Bioavailability and pharmacokinetics of oxazepam

  title={Bioavailability and pharmacokinetics of oxazepam},
  author={Jesper Sonne and Steffen Loft and Martin D{\o}ssing and Anne Vollmer-Larsen and K. -L. Olesen and M A Victor and Frederik Andreasen and Per Buch Andreasen},
  journal={European Journal of Clinical Pharmacology},
SummarySix healthy volunteers received oxazepam 15 mg i.v. and orally at an interval of at least one week. The kinetic variables of i.v. oxazepam were: elimination half-life (t1/2β) 6.7 h, total clearance (CL) 1.07 ml·min−1·kg−1, volume of distribution (Vc) 0.27 l·kg−1 (0.21–0.49) and volume of distribution at steady-state (Vss) 0.59 l·kg−1. The intravenous disposition of unbound oxazepam was characterized by a clearance of 22.5ml·min−1·kg−1 and a distribution volume of 12.3 l·kg−1. After oral… 

Population Pharmacokinetics of High-Dose Oxazepam in Alcohol-Dependent Patients: Is There a Risk of Accumulation?

Oxazepam exhibited a linear pharmacokinetics with a proportional relationship from 20 to 300 mg per day, the dose range currently used in alcohol-dependent patients treated for alcohol withdrawal syndrome, and there was no evidence of drug accumulation with these doses.

Influence of a very low calorie diet on the clearance of oxazepam and antipyrine in man

It appears that a very low calorie diet with a sufficient protein and a veryLow carbohydrate content decreases the metabolism of oxazepam by glucuro-conjugation, whereas no effect was seen on the oxidative metabolism of antipyrine.

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

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Detection Time of Oxazepam and Zopiclone in Urine and Oral Fluid after Experimental Oral Dosing.

Examination of the detection time in urine and oral fluid after single oral doses of oxazepam and zopiclone shows that the transfer into oral fluid is significant and can be helpful when interpreting drug testing analyzes.

Prediction of pharmacokinetics prior to in vivo studies. 1. Mechanism-based prediction of volume of distribution.

The present study is the first attempt to develop and validate a mechanistic distribution model for predicting rat and human V(ss) of drugs prior to in vivo studies.

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To increase confidence in predicting extra-hepatic clearance, improvement of enzyme phenotyping for UGT substrates and more quantitative tissue expression levels of UGT enzymes are both needed.

The physicochemical and pharmacokinetic properties of benzodiazepines appearing as new psychoactive substances

The lipophilicity, the pKa and the plasma protein binding were determined for benzodiazepines appearing as new psychoactive substances and these were compared to theoretical values from software packages and none of the software packages were able to predict parameters to a su_cient degree of accuracy and in vitro data is currently preferable.

The effect of dietary energy and protein deficiency on drug metabolism

Both a low energy and a low protein intake decreased the glucuronidation of oxazepam, whereas no effect was observed on the rate of oxidation, expressed as the metabolism of antipyrine and metronidazole.

Predicting Passive Intestinal Absorption Using A Single Parameter

The model based on the new absorption parameter is shown to have wider applicability than current available models for predicting the fraction absorbed and to be validated using experimental human gastrointestinal absorption data for 98 compounds.

Glucuronidation in therapeutic drug monitoring.

  • M. ShipkovaE. Wieland
  • Biology, Medicine
    Clinica chimica acta; international journal of clinical chemistry
  • 2005



The influence of diflunisal on the pharmacokinetics of oxazepam.

The data suggest that the observed interaction between oxazepam and diflunisal results from a presystemic displacement of oxzepam from its plasma protein binding sites by dif lunisal and from an inhibition of the tubular secretion of oxZepam glucuronide by the glucuronides of difLunisal.

Disposition of oxazepam in relation to age, sex, and cigarette smoking

Smoking is a more important determinant of oxazepam clearance than age or sex, and the kinetics of single 30-mg oral doses of oxzepam were determined in 22 male and nine female volunteers.

Oxazepam kinetics: effects of age and sex.

Sex is a more important determinant of oxazepam clearance than is age, which was associated with heavy cigarette smoking but this did not explain the sex-related difference.

Disposition of three benzodiazepines after single oral administration in man.

The absorption of diazepam was most rapid and the mean time required to reach peak serum concentration was 45 minutes, followed by N-desmethyldiazepam 80 minutes and oxazepam 114 minutes, while slightly shorter terminal half-lives were obtained in the curve fitting of mean serum data.

Effects of different rates of absorption of two benzodiazepins on subjective and objective parameters

  • Å. Bliding
  • Medicine
    European Journal of Clinical Pharmacology
  • 2004
It is shown that relatively large diurnal variations in serum concentrations might occur during continuous treatment for more than four weeks and that a preparation with a high rate of absorption could still produce a subjectively apparent experience after each individual dose and it seems reasonable to assume that the risk of abuse is related to subjectively experienced effects.

The binding of thiopental to serum proteins determined by ultrafiltration and equilibrium dialysis.

It is concluded that the binding parameters for thiopental are influenced by the albumin concentration, and the ultrafiltration method used to estimate the protein bound fraction of a drug at its original concentration in a serum sample.

Propylene glycol as a cause of lactic acidosis.

Patients receiving intravenous medications containing PG as a vehicle may be an important cause of lactic acidosis in the hospitalized patient.

A physiological approach to hepatic drug clearance

The proposed classification of drug metabolism based on the hepatic extraction ratio allows prediction and interpretation of the effects of individual variations in drug‐metabolizing activity, route of administration, pharmacokinetic interactions, and disease states on hepatic drug elimination.

Multiple-dose kinetics and dialyzability of oxazepam in renal insufficiency.

7 patients with chronic renal insufficiency and 6 healthy controls received single 15-mg oral doses of oxazepam for 7 consecutive days to treat multiple venous thrombosis.