2951 Oxazepam Oxazepam is only found in individuals that have used or taken this drug. It is an intermediate-acting benzodiazepine used to treat alcohol withdrawal and anxiety disorders. 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 18 subtypes of the GABA receptor subunits. The α₂ subunit of the α₂β₃γ₂ receptor complex is thought to mediate anxiolytic effects while the α₁ subunit of the α₁β₂γ₂ receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects. Oxazepam is also the metabolite of other benzodiazpines. 604-75-1 4616 C15H11ClN2O2 286.050910 White powder. 205-206°C 179 mg/L Well absorbed from the gastrointestinal tract following oral administration however is absorbed at a slower rate compared to other benzodiazepines like diazepam or flurazepam. Time to peak concentration = 2-4 hours. Onset of action is slow, > 3 hours, following oral administration. 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 18 subtypes of the GABA receptor subunits. The α₂ subunit of the α₂β₃γ₂ receptor complex is thought to mediate anxiolytic effects while the α₁ subunit of the α₁β₂γ₂ receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects. The metabolism of is Oxazepam hepatic. Moreover, it is a metabolite of diazepam, prazepam and temazepam. Therefore, there is likely an overlap in possible interactions with other drugs or food, with exception of the pharmacokinetic CYP450 interactions (e.g. with cimetidine). [Wikipedia]. No active metabolites. It is hepatically metabolized and undergoes glucuronidation. The glucuronidation of the S-isomer is catalyzed by UGT2B15. The glucuronidation of the R-isomer is catalyzed by UGT2B7 and UGT1A9. Route of Elimination: This product has a single, major inactive metabolite in man, a glucuronide excreted in the urine. Half Life: Mean elimination half-life - 8.2 hours (range of 5.7 to 10.9 hours) 2B, possibly carcinogenic to humans. (L135) used extensively since the 1960s for the treatment of anxiety and insomnia and in the control of symptoms of alcohol withdrawal. [Wikipedia] They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. Symptoms of overdose include confusion, drowsiness, and lethargy. Induced vomiting and/or gastric lavage should be undertaken, followed by general supportive care, monitoring of vital signs, and close observation of the patient. Hypotension, though unlikely, usually may be controlled with norepinephrine bitartrate Injection. The value of dialysis has not been adequately determined for oxazepam. The benzodiazepine antagonist flumazenil may be used In hospitalized patients as an adjunct to, not as a substitute for, proper management of benzodiazepine overdose. (L1712) 2009-07-21T20:27:47Z 2014-12-24T20:25:53Z Oxazepam C07359 7823 Oxazepam DB00842 true OC1N=C(C2=CC=CC=C2)C2=C(C=CC(Cl)=C2)N=C1O C15H11ClN2O2 InChI=1/C15H11ClN2O2/c16-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)18-15(20)14(19)17-12/h1-8,15,20H,(H,17,19) InChIKey=ADIMAYPTOBDMTL-UHFFFAOYNA-N 286.713 286.050905313 Exogenous Solid 2.24 HMDB14980 CHEMBL568 4455