物质信息
ID:982
名称和标识
商标名
DimerinNoludarNodularNoctan
别名
MetipriloneDea No. 2575Methyprylon [INN]MethyprylonMethyprylonum [INN-Latin]MethyprolonMetiprilonMetiprilona [INN-Spanish]Methyprylone [INN-French]Methprylon
IUPAC标准名
3,3-diethyl-5-methylpiperidine-2,4-dione
IUPAC传统名
dimerin
化合物性质
理化性质
溶解度
1.15E+004 mg/L
疏水性(logP)
1.2
描述信息
Drug Groups
illicit; approved; withdrawn
Description
Methyprylon is a sedative of the piperidinedione derivative family. This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with less side effects, such as benzodiazepines. Methyprylon was withdrawn from the US market in June 1965 and the Canadian market in September 1990. [Wikipedia]
Indication
For the treatment of insomnia.
Pharmacology
Methyprylon, a piperidinedione CNS depressant, is close to barbituric acid in structure, but different enough to be called a "non-barbiturate" sedative-hynotic. Methyprylon is used for insomnia and daytime tension. Methyprylon depresses the activity of muscle tissues, the heart, and the respiratory system.
Toxicity
Symptoms of overdose include excitation and convulsions.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic. Methyprylon is almost completely metabolized.
Half Life
6-16 hours
Protein Binding
60%
References
•
Contos DA, Dixon KF, Guthrie RM, Gerber N, Mays DC: Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;80(8):768-71.
[Pubmed]
•
Gwilt PR, Pankaskie MC, Thornburg JE, Zustiak R, Shoenthal DR: Pharmacokinetics of methyprylon following a single oral dose. J Pharm Sci. 1985 Sep;74(9):1001-3.
[Pubmed]
•
Lomen P, Linet OI: Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients. J Int Med Res. 1976;4(1):55-8.
[Pubmed]
External Links
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参考文献
• Contos DA, Dixon KF, Guthrie RM, Gerber N, Mays DC: Nonlinear elimination of methyprylon (noludar) in an overdosed patient: correlation of clinical effects with plasma concentration. J Pharm Sci. 1991 Aug;80(8):768-71. Pubmed
• Lomen P, Linet OI: Hypnotic efficacy of triazolam and methyprylon ininsomniac in-patients. J Int Med Res. 1976;4(1):55-8. Pubmed
• Gwilt PR, Pankaskie MC, Thornburg JE, Zustiak R, Shoenthal DR: Pharmacokinetics of methyprylon following a single oral dose. J Pharm Sci. 1985 Sep;74(9):1001-3. Pubmed