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https://www.readbyqxmd.com/read/29042451/biased-signaling-of-the-proton-sensing-receptor-ogr1-by-benzodiazepines
#1
Tonio Pera, Deepak A Deshpande, Michael Ippolito, Bin Wang, Adelina Gavrila, James V Michael, Ajay P Nayak, Eric Tompkins, Eleni Farrell, Wesley K Kroeze, Bryan L Roth, Reynold A Panettieri, Jeffrey L Benovic, Steven S An, Nickolai O Dulin, Raymond B Penn
GPCRs have diverse signaling capabilities, based on their ability to assume various conformations. Moreover, it is now appreciated that certain ligands can promote distinct receptor conformations and thereby bias signaling toward a specific pathway to differentially affect cell function. The recently deorphanized G protein-coupled receptor OGR1 [ovarian cancer G protein-coupled receptor 1 (GPR68)] exhibits diverse signaling events when stimulated by reductions in extracellular pH. We recently demonstrated airway smooth muscle cells transduce multiple signaling events, reflecting a diverse capacity to couple to multiple G proteins...
October 17, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29037589/a-twin-purification-enrichment-procedure-based-on-two-versatile-solid-liquid-extracting-agents-for-efficient-uptake-of-ultra-trace-levels-of-lorazepam-and-clonazepam-from-complex-bio-matrices
#2
Maryam Hemmati, Maryam Rajabi, Alireza Asghari
In this research work, two consecutive dispersive solid/liquid phase microextractions based on efficient extraction media were developed for the influential and clean pre-concentration of clonazepam and lorazepam from complicated bio-samples. The magnetism nature of the proposed nanoadsorbent proceeded the clean-up step conveniently and swiftly (∼5min), pursued by a further enrichment via a highly effective and rapid emulsification microextraction process (∼4min) based on a deep eutectic solvent (DES). Finally, the instrumental analysis step was practicable via high performance liquid chromatography-ultraviolet detection...
September 21, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29030176/physiologically-based-pharmacokinetic-modeling-of-disposition-and-drug-drug-interactions-for-valproic-acid-and-divalproex
#3
Todd M Conner, Vahagn C Nikolian, Patrick E Georgoff, Manjunath P Pai, Hasan B Alam, Duxin Sun, Ronald C Reed, Tao Zhang
Valproic acid (VPA) is an older first-line antiepileptic drug with a complex pharmacokinetic (PK) profile, currently under investigation for several novel neurologic and non-neurologic indications. Our study objective was to design and validate a mechanistic model of VPA disposition in adults and children; and evaluate its predictive performance of drug-drug interactions (DDIs). This study expands upon existing physiologically based pharmacokinetic (PBPK) models for VPA by incorporating UGT enzyme kinetics and an advanced dissolution, absorption, and metabolism (ADAM) model for extended-release (ER) formulation...
October 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29027336/trends-in-utilization-of-benzodiazepine-and-z-drugs-in-israel
#4
Erez Berman, Sara Eyal, Eli Marom
BACKGROUND: Studies on benzodiazepine (BZDs) as well as Zopiclone and Zolpidem (Z-drugs) utilization are important for estimating the prevalence of medical conditions, providing the basis for pharmacovigilance, and identifying temporal trends of consumption. Such studies that involve the Israeli population have not been conducted yet. PURPOSE: Identify trends over time in utilization of BZDs and Z-drugs in a nationwide population in Israel. METHODS: Data on BZD and Z-drugs utilization (for all indications) for the period 2005 to 2013 were obtained from pharmaceutical companies that distribute BZDs in Israel...
October 13, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28988045/prescribing-practices-in-southeastern-europe-focus-on-benzodiazepine-prescription-at-discharge-from-nine-university-psychiatric-hospitals
#5
Nadja P Maric, Milan Latas, Sanja Andric Petrovic, Ivan Soldatovic, Slavica Arsova, Danijel Crnkovic, Dragoslava Gugleta, Aleksandar Ivezic, Vladimir Janjic, Dalibor Karlovic, Dusica Lecic Tosevski, Alma Mihaljevic-Peles, Antoni Novotni, Bojana Pejuskovic, Branimir Radmanovic, Djendji Siladji Mladenovic, Violeta M Slavkovic, Zoran Stimac, Olivera Zikic
There is much concern about the widespread long-term use of benzodiazepines. Our manuscript addressed its use in the region of Southeastern Europe, which seems extensive, but insufficiently explored. At nine university psychiatric hospitals (Croatia, Macedonia and Serbia), we retrospectively analyzed discharge summary documents to find the prevalence of discharge benzodiazepine prescriptions and the prescribed benzodiazepine doses. This study included 1047 adult subjects and showed that 81.9% of them had benzodiazepines prescribed in the discharge summary document, with high mean daily dose of around 5mg lorazepam equivalents...
