benzodiazepines

Summary

Summary: A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring. Permitted is any degree of hydrogenation, any substituents and any H-isomer.

Top Publications

  1. ncbi Clinical factors influencing the prescription of antidepressants and benzodiazepines: results from the European study of the epidemiology of mental disorders (ESEMeD)
    Koen Demyttenaere
    Department of Psychiatry, University Hospital Gasthuisberg, Leuven, Belgium
    J Affect Disord 110:84-93. 2008
  2. ncbi Effectiveness of antipsychotic drugs in patients with chronic schizophrenia
    Jeffrey A Lieberman
    Department of Psychiatry, College of Physicians and Surgeons, Columbia University, New York State Psychiatric Institute, New York, NY 10032, USA
    N Engl J Med 353:1209-23. 2005
  3. pmc Head-to-head comparisons of metabolic side effects of second generation antipsychotics in the treatment of schizophrenia: a systematic review and meta-analysis
    Christine Rummel-Kluge
    Klinik und Poliklinik fur Psychiatrie und Psychotherapie der Technischen Universitat Munchen, Klinikum rechts der Isar, Möhlstr 26, 81675 Munchen, Germany
    Schizophr Res 123:225-33. 2010
  4. pmc Benzodiazepine use and risk of dementia: prospective population based study
    Sophie Billioti de Gage
    Université Bordeaux Segalen, F 33000 Bordeaux, France
    BMJ 345:e6231. 2012
  5. ncbi Discovery and characterization of small molecule inhibitors of the BET family bromodomains
    Chun wa Chung
    Molecular Discovery Research, GlaxoSmithKline R and D, Stevenage SG5 4HT, UK
    J Med Chem 54:3827-38. 2011
  6. ncbi Effects of anxiolytics in zebrafish: similarities and differences between benzodiazepines, buspirone and ethanol
    Daiane L Gebauer
    Laboratório de Neuroquímica e Psicofarmacologia, Departamento de Biologia Celular e Molecular, Programa de Pós Graduação em Biologia Celular e Molecular, Faculdade de Biociencias, Pontificia Universidade Catolica do Rio Grande do Sul, Avenida Ipiranga, 6681, 90619 900 Porto Alegre, RS, Brazil
    Pharmacol Biochem Behav 99:480-6. 2011
  7. ncbi Benzodiazepines revisited--will we ever learn?
    Malcolm Lader
    Addiction Research Centre, Institute of Psychiatry, King s College London, London, UK
    Addiction 106:2086-109. 2011
  8. ncbi Safety of benzodiazepines in the geriatric population
    Subramoniam Madhusoodanan
    Department of Psychiatry, St John s Episcopal Hospital, South Shore, 327 Beach 19th Street, Far Rockaway, New York, USA
    Expert Opin Drug Saf 3:485-93. 2004
  9. ncbi A 3-week, randomized, placebo-controlled trial of asenapine in the treatment of acute mania in bipolar mania and mixed states
    Roger S McIntyre
    Department of Psychiatry and Pharmacology, University of Toronto, Toronto, ON, Canada
    Bipolar Disord 11:673-86. 2009
  10. pmc Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes
    Uwe Rudolph
    Laboratory of Genetic Neuropharmacology, McLean Hospital and Department of Psychiatry, Harvard Medical School, Belmont, Massachusetts 02478, USA urudolph mclean harvard edu
    Nat Rev Drug Discov 10:685-97. 2011

Research Grants

Detail Information

Publications375 found, 100 shown here

  1. ncbi Clinical factors influencing the prescription of antidepressants and benzodiazepines: results from the European study of the epidemiology of mental disorders (ESEMeD)
    Koen Demyttenaere
    Department of Psychiatry, University Hospital Gasthuisberg, Leuven, Belgium
    J Affect Disord 110:84-93. 2008
    To examine factors associated with the use of antidepressants (AD) and benzodiazepines (BZD) in 6 European countries.
  2. ncbi Effectiveness of antipsychotic drugs in patients with chronic schizophrenia
    Jeffrey A Lieberman
    Department of Psychiatry, College of Physicians and Surgeons, Columbia University, New York State Psychiatric Institute, New York, NY 10032, USA
    N Engl J Med 353:1209-23. 2005
    ..We compared a first-generation antipsychotic, perphenazine, with several newer drugs in a double-blind study...
  3. pmc Head-to-head comparisons of metabolic side effects of second generation antipsychotics in the treatment of schizophrenia: a systematic review and meta-analysis
    Christine Rummel-Kluge
    Klinik und Poliklinik fur Psychiatrie und Psychotherapie der Technischen Universitat Munchen, Klinikum rechts der Isar, Möhlstr 26, 81675 Munchen, Germany
    Schizophr Res 123:225-33. 2010
    ..We conducted a meta-analysis of studies comparing the metabolic side effects of the following SGAs head-to-head: amisulpride, aripiprazole, clozapine, olanzapine, quetiapine, risperidone, sertindole, ziprasidone, zotepine...
  4. pmc Benzodiazepine use and risk of dementia: prospective population based study
    Sophie Billioti de Gage
    Université Bordeaux Segalen, F 33000 Bordeaux, France
    BMJ 345:e6231. 2012
    To evaluate the association between use of benzodiazepines and incident dementia.
