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Ugeskrift For Laeger Jun 2022In this case report we describe a life-threatening episode of delirium in a 51-year-old man. The condition was triggered by an abrupt withdrawal of benzodiazepines. The...
In this case report we describe a life-threatening episode of delirium in a 51-year-old man. The condition was triggered by an abrupt withdrawal of benzodiazepines. The patient had been taking multiple sedatives for several years but a large proportion of the drugs were not available in Denmark. His general practitioner substituted and prescribed oxazepam and zolpidem for ten days. Afterwards the patient did not have access to benzodiazepines and developed a severe benzodiazepine withdrawal delirium. He was treated with diazepam and olanzapine with gradual dose reduction.
Topics: Alcohol Withdrawal Delirium; Benzodiazepines; Delirium; Diazepam; Humans; Male; Middle Aged; Oxazepam; Substance Withdrawal Syndrome
PubMed: 35703059
DOI: No ID Found -
Biomedical Papers of the Medical... Mar 2015Delirium tremens represents the most severe complication of alcohol withdrawal syndrome and, in its complications, significantly increases the morbidity and mortality of... (Review)
Review
OBJECTIVE
Delirium tremens represents the most severe complication of alcohol withdrawal syndrome and, in its complications, significantly increases the morbidity and mortality of patients. Alcohol withdrawal delirium is characterized by features of alcohol withdrawal itself (tremor, sweating, hypertension, tachycardia etc.) together with general delirious symptoms such as clouded consciousness, disorientation, disturbed circadian rhythms, thought processe and sensory disturbances, all of them fluctuating in time. The treatment combines a supportive and symptomatic approach. Benzodiazepines in supramaximal doses are usually used as drugs of choice but in some countries such as the Czech Republic or Germany, clomethiazole is frequently used as well.
METHOD
A computer search of the all the literature published between 1966 and December 2012 was accomplished on MEDLINE and Web of Science with the key words "delirium tremens", "alcohol withdrawal", "treatment" and "pharmacotherapy". There were no language or time limits applied.
CONCLUSIONS
When not early recognized and treated adequately, delirium tremens may result in death due to malignant arrhythmia, respiratory arrest, sepsis, severe electrolyte disturbance or prolonged seizures and subsequent trauma. Owing to these possible fatalities and other severe unexpected complications, delirium tremens should be managed at an ICU or wards ensuring vital signs monitoring. In symptomatic treatment, high doses of benzodiazepines, especially lorazepam, diazepam and oxazepam are considered the gold standard drugs. Supportive therapy is also of great importance.
Topics: Alcohol Withdrawal Delirium; Benzodiazepines; Disease Management; Humans; Psychometrics
PubMed: 24399242
DOI: 10.5507/bp.2013.089 -
Advanced Biomedical Research 2022This study aimed to compare the efficacy of gabapentin and oxazepam on sleep quality, the severity of anxiety, and pain level in patients admitted to the coronary care...
Comparison the Effects of Gabapentin and Oxazepam on Sleep Quality, Anxiety, and Pain in Unstable Angina Patients Admitted to Coronary Care Unit of Hazrat Rasool Akram Hospital.
BACKGROUND
This study aimed to compare the efficacy of gabapentin and oxazepam on sleep quality, the severity of anxiety, and pain level in patients admitted to the coronary care unit (CCU).
MATERIALS AND METHODS
This double-blind randomized clinical trial was done on the patients with unstable angina (UA) admitted to the CCU of Hazrat Rasool Akram Hospital in Tehran. A total of 56 patients were entered the study and randomly divided into two groups of 26. The first group was given a gabapentin capsule at a dose of 300-1200 mg/day, and the second group was given 10-20 mg of oxazepam tablets per day until hospitalization in the CCU. On the first and 4 days of hospitalization, Groningen sleep quality score (GSQS), Beck Anxiety Inventory, and severity of pain experienced by Visual Analogue Scale were recorded, and the mean frequency of chest pains was calculated in 24 h during the first 4 days. The amount of drug (morphine) prescription in CCU also compared between the two groups.
RESULTS
There was no significant difference in GSQS scores between both groups. The mean score of Beck's anxiety scale did not differ significantly between the two groups. However, the incidence of chest pain was significantly lower in the gabapentin-receiving group than in the oxazepam-receiving group (<0.001). The days that the patients experienced chest pain were significantly less in the gabapentin-receiving group than in the oxazepam-receiving group (<0.001).
CONCLUSION
The results of our study showed that gabapentin compared to oxazepam could significantly reduce chest pain in patients with UA.
