2,939 results match your criteria Toxicity Benzodiazepine


Discovery of a novel chemotype of histone lysine methyltransferase EHMT1/2 (GLP/G9a) inhibitors: rational design, synthesis, biological evaluation and co-crystal structure.

J Med Chem 2019 Feb 12. Epub 2019 Feb 12.

Since the discovery of compound BIX01294 over 10 years ago, only a very limited number of non-quinazoline inhibitors of H3K9-specific methyltransferases G9a and GLP have been reported. Herein we report the identification of a novel chemotype for G9a/GLP inhibitors, based on the under-investigated 2-alkyl-5-amino- and 2-aryl-5-amino-substituted 3H-benzo[e][1,4]diazepine scaffold. Our research efforts yielded the identification of compound 12a (EML741), which not only maintained the high in vitro and cellular potency of its quinazoline counterpart, but also displayed improved inhibitory potency against DNMT1, improved selectivity against other methyltransferases, low cell toxicity, and improved apparent permeability values in both PAMPA and PAMPA-BBB assays and, therefore, might potentially be a better candidate for animal studies. Read More

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http://dx.doi.org/10.1021/acs.jmedchem.8b02008DOI Listing
February 2019
1 Read

Baclofen Neurotoxicity: A Metabolic Encephalopathy Susceptible to Exacerbation by Benzodiazepine Therapy.

J Clin Neurophysiol 2019 Jan 24. Epub 2019 Jan 24.

Department of Neurology, Royal Perth Hospital, Perth, Australia.

Purpose: Baclofen has been reported to cause both a metabolic encephalopathy and nonconvulsive status epilepticus. Baclofen is typically used in the management of muscle spasticity but is being increasingly used to manage alcohol withdrawal and opiate dependency. Given the increasing use of baclofen we describe the clinical and electrographical features of baclofen neurotoxicity seen at our institution. Read More

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http://dx.doi.org/10.1097/WNP.0000000000000565DOI Listing
January 2019
2 Reads

Antipsychotics for the treatment of sympathomimetic toxicity: A systematic review.

Am J Emerg Med 2019 Jan 6. Epub 2019 Jan 6.

Department of Emergency Medicine, McGill University Health Centre, Montréal, Québec, Canada; Centre Antipoison Du Québec, Montréal, Québec, Canada; Département d'urgence, Hôpital Charles-Lemoyne, Greenfield Park, Qc, Canada.

Objective: Benzodiazepines are often recommended first-line for management of cocaine and amphetamine toxicity while antipsychotic treatment is discouraged due to the potential for lowering seizure threshold, prolonging the QT interval, and decreasing heat dissipation. We performed a systematic review including animal and human studies to elucidate the efficacy and safety of antipsychotics in managing sympathomimetic toxicity specifically evaluating the effect of treatment on mortality, seizures, hyperthermia, and cardiovascular effects.

Methods: We searched MEDLINE, Embase, BIOSIS Previews, Web of Science, Scopus, CENTRAL and gray literature from inception to 31 May 2017 to answer: Can antipsychotics be used safely and effectively to treat cocaine or amphetamine toxicity? Citations were screened by title and abstract. Read More

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http://dx.doi.org/10.1016/j.ajem.2019.01.001DOI Listing
January 2019
2 Reads

Pharmacological basis for sedative and hypnotic like effects of Pyrus pashia using in vivo experimental models.

Int J Geriatr Psychiatry 2019 Jan 4. Epub 2019 Jan 4.

Department of Pharmacy, Abdul Wali Khan University, Mardan, Pakistan.

Objective: Pyrus pashia has traditionally been used as a therapeutic agent including sedative. In this regard, hydroethanolic extract of Pyrus pashia (HEPP) was screened for phytochemical investigation, acute toxicity, and sedative-hypnotic activity to provide a scientific rationale to its ethno-medicinal uses.

Methods: Mice were used in acute toxicity test; sedative potential was observed in open field test while thiopental-induced sleeping time and barbiturate-induced sleeping time tests were used for the assessment of hypnotic like effects of HEPP. Read More

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http://doi.wiley.com/10.1002/gps.5059
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http://dx.doi.org/10.1002/gps.5059DOI Listing
January 2019
13 Reads

Investigating tissue bioconcentration and the behavioural effects of two pharmaceutical pollutants on sea trout (Salmo trutta) in the laboratory and field.

Aquat Toxicol 2019 Feb 1;207:170-178. Epub 2018 Dec 1.

Department of Ecology and Environmental Science, Umeå University, SE-90187, Umeå, Sweden; Department of Wildlife, Fish and Environmental Studies, Swedish University of Agricultural Sciences, SE-90183, Umeå, Sweden.

Pharmaceuticals entering aquatic ecosystems via wastewater effluents are of increasing concern for wild animals. Because some pharmaceuticals are designed to modulate human behaviour, measuring the impacts of exposure to pharmaceuticals on fish behaviour has become a valuable endpoint. While laboratory studies have shown that pharmaceuticals can affect fish behaviour, there is a lack of understanding if behaviour is similarly affected in natural environments. Read More

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http://dx.doi.org/10.1016/j.aquatox.2018.11.028DOI Listing
February 2019
1 Read

First aid interventions by laypeople for acute oral poisoning.