September 25, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28975307/effect-of-lorazepam-with-haloperidol-vs-haloperidol-alone-on-agitated-delirium-in-patients-with-advanced-cancer-receiving-palliative-care-a-randomized-clinical-trial
#6
RANDOMIZED CONTROLLED TRIAL
David Hui, Susan Frisbee-Hume, Annie Wilson, Seyedeh S Dibaj, Thuc Nguyen, Maxine De La Cruz, Paul Walker, Donna S Zhukovsky, Marvin Delgado-Guay, Marieberta Vidal, Daniel Epner, Akhila Reddy, Kimerson Tanco, Janet Williams, Stacy Hall, Diane Liu, Kenneth Hess, Sapna Amin, William Breitbart, Eduardo Bruera
Importance: The use of benzodiazepines to control agitation in delirium in the last days of life is controversial. Objective: To compare the effect of lorazepam vs placebo as an adjuvant to haloperidol for persistent agitation in patients with delirium in the setting of advanced cancer. Design, Setting, and Participants: Single-center, double-blind, parallel-group, randomized clinical trial conducted at an acute palliative care unit at MD Anderson Cancer Center, Texas, enrolling 93 patients with advanced cancer and agitated delirium despite scheduled haloperidol from February 11, 2014, to June 30, 2016, with data collection completed in October 2016...
September 19, 2017: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/28966786/urgent-release-of-severe-psychomotor-retardation-with-intramuscular-lorazepam-a-case-report
#7
Mark Kanzawa, Beena Premkumar
No abstract text is available yet for this article.
October 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28962597/periodic-catatonia-with-long-term-treatment-a-case-report
#8
Ruei-An Chen, Tiao-Lai Huang
BACKGROUND: Periodic catatonia has long been a challenging diagnosis and there are no absolute guidelines for treatment when precipitating factors are also unclear. We report a schizophrenia patient with periodic catatonia with a 15-year treatment course. A possible correlation between decreased daylight exposure and periodic attacks has been observed. CASE PRESENTATION: We describe a 49-year-old woman with periodic catatonia associated with schizophrenia with 15 years of follow-up...
September 29, 2017: BMC Psychiatry
https://www.readbyqxmd.com/read/28942593/psychoactive-drugs-occurrence-in-aquatic-environment-analytical-methods-and-ecotoxicity-a-review
#9
Deivisson Lopes Cunha, Frederico Goytacazes de Araujo, Marcia Marques
This review focused on seven psychoactive drugs being six benzodiazepines (alprazolam, bromazepam, clonazepam, diazepam, lorazepam, and oxazepam) and one antidepressant (citalopram) widely consumed by modern society and detected in different aqueous matrices (drinking water, surface water, groundwater, seawater, estuary water, influent and effluent of wastewater treatment plants). The review included 219 selected scientific papers from which 1642 data/entries were obtained, each entry corresponding to one target compound in one aqueous matrix...
September 23, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28941387/management-protocols-for-status-epilepticus-in-the-pediatric-emergency-room-systematic-review-article
#10
REVIEW
Cheuk C Au, Ricardo G Branco, Robert C Tasker
OBJECTIVE: This systematic review of national or regional guidelines published in English aimed to better understand variance in pre-hospital and emergency department (ED) treatment of status epilepticus. SOURCES: Systematic search of national or regional guidelines (January 2000 to February 2017) contained within PubMed and Google Scholar databases, and article reference lists. The search keywords were status epilepticus, prolonged seizure, treatment, and guideline...
