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Benzodiazepines

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https://www.readbyqxmd.com/read/29236387/effect-of-3-substituted-1-4-benzodiazepin-2-ones-on-bradykinin-induced-smooth-muscle-contraction
#1
P A Virych, O V Shelyuk, T A Kabanova, E I Khalimova, V S Martynyuk, V I Pavlovsky, S A Andronati
Biochemical properties of 3-substituted 1,4-benzodiazepine determined by the characteristics of their chemical structure. Influence of 3-substituted 1,4-benzodiazepin-2-ones on maximal normalized rate and amplitudes of isometric smooth muscle contraction in rats was investigated. Compounds MX-1775 and MX-1828 demonstrated the similar inhibition effect on bradykinin-induced contraction of smooth muscle like competitive inhibitor des-arg9-bradykinin-acetate to bradykinin B2-receptors. MX-1626 demonstrated unidirectional changes of maximal normalized rate and force of smooth muscle that proportionally depended on bradykinin concentration in the range 10-10-10-6 M...
January 2017: Ukrainian Biochemical Journal
https://www.readbyqxmd.com/read/29236349/direct-and-enantioselective-synthesis-of-n-h-free-1-5-benzodiazepin-2-ones-via-nhc-catalyzed-3-4-annulation-reaction
#2
Ding Du, Jing Cao, Chao Fang, Kewen Sun, Jindong Zhu, Tao Lu
An NHC-catalyzed formal [3+4] annulation of alfa,beta-unsaturated acylazoliums with protecting group-free aryl 1,2-diamines was developed for a direct and highly enantioselective synthesis of 4-aryl N-H-free 1,5-benzodiazepin-2-ones. This methodology offers an efficient and rapid access to a wide range of enantioenriched target compounds from easily accessible starting materials. The protocol is also scalable and the desired products can easily undergo subsequent N-functionalization to afford diverse N-substituted derivatives...
December 13, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29235430/prevalence-and-risk-factors-for-delirium-diagnosis-in-patients-followed-in-general-practices-in-germany
#3
Jens Bohlken, Karel Kostev
BACKGROUND: The aim of this study is to identify the prevalence and risk factors of documented delirium in general practices in Germany. METHODS: The present study includes 2,194 patients over the age of 65 years with delirium and 2,194 controls without delirium from a sample of 6,180,042 patients from 1,262 general practices. Multivariate logistic regression models were fitted with delirium as a dependent variable and other disorders and drugs as potential predictors...
December 13, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29230398/insulin-signaling-deficiency-produces-immobility-in-caenorhabditis-elegans-that-models-diminished-motivation-states-in-man-and-responds-to-antidepressants
#4
Julie Dagenhardt, Angeline Trinh, Halen Sumner, Jeffrey Scott, Eric Aamodt, Donard S Dwyer
Defects in insulin signaling have been reported in schizophrenia and major depressive disorder, which also share certain negative symptoms such as avolition, anhedonia, and apathy. These symptoms reflect diminished motivational states, which have been modeled in rodents as increased immobility in the forced swimming test. We have discovered that loss-of-function mutations in the insulin receptor (daf-2) and syntaxin (unc-64) genes in Caenorhabditis elegans, brief food deprivation, and exposure to DMSO produce immobility and avolition in non-dauer adults...
November 2017: Molecular Neuropsychiatry
https://www.readbyqxmd.com/read/29227934/gabaa-receptor-activity-modulating-piperine-analogs-in-vitro-metabolic-stability-metabolite-identification-cyp450-reaction-phenotyping-and-protein-binding
#5
Volha Zabela, Timm Hettich, Götz Schlotterbeck, Laurin Wimmer, Marko D Mihovilovic, Fabrice Guillet, Belkacem Bouaita, Bénédicte Shevchenko, Matthias Hamburger, Mouhssin Oufir
In a screening of natural products for allosteric modulators of GABAA receptors (γ-aminobutyric acid type A receptor), piperine was identified as a compound targeting a benzodiazepine-independent binding site. Given that piperine is also an activator of TRPV1 (transient receptor potential vanilloid type 1) receptors involved in pain signaling and thermoregulation, a series of piperine analogs were prepared in several cycles of structural optimization, with the aim of separating GABAA and TRPV1 activating properties...