Cochrane Database Syst Rev 2018 12 19;12:CD013230. Epub 2018 Dec 19.

Centre for Evidence-Based Practice (CEBaP), Belgian Red Cross, Motstraat 42, Mechelen, Belgium, 2800.

Background: Oral poisoning is a major cause of mortality and disability worldwide, with estimates of over 100,000 deaths due to unintentional poisoning each year and an overrepresentation of children below five years of age. Any effective intervention that laypeople can apply to limit or delay uptake or to evacuate, dilute or neutralize the poison before professional help arrives may limit toxicity and save lives.

Objectives: To assess the effects of pre-hospital interventions (alone or in combination) for treating acute oral poisoning, available to and feasible for laypeople before the arrival of professional help. Read More

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http://doi.wiley.com/10.1002/14651858.CD013230
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http://dx.doi.org/10.1002/14651858.CD013230DOI Listing
December 2018
6 Reads

Treatment of caffeine toxicity with metoprolol.

Am J Emerg Med 2018 Nov 26. Epub 2018 Nov 26.

Department of Emergency Medicine, Jacobi Medical Center, Bronx, NY, United States of America.

A 27-year-old man presented with an intentional overdose of concentrated caffeine powder that he bought over the internet. The patient received benzodiazepines and ondansetron for symptomatic treatment when he arrived in the Emergency Department (ED). Subsequently, he developed recurrent supraventricular tachycardia in the ED. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S07356757183095
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http://dx.doi.org/10.1016/j.ajem.2018.11.038DOI Listing
November 2018
7 Reads

Determination of emerging chlorinated byproducts of diazepam in drinking water.

Chemosphere 2019 Mar 15;218:223-231. Epub 2018 Nov 15.

Beijing Advanced Innovation Center for Food Nutrition and Human Health, College of Veterinary Medicine, China Agricultural University, Beijing, 100193, China; Beijing Key Laboratory of Diagnostic and Traceability Technologies for Food Poisoning, Beijing Center for Disease Prevention and Control, Beijing, 100013, China. Electronic address:

Diazepam (DZP) is often found in source water and drinking water at dozens of nanograms per liter levels. The transformation of DZP in water chlorination disinfection process has aroused new concern because the toxic disinfection byproducts (DBPs) might be produced. However, the DBPs of DZP have not been fully identified, and their occurrence levels in drinking water have not been reported. Read More

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http://dx.doi.org/10.1016/j.chemosphere.2018.11.076DOI Listing
March 2019
1 Read

Translational research on chemical nerve agents.

Neurobiol Dis 2018 Nov 20. Epub 2018 Nov 20.

National Institute of Neurological Disorders and Stroke, National Institutes of Health, United States.

This special issue will describe cutting-edge translational research on the development of safe and effective therapeutics for treating exposure to toxic chemical threat agents that target the nervous system. These studies are supported by the National Institutes of Health (NIH) Countermeasures Against Chemical Threats (CounterACT) program. Chemical threats include chemical warfare agents, pesticides and other toxic chemicals whose primary mode of action is targeted within the nervous system. Read More

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http://dx.doi.org/10.1016/j.nbd.2018.11.020DOI Listing
November 2018
3 Reads

Camphor Poisoning: A Rare Cause of Acute Symptomatic Seizures in Children.

J Emerg Trauma Shock 2018 Jul-Sep;11(3):228-229

Department of Emergency Medicine and Critical Care, Amrita University, Kochi, Kerala, India.

Camphor is a toxic compound easily available over the counter, which can cause fatal seizures in children when ingested. It is available in several forms and is commonly used in Indian households, especially for religious rituals and for its cough-suppressive and nasal-decongestant effect. The toxic effect remains unknown in most homes. Read More

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http://dx.doi.org/10.4103/JETS.JETS_21_18DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6182968PMC
November 2018
1 Read

Practical guide for the management of systemic toxicity caused by local anesthetics.

Authors:

J Anesth 2019 Feb 11;33(1):1-8. Epub 2018 Nov 11.

Systemic toxicity from local anesthetics can occur in any of the wide range of situations in which these agents are used. This practical guide is created to generate a shared awareness of the prevention, diagnosis, and treatment of local anesthetic systemic toxicity among all medical professionals who perform nerve blocks. Systemic toxicity of local anesthetic is induced by an increase of its protein-unbound plasma concentration. Read More

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http://link.springer.com/10.1007/s00540-018-2542-4
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http://dx.doi.org/10.1007/s00540-018-2542-4DOI Listing
February 2019
17 Reads

Diazepam Toxicity Presenting as a Dementia Disorder.

J Alzheimers Dis 2018 ;66(3):935-938

Department of Neurology, University of Louisville, Louisville, KY, USA.