September 20, 2017: Jornal de Pediatria
https://www.readbyqxmd.com/read/28936082/catatonia-in-patients-with-dementia-admitted-to-a-geriatric-psychiatry-ward
#11
Puja Sharma, Ina Sawhney, Walter Jaimes-Albornoz, Jordi Serra-Mestres
To determine the frequency and characteristics of catatonia in persons with dementia, all patients admitted to an old age psychiatry ward were screened for catatonia with the Bush-Francis Catatonia Screening Instrument (BFCSI) over a period of 6 months. Thirty-seven patients were admitted, and there were 14 patients with dementia. The rate of catatonia in these patients was 42.8% (6 out of 14). Five out of six of these patients received treatment for catatonia with lorazepam, all achieving complete remission...
August 2017: Journal of Neurosciences in Rural Practice
https://www.readbyqxmd.com/read/28929601/conversion-of-benzoic-acid-into-phenol-in-an-itms-under-ci-ms-n-conditions-recognition-of-ortho-chlorobenzoyl-derivatives
#12
Michela Begala
Isomeric chlorobenzoyl cations (m/z 139), under collision induced experiments, fragment identically. Chlorobenzoyl cations can be efficiently converted into cholorophenol radical cations by the reaction with methanol in the ion trap analyser under CI-MS(n) conditions. The substitution of the carbonyl group with a hydroxyl moiety is able to induce an ortho effect, which is absent in the starting ortho-chlorobenzoyl cation. This transformation could be useful to recognize ortho-chlorinated benzoyl derivatives without the need of MS spectra comparison of the whole set of isomers...
September 19, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28919386/comparison-of-lacosamide-versus-sodium-valproate-in-status-epilepticus-a-pilot-study
#13
Usha K Misra, Deepanshu Dubey, Jayantee Kalita
PURPOSE: The purpose of this study was to compare the efficacy and safety of lacosamide (LCM) and sodium valproate (SVA) in lorazepam (LOR)-resistant SE. METHODS: Patients with LOR-resistant SE were randomized to intravenous LCM 400mg at the rate of 60mg/kg/min or SVA 30mg/kg at the rate of 100mg/min. The SE severity score (STESS), duration of SE and its etiology, and MRI findings were noted. Primary outcome was seizure cessation for 1h, and secondary outcomes were 24h seizure remission, in-hospital death, and severe adverse events (SAE)...
September 14, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28869786/population-pharmacokinetic-pharmacodynamic-modelling-of-auditory-evoked-event-related-potentials-with-lorazepam
#14
Aurélie Lombard, Claire Brittain, Graham Wishart, Stephen Lowe, Andrew McCarthy, William Landschulz, Georg Dorffner, Peter Anderer, Eunice Yuen
Event-Related Potentials (ERPs) are commonly used in Neuroscience research, particularly the P3 waveform because it is associated with cognitive brain functions and is easily elicited by auditory or sensory inputs. ERPs are affected by drugs such as lorazepam, which increase the latency and decrease the amplitude of the P3 wave. In this study, auditory-evoked ERPs were generated in 13 older healthy volunteers using an oddball tone paradigm, after administration of single 0.5 and 2mg doses of lorazepam. Population pharmacokinetics (PK)/ pharmacodynamics (PD) models were developed using non-linear mixed effects methods in order to assess the effect of lorazepam on the latency and amplitude of the P3 waveforms...
September 4, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28851658/benzodiazepines-use-and-breast-cancer-risk-a-population-based-study-and-gene-expression-profiling-evidence
#15
Usman Iqbal, Tzu-Hao Chang, Phung-Anh Nguyen, Shabbir Syed-Abdul, Hsuan-Chia Yang, Chih-Wei Huang, Suleman Atique, Wei-Chung Yang, Max Moldovan, Wen-Shan Jian, Min-Huei Hsu, Yun Yen, Yu-Chuan Jack Li
The aim of this study was to investigate whether long-term use of Benzodiazepines (BZDs) is associated with breast cancer risk through the combination of population-based observational and gene expression profiling evidence. We conducted a population-based case-control study by using 1998 to 2009year Taiwan National Health Insurance Research Database and investigated the association between BZDs use and breast cancer risk. We selected subjects age of >20years old and six eligible controls matched for age, sex and the index date (i...