PubMed: 36124023
DOI: 10.4103/abr.abr_154_20 -
Journal of Clinical and Experimental... 2022Alcohol withdrawal syndrome (AWS) is a common condition that is seen in treatment-seeking patients with Alcohol use disorder (AUD) and alcoholic liver disease (ALD).... (Review)
Review
Alcohol withdrawal syndrome (AWS) is a common condition that is seen in treatment-seeking patients with Alcohol use disorder (AUD) and alcoholic liver disease (ALD). AWS, which typically starts within 4-6 h of the last alcohol use, can range from mild symptoms such as insomnia, tremors, and autonomic hyperactivity to more severe symptoms such as seizures and delirium tremens. Clinical Institute Withdrawal Assessment Scale-Alcohol Revised (CIWA-Ar) is the most commonly used scale to assess AWS in clinical practice. The presence of moderate withdrawal as indicated by a score of more than 8 is an indication for pharmacotherapy. Lorazepam and oxazepam are preferred agents for the management of AWS in the setting of ALD. In severe ALD, benzodiazepines should be used cautiously with monitoring due to the risk of excessive sedation or precipitating hepatic encephalopathy.
PubMed: 36340306
DOI: 10.1016/j.jceh.2022.03.003 -
European Review For Medical and... Jan 2022Drug-facilitated sexual assault (DFSA) is an act of sexual violence towards a victim who is incapacitated due to the voluntary or involuntary consumption of intoxicating... (Review)
Review
OBJECTIVE
Drug-facilitated sexual assault (DFSA) is an act of sexual violence towards a victim who is incapacitated due to the voluntary or involuntary consumption of intoxicating substances. Sexual assaults are generally considered underreported and the toxicological analysis of DFSA cases is particularly challenging when there is a time delay from assault to medical examination. The aim of this review was to investigate typical toxicological findings in global DFSA cases and describe a typical DFSA case.
MATERIALS AND METHODS
A database search was conducted in PubMed using relevant search terms in order to identify studies reporting toxicological results in DFSA cases.
RESULTS
In total, 22 studies were included, covering toxicological findings in DFSA cases in North America, Europe, Asia, South Africa and Australasia from 1996 to 2018. Biological matrices used for analysis included blood, urine and hair. Toxicological findings were comparable among countries, with ethanol, cocaine, cannabis, benzodiazepines, amphetamines and analgesics being among the most frequently detected substances. Ethanol was frequently detected in combination with one or more drugs. A variety of benzodiazepines were observed, with the most common being diazepam, clonazepam, alprazolam, and oxazepam. The majority of cases involved women (87%-100%).
CONCLUSIONS
The findings suggest that a diverse range of substances are associated with DFSA and that victims are rendered vulnerable through recreational substance consumption at social events. As such, typical DFSA cases appear to be opportunistic in nature and primarily involves women in their mid-twenties and an acquaintance as the perpetrator.
Topics: Benzodiazepines; Crime Victims; Female; Forensic Toxicology; Humans; Sex Offenses; Substance Abuse Detection
PubMed: 35048994
DOI: 10.26355/eurrev_202201_27767 -
Drugs in R&D Mar 2022Urine is conventionally used as a specimen to document diazepam-related crimes; however, few reports have described the pharmacokinetics of diazepam and its metabolites...
BACKGROUND
Urine is conventionally used as a specimen to document diazepam-related crimes; however, few reports have described the pharmacokinetics of diazepam and its metabolites in urine.
OBJECTIVE
This study aimed to investigate the pharmacokinetics of diazepam and its metabolites, including glucuronide compounds, in the urine of Chinese participants.
METHODS
A total of 28 volunteers were recruited and each participant ingested 5 mg of diazepam orally. Ten milliliters of urine were collected from each participant at post-consumption timepoints of prior (zero), 1, 2, 4, 8, 12, and 24 h and 2, 3, 6, 12, and 15 days. All samples were extracted by solid-phase extraction and analyzed using high-performance liquid chromatography-tandem mass spectrometry. Diazepam and its main metabolites, except for temazepam, were detected in the urine of volunteers. Pharmacokinetic parameters were analyzed using the pharmacokinetic software DAS according to the non-compartment model.
RESULTS
Urinary diazepam peaked at 2.38 ng/mL (C) and 1.93 h (T). The urinary metabolite nordiazepam peaked at 1.17 ng/mL and 100.21 h; temazepam glucuronide (TG) peaked at 145.61 ng/mL and 41.14 h; and oxazepam glucuronide (OG) peaked at 101.57 ng/mL and 165.86 h. The elimination half-life (t) and clearance (CLz/F) for diazepam were 119.58 h and 65.77 L/h, respectively. The t of the metabolites nordiazepam, TG, and OG was 310.58 h, 200.17 h, and 536.44 h, respectively. Finally, this study found that both diazepam and its main metabolites in urine were detectable for at least 15 days, although there were individual differences.
CONCLUSION
The results regarding diazepam pharmacokinetics in urine would be of great help in forensic science and drug screening.
Topics: China; Chromatography, High Pressure Liquid; Diazepam; Humans; Nordazepam; Solid Phase Extraction
PubMed: 35099786
DOI: 10.1007/s40268-021-00375-y -
Molecules (Basel, Switzerland) Oct 2021Partially and exhaustively methylated β-cyclodextrins [(2-methyl)-β-CD (MCD), heptakis-(2,6-di--methyl)-β-CD (DIMEB), and heptakis-(2,3,6-tri--methyl)-β-CD (TRIMEB)]...