  5. ncbi Discovery and characterization of small molecule inhibitors of the BET family bromodomains
    Chun wa Chung
    Molecular Discovery Research, GlaxoSmithKline R and D, Stevenage SG5 4HT, UK
    J Med Chem 54:3827-38. 2011
    ..X-ray crystal structures of compounds bound into bromodomains of Brd2 and Brd4 elucidate the molecular interactions of binding and explain the precisely defined stereochemistry required for activity...
  6. ncbi Effects of anxiolytics in zebrafish: similarities and differences between benzodiazepines, buspirone and ethanol
    Daiane L Gebauer
    Laboratório de Neuroquímica e Psicofarmacologia, Departamento de Biologia Celular e Molecular, Programa de Pós Graduação em Biologia Celular e Molecular, Faculdade de Biociencias, Pontificia Universidade Catolica do Rio Grande do Sul, Avenida Ipiranga, 6681, 90619 900 Porto Alegre, RS, Brazil
    Pharmacol Biochem Behav 99:480-6. 2011
    ..The second task was the assessment of light/dark preference for 5 min. The benzodiazepines clonazepam, bromazepam, diazepam, and a moderate dose of ethanol significantly reduced shoal cohesion...
  7. ncbi Benzodiazepines revisited--will we ever learn?
    Malcolm Lader
    Addiction Research Centre, Institute of Psychiatry, King s College London, London, UK
    Addiction 106:2086-109. 2011
    To re-examine various aspects of the benzodiazepines (BZDs), widely prescribed for 50 years, mainly to treat anxiety and insomnia...
  8. ncbi Safety of benzodiazepines in the geriatric population
    Subramoniam Madhusoodanan
    Department of Psychiatry, St John s Episcopal Hospital, South Shore, 327 Beach 19th Street, Far Rockaway, New York, USA
    Expert Opin Drug Saf 3:485-93. 2004
    b>Benzodiazepines are the most frequently prescribed antianxiety drugs in the elderly. Despite their usefulness and safety in the younger population, there is concern about the rationale for their use in the elderly...
  9. ncbi A 3-week, randomized, placebo-controlled trial of asenapine in the treatment of acute mania in bipolar mania and mixed states
    Roger S McIntyre
    Department of Psychiatry and Pharmacology, University of Toronto, Toronto, ON, Canada
    Bipolar Disord 11:673-86. 2009
    ..Asenapine is approved for bipolar disorder and schizophrenia. This was a 3-week, randomized, double-blind, placebo-controlled trial of asenapine for treating acute bipolar mania...
  10. pmc Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes
    Uwe Rudolph
    Laboratory of Genetic Neuropharmacology, McLean Hospital and Department of Psychiatry, Harvard Medical School, Belmont, Massachusetts 02478, USA urudolph mclean harvard edu
    Nat Rev Drug Discov 10:685-97. 2011
    ..b>Benzodiazepines - which non-selectively target GABA(A) receptors containing the α1, α2, α3 or α5 subunits - have been in ..
  11. ncbi Olanzapine long-acting injection: a 24-week, randomized, double-blind trial of maintenance treatment in patients with schizophrenia
    John M Kane
    Department of Psychiatry, Zucker Hillside Hospital, North Shore Long Island Jewish Health System, Albert Einstein College of Medicine, 75 59 263rd St, Glen Oaks, NY 11004, USA
    Am J Psychiatry 167:181-9. 2010
    ..The purpose of the present study was to evaluate the efficacy and tolerability of olanzapine long-acting injection for maintenance treatment of schizophrenia...
  12. ncbi The impact of benzodiazepines on occurrence of pneumonia and mortality from pneumonia: a nested case-control and survival analysis in a population-based cohort
    Eneanya Obiora
    Division of Epidemiology and Public Health, University of Nottingham, Nottingham, UK
    Thorax 68:163-70. 2013
    b>Benzodiazepines have been associated with an increased incidence of infections, and mortality from sepsis, in the critically ill...
  13. ncbi Olanzapine treatment and metabolic dysfunction: a dose response study in female Sprague Dawley rats
    Katrina Weston-Green
    School of Health Sciences, University of Wollongong, Wollongong, 2522, NSW, Australia
    Behav Brain Res 217:337-46. 2011
    ..The animal model used in the present study of self-administered oral olanzapine treatment (t.i.d.) at a dosage range of 0.5-2.0mg/kg (but not 0.25mg/kg) mimics aspects of the clinic...
  14. ncbi Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
    Panagis Filippakopoulos
    University of Oxford, Nuffield Department of Clinical Medicine, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7LD, UK
    Bioorg Med Chem 20:1878-86. 2012
    b>Benzodiazepines are psychoactive drugs with anxiolytic, sedative, skeletal muscle relaxant and amnestic properties...
  15. ncbi Gender-dependent consequences of chronic olanzapine in the rat: effects on body weight, inflammatory, metabolic and microbiota parameters
    Kieran J Davey
    Alimentary Pharmabiotic Centre, Laboratory of Neurogastroenterology, University College Cork, Cork, Ireland
    Psychopharmacology (Berl) 221:155-69. 2012
    ..Thus, we investigated the effects of olanzapine on body weight, behaviour, gut microbiota and inflammatory and metabolic markers in both male and female rats...