The toxicity associated with long-standing benzodiazepine use in older persons is a critical issue. Several epidemiological reports have studied correlation between benzodiazepine use and risk of dementia development. In this manuscript, we used a case report to demonstrate how chronic diazepam use can cause cognitive deficits that resemble Alzheimer's disease and related conditions. Read More

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http://dx.doi.org/10.3233/JAD-180745DOI Listing
January 2018
1 Read

Hydroalcoholic extract of Cuscuta epithymum enhances pentobarbital-induced sleep: possible involvement of GABAergic system.

Curr Drug Discov Technol 2018 Nov 4. Epub 2018 Nov 4.

Pharmacological Research Center of Medicinal Plants, Mashhad University of Medical Sciences, Mashhad. Iran.

Background: Insomnia is the most common sleep disorder. The present study was undertaken to evaluate the sedative-hypnotic potential of hydroalcoholic extract (HAE) of Cuscuta epithymum and its fractions.

Method: HAE and its fractions including: water fraction (WF), ethyl acetate fraction (EAF) and n-hexan fraction (NHF) were i. Read More

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http://www.eurekaselect.com/167001/article
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http://dx.doi.org/10.2174/1570163815666181105091801DOI Listing
November 2018
12 Reads

Linezolid-associated serotonin toxicity after escitalopram discontinuation: concomitant drug considerations.

BMJ Case Rep 2018 Oct 30;2018. Epub 2018 Oct 30.

College of Pharmacy, University of Florida, Gainesville, Florida, USA.

We report a case of a hospitalised patient who developed probable serotonin toxicity shortly after the initiation of linezolid in whom the selective serotonin reuptake inhibitor (SSRI) escitalopram had been recently discontinued. On day 2 of linezolid administration, the patient reported severe anxiety and was observed to have full body jerking and twitching motions without mental status change. Notably, the patient was concomitantly receiving the antidepressant, trazodone and the benzodiazepine, clonazepam possibly affecting the severity and manifestations of serotonin toxicity. Read More

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http://dx.doi.org/10.1136/bcr-2018-226597DOI Listing
October 2018
4 Reads

Soman-induced status epilepticus, epileptogenesis, and neuropathology in carboxylesterase knockout mice treated with midazolam.

Epilepsia 2018 Dec 25;59(12):2206-2218. Epub 2018 Oct 25.

US Army Medical Research Institute of Chemical Defense, Aberdeen Proving Ground, Maryland.

Objective: Exposure to chemical warfare nerve agents (CWNAs), such as soman (GD), can induce status epilepticus (SE) that becomes refractory to benzodiazepines when treatment is delayed, leading to increased risk of epileptogenesis, severe neuropathology, and long-term behavioral and cognitive deficits. Rodent models, widely used to evaluate novel medical countermeasures (MCMs) against CWNA exposure, normally express plasma carboxylesterase, an enzyme involved in the metabolism of certain organophosphorus compounds. To better predict the efficacy of novel MCMs against CWNA exposure in human casualties, it is crucial to use appropriate animal models that mirror the human condition. Read More

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http://doi.wiley.com/10.1111/epi.14582
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http://dx.doi.org/10.1111/epi.14582DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6334636PMC
December 2018
12 Reads

Presentations to the emergency department with non-medical use of benzodiazepines and Z-drugs: profiling and relation to sales data.

Eur J Clin Pharmacol 2019 Jan 22;75(1):77-85. Epub 2018 Sep 22.

Clinical Toxicology, Guy's and St Thomas' Hospitals NHS Foundation Trust, and King's Health Partners, London, UK.

Background: Non-medical use of benzodiazepines and Z-drugs is common; however, there is limited information available on the extent of harm related to this in Europe, as well as the relationship between misuse and availability.

Aim: To describe presentations to the emergency department in Europe related to the recreational use of benzodiazepines and Z-drugs and compare regional differences in these presentations with legal drug sales of benzodiazepines and Z-drugs within each country.

Methods: Emergency department presentations with recreational misuse of benzodiazepines and Z-drugs were obtained from the Euro-DEN dataset for the period from October 2013 to September 2015; data extracted included demographics, clinical features, reported coused drugs, and outcome data. Read More

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http://link.springer.com/10.1007/s00228-018-2550-1
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http://dx.doi.org/10.1007/s00228-018-2550-1DOI Listing
January 2019
22 Reads

Pyrrolo[2,1-c][1,4] benzodiazepine-3,11-diones protect SHSY-5Y cells from Cd-induced apoptosis involving suppression of endoplasmic reticulum stress.

Bioorg Med Chem 2018 Oct 11;26(18):5151-5158. Epub 2018 Sep 11.

Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China. Electronic address:

Cadmium (Cd) is a potent toxic heavy metal, some studies showed that Cd-induced apoptosis is through ER stress pathway. Compounds of pyrrolo[2,1-c][1,4]benzodiazepine (PBD)-3,11-diones were discovered as potent neuroprotective agents against Cd-induced toxicity in SH-SY5Y cells for the first time. In this study, twenty-six PBD-3,11-dione derivatives were synthesized and evaluated for their neuroprotective activity against Cd-induced toxicity by CCK-8 assay. Read More

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http://dx.doi.org/10.1016/j.bmc.2018.09.011DOI Listing
October 2018
3 Reads

Sevoflurane addiction due to workplace exposure: A case report and literature review.

