The concentration of oxazepam and oxazepam glucuronide in oral fluid, blood and serum after controlled administration of 15 and 30 mg oxazepam

Br J Clin Pharmacol. 2008 Oct;66(4):556-60. doi: 10.1111/j.1365-2125.2008.03252.x. Epub 2008 Jun 28.

Abstract

Aims: 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.

Methods: 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.

Results: 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.

Conclusion: 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.

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Drug Administration Routes
  • Humans
  • Hypnotics and Sedatives / administration & dosage
  • Hypnotics and Sedatives / pharmacokinetics*
  • Male
  • Oxazepam / administration & dosage
  • Oxazepam / analogs & derivatives*
  • Oxazepam / pharmacokinetics*
  • Predictive Value of Tests
  • Saliva / drug effects*
  • Serum / drug effects*
  • Substance Abuse Detection / legislation & jurisprudence
  • Substance Abuse Detection / methods*
  • Treatment Outcome

Substances

  • Hypnotics and Sedatives
  • oxazepam glucuronide
  • Oxazepam