Partially and exhaustively methylated β-cyclodextrins [(2-methyl)-β-CD (MCD), heptakis-(2,6-di--methyl)-β-CD (DIMEB), and heptakis-(2,3,6-tri--methyl)-β-CD (TRIMEB)] have been compared in the hydrolysis and enantiodiscrimination of benzodiazepine derivative ()- or ()-oxazepam hemisuccinate (OXEMIS), using nuclear magnetic resonance (NMR) spectroscopy as an investigation tool. After 6 h, MCD induced an 11% hydrolysis of OXEMIS, remarkably lower in comparison with underivatized β-CD (48%), whereas no hydrolysis was detected in the presence of DIMEB or TRIMEB after 24 h. DIMEB showed greater ability to differentiate OXEMIS enantiomers in comparison to TRIMEB, by contrast MCD did not produce any splitting of racemic OXEMIS resonances. Both enantiomers of OXEMIS underwent deep inclusion of their phenyl pendant into cyclodextrins cavities from their wider rims, but tighter complexes were formed by DIMEB with respect to TRIMEB.
Topics: Hydrolysis; Magnetic Resonance Spectroscopy; Methylation; Models, Molecular; Molecular Structure; Oxazepam; beta-Cyclodextrins
PubMed: 34770758
DOI: 10.3390/molecules26216347 -
International Journal of Molecular... Sep 2023In this study, atomistic simulations were carried out to study the difference in the adsorption process between two similar molecules, diazepam and oxazepam, on...
In this study, atomistic simulations were carried out to study the difference in the adsorption process between two similar molecules, diazepam and oxazepam, on Na-montmorillonite. Kinetic and XRD measurements showed a contrasting adsorption mechanism of these two molecules, differing only by the presence/absence of methyl and hydroxyl groups, with a larger adsorption amount and intercalation for the oxazepam. The structural characterization of these molecules was investigated through DFT calculations and showed the vicinity of hydroxyl and carbonyl groups for only the chair conformation of oxazepam compared to the boat conformation. Classical molecular dynamics simulations of diazepam and the two forms of oxazepam on the external surface of Na-montmorillonite highlighted the better coordination of the oxazepam-chair conformation, compared to its boat counterpart and diazepam. This has been confirmed through DFT calculations, from which a coordination energy that is greater by 10 kcal·mol is observed. This strongly suggests that the experimentally observed intercalation of oxazepam occurs only in the chair form because of the strong coordination with the Na cation present in the Na-Mt interlayer. Classical MD simulations of the intercalated oxazepam chair molecule in the Na-Mt interlayer allowed the evaluation of the interlayer spacing d001, which was in very good agreement with the experimental XRD measurement.
Topics: Clay; Bentonite; Adsorption; Oxazepam; Diazepam
PubMed: 37834226
DOI: 10.3390/ijms241914781 -
The International Journal of... Mar 2003The phase I cytochrome P450 (CYP) isoenzymes have received substantial attention in the pharmacogenetic literature. Researchers are beginning to examine the role of the... (Review)
Review
The phase I cytochrome P450 (CYP) isoenzymes have received substantial attention in the pharmacogenetic literature. Researchers are beginning to examine the role of the phase II UDP-glucuronosyltransferase (UGT) enzymes, which produce products that are more water-soluble, less toxic and more readily excreted than the parent compounds. Several reasons may have contributed to neglect of UGTs (compared to CYPs) including: (1) the overlapping activity of UGTs and lack of selective probes; (2) the complexity of the glucuronidation cycle; and (3) the difficulty in developing analytic methods to measure glucuronides. Current CYP knowledge is used as a model to predict advances in UGT knowledge. At least 24 different UGT human genes have been identified and are classified in two families (UGT1 and UGT2) based on sequence homology. The UGT1A subfamily (genes located on chromosome 2) glucuronidates bilirubin, thyroid hormones, and some medications. UGT1A4 metabolizes tricyclic antidepressants and some antipsychotics. The UGT2B subfamily (genes located on chromosome 6) glucuronidates sexual steroids and bile acids. Oxazepam and lorazepam are mainly metabolized by glucuronidation. Anti-epileptics with mood-stabilizing properties are frequently metabolized by UGTs. Opioid and nicotine addiction may also be influenced by glucuronidation. Glucuronidation of serotonin may be important during fetal development. UGTs appear to be in small concentrations in brain tissue (and higher concentrations at brain capillaries). However, UGTs may be localized in certain brain areas to provide a neuroprotective function. This review illustrates the importance of glucuronidation and the implications for psychiatry.
Topics: Animals; Glucuronosyltransferase; Humans; Lorazepam; Oxazepam; Polymorphism, Genetic; Psychiatry; Serotonin
PubMed: 12899737
DOI: 10.1017/S1461145703003249