Beitske E Smink, Berendina J A Hofman, Albert Dijkhuizen, Klaas J Lusthof, Johan J de Gier, Antoine C G Egberts, Donald R A Uges
Index: Br. J. Clin. Pharmacol. 66(4) , 556-60, (2008)
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To measure and compare the concentration-time profiles of oxazepam and oxazepam glucuronide in blood, serum and oral fluid within the scope of roadside testing.Biological samples were collected from eight male subjects after ingestion of 15 or 30 mg oxazepam on separate dosing occasions with an interval of 7 days. The concentration-time profiles of oxazepam and oxazepam glucuronide were fitted by using a one-compartment model.For oxazepam and oxazepam glucuronide, the mean oral fluid/blood ratios were 0.05 (range 0.04-0.07) and 0.004 (range 0.002-0.006), respectively. The concentration-time profiles in oral fluid paralleled those in blood.After oral administration of therapeutic doses of oxazepam, concentrations in oral fluid are very much lower than those in blood, and those of oxazepam glucuronide are much lower than those of the parent compound. Nevertheless, assay of oral fluid for oxazepam can be used to detect recent ingestion of the drug in drivers suspected of impaired driving performance.
| Structure | Name/CAS No. | Molecular Formula | Articles |
|---|---|---|---|
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O1-(7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-β-D-glucopyranuronic acid
CAS:6801-81-6 |
C21H19ClN2O8 |
|
Factors and conditions affecting the glucuronidation of oxaz...
1993-01-01 [Pharmacol. Toxicol. 73 Suppl 1 , 1-23, (1993)] |
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(S)oxazepam glucuronidation is inhibited by ketoprofen and o...
1995-02-01 [Pharmacogenetics 5(1) , 43-9, (1995)] |
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Physiological modeling of drug and metabolite: disposition o...
1990-10-01 [J. Pharmacokinet. Biopharm. 18(5) , 423-48, (1990)] |
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The influence of diflunisal on the pharmacokinetics of oxaze...
1985-09-01 [Br. J. Clin. Pharmacol. 20(3) , 225-34, (1985)] |
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Bioavailability and pharmacokinetics of oxazepam.
1988-01-01 [Eur. J. Clin. Pharmacol. 35(4) , 385-9, (1988)] |
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![O1-(7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-β-D-glucopyranuronic acid Structure](https://image.chemsrc.com/caspic/164/6801-81-6.png)