December 2, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29227519/pediatric-poisoning-by-ingestion-developmental-overview-and-synopsis-of-national-trends
#6
Vincent R Lee, Michael Connolly, Diane P Calello
The American Association of Poison Control Centers' National Poison Data Surveillance System provides real-time toxico-surveillance and epidemiologic trends, and pediatric ingestions comprise most of those reports. The sequences in social and physical developmental milestones from young childhood to adolescence reveal the vulnerability of these age groups to a wide variety of potential poisonous ingestions. Most pediatric ingestions are exploratory. Some common agents associated with pediatric fatalities include disc batteries, laundry detergent "pods," opioid analgesics, acetaminophen, benzodiazepines, and amphetamines...
December 1, 2017: Pediatric Annals
https://www.readbyqxmd.com/read/29227273/-poisoning-by-psychopharmacological-drugs-in-azerbaijan-the-results-of-8-year-prospective-observation
#7
I Afandiyev, V Azizov
Acute poisoning of chemical etiology is a significant global public health problem. The aim of this study was the analysis of the toxicoepidemiological structure of psychopharmacological drugs poisoning in Azerbaijan. We collected and analyzed the data on all cases of acute poisoning by psychopharmacological drugs (codes of categories T42/T43 ICD-10) undergoing inpatient treatment at the Center of Clinical Toxicology in Baku, Azerbaijan in 2009-2016. The total number of patients with acute intoxication by psychopharmacological drugs was 3,413, which was 48...
November 2017: Georgian Medical News
https://www.readbyqxmd.com/read/29227118/complex-suicide-involving-pyrethroid-ingestion-mosquito-coils-and-fatal-self-wounding-by-sharp-force
#8
Maria -Valeria Karakasi, Pavlos Pavlidis, Epameinondas Vasilikos, Doxakis Anestakis, Nikolaos Raikos
"Complex suicide" is a term referring to the suicidal pattern in which more than one suicidal method is applied in the purpose of inducing death. The present paper aims to review complex suicide literature shortly and investigate an unusual planned complex suicide incident, the rarity of which is attributable to the combination of suicide methods as well as the type and quantity of substances applied to induce poisoning. A 33-year-old man with a history of psychotic depression was found dead in his bedroom lying within a large quantity of blood...
2017: Soudní Lékarství
https://www.readbyqxmd.com/read/29227117/an-autopsy-case-of-death-by-combined-use-of-benzodiazepines-and-diphenidine
#9
Hiroshi Kinoshita, Naoko Tanaka, Ayaka Takakura, Hiroko Abe, Mitsuru Kumihashi, Takayuki Shibayama, Mostofa Jamal, Asuka Ito, Kunihiko Tsutsui, Shoji Kimura, Hirotaro Iwase, Kiyoshi Ameno
We present an autopsy case involving benzodiazepines and diphenidine. Quantitative toxicological analysis showed concentrations of 7-aminoflunitrazepam (a flunitrazepam metabolite), 7-aminonimetazepam (a nimetazepam metabolite), chlorpheniramine and diphenidine in femoral blood of 0.086 µg/ml, 0.027 µg/ml, 0.066 µg/ml, and 0.073 µg/ml, respectively. Death was attributed to combined toxicity due to the influence of multiple drug interactions.
2017: Soudní Lékarství
https://www.readbyqxmd.com/read/29226017/buprenorphine-for-medication-assisted-treatment-of-opioid-use-disorder-in-pregnancy-relationship-to-neonatal-opioid-withdrawal-syndrome
#10
Niraj R Chavan, Kristin B Ashford, Amanda T Wiggins, Michelle R Lofwall, Agatha S Critchfield
Objective  To examine the relationship between antepartum buprenorphine dose for medication-assisted treatment (MAT) of opioid use disorder (OUD) and incident neonatal opioid withdrawal syndrome (NOWS). Study Design  We performed a prospective cohort study of pregnant women with a singleton gestation diagnosed with OUD and receiving buprenorphine for MAT at a tertiary care academic institution from July 2015 to January 2017. We divided the study cohort into two groups-pregnancies with versus without NOWS...
