Product Name

Oxazepam

CAS Number

604-75-1

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Product Name:
Oxazepam
CAS Number:
604-75-1
Indication:
For the treatment of anxiety disorders and alcohol withdrawal.
Mode of Action:

Similar to other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA-A receptors through a cooperative mechanism of action. GABA receptors are ionotropic chloride-linked channel receptors that produce inhibitory postsynaptic potentials. When activated by GABA, the GABA receptor/chloride ionophore complex undergoes a conformational change that allows the passage of chloride ions through the channel. Benzodiazepines are believed to exert their effect by increasing the effect of GABA at its receptor. Benzodiazepine binding increases chloride conductance in the presence of GABA by increasing the frequency at which the channel opens. In contrast, barbiturates increase chloride conductance in the presence of GABA by prolonging the time in which the channel remains open. There are _8 subtypes of the GABA receptor subunits. The __ subunit of the ______ receptor complex is thought to mediate anxiolytic effects while the __ subunit of the ______ receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects.

Pharmacodynamics:

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.

Metabolism:

No active metabolites. Metabolized via conjugation prior to elimination.

Toxicity:

Symptoms of overdose include confusion, drowsiness, and lethargy.

IUPAC:
7-chloro-3-hydroxy-5-phenyl-2, 3-dihydro-1H-1, 4-benzodiazepin-2-one
ATC:
N05BA04
PubChem:
4616
DrugBank:
DB00842 (APRD01152)
Formula:
C19H20N2O3
Molecular Mass:
286.713
Synonyms:
Oxazipam Oxozepam
SMILES:
OC1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2
AHFS Code:
28:24.1
InChi:
ADIMAYPTOBDMTL-UHFFFAOYSA-N
General Reference:
General Reference:

  1. Peppers MP: Benzodiazepines for alcohol withdrawal in the elderly and in patients with liver disease. Pharmacotherapy. 1996 Jan-Feb;16(1):49-57. Pubmed
  2. 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
  3. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
  4. 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
  5. Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine] Arch Fr Pediatr. 1977 Jan;34(1):74-89. Pubmed

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