Medicine (Baltimore) 2018 Sep;97(38):e12454

Department of Anesthesiology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Rationale: Anesthesiologists have a well-known increased risk of substance abuse. High-concentration of inhalation anesthetics in exhaled air of operating room personnel is detected. such secondhand exposure produces neurobiological sensitization to the reinforcing effects of inhalation anesthetics. Read More

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http://dx.doi.org/10.1097/MD.0000000000012454DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6160252PMC
September 2018
2 Reads

Midazolam is effective to reduce cortical network activity in organotypic cultures during severe cholinergic overstimulation with soman.

Toxicol Lett 2018 Nov 27;297:19-23. Epub 2018 Aug 27.

Experimental Anesthesiology Section, Department of Anesthesiology and Intensive Care Medicine, Eberhard-Karls-University, Waldhoernlestrasse 22, 72072 Tuebingen, Germany. Electronic address:

Intoxication with organophosphorus compounds can result in life-threatening organ dysfunction and refractory seizures. Sedation or hypnosis is essential to facilitate mechanical ventilation and control seizure activity. The range of indications for midazolam includes both hypnosis and seizure control. Read More

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http://dx.doi.org/10.1016/j.toxlet.2018.08.016DOI Listing
November 2018
25 Reads
3.262 Impact Factor

Acute and long-term consequences of exposure to organophosphate nerve agents in humans.

Epilepsia 2018 Oct 29;59 Suppl 2:92-99. Epub 2018 Aug 29.

Department of Neurology and Program in Neuroscience, Uniformed Services University of the Health Sciences, Bethesda, MD, USA.

Nerve agents are organophosphate (OP) compounds and among the most powerful poisons known to man. A terrorist attack on civilian or military populations causing mass casualties is a real threat. The OP nerve agents include soman, sarin, cyclosarin, tabun, and VX. Read More

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http://dx.doi.org/10.1111/epi.14500DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6172147PMC
October 2018
27 Reads

Catatonia After Liver Transplantation.

Ann Transplant 2018 Aug 28;23:608-614. Epub 2018 Aug 28.

Department of Surgery, Division of Abdominal Transplant, University of North Carolina at Chapel Hill School of Medicine, Chapel Hill, NC, USA.

BACKGROUND Central nervous system complications after transplantation occur in up to 40% of recipients and these complications are associated with increased length of hospital stay and mortality. Catatonia is a neuropsychiatric clinical syndrome which has been described in case reports and in a small case series as occurring in the immediate post-solid organ transplantation (SOT) period, and it has been attributed to calcineurin inhibitor neurotoxicity, psychological vulnerability, and depression. Among transplant recipients, the incidence of catatonia is unknown; it may be under diagnosed in part due to a broad differential diagnosis in the post-transplantation setting, which includes hypoactive delirium, non-convulsive status epilepticus, drug toxicity, conversion disorder, and volitional uncooperativeness. Read More

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https://www.annalsoftransplantation.com/abstract/index/idArt
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http://dx.doi.org/10.12659/AOT.910298DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6248284PMC
August 2018
8 Reads

Detection of the designer benzodiazepine flunitrazolam in urine and preliminary data on its metabolism.

Drug Test Anal 2018 Aug 14. Epub 2018 Aug 14.

Institut de médecine légale, Strasbourg, France.

Designer benzodiazepines have emerged as recreational drugs. They are available via the Internet without control and are found in the form of falsified (fake) medicines. For some of them, limited information concerning their effects, their toxicity, and their detection in bio fluids is available in the literature. Read More

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http://dx.doi.org/10.1002/dta.2480DOI Listing
August 2018
17 Reads

Comparing the contribution of prescribed opioids to opioid-related hospitalizations across Canada: A multi-jurisdictional cross-sectional study.

Drug Alcohol Depend 2018 10 31;191:86-90. Epub 2018 Jul 31.

Institute for Clinical Evaluative Sciences, 2075 Bayview Ave, Toronto, Ontario M4N 3M5, Canada; Department of Medicine at the University of Toronto, 1 King's College Circle, Medical Sciences Building, Toronto, Ontario M5S 1A8, Canada.

Background: The Canadian opioid crisis is a complex, multifaceted problem involving prescribed, diverted and illicitly manufactured opioids. This study sought to characterize the contribution of prescribed opioids to opioid-related hospitalizations in Canada.

Methods: We conducted a cross-sectional study of all individuals who were admitted to hospital for opioid toxicity in British Columbia (BC), Manitoba and Ontario between April 2015 and March 2016. Read More

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http://dx.doi.org/10.1016/j.drugalcdep.2018.06.028DOI Listing
October 2018
5 Reads
3.423 Impact Factor

Harms associated with extramedical use of prescription opioid analgesics in Australia: A scoping review.

Res Social Adm Pharm 2018 Jul 3. Epub 2018 Jul 3.

Centre for Medicine Use and Safety, Faculty of Pharmacy and Pharmaceutical Sciences, Monash University, Melbourne, Australia; School of Public Health and Preventive Medicine, Faculty of Medicine, Nursing and Health Sciences, Monash University, Melbourne, Australia; School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, Australia.

