物质信息
ID:116
名称和标识
别名
MethyloxazepamN-MethyloxazepamTemazepamHydroxydiazepamOxydiazepam
IUPAC传统名
temazepam
商标名
Apo-TemazepamCrisonarLevanxolSignopamNormisonNovo-TemazepamPerdormPlanumRestorilMabertinTemazEuipnosLevanzeneRemestanCerepaxEuhypnosGelthixLevanxene
IUPAC标准名
7-chloro-3-hydroxy-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
化合物性质
理化性质
溶解度
164 mg/L
疏水性(logP)
3
描述信息
Drug Groups
approved
Description
A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem]
Indication
For the short-term treatment of insomnia (generally 7-10 days).
Pharmacology
Temazepam is a benzodiazepine used as a hypnotic agent in the management of insomnia. Temazepam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Temazepam increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%).
Absorption
Well absorbed, minimal first-pass metabolism.
Half Life
10-20 hours
Protein Binding
96%
Elimination
Temazepam was completely metabolized through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine.
References
•
Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41.
[Pubmed]
•
Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72.
[Pubmed]
•
Vozeh S: [Pharmacokinetic of benzodiazepines in old age] Schweiz Med Wochenschr. 1981 Nov 21;111(47):1789-93.
[Pubmed]
•
Shats V, Kozacov S: [Falls in the geriatric department: responsibility of the care-giver and the hospital] Harefuah. 1995 Jun 1;128(11):690-3, 743.
[Pubmed]
•
Rooke KC: The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice. J Int Med Res. 1976;4(5):355-9.
[Pubmed]
External Links
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参考文献
• Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
• Shats V, Kozacov S: [Falls in the geriatric department: responsibility of the care-giver and the hospital] Harefuah. 1995 Jun 1;128(11):690-3, 743. Pubmed
• Rooke KC: The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice. J Int Med Res. 1976;4(5):355-9. Pubmed
• Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41. Pubmed
• Vozeh S: [Pharmacokinetic of benzodiazepines in old age] Schweiz Med Wochenschr. 1981 Nov 21;111(47):1789-93. Pubmed