of methyprylon following a single oral dose". Journal of Pharmaceutical Sciences. 74 (9): 1001–3. doi:10.1002/jps.2600740920. PMID 2866242.
- ^ Contos DA, Dixon KF, Guthrie RM, Gerber N, Mays DC (August 1991). "Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration". Journal of Pharmaceutical Sciences. 80 (8): 768–71. doi:10.1002/jps.2600800813. PMID 1686463.