Background: Evidence is accumulating globally on harms from extramedical prescription opioid analgesic (POA) use.

Objective: The aim of this scoping review was to explore harms and documented risk factors associated with extramedical POA use in Australia.

Methods: MEDLINE, EMBASE, PsycINFO and CINAHL were searched for original studies published between January 2000 and February 2018. Read More

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http://dx.doi.org/10.1016/j.sapharm.2018.07.001DOI Listing
July 2018
3 Reads

Toxicity of muscimol and ibotenic acid containing mushrooms reported to a regional poison control center from 2002-2016.

Clin Toxicol (Phila) 2018 Aug 3:1-5. Epub 2018 Aug 3.

a Department of Emergency Medicine , Oregon Health and Science University , Portland , OR , USA.

Background: Amanita muscaria (AM) and A. pantherina (AP) contain ibotenic acid and muscimol and may cause both excitatory and sedating symptoms. Gastrointestinal (GI) symptoms are not classically described but have been reported. Read More

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http://dx.doi.org/10.1080/15563650.2018.1497169DOI Listing
August 2018
1 Read

Characteristics of Tianeptine Exposures Reported to the National Poison Data System - United States, 2000-2017.

MMWR Morb Mortal Wkly Rep 2018 Aug 3;67(30):815-818. Epub 2018 Aug 3.

Tianeptine (marketed as Coaxil or Stablon) is an atypical tricyclic drug used as an antidepressant in Europe, Asia, and Latin America. In the United States, tianeptine is not approved by the Food and Drug Administration (FDA) for medical use and is an unscheduled pharmaceutical agent* (1). Animal and human studies show that tianeptine is an opioid receptor agonist (2). Read More

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http://dx.doi.org/10.15585/mmwr.mm6730a2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072055PMC
August 2018
7 Reads

Concurrent Use of Benzodiazepine by Heroin Users-What Are the Prevalence and the Risks Associated with This Pattern of Use?

J Med Toxicol 2019 Jan 31;15(1):4-11. Epub 2018 Jul 31.

Clinical Toxicology, Guy's and St Thomas' NHS Foundation Trust and King's Health Partners, London, UK.

Introduction: Polydrug use involving heroin and benzodiazepines is common. The potential risk of additive pharmacological effects may be associated with poorer outcomes in patients who use benzodiazepines together with heroin. The aim of this study was to determine the clinical picture of patients presenting to the emergency department following acute drug toxicity involving heroin and benzodiazepines. Read More

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http://dx.doi.org/10.1007/s13181-018-0674-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6314928PMC
January 2019
3 Reads

Serotonin Syndrome in the Perioperative Setting.

Am J Case Rep 2018 Jul 16;19:833-835. Epub 2018 Jul 16.

Department of Anesthesiology and Perioperative Medicine, Mayo Clinic, Rochester, MN, USA.

BACKGROUND Serotonin syndrome is a life-threatening condition that can lead to neurologic complications and is associated with the use of serotonergic medications. As the use of antidepressant medications has increased, the incidence of perioperative serotonin syndrome has transitioned from a rare diagnosis to one that should be considered as a differential diagnosis for any patient displaying signs of neuroexcitation. CASE REPORT A 70-year-old man (ASA 2) with a history of vestibular migraines (treated with venlafaxine), gastroesophageal reflux disease, and benign prostatic hyperplasia presented to our institution for photoselective vaporization of the prostate. Read More

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http://dx.doi.org/10.12659/AJCR.909497DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6061453PMC
July 2018
14 Reads

Risks of fatal opioid overdose during the first year following nonfatal overdose.

Drug Alcohol Depend 2018 09 4;190:112-119. Epub 2018 Jul 4.

National Institute on Drug Abuse, Division of Epidemiology, Services, and Prevention Research, Rockville, MD, USA.

Background: Little is known about risk factors for repeated opioid overdose and fatal opioid overdose in the first year following nonfatal opioid overdose.

Methods: We identified a national retrospective longitudinal cohort of patients aged 18-64 years in the Medicaid program who received a clinical diagnosis of nonfatal opioid overdose. Repeated overdoses and fatal opioid overdoses were measured with the Medicaid record and the National Death Index. Read More

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http://dx.doi.org/10.1016/j.drugalcdep.2018.06.004DOI Listing
September 2018
13 Reads

Sociodemographic factors, prescription history and opioid overdose deaths: a statewide analysis using linked PDMP and mortality data.

Drug Alcohol Depend 2018 09 13;190:62-71. Epub 2018 Jun 13.

Tennessee Department of Health, Office of Informatics and Analytics, Andrew Johnson Tower, 7th Floor, 710 James Robertson Parkway, Nashville, TN, 37243, United States; Department of Health Policy, Vanderbilt University Medical Center, 2525 West End Ave, Suite 1200, Nashville, TN, 37203, United States.