October 2017: American Journal of Perinatology Reports
https://www.readbyqxmd.com/read/29225747/a-prospective-randomized-controlled-double-blind-trial-to-assess-the-effects-of-dexmedetomidine-during-cleft-palate-surgery
#11
Priyanka Surana, Devangi A Parikh, Geeta A Patkar, Bharati A Tendolkar
Background: We investigated whether the intraoperative administration of dexmedetomidine would attenuate the profound sympathoadrenal response associated with cleft palate (CP) surgery. Methods: Sixty children aged 6 months to 12 years undergoing CP surgery under general anesthesia were randomly assigned to the control (C) or dexmedetomidine (D) groups. Group C received benzodiazepine (0.05 mg/kg midazolam followed by infusion of normal saline) fentanyl isoflurane anesthesia, and Group D received dexmedetomidine (loading 1 µg/kg followed by infusion of 0...
December 2017: Korean Journal of Anesthesiology
https://www.readbyqxmd.com/read/29225045/post-reexposure-administration-of-riluzole-attenuates-the-reconsolidation-of-conditioned-fear-memory-in-rats
#12
Kie Akagi, Misa Yamada, Akiyoshi Saitoh, Jun-Ichiro Oka, Mitsuhiko Yamada
Recently, we demonstrated that riluzole, which has been shown to block the glutamatergic system, facilitates fear extinction in rats. Here, we undertook experiments on contextual fear conditioning to clarify the actions of riluzole on the reconsolidation of fear memory in rats. We used the fast-acting benzodiazepine midazolam as a reconsolidation-inhibiting control drug. We demonstrated that riluzole (3 mg/kg) and midazolam (1 mg/kg) impaired the reconsolidation of contextual fear memory. Results from spontaneous recovery experiments also suggested that riluzole attenuated reconsolidation...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29224571/-worried-to-death-the-assessment-and-management-of-anxiety-in-patients-with-advanced-life-limiting-disease-a-national-survey-of-palliative-medicine-physicians
#13
N Atkin, V Vickerstaff, B Candy
BACKGROUND: Anxiety adversely affects quality of life and is common in adults with advanced life-limiting disease. There are no UK-wide guidelines on the assessment and management of anxiety in this specific population and there is little evidence regarding drug treatments. This study aimed to explore how palliative care physicians assess and manage anxiety in their patients, and to identify barriers encountered. METHODS: A cross-sectional survey was undertaken of all physicians working in specialist palliative care in the UK who were members of the Association for Palliative Medicine...
December 11, 2017: BMC Palliative Care
https://www.readbyqxmd.com/read/29224234/an-observational-study-of-benzodiazepine-prescription-during-inpatient-alcohol-detoxification-for-patients-with-versus-without-chronic-pretreatment-with-high-dosage-baclofen
#14
Laura Martinez, Florence Vorspan, Xavier Declèves, Julien Azuar, Maeva Fortias, Franck Questel, Alexandra Dereux, Leslie Grichy, Hélène Barreteau, Frank Bellivier, Jean-Pierre Lépine, Vanessa Bloch
High dose baclofen is prescribed as a maintenance treatment to reduce alcohol use in patients with alcohol use disorder. Nevertheless, some patients still have massive alcohol intakes and require inpatient alcohol withdrawal. AIM: to compare the oral dose of benzodiazepine prescribed to manage alcohol withdrawal symptoms in patients with versus without steady state pre-treatment with high dose baclofen. METHODS: Retrospective chart review study. Prescribed benzodiazepine dose expressed in diazepam-equivalent was compared between groups...
December 10, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29223863/what-can-predict-and-prevent-the-long-term-use-of-benzodiazepines
#15
Takeo Hata, Tetsufumi Kanazawa, Takeshi Hamada, Masami Nishihara, Ashley Ian Bush, Hiroshi Yoneda, Miki Nakajima, Takahiro Katsumata
Although benzodiazepines (BZDs) are commonly prescribed for insomnia or anxiety, long-term use of BZDs causes serious adverse effects such as daytime drowsiness and cognitive decline. In the current study, we evaluated the predictors and preventers of long-term usage of BZDs from a retrospective survey by utilizing the 12-year prescription record of a university hospital. From the prescription data of 92,005 people, users of BZDs (n = 3,470, male = 39.2%, mean age = 60 ± 17.5) were analyzed. During this period, both the number of prescriptions (2722 in 2004 to 1019 in 2016) and the number of BZDs (1...
