Methyprylon
| File:Methyprylon structure.svg | |
| File:Methyprylon ball-and-stick.png | |
| Clinical data | |
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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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| E number | {{#property:P628}} |
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| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value). |
| 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in the 1940s by Hoffmann-La Roche.[2] This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines.[3]
Methyprylon was withdrawn from the US market in June 1975 and the Canadian market in September 1990.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 | edit source]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 | edit source]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 | edit source]References
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