Background: Opioid overdose deaths have continued to rise in Tennessee (TN) with fentanyl emerging as a major contributor. Current data are needed to identify at-risk populations to guide prevention strategies. We conducted a large statewide observational study among TN adult decedents (2013-2016) to evaluate the association of sociodemographic factors and prescribing patterns with opioid overdose deaths. Read More

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http://dx.doi.org/10.1016/j.drugalcdep.2018.05.004DOI Listing
September 2018
9 Reads

A Case Study Involving U-47700, Diclazepam and Flubromazepam-Application of Retrospective Analysis of HRMS Data.

J Anal Toxicol 2018 Nov;42(9):655-660

Forensic Science SA (Toxicology), Adelaide, South Australia, Australia.

The number of new psychoactive substances (NPS) available is constantly increasing, making it difficult for toxicology laboratories to keep screening methods up to date. Full scan high-resolution mass spectrometry (HRMS) is a versatile technique which allows for progressive updating of spectral databases to increase the scope of screening. It also allows for retrospective screening of data-specifically, reprocessing of data files using an updated spectral database without the need for re-extraction or reanalysis. Read More

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http://dx.doi.org/10.1093/jat/bky039DOI Listing
November 2018
11 Reads

Acetyl Fentanyl: Trends and Concentrations in Metro Detroit.

J Forensic Sci 2019 Jan 25;64(1):149-153. Epub 2018 Jun 25.

Michigan Medicine Department of Pathology/Wayne County Medical Examiner's Office, 1300 E Warren Ave, Detroit, MI, 48207.

Acetyl fentanyl (N-[1-phenethylpiperidin-4-yl]-N-phenylacetamide) is a potent opioid analgesic with no medicinal uses. We report deaths between 2016 and 2017 at the Medical Examiner's Office in Detroit, MI where acetyl fentanyl was found in the decedent's blood and compare them to previously published deaths between 2015 and 2016. The recent cases (cohort B) had a mean acetyl fentanyl concentration of 0. Read More

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http://dx.doi.org/10.1111/1556-4029.13840DOI Listing
January 2019
8 Reads

Successful intravenous lipid emulsion therapy: Olanzapine intoxication.

Acute Med 2018 ;17(2):96-97

Haseki Training and Research Hospital, Department of Emergency Medicine, Istanbul, Turkey.

Olanzapine is an antipsychotic drug used in psychiatric diseases. At high doses it exhibits cardiovascular and neurological sideeffects in particular. Lipid emulsion therapy for the removal of medication from plasma in high-dose lipophilic drug use has recently become very widespread. Read More

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October 2018
8 Reads

Influence of ethanol on the metabolism of alprazolam.

Expert Opin Drug Metab Toxicol 2018 Jun;14(6):551-559

a Department of Forensic Medicine, School of Basic Medical Sciences , Fudan University , Shanghai , China.

Background: Alprazolam is a commonly used benzodiazepine in clinical practice, and when coingested with ethanol, alprazolam can increase behavioral irritability and aggression. However, the mechanism of its interaction with ethanol remains unknown.

Research Design And Methods: The pharmacokinetics of alprazolam was studied in vivo in rat experiments involving the simultaneous administration of alprazolam and ethanol, and the interactions between ethanol and alprazolam were investigated in vitro in human liver microsomes. Read More

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http://dx.doi.org/10.1080/17425255.2018.1483338DOI Listing
June 2018
3 Reads

Synthesis and Pharmacological Valorization of Derivatives of 4-Phenyl-1,5-Benzodiazepin-2-One.

Adv Pharmacol Sci 2018 1;2018:6042602. Epub 2018 Apr 1.

PharmacodynamyResearch Team PRT, Laboratory of Pharmacology and Toxicology, Faculty of Medicine and Pharmacy, Mohammed V University, BP 6203, Rabat, Morocco.

The objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine as a hydrophilic head and a carbon chain as a hydrophobic tail. First, we studied the acute toxicity of the above mentioned 4-phenyl-1,5-benzodiazepin-2-one derivatives. This study was conducted according to OECD 423 guidelines in female mice and revealed that these compounds are nontoxic. Read More

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https://www.hindawi.com/journals/aps/2018/6042602/
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http://dx.doi.org/10.1155/2018/6042602DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5902104PMC
April 2018
23 Reads

Benzodiazepine-refractory status epilepticus, neuroinflammation, and interneuron neurodegeneration after acute organophosphate intoxication.

Biochim Biophys Acta Mol Basis Dis 2018 09 23;1864(9 Pt B):2845-2858. Epub 2018 May 23.

Department of Neuroscience and Experimental Therapeutics, Texas A&M University Health Science Center, College of Medicine, Bryan, TX 77807, USA. Electronic address:

Nerve agents and some pesticides such as diisopropylfluorophosphate (DFP) cause neurotoxic manifestations that include seizures and status epilepticus (SE), which are potentially lethal and carry long-term neurological morbidity. Current antidotes for organophosphate (OP) intoxication include atropine, 2-PAM and diazepam (a benzodiazepine for treating seizures and SE). There is some evidence for partial or complete loss of diazepam anticonvulsant efficacy when given 30 min or later after exposure to an OP; this condition is known as refractory SE. Read More

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http://dx.doi.org/10.1016/j.bbadis.2018.05.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6066461PMC
September 2018
5 Reads

Synthesis and Biological Evaluation of Novel 2,3-disubstituted Benzofuran Analogues of GABA as Neurotropic Agents.

