物质信息
ID:722
名称和标识
IUPAC传统名
oxazepam
IUPAC标准名
7-chloro-3-hydroxy-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
商标名
AnxiolitAstressDrimuelDroxacepamDurazepamEnidrelAzutranquilOxanidPacienxSeraxSerenid-DZaxopamQuilibrexSedigoaSerenalSerestaVabenHi-LongIsodinNesontilNoctazepamNotaralOxa-purenSobrilTacepamUskanWy-3498 sticBonareAplakilLederpamMurelaxRondarSerepaxSerpaxSigacalmTazepamAdumbranAnsioxacepamLimbialPraxitenPropaxPsiquiwasQUENSerenid
别名
d-Oxazepam hemisuccinateOxazepamOxozepamOxazipam
化合物性质
理化性质
溶解度
179 mg/L
疏水性(logP)
2.8
描述信息
Drug Groups
approved
Description
Oxazepam is an intermediate-acting benzodiazepine used to treat alcohol withdrawal and anxiety disorders.
Indication
For the treatment of anxiety disorders and alcohol withdrawal.
Pharmacology
Oxazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.
Toxicity
Symptoms of overdose include confusion, drowsiness, and lethargy.
Affected Organisms
Humans and other mammals
Biotransformation
No active metabolites. Metabolized via conjugation prior to elimination.
Absorption
Well absorbed from the gastrointestinal tract following oral administration. Time to peak concentration = 2-4 hours. Onset of action is slow, > 3 hours, following oral administration.
Half Life
5-15 hours
Protein Binding
80-99%
Elimination
This product has a single, major inactive metabolite in man, a glucuronide excreted in the urine.
References
•
Peppers MP: Benzodiazepines for alcohol withdrawal in the elderly and in patients with liver disease. Pharmacotherapy. 1996 Jan-Feb;16(1):49-57.
[Pubmed]
•
Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8.
[Pubmed]
•
Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72.
[Pubmed]
•
Christensen P, Lolk A, Gram LF, Kragh-Sorensen P: Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers. Psychopharmacology (Berl). 1992;106(4):511-6.
[Pubmed]
•
Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine] Arch Fr Pediatr. 1977 Jan;34(1):74-89.
[Pubmed]
External Links
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参考文献
• Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. Pubmed
• Peppers MP: Benzodiazepines for alcohol withdrawal in the elderly and in patients with liver disease. Pharmacotherapy. 1996 Jan-Feb;16(1):49-57. Pubmed
• Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
• Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine] Arch Fr Pediatr. 1977 Jan;34(1):74-89. Pubmed
• Christensen P, Lolk A, Gram LF, Kragh-Sorensen P: Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers. Psychopharmacology (Berl). 1992;106(4):511-6. Pubmed