October 2017: Journal of Biomedical Informatics
https://www.readbyqxmd.com/read/28758203/haloperidol-for-psychosis-induced-aggression-or-agitation-rapid-tranquillisation
#16
REVIEW
Edoardo G Ostinelli, Melanie J Brooke-Powney, Xue Li, Clive E Adams
BACKGROUND: Haloperidol used alone is recommended to help calm situations of aggression or agitation for people with psychosis. It is widely accessible and may be the only antipsychotic medication available in limited-resource areas. OBJECTIVES: To examine whether haloperidol alone is an effective treatment for psychosis-induced aggression or agitation, wherein clinicians are required to intervene to prevent harm to self and others. SEARCH METHODS: We searched the Cochrane Schizophrenia Group's Study-Based Register of Trials (26th May 2016)...
July 31, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28750419/pipamperone-and-delirium-a-preliminary-evaluation-of-its-effectiveness-in-the-management-of-delirium-and-its-subtypes
#17
Soenke Boettger, Silvana Knöpfel, Maria Schubert, David Garcia Nuñez, Michael Martin Plichta, Richard Klaghofer, Josef Jenewein
INTRODUCTION: Delirium has been recognised as an underdiagnosed and undermanaged syndrome with substantial prevalence rates and potentially deleterious consequences in the medically ill population. Despite its frequent administration in the management of delirium, the effectiveness of pipamperone has not yet been evaluated. METHODS: In this retrospective, descriptive cohort study of 192 patients, pipamperone as monotherapy and as an adjunct to haloperidol, haloperidol alone, or atypical antipsychotics were compared with respect to their effectiveness in the management of delirium and its subtypes over the course of 20 days...
July 27, 2017: Swiss Medical Weekly
https://www.readbyqxmd.com/read/28718026/solid-phase-extraction-of-multi-class-pharmaceuticals-from-environmental-water-samples-onto-modified-multi-walled-carbon-nanotubes-followed-by-lc-ms-ms
#18
Bojana Lalović, Tatjana Đurkić, Marija Vukčević, Ivona Janković-Častvan, Ana Kalijadis, Zoran Laušević, Mila Laušević
In this paper, pristine and chemically treated multi-walled carbon nanotubes (MWCNTs) were employed as solid-phase extraction sorbents for the isolation and enrichment of multi-class pharmaceuticals from the surface water and groundwater, prior to liquid chromatography-tandem mass spectrometry analysis. Thirteen pharmaceuticals that belong to different therapeutical classes (erythromycin, azithromycin, sulfamethoxazole, diazepam, lorazepam, carbamazepine, metoprolol, bisoprolol, enalapril, cilazapril, simvastatin, clopidogrel, diclofenac) and two metabolites of metamizole (4-acetylaminoantipyrine and 4-formylaminoantipyrine) were selected for this study...
July 17, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28680170/pharmacokinetic-interactions-between-valproic-acid-and-lorazepam-pivotal-study-a-review-of-site-specific-practices
#19
Joane Y Tang, Tony K L Kiang, Mary H H Ensom
BACKGROUND: Coadministration of lorazepam and valproic acid is identified by tertiary references as causing a major drug interaction that requires therapy modification and dosage adjustments. The proposed mechanism involves inhibition of lorazepam glucuronidation via direct inhibition of uridine 5'-diphosphate-glucuronosyltransferase enzymes by valproic acid. However, the clinical significance of this interaction is unclear. OBJECTIVES: To identify site-specific practices and assess clinical responses to the interaction between valproic acid and lorazepam...
May 2017: Canadian Journal of Hospital Pharmacy
https://www.readbyqxmd.com/read/28650904/pediatric-procedural-sedation-using-the-combination-of-ketamine-and-propofol-outside-of-the-emergency-department-a-report-from-the-pediatric-sedation-research-consortium
#20
Jocelyn R Grunwell, Curtis Travers, Anne G Stormorken, Patricia D Scherrer, Corrie E Chumpitazi, Jana A Stockwell, Mark G Roback, Joseph Cravero, Pradip P Kamat
OBJECTIVES: Outcomes associated with a sedative regimen comprised ketamine + propofol for pediatric procedural sedation outside of both the pediatric emergency department and operating room are underreported. We used the Pediatric Sedation Research Consortium database to describe a multicenter experience with ketamine + propofol by pediatric sedation providers. DESIGN: Prospective observational study of children receiving IV ketamine + propofol for procedural sedation outside of the operating room and emergency department using data abstracted from the Pediatric Sedation Research Consortium during 2007-2015...
August 2017: Pediatric Critical Care Medicine
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