  16. ncbi Polypharmacy with antipsychotics, antidepressants, or benzodiazepines and mortality in schizophrenia
    Jari Tiihonen
    Department of Forensic Psychiatry, University of Eastern Finland, Niuvanniemi Hospital, FI 70240 Kuopio, Finland
    Arch Gen Psychiatry 69:476-83. 2012
    ..Polypharmacy is widely used in the treatment of schizophrenia, although it is believed to have major adverse effects on the well-being of patients...
  17. pmc Cardiometabolic risk of second-generation antipsychotic medications during first-time use in children and adolescents
    Christoph U Correll
    Zucker Hillside Hospital, Psychiatry Research, North Shore Long Island Jewish Health System, 75 59 263rd St, Glen Oaks, NY 11004, USA
    JAMA 302:1765-73. 2009
    ..Cardiometabolic effects of second-generation antipsychotic medications are concerning but have not been sufficiently studied in pediatric and adolescent patients naive to antipsychotic medication...
  18. ncbi Why olanzapine beats risperidone, risperidone beats quetiapine, and quetiapine beats olanzapine: an exploratory analysis of head-to-head comparison studies of second-generation antipsychotics
    Stephan Heres
    Klinik und Poliklinik für Psychiatrie und Psychotherapie der Technischen Universität München am Klinikum rechts der Isar, Moehlstrasse 26, 81675 Munich, Germany
    Am J Psychiatry 163:185-94. 2006
    ....
  19. pmc A double blind, placebo-controlled, randomized crossover study of the acute metabolic effects of olanzapine in healthy volunteers
    Vance L Albaugh
    Department of Cellular and Molecular Physiology, The Pennsylvania State University College of Medicine, Hershey, Pennsylvania, United States of America
    PLoS ONE 6:e22662. 2011
    ..The adverse events are preceded by acute worsening of oral glucose tolerance (oGTT) along with reduced plasma free fatty acids (FFA) and leptin in animal models. It is unclear whether the same acute effects occur in humans...
  20. pmc Olanzapine promotes fat accumulation in male rats by decreasing physical activity, repartitioning energy and increasing adipose tissue lipogenesis while impairing lipolysis
    V L Albaugh
    Department of Cellular and Molecular Physiology, The Pennsylvania State University College of Medicine, Hershey, PA 17033, USA
    Mol Psychiatry 16:569-81. 2011
    ..Collectively, these results suggest that olanzapine exerts several metabolic effects that together favor increased accumulation of fuel into adipose tissue, thereby increasing adiposity...
  21. pmc Meta-analysis of benzodiazepine use in the treatment of insomnia
    A M Holbrook
    Centre for Evaluation of Medicines, St Joseph s Hospital, Hamilton, Ont
    CMAJ 162:225-33. 2000
    To systematically review the benefits and risks associated with the use of benzodiazepines to treat insomnia in adults.
  22. pmc Neural bases for addictive properties of benzodiazepines
    Kelly R Tan
    Department of Basic Neurosciences, Medical Faculty, University of Geneva, CH 1211 Geneva, Switzerland
    Nature 463:769-74. 2010
    b>Benzodiazepines are widely used in clinics and for recreational purposes, but will lead to addiction in vulnerable individuals...
  23. ncbi Profiling multiple provider prescribing of opioids, benzodiazepines, stimulants, and anorectics
    B L Wilsey
    VA Northern California Health Care System, Sacramento, CA 95655, USA
    Drug Alcohol Depend 112:99-106. 2010
    ..PMPs monitor the final allocation of controlled substances from pharmacist to patient. The primary purpose of this scrutiny is to diminish the utilization of multiple providers for controlled substances...
  24. ncbi Psychomotor development in children exposed in utero to benzodiazepines, antidepressants, neuroleptics, and anti-epileptics
    J T Mortensen
    Department of Clinical Epidemiology, Aarhus University and Aalborg Hospitals, Stengade 10, Box 561, Aalborg, Denmark
    Eur J Epidemiol 18:769-71. 2003
    ..Any abnormal test result was seen much more frequently among exposed (16%) than for not exposed (4%). The study has several limitations but raises concern that should be addressed in other and better designed studies...
  25. ncbi The early effect of olanzapine and risperidone on insulin secretion in atypical-naïve schizophrenic patients
    Chih Chiang Chiu
    Department of Psychiatry, Songde Branch, Taipei City Hospital, Taipei, Taiwan
    J Clin Psychopharmacol 26:504-7. 2006
    ..The results of this study support the hypothesis that olanzapine might directly impair pancreatic beta-cell function...
  26. ncbi A single histidine in GABAA receptors is essential for benzodiazepine agonist binding
    H A Wieland
    Laboratory of Molecular Neuroendocrinology, University of Heidelberg, Germany
    J Biol Chem 267:1426-9. 1992
    b>Benzodiazepines (BZ) modulate neurotransmitter-evoked chloride currents at the gamma-aminobutyric acid type A (GABAA) receptor, the major inhibitory ion channel in the mammalian brain...
  27. ncbi Effects of aripiprazole, olanzapine, and haloperidol in a model of cognitive deficit of schizophrenia in rats: relationship with glutamate release in the medial prefrontal cortex
    Mirjana Carli
    Laboratory of Neurochemistry and Behavior, Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri, Via G La Masa 19, 20156, Milan, Italy
    Psychopharmacology (Berl) 214:639-52. 2011
    ..Disruption in cognition is characteristic of psychiatric illnesses such as schizophrenia. Studies of drugs that improve cognition might provide a better insight into the mechanisms underlying cognitive deficits...
