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Pharmacokinetic testing In twelve volunteers demonstrated that when given as a single 30 mg dose, the capsule, tablet, and suspension were equivalent in extent of absorption. For the capsule and tablet, peak plasma levels averaged 450 ng/mL and were observed to occur about 3 hours after dosing. The mean elimination half-life for oxazepam was approximately 8.2 hours (range 5.7 to 10.9 hours). This product has a single, major inactive metabolite in man, a glucuronide excreted in the urine.
Age (< 80 years old) does not appear to have a clinically significant effect on oxazepam kinetics. A statistically significant increase in elimination half-life in the very elderly (> 80 years of age) as compared to younger subjects has been reported, due to a 30% increase in volume of distribution, as well as a 50% reduction in unbound clearance of oxazepam in the very elderly, (see PRECAUTIONS, Geriatric Use).
Animal Pharmacology And Toxicology
In mice, Serax (oxazepam) exerts an anticonvulsant (anti-Metrazol) activity at 50-per-cent-effective doses of about 0.6 mg/kg orally. (Such anticonvulsant activity of benzodiazepines correlates with their tranquilizing properties.) To produce ataxia (rotabar test) and sedation (abolition of spontaneous motor activity), the 50-percent-effective doses of this product are greater than 5 mg/kg orally. Thus, about ten times the therapeutic (anticonvulsant) dose must be given before ataxia ensues, indicating a wide separation of effective doses and doses inducing side effects.
In evaluation of anti anxiety activity of compounds, conflict behavioral tests in rats differentiate continuous response for food in the presence of anxiety-provoking stress (shock) from drug-induced motor in coordination. This product shows significant separation of doses required to relieve anxiety and doses producing sedation or ataxia. Ataxia-producing doses exceed those of related CNS-acting drugs.
Acute oral LDM in mice is greater than 5000 mg/kg, compared to 800 mg/kg for a related compound (chlordiazepoxide). Subacute toxicity studies in dogs for four weeks at 480 mg/kg daily showed no specific changes; at 960 mg/kg two out of eight died with evidence of circulatory collapse. This wide margin of safety is significant compared to chlordiazepoxide HCL, which showed nonspecific changes in six dogs at 80 mg/kg. On chlordiazepoxide, two out of six died with evidence of circulatory collapse at 127 mg/kg, and six out of six died at 200 mg/kg daily. Chronic toxicity studies of Serax (oxazepam) in dogs at 120 mg/kg/day for 52 weeks produced no toxic manifestation. Fatty metamorphosis of the liver has been noted in six-week toxicity studies in rats given this product at 0.5% of the diet. Such accumulations of fat are considered reversible, as there is no liver necrosis or fibrosis. Breeding studies in rats through two successive litters did not produce fetal abnormality.
Oxazepam has not been adequately evaluated for mutagenic activity. In a carcinogenicity study, oxazepam was administered with diet to rats for two years. Male rats receiving 30 times the maximum human dose showed a statistical increase, when compared to controls, in benign thyroid follicular cell tumors, testicular interstitial cell adenomas, and prostatic adenomas. An earlier published study reported that mice fed dietary dosages of 35 or 100 times the human daily dose of oxazepam for 9 months developed a dose-related increase in liver adenomas.' In an independent analysis of some of the microscopic slides from this mouse study, several of these tumors were classified as liver carcinomas. At this time, there is no evidence that clinical use of oxazepam is associated with tumors.
Last reviewed on RxList: 3/20/2009
This monograph has been modified to include the generic and brand name in many instances.
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