Pharmacokinetic and pharmacodynamic studies of diazepam, temazepam and ceftriaxone
Diazepam is a widely used drug in the management of anxiety and convulsion. Young, mature and senescent male Fischer 344 rats were injected with 180 {mu}g/kg body weight of {sup 14}C-diazepam and the brain levels of the drug and its active metabolites were determined by HPLC and reverse isotope dilution techniques. During the two hours after injection, the areas under the brain level-time curves (AUCs) of diazepam, N-desmethyldiazepam and temazepam were greater in senescent rats than in mature and young rats. Temazepam, an active metabolite of diazepam, is used as a hypnotic. Brain exposure to the behaviorally active dose of temazepam during the initial two hours after its iv administration was studied in young, mature and senescent rats. Similar brain levels in young and old rats indicated the possible existence of a level in brain above which temazepam impaired passive-avoidance acquisition. Ceftriaxone is a new cephalosporin antibiotic with a relatively long half-life. In male Sprague-Dawley rats, ethanol administration did not affect the pharmacokinetic parameters of ceftriaxone.
- Research Organization:
- Washington State Univ., Pullman, WA (USA)
- OSTI ID:
- 7244605
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
560300 -- Chemicals Metabolism & Toxicology
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
AGE DEPENDENCE
ALCOHOLS
ANIMALS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
BIOLOGICAL HALF-LIFE
BODY
BRAIN
CARBON 14 COMPOUNDS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHROMATOGRAPHY
DRUGS
ETHANOL
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPE DILUTION
KINETICS
LABELLED COMPOUNDS
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
METABOLITES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
RATS
REACTION KINETICS
RODENTS
SEPARATION PROCESSES
TRACER TECHNIQUES
VERTEBRATES