  28. pmc Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines
    Radovan Spurny
    Department of Cellular and Molecular Medicine, Laboratory of Structural Neurobiology, Catholic University of Leuven, 3000 Leuven, Belgium
    Proc Natl Acad Sci U S A 109:E3028-34. 2012
    ..neurotransmission and are allosterically modulated by the anxiolytic, anticonvulsant, and sedative-hypnotic benzodiazepines. Here we show that the prokaryotic homolog ELIC also is activated by GABA and is modulated by benzodiazepines ..
  29. ncbi A systematic review of research examining benzodiazepine-related mortality
    Fiona Charlson
    National Drug and Alcohol Research Centre, University of New South Wales, Australia
    Pharmacoepidemiol Drug Saf 18:93-103. 2009
    ..This paper will review literature examining the association of benzodiazepine use and mortality...
  30. ncbi Benzodiazepine use and risk of dementia: evidence from the Caerphilly Prospective Study (CaPS)
    John Gallacher
    Department of Primary Care and Public Health, Cardiff University, Cardiff, UK
    J Epidemiol Community Health 66:869-73. 2012
    ..Benzodiazepine use is widespread in older people, although its benefit is uncertain...
  31. ncbi Olanzapine, but not aripiprazole, weight-independently elevates serum triglycerides and activates lipogenic gene expression in female rats
    Silje Skrede
    Dr Einar Martens Research Group for Biological Psychiatry, Department of Clinical Medicine, University of Bergen, Norway
    Int J Neuropsychopharmacol 15:163-79. 2012
    ..Our findings support the existence of tissue-specific, weight-independent direct effects of olanzapine on lipid metabolism...
  32. ncbi Comparative safety of antipsychotics in the WHO pharmacovigilance database: the haloperidol case
    Carla Meyer-Massetti
    Clinical Pharmacy and Epidemiology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland
    Int J Clin Pharm 33:806-14. 2011
    ..Intravenous haloperidol is commonly used as a first line treatment for acute delirium. Consequently, the extended warning has caused uncertainty among health care professionals...
  33. ncbi Early perturbation in feeding behaviour and energy homeostasy in olanzapine-treated rats
    Montserrat Victoriano
    UMR914 Physiologie de la Nutrition et du Comportement Alimentaire, INRA, 16 rue Claude Bernard, 75005, Paris, France
    Psychopharmacology (Berl) 206:167-76. 2009
    ..The antipsychotic drug, olanzapine, often induces weight gain and glucose metabolism disturbances, which may result from feeding pattern abnormalities...
  34. pmc Alterations to melanocortinergic, GABAergic and cannabinoid neurotransmission associated with olanzapine-induced weight gain
    Katrina Weston-Green
    Centre for Translational Neuroscience, School of Health Sciences, University of Wollongong, Wollongong, Australia
    PLoS ONE 7:e33548. 2012
    ..This study examined the effects of low to high doses of olanzapine on appetite/metabolic regulatory signals in the hypothalamus and brainstem to elucidate the mechanisms underlying olanzapine-induced obesity...
  35. pmc Atypical antipsychotics and the neural regulation of food intake and peripheral metabolism
    Karen L Teff
    Monell Chemical Senses Center, 3500 Market Street, Philadelphia, PA 19104, USA
    Physiol Behav 104:590-8. 2011
    ..Furthermore, we examine how inhibition of the histaminergic pathway may mediate increases in food intake and the potential role of the vagus nerve in the reported peripheral metabolic effects...
  36. ncbi The World Federation of Societies of Biological Psychiatry (WFSBP) Guidelines for the Biological Treatment of Bipolar Disorders: Update 2010 on the treatment of acute bipolar depression
    Heinz Grunze
    Newcastle University, RVI, Division of Psychiatry, Institute of Neuroscience, Newcastle upon Tyne, UK
    World J Biol Psychiatry 11:81-109. 2010
    ..Their purpose is to supply a systematic overview of all scientific evidence pertaining to the treatment of acute bipolar depression in adults...
  37. pmc Reimbursement restriction and moderate decrease in benzodiazepine use in general practice
    Joëlle M Hoebert
    Division of Pharmacoepidemiology and Clinical Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, The Netherlands
    Ann Fam Med 10:42-9. 2012
    To limit misuse and save costs, on January 1, 2009, benzodiazepines were excluded from the Dutch reimbursement list when used as anxiolytic, hypnotic, or sedative...
  38. ncbi Comparison of metabolic and prolactin variables from a six-month randomised trial of olanzapine and quetiapine in schizophrenia
    C Bushe
    Eli Lilly and Company, Basingstoke, UK
    J Psychopharmacol 24:1001-9. 2010
    ..9%; QUE 31.4%), but after 2 weeks of treatment prolactin values had reverted to normal for nearly all patients (OLZ 100%; QUE 99.4%). There were no significant treatment differences in any variable between cohorts...
  39. ncbi Plasma nitric oxide and leptin values in patients with olanzapine-induced weight gain
    Murad Atmaca
    Firat University, School of Medicine, Department of Psychiatry, Elazig 23119, Turkey
    J Psychiatr Res 41:74-9. 2007
    ..In addition, there was a severe significant negative correlation between the changes in leptin levels and NO levels (r=0.73, P<0.01). The results confirmed that leptin and NO might be associated with olanzapine-induced weight gain...