Med Chem 2019 ;15(1):77-86

Escuela Superior de Medicina, Instituto Politecnico Nacional, Plan de San Luis y Díaz Mirón s/n Col. Casco de Santo Tomas, Del. Miguel Hidalgo, 11340, Mexico City, Mexico.

Background: Benzofurans are heterocyclic compounds with neurotropic activity. Some have been developed for the treatment of acute and degenerative neuronal injuries.

Objective: The study aimed to evaluate the in silico binding of some promising benzofurans on the GABA receptors, and the in vivo neurotropic activity of benzofuran analogues (BZF 6-10) of gamma-aminobutyric acid (GABA) on a seizure model. Read More

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http://dx.doi.org/10.2174/1573406414666180524091745DOI Listing
January 2019
6 Reads

Beneficial Outcome of Urethane Treatment Following Status Epilepticus in a Rat Organophosphorus Toxicity Model.

eNeuro 2018 Mar-Apr;5(2). Epub 2018 Apr 17.

Department of Pharmacology, Emory University, Atlanta, GA 30322.

The efficacy of benzodiazepines to terminate electrographic status epilepticus (SE) declines the longer a patient is in SE. Therefore, alternative methods for ensuring complete block of SE and refractory SE are necessary. We compared the ability of diazepam and a subanesthetic dose of urethane to terminate prolonged SE and mitigate subsequent pathologies. Read More

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http://eneuro.org/lookup/doi/10.1523/ENEURO.0070-18.2018
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http://dx.doi.org/10.1523/ENEURO.0070-18.2018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5952304PMC
January 2019
6 Reads

Tramadol: Understanding the Risk of Serotonin Syndrome and Seizures.

Am J Med 2018 Nov 10;131(11):1382.e1-1382.e6. Epub 2018 May 10.

Department of Psychiatry and Behavioral Neurosciences, Cedars-Sinai Medical Center, Los Angeles, Calif.

Tramadol is commonly prescribed for pain control because it presents a lower risk for addiction and respiratory depression compared to other opioids. However, tramadol's serotonin and norepinephrine reuptake inhibitory effects result in a unique adverse effect profile. Two such adverse events are serotonin syndrome and seizures. Read More

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http://dx.doi.org/10.1016/j.amjmed.2018.04.025DOI Listing
November 2018
2 Reads

Pathophysiological investigations, anxiolytic effects and interaction of a semisynthetic riparin with benzodiazepine receptors.

Biomed Pharmacother 2018 Jul 25;103:973-981. Epub 2018 Apr 25.

Postgraduate Program in Biotechnology, Federal University of Piauí, Teresina, Piauí, Brazil; Department of Chemistry, Laboratory of Computational Quantum Chemistry and Drug Planning Laboratory, State University of Piauí, Teresina, Piauí, Brazil.

We have reported Riparin A as a promising antiparasitic molecule ​​against Leishmania amazonensis promastigotes. This work evaluated the acute oral toxicity of Riparin A and its anxiolytic effects using in vivo models and computational tools. Mice were submitted to acute oral toxicity tests (Guideline OECD 423). Read More

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http://dx.doi.org/10.1016/j.biopha.2018.04.130DOI Listing
July 2018
5 Reads

Polypharmacy and patterns of prescription medication use among cancer survivors.

Cancer 2018 Jul 12;124(13):2850-2857. Epub 2018 Apr 12.

Department of Clinical Sciences, University of Texas Southwestern Medical Center, Dallas, Texas.

Background: The population of cancer survivors is rapidly growing in the United States. Long-term and late effects of cancer, combined with the ongoing management of other chronic conditions, make survivors particularly vulnerable to polypharmacy and its adverse effects. In the current study, the authors examined patterns of prescription medication use and polypharmacy in a population-based sample of cancer survivors. Read More

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http://dx.doi.org/10.1002/cncr.31389DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6147245PMC
July 2018
6 Reads

Propofol: a safe anaesthetic drug in experimental cardiac surgery in rabbits.

Ann Ital Chir 2018 ;89:92-94

Ackground: Experimental surgery needs a pharmacological approach that can interfere with cardiac function.

Case Report: In a animal model of regenerative medicine of myocardium we use an anaesthesiological protocol that included Propofol, a benzodiazepine (Midazolam) and an alpha-2 adrenergic agent.

Results: In a group of 15 rabbits undergoing cardiac surgery we reported 1 arrhythmic complication during stem cell injection. Read More

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November 2018
12 Reads

Does high-dose benzodiazepine abuse really produce liver toxicity? Results from a series of 201 benzodiazepine monoabusers.

Expert Opin Drug Saf 2018 May 6;17(5):451-456. Epub 2018 Apr 6.

c Department of Internal Medicine, Gastroenterology and Hepatology , Catholic University of Rome , Rome , Italy.