November 24, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/29223805/development-of-pyrrolo-2-1-c-1-4-benzodiazepine-%C3%AE-glucoside-prodrugs-for-selective-therapy-of-cancer
#16
Praveen Reddy Adiyala, Venkatesh Tekumalla, Ibrahim Bin Sayeed, V Lakshma Nayak, Apoorva Nagarajan, Mohd Adil Shareef, Burri Nagaraju, Ahmed Kamal
Cancer chemotherapy has several limitations such as often insufficient differentiation between malign tissue and benign tissue. The clinical utility of the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are inadequate because of the lack of selectivity for tumor tissues, high reactivity of the pharmacophoric imine functionality, low water solubility, and stability. To address these limitations two new β-glucoside prodrugs of PBDs have been synthesized and evaluated for their potential use in selective therapy of solid tumors by ADEPT...
December 7, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29223172/association-between-the-use-of-benzodiazepines-and-opioids-with-the-risk-of-falls-and-hip-fractures-in-older-adults
#17
Manuel E Machado-Duque, Juan Pablo Castaño-Montoya, Diego A Medina-Morales, Alejandro Castro-Rodríguez, Alexandra González-Montoya, Jorge E Machado-Alba
BACKGROUND: To determine the association between the use of opioids and benzodiazepines and the risk of falls with hip fracture in populations older than 65 years in Colombia. METHODS: A case-control study with patients older than 65 years with diagnosis of hip fracture. Two controls were obtained per case. The drugs dispensed in the previous 30 days were identified. Sociodemographic, diagnostic, pharmacological (opioids and benzodiazepines), and polypharmacy variables were analyzed...
December 10, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29219171/benzodiazepines-for-psychosis-induced-aggression-or-agitation
#18
REVIEW
Hadar Zaman, Stephanie J Sampson, Alison Ls Beck, Tarang Sharma, Fiona J Clay, Styliani Spyridi, Sai Zhao, Donna Gillies
BACKGROUND: Acute psychotic illness, especially when associated with agitated or violent behaviour, can require urgent pharmacological tranquillisation or sedation. In several countries, clinicians often use benzodiazepines (either alone or in combination with antipsychotics) for this outcome. OBJECTIVES: To examine whether benzodiazepines, alone or in combination with other pharmacological agents, is an effective treatment for psychosis-induced aggression or agitation when compared with placebo, other pharmacological agents (alone or in combination) or non-pharmacological approaches...
December 8, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29219048/sodium-oxybate-therapy-for-the-treatment-of-alcohol-withdrawal-syndrome-and-the-maintenance-of-alcohol-abstinence
#19
Carmen Mannucci, Simona Pichini, Elvira Ventura Spagnolo, Fabrizio Calapai, Sebastiano Gangemi, Michele Navarra, Gioacchino Calapai
BACKGROUND: Gamma-hydroxybutyrate (GHB or sodium oxybate) is both an exogenous and endogenous molecule with neuromodulator properties. In the United States, GHB is an approved drug for the treatment of narcolepsy and narcolepsy with cataplexy in adults. In some European Union countries, sodium oxybate is applied for the treatment of opioid and alcohol withdrawal. OBJECTIVE: The aim of the present review was to describe the state of art of the pre-clinical research and the clinical evidence related to GHB used alone or in combination with other treatments in alcohol withdrawal syndrome and alcohol abstinence maintenance...
December 7, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/29217165/anxiolytic-and-antidepressant-like-activities-of-a-methanolic-extract-of-morinda-citrifolia-linn-noni-fruit-in-mice-involvement-of-benzodiazepine-gabaaergic-serotonergic-and-adrenergic-systems
#20
Megala Narasingam, Kamini Vijeepallam, Zahurin Mohamed, Vijayapandi Pandy
This study presents anxiolytic- and antidepressant-like effects of a methanolic extract of Morinda citrifolia Linn. (noni) fruit (MMC) in well-established mouse models of anxiety and depression. The administration of MMC (1 g/kg, p.o.) and diazepam (1 mg/kg, i.p.) significantly attenuated anxiety-like behaviour in mice by increasing the percentage of time spent and number of entries in the open arms in the elevated plus maze (EPM), and significantly enhanced the exploration in the light box in the light/dark test (LDT)...
December 4, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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