  40. ncbi Effect of benzodiazepine discontinuation on dementia risk
    Chi Shin Wu
    Department of Psychiatry, Far Eastern Memorial Hospital, Taiwan
    Am J Geriatr Psychiatry 19:151-9. 2011
    ..This study aimed to examine whether benzodiazepine (BZD) discontinuation would decrease the risk of dementia...
  41. pmc Olanzapine-induced hyperphagia and weight gain associate with orexigenic hypothalamic neuropeptide signaling without concomitant AMPK phosphorylation
    Johan Fernø
    Dr Einar Martens Research Group for Biological Psychiatry, Department of Clinical Medicine, University of Bergen, Bergen, Norway
    PLoS ONE 6:e20571. 2011
    ..Our data shed new light on the hypothalamic mechanism underlying antipsychotic-induced hyperphagia and weight gain, and provide the basis for alternative targets to control energy balance...
  42. ncbi Targeted deletion of the GABRA2 gene encoding alpha2-subunits of GABA(A) receptors facilitates performance of a conditioned emotional response, and abolishes anxiolytic effects of benzodiazepines and barbiturates
    C I Dixon
    Department of Psychology University of Sussex, Falmer, Brighton, BN1 9QG, UK
    Pharmacol Biochem Behav 90:1-8. 2008
    ..receptor subunits (rendering them diazepam insensitive) are resistant to the anxiolytic-like effects of benzodiazepines (BZs) in the conditioned emotional response (CER) test, but show normal anxiolytic effects of a barbiturate...
  43. pmc Olanzapine versus other atypical antipsychotics for schizophrenia
    Katja Komossa
    , , Moehlstrasse 26, , Germany, 81675
    Cochrane Database Syst Rev 3:CD006654. 2010
    ..Further large, well-designed trials are necessary to establish the relative effects of different second generation antipsychotic drugs...
  44. ncbi Olanzapine differentially affects 5-HT2Aand2C receptor mRNA expression in the rat brain
    Xu Feng Huang
    Neurobiology Research Centre of Metabolic and Psychiatric Disorders, School of Health Science, University of Wollongong, NSW, Australia
    Behav Brain Res 171:355-62. 2006
    ..5-HT(2C) receptor mRNA expressions were decreased in the substantia nigra. Correlations between 5-HT(2A) receptor mRNA expression and total food intake, weight gain and energy efficiency were observed...
  45. ncbi Atypical antipsychotic administration during late pregnancy: placental passage and obstetrical outcomes
    D Jeffrey Newport
    Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, Atlanta, GA 30322, USA
    Am J Psychiatry 164:1214-20. 2007
    ..The objectives of the current study were to quantify placental permeability to antipsychotic medications and to document obstetrical outcomes for women taking these agents proximate to delivery...
  46. ncbi Are we going to increase the use of antidepressants up to that of benzodiazepines?
    Arcangelo Ciuna
    Servizio Farmaceutico ULSS 20, Verona, Italy
    Eur J Clin Pharmacol 60:629-34. 2004
    ..We investigated whether the increasing use of antidepressants is associated with a progressive reduction in benzodiazepine use...
  47. ncbi Pyrrolobenzodiazepine dimers: novel sequence-selective, DNA-interactive, cross-linking agents with activity against Gram-positive bacteria
    Tsveta Hadjivassileva
    School of Pharmacy, 29 39 Brunswick Square, London WC1N 1AX, UK
    J Antimicrob Chemother 56:513-8. 2005
    ..We investigated the antibacterial activity of three dimers, SJG-136, DRG-16 and ELB-21, which differ in the structure of the PBD monomeric unit and the length of the linker region between the two identical PBD monomers...
  48. ncbi Asenapine for long-term treatment of bipolar disorder: a double-blind 40-week extension study
    Roger S McIntyre
    Mood Disorders Psychopharmacology Unit, University Health Network, University of Toronto, Toronto, ON, Canada
    J Affect Disord 126:358-65. 2010
    ..We report the results of long-term treatment with asenapine in patients with bipolar I disorder...
  49. ncbi The distinct effects of subchronic antipsychotic drug treatment on macronutrient selection, body weight, adiposity, and metabolism in female rats
    M J Fell
    Bradford School of Pharmacy, University of Bradford, Bradford BD7 1DP, UK
    Psychopharmacology (Berl) 194:221-31. 2007
    ..The aim of the present study was to investigate the effect of atypical antipsychotic drugs on dietary macronutrient selection, body weight, body composition and biochemical parameters related to obesity in female rats...
  50. ncbi Efficacy of olanzapine and olanzapine-fluoxetine combination in the treatment of bipolar I depression
    Mauricio Tohen
    Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Arch Gen Psychiatry 60:1079-88. 2003
    ....
  51. ncbi Long-term benzodiazepine use and cognitive decline in the elderly: the Epidemiology of Vascular Aging Study
    Sabrina Paterniti
    Institut National de la Sante et de la Recherche Medicale, Paris, France
    J Clin Psychopharmacol 22:285-93. 2002
    Several cross-sectional studies have found cognitive impairment in subjects taking benzodiazepines for long periods. However, it is not known whether long-term use of benzodiazepines accelerates cognitive decline in the elderly...