Background: Several side-effects related to prolonged benzodiazepines (BZD) use have been reported. Given the primary role of liver in BZD metabolism, toxicity related to prolonged high-dose BZD use could be conceivable. No data are available on the long-term impact of high-dose BZD use on liver. Read More

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http://dx.doi.org/10.1080/14740338.2018.1457646DOI Listing
May 2018
14 Reads

Cytochrome P450-dependent drug oxidation activities in commercially available hepatocytes derived from human induced pluripotent stem cells cultured for 3 weeks.

J Toxicol Sci 2018 ;43(4):241-245

Hepatocyte-like cells differentiated from human induced pluripotent stem (iPS) cells are of great interest for applications in pharmacological research. For drug metabolism testing, commercially available hepatocytes derived from human iPS cells are generally recommended to be used 1 week after seeding on plates. In this study, however, after 3-4 weeks of culture according to the manufacturer's instructions, human cytochrome P450 (P450) 2C9- and 2C19-dependent diclofenac 4'-hydroxylation and omeprazole 5-hydroxylation activities of the iPS-derived hepatocytes had significantly increased above the activities at 1 week and had reached levels similar to those in HepaRG cells, a human hepatocyte-like cell line. Read More

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http://dx.doi.org/10.2131/jts.43.241DOI Listing
August 2018
4 Reads

The care of patients using methamphetamine in the emergency department: Perception of nurses, residents, and faculty.

Subst Abus 2018 Mar 29:1-7. Epub 2018 Mar 29.

a Department of Emergency Medicine , University of California Davis Medical Center , Sacramento , California , USA.

Background: To determine differences in perception between nurses, residents, and faculty regarding characteristics and treatment of patients who use methamphetamine (meth).

Methods: Survey study performed at an urban, university Level I trauma medical center.

Results: A total of 80 nurses, 39 residents, and 45 faculty completed the survey. Read More

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http://dx.doi.org/10.1080/08897077.2018.1449170DOI Listing
March 2018
2 Reads

Effects of isopentyl ferulate on oxidative stress biomarkers and a possible GABAergic anxiolytic-like trait in Swiss mice.

Chem Biol Interact 2018 Jun 20;289:119-128. Epub 2018 Mar 20.

Postgraduate Program in Pharmacology, Federal University of Piauí, Teresina, Piauí, 64.049-550, Brazil; Laboratory of Research in Experimental Neurochemistry of Postgraduate Program in Pharmaceutical Sciences, Federal University of Piauí, Teresina, Piauí, 64.049-550, Brazil.

This study aimed to evaluate the anxiolytic-like effect and the possible neuronal mechanism of action of isopentyl ferulate (IF). For this purpose, we used the marble burying test in Swiss albino mice. The biomarkers involved in oxidative stress were measured in the hippocampus homogenate of the test animals. Read More

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http://dx.doi.org/10.1016/j.cbi.2018.03.009DOI Listing
June 2018
4 Reads

Cannabinoid Hyperemesis Syndrome: Public Health Implications and a Novel Model Treatment Guideline.

West J Emerg Med 2018 Mar 8;19(2):380-386. Epub 2017 Nov 8.

University of California, San Diego, Department of Emergency Medicine, San Diego, California.

Introduction: Cannabinoid hyperemesis syndrome (CHS) is an entity associated with cannabinoid overuse. CHS typically presents with cyclical vomiting, diffuse abdominal pain, and relief with hot showers. Patients often present to the emergency department (ED) repeatedly and undergo extensive evaluations including laboratory examination, advanced imaging, and in some cases unnecessary procedures. Read More

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http://dx.doi.org/10.5811/westjem.2017.11.36368DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5851514PMC
March 2018
11 Reads

Differentiating Pathway-Specific From Nonspecific Effects in High-Throughput Toxicity Data: A Foundation for Prioritizing Adverse Outcome Pathway Development.

Toxicol Sci 2018 Jun;163(2):500-515

U.S. EPA National Health and Environmental Effects Research Laboratory, Mid-Continent Ecology Division, 6201 Congdon Blvd, Duluth, MN 55804.

The U.S. Environmental Protection Agency's ToxCast program has screened thousands of chemicals for biological activity, primarily using high-throughput in vitro bioassays. Read More

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http://dx.doi.org/10.1093/toxsci/kfy049DOI Listing
June 2018
27 Reads

Overdoses and Substance Toxicity in Patients Admitted to Intensive Care Units in a Midwestern U.S. City.

J Trauma Nurs 2018 Mar/Apr;25(2):87-91

Internal Medicine Residency Program, University of Iowa-Des Moines (Drs Schuring, Dodge, Whitcomb, Wall, and Smith); College of Pharmacy and Health Sciences, Drake University, Des Moines, Iowa (Dr Wall); and Pulmonary and Critical Care Medicine, The Iowa Clinic, Des Moines, Iowa (Dr Hicklin).

Toxic exposures with serious outcomes have increased over the last decade. Limited data exists on the pattern and outcomes of overdose-exposure patients requiring intensive care unit (ICU) admission. The primary objective of this study was to characterize the causes, treatments, and outcomes of toxic exposures in a mid-sized Midwestern health system. Read More

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http://dx.doi.org/10.1097/JTN.0000000000000349DOI Listing
September 2018
8 Reads