The transfer across the placenta and the maternal and neonatal kinetics of oxazepam and its conjugate was studied in 12 patients and their newborns. Oxazepam was readily absorbed and peak plasma concentrations were similar to those in healthy non-pregnant volunteers. When meperidine was given within one hour of the dose of oxazepam the absorption was delayed but the bioavailability did not decrease. In the newborns the umbilical vein plasma concentration of oxazepam usually exceeded that of the conjugate. The reverse was true for all subsequent plasma samples from the newborn. The half-life of oxazepam in the newborn averaged 22 hours as compared to 6.5 hours in the mothers. A significant rise of the plasma concentration of oxazepam conjugate was noted in three newborns during the first 6-10 hours of extrauterine life. This shows that the newborn is able to conjugate oxazepam. The Apgar score values were normal.
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http://dx.doi.org/10.1111/j.1600-0447.1978.tb02389.x | DOI Listing |
Forensic Toxicol
July 2024
Department of Legal Medicine, Aichi Medical University School of Medicine, 1-1 Yazakokarimata, Nagakute, Aichi, 480-1195, Japan.
Purpose: Toxicological analyses of biological samples play important roles in forensic and clinical investigations. Ingested drugs are excreted in urine as conjugates with endogenous substances such as glucuronic acid; hydrolyzing these conjugates improves the determination of target drugs by liquid chromatography-tandem mass spectrometry (LC-MS/MS). In this study, we sought to improve the enzymatic hydrolysis of glucuronide conjugates of five psychoactive drugs (11-nor-9-carboxy-Δ-tetrahydrocannabinol, oxazepam, lorazepam, temazepam, and amitriptyline).
View Article and Find Full Text PDFDrug Metab Rev
November 2017
a IINFACTS - Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences , University Institute of Health Sciences (IUCS), CESPU, CRL , Gandra , Portugal.
Anxiolytic drugs, namely benzodiazepines, are the most commonly used psychoactive substances since anxiety disorders are prevalent mental disorders particularly in the Western world. Oxazepam is a short-acting benzodiazepine and one of the most frequently prescribed anxiolytic drugs. It is also the active metabolite of a wide range of other benzodiazepines, such as diazepam, ketazolam, temazepam, chlordiazepoxide, demoxazepam, halazepam, medazepam, prazepam, pinazepam, and chlorazepate.
View Article and Find Full Text PDFJ Chromatogr B Analyt Technol Biomed Life Sci
October 2017
Medical Bureau of Road Safety, Health Science Centre, University College Dublin, Belfield, D. 4, Ireland. Electronic address:
The objective of this work was to establish an analytical method for the analysis of 7 Benzodiazepines (diazepam, oxazepam, temazepam, nordiazepam, desalkylflurazepam, alprazolam and α-hydroxyalprazolam) in urine specimens taken from drivers suspected of driving under the influence of drugs. The specimen, calibrator and control preparation involved hydrolysis of conjugated benzodiazepines using β-glucuronidase in sodium acetate buffer, with incubation at 60°C for 2h. Specimens were then centrifuged, before being diluted 1 in 5 (total dilution 1 in 10), with 10% acetonitrile in water.
View Article and Find Full Text PDFMol Pharm
September 2017
Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Bari 70125, Italy.
The neurotransmitter dopamine (DA) was covalently linked to oxazepam (OXA), a well-known positive allosteric modulator of γ-aminobutyric acid type-A (GABA) receptor, through a carbamate linkage (4) or a succinic spacer (6). These conjugates were synthesized with the aim of improving the delivery of DA into the brain and enhancing GABAergic transmission, which may be useful for the long-term treatment of Parkinson disease (PD). Structure-based permeability properties, in vitro stability, and blood-brain barrier (BBB) permeability studies led to identify the OXA-DA carbamate conjugate 4a as the compound better combining sufficient stability and ability to cross BBB.
View Article and Find Full Text PDFToxicol Sci
July 2017
Laboratory of Toxicology, Department of Environmental Veterinary Science, Graduate School of Veterinary Medicine, Hokkaido University, N18, W9, Kita-ku, Sapporo 060-0818, Japan.
UDP-glucuronosyltransferases (UGTs) are among the most important xenobiotic metabolizing enzymes that conjugate a wide range of chemicals. Previous studies showed that Felidae and Pinnipedia species have very low UGT activities toward some phenolic compounds because of the UGT1A6 pseudogene and small numbers of UGT1A isozymes. In addition to the UGT1As, UGT2Bs isozymes also conjugate various endogenous (eg, estrogens, androgens, and bile acids) and exogenous compounds (opioids, non-steroidal anti-inflammatory drugs, and environmental pollutants).
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