  52. pmc Benzodiazepine-insensitive mice generated by targeted disruption of the gamma 2 subunit gene of gamma-aminobutyric acid type A receptors
    U Gunther
    Institute of Pharmacology, University of Zurich, Switzerland
    Proc Natl Acad Sci U S A 92:7749-53. 1995
    ..The lack of postnatal GABAA receptor regulation by endogenous ligands of BZ sites might contribute to this phenotype...
  53. ncbi Conditional analgesia, defensive freezing, and benzodiazepines
    M S Fanselow
    Department of Psychology, Dartmouth College, Hanover, New Hampshire 03755
    Behav Neurosci 102:233-43. 1988
    ..In the present experiments, the effects of three benzodiazepines on both of these responses were examined. Pain sensitivity was measured with the formalin test...
  54. ncbi Comparison of ELISAs for opiates, methamphetamine, cocaine metabolite, benzodiazepines, phencyclidine, and cannabinoids in whole blood and urine
    S Kerrigan
    California Department of Justice, Bureau of Forensic Services, Toxicology Laboratory, 4949 Broadway, Sacramento, CA 95820, USA
    Clin Chem 47:540-7. 2001
    ..ELISAs are widely utilized in forensic drug analysis. A comparative assessment of microtiter plate assays for the detection of six common classes of drug in blood and urine is described...
  55. ncbi The effect of chronic benzodiazepine use on cognitive functioning in older persons: good, bad or indifferent?
    E J M Bierman
    Department of Psychiatry, Institute for Research in Extramural Medicine EMGO Institute, VU Medical Centre, Amsterdam, The Netherlands
    Int J Geriatr Psychiatry 22:1194-200. 2007
    ..This study investigates the effects of benzodiazepine (BZ) use on cognitive performance in elderly persons in a longitudinal design...
  56. ncbi Acute effects of atypical antipsychotics on whole-body insulin resistance in rats: implications for adverse metabolic effects
    Karen L Houseknecht
    Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA
    Neuropsychopharmacology 32:289-97. 2007
    ..OLAN and CLOZ can thus rapidly induce marked insulin resistance, which could contribute to the hyperglycemia and ketoacidosis reported for patients receiving those therapies...
  57. ncbi Benzodiazepines in epilepsy: pharmacology and pharmacokinetics
    J Riss
    Center for Orphan Drug Research, Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA
    Acta Neurol Scand 118:69-86. 2008
    b>Benzodiazepines (BZDs) remain important agents in the management of epilepsy...
  58. ncbi Psychotropic medications and the risk of fracture: a meta-analysis
    Bahi Takkouche
    Department of Preventive Medicine, Faculty of Medicine, University of Santiago de Compostela, Santiago de Compostela, Spain
    Drug Saf 30:171-84. 2007
    ..Many studies have examined the relationship between the use of psychotropic medications and the risk of fractures, but these studies have reported conflicting results...
  59. ncbi Older adults and withdrawal from benzodiazepine hypnotics in general practice: effects on cognitive function, sleep, mood and quality of life
    H V Curran
    Psychopharmacology Research Unit, Clinical Health Psychology, University College London
    Psychol Med 33:1223-37. 2003
    ..This study therefore aimed to determine if withdrawing from BZDs leads to changes in patients' cognitive function, quality of life, mood and sleep...
  60. ncbi Effects of olanzapine and haloperidol on the metabolic status of healthy men
    Solrun Vidarsdottir
    Department of Endocrinology and Metabolism, Leiden University Medical Center, Leiden, The Netherlands
    J Clin Endocrinol Metab 95:118-25. 2010
    ..The aim of this study was to determine the effect of short-term olanzapine (atypical antipsychotic drug) and haloperidol (conventional antipsychotic drug) treatment on glucose and lipid metabolism...
  61. ncbi The effects of benzodiazepines on cognition
    Samantha A Stewart
    Massachusetts General Hospital, Boston, MA 02478, USA
    J Clin Psychiatry 66:9-13. 2005
    Initially thought to be virtually free of negative effects, benzodiazepines are now known to carry risks of dependence, withdrawal, and negative side effects. Among the most controversial of these side effects are cognitive effects...
  62. pmc Hormonal and metabolic effects of olanzapine and clozapine related to body weight in rodents
    Vance L Albaugh
    Department of Cellular and Molecular Physiology, Pennsylvania State University College of Medicine, 500 University Drive, Hershey, PA 17033, USA
    Obesity (Silver Spring) 14:36-51. 2006
    ..To characterize a model of atypical antipsychotic drug-induced obesity and evaluate its mechanism...
  63. ncbi Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines
    Gaochao Tian
    Department of Lead Discovery, AstraZeneca Pharmaceuticals, Wilmington, Delaware 19850, USA
    J Biol Chem 277:31499-505. 2002
    ..Sulfonamides and benzodiazepines, which do not resemble transition state analogs of aspartyl proteases, also displayed potent, non-competitive ..
  64. ncbi Clozapine treatment for suicidality in schizophrenia: International Suicide Prevention Trial (InterSePT)
    Herbert Y Meltzer
    Psychiatric Hospital at Vanderbilt, 1601 23rd Ave S, Suite 306, Nashville, TN 37212, USA
    Arch Gen Psychiatry 60:82-91. 2003
    ..Approximately 50% of patients with schizophrenia or schizoaffective disorder attempt suicide, and approximately 10% die of suicide. Study results suggest that clozapine therapy significantly reduces suicidal behavior in these patients...
  65. ncbi Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines
    Rebecca Dias
    The Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Harlow, Essex CM20 2QR, United Kingdom
    J Neurosci 25:10682-8. 2005
    The GABA(A) receptor subtypes responsible for the anxiolytic effects of nonselective benzodiazepines (BZs) such as chlordiazepoxide (CDP) and diazepam remain controversial...
  66. ncbi Weight gain associated with increased food intake and low habitual activity levels in male adolescent schizophrenic inpatients treated with olanzapine
    Doron Gothelf
    Behavioral Genetic Clinic, Richard E Feinberg Department of Psychiatry, Schneider Children s Medical Center of Israel, Petah Tiqwa
    Am J Psychiatry 159:1055-7. 2002
    ..The authors studied weight gain mechanisms and energy balance in patients treated with olanzapine...
  67. ncbi Olanzapine induces SREBP-1-related adipogenesis in 3T3-L1 cells
    Li Hung Yang
    Institute of Pharmaceutical Sciences, College of Medicine, National Taiwan University, Taipei 10051, Taiwan
    Pharmacol Res 56:202-8. 2007
    ..Taken together, olanzapine may cause body weight gain not only through influencing CNS receptors, but also affecting the peripheral adipogenesis regulated by SREBP-1...
  68. ncbi Benzodiazepine use and risk of dementia: a nested case-control study
    Rajaa Lagnaoui
    Departement de Pharmacologie, Universite Victor Segalen, Bordeaux 2, 33 076 Bordeaux, France
    J Clin Epidemiol 55:314-8. 2002
    ..The main outcome measures were the use of benzodiazepines in incident cases of dementia versus nondemented controls...
  69. ncbi Benzodiazepines and injurious falls in community dwelling elders
    Antoine Pariente
    Institut National de la Santé et la Recherche Médicale INSERM, U657, Bordeaux, France
    Drugs Aging 25:61-70. 2008
    b>Benzodiazepines are frequently used medications in the elderly, in whom they are associated with an increased risk of falling, with sometimes dire consequences.
  70. ncbi A new benzodiazepine pharmacology
    H Mohler
    Institute of Pharmacology and Toxicology, University of Zurich, Zurich, Switzerland
    J Pharmacol Exp Ther 300:2-8. 2002
    ..Only restricted neuronal networks will be modulated by the new subtype-selective drugs. Promising new anxiolytics have already been developed. A new pharmacology of the benzodiazepine site is on the horizon...
  71. ncbi Enhancement of GABAergic activity: neuropharmacological effects of benzodiazepines and therapeutic use in anesthesiology
    Teijo I Saari
    Department of Anesthesiology, Intensive Care, Emergency Care and Pain Medicine, Turku University Hospital, P O Box 52 Kiinamyllynkatu 4 8, FI 20520 Turku, Finland
    Pharmacol Rev 63:243-67. 2011
    ..parts of CNS are thought to be involved in versatile effects caused by inhaled anesthetics and classic benzodiazepines (BZD), both of which are widely used in clinical anesthesiology...
  72. ncbi The time-dependent change of insulin secretion in schizophrenic patients treated with olanzapine
    Chih Chiang Chiu
    Department of Psychiatry, School of Medicine, Taipei Medical University, Taipei, Taiwan
    Prog Neuropsychopharmacol Biol Psychiatry 34:866-70. 2010
    ..The results of this study support that olanzapine might directly influence pancreatic beta cell function...
  73. ncbi Effectiveness of antipsychotic drugs in first-episode schizophrenia and schizophreniform disorder: an open randomised clinical trial
    Rene S Kahn
    Department of Psychiatry, Rudolf Magnus Institute of Neuroscience, University Medical Centre Utrecht, Utrecht, Netherlands
    Lancet 371:1085-97. 2008
    ..We aimed to compare the effectiveness of second-generation antipsychotic drugs with that of a low dose of haloperidol, in first-episode schizophrenia...
  74. ncbi Olanzapine versus placebo in adolescents with schizophrenia: a 6-week, randomized, double-blind, placebo-controlled trial
    Ludmila Kryzhanovskaya
    Eli Lilly and Company
    J Am Acad Child Adolesc Psychiatry 48:60-70. 2009
    ..To assess olanzapine's efficacy and tolerability in adolescents with schizophrenia...
  75. ncbi Prescription of benzodiazepines and antidepressants to outpatients attending a Japanese university hospital
    M Nakao
    Department of Hygiene and Public Health, Teikyo University School of Medicine, Tokyo, Japan
    Int J Clin Pharmacol Ther 45:30-5. 2007
    ..Although more benzodiazepines are prescribed in Japan than in any other country, no hospital-based report has documented this phenomenon...
  76. pmc Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different
    Susan M Hanson
    Department of Physiology and Program in Molecular and Cellular Pharmacology, University of Wisconsin Madison, Madison, Wisconsin 53711, USA
    J Med Chem 51:7243-52. 2008
    ....
  77. pmc Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates
    James K Rowlett
    Harvard Medical School, New England Primate Research Center, One Pine Hill Road, Box 9102, Southborough, MA 01772, USA
    Proc Natl Acad Sci U S A 102:915-20. 2005
    b>Benzodiazepines exert their effects by binding to multiple subtypes of the GABAA receptor, the predominant subtypes in the brain being those that contain alpha1-, alpha2-, alpha3-, and alpha5-subunits...
  78. ncbi Relapse prevention in bipolar I disorder: 18-month comparison of olanzapine plus mood stabiliser v. mood stabiliser alone
    Mauricio Tohen
    Lilly Research Laboratories, Indianapolis, Indiana 46285, USA
    Br J Psychiatry 184:337-45. 2004
    ..Aims To evaluate whether olanzapine plus either lithium or valproate reduces the rate of relapse, compared with lithium or valproate alone...
  79. ncbi Effects of antipsychotic medications on psychosocial functioning in patients with chronic schizophrenia: findings from the NIMH CATIE study
    Marvin S Swartz
    Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC, USA
    Am J Psychiatry 164:428-36. 2007
    ..This study examined the relative effects of the second-generation antipsychotic drugs and an older representative agent on psychosocial functioning in patients with chronic schizophrenia...
  80. ncbi Long-term weight gain in patients treated with open-label olanzapine in combination with fluoxetine for major depressive disorder
    Scott W Andersen
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Clin Psychiatry 66:1468-76. 2005
    ..g., age and gender) and correlates (e.g., cholesterol and glucose levels) of weight gain were investigated in OFC-treated patients with MDD...
  81. pmc Atypical antipsychotics rapidly and inappropriately switch peripheral fuel utilization to lipids, impairing metabolic flexibility in rodents
    Vance L Albaugh
    Department of Cellular and Molecular Physiology, Penn State College of Medicine, Hershey, PA 17033, USA
    Schizophr Bull 38:153-66. 2012
    ....
  82. pmc Change in level of productivity in the treatment of schizophrenia with olanzapine or other antipsychotics
    Hong Liu-Seifert
    Lilly Research Laboratories, Indianapolis, Indiana, USA
    BMC Psychiatry 11:87. 2011
    ..We also assessed the links between productivity level and other clinical outcomes...
  83. ncbi Asenapine versus olanzapine in people with persistent negative symptoms of schizophrenia
    Robert W Buchanan
    Department of Psychiatry, University of Maryland School of Medicine, Baltimore, MD, USA
    J Clin Psychopharmacol 32:36-45. 2012
    ..In conclusion, asenapine superiority over olanzapine was not observed in the core studies. Both treatments improved persistent negative symptoms, but discontinuation rates were higher with asenapine...
  84. ncbi A novel augmentation strategy for treating resistant major depression
    R C Shelton
    Department of Psychiatry, Vanderbilt University Medical Center, Nashville, TN 37212, USA
    Am J Psychiatry 158:131-4. 2001
    ..The authors hypothesized that fluoxetine could be augmented with olanzapine to successfully treat resistant depression...
  85. ncbi Olanzapine long-acting injection: a review of its use in the treatment of schizophrenia
    James E Frampton
    Adis, a Wolters Kluwer Business, Auckland, New Zealand
    Drugs 70:2289-313. 2010
    ....
  86. pmc Antipsychotics associated with the development of type 2 diabetes in antipsychotic-naïve schizophrenia patients
    Jimmi Nielsen
    Unit for Psychiatric Research, Aalborg Psychiatric Hospital, Aarhus University Hospital, Mølleparkvej 10, Aalborg, Denmark
    Neuropsychopharmacology 35:1997-2004. 2010
    ..Patients discontinuing olanzapine or mid-potency FGA had no increased risk of diabetes compared with patient not treated with the drugs at anytime...
  87. ncbi Time course of the antipsychotic effect and the underlying behavioral mechanisms
    Ming Li
    Schizophrenia PET program, Centre for Addiction and Mental Health, Toronto, ON, Canada
    Neuropsychopharmacology 32:263-72. 2007
    ....
  88. ncbi Lower weight gain with the orally disintegrating olanzapine than with standard tablets in first-episode never treated psychotic patients
    B Arranz
    Hospital San Rafael, Barcelona, Spain
    Hum Psychopharmacol 22:11-5. 2007
    ..orally disintegrating formulation)...
  89. pmc Impact of drug interactions, dosage, and duration of therapy on the risk of hip fracture associated with benzodiazepine use in older adults
    Kristina Zint
    Department of Clinical Pharmacology and Pharmacoepidemiology, University of Heidelberg, Heidelberg, Germany
    Pharmacoepidemiol Drug Saf 19:1248-55. 2010
    To determine how concomitant use of potentially interacting drugs, drug dosage, and duration of therapy modify the risk of hip fracture associated with use of benzodiazepines and benzodiazepine-related drugs (BDZ) in older adults.
  90. pmc Amygdala-specific reduction of alpha1-GABAA receptors disrupts the anticonvulsant, locomotor, and sedative, but not anxiolytic, effects of benzodiazepines in mice
    Scott A Heldt
    Department of Psychiatry and Behavioral Sciences, Yerkes National Primate Research Center, Emory University, Atlanta, Georgia 30329, USA
    J Neurosci 30:7139-51. 2010
    ....
  91. ncbi Randomised, double-blind, placebo-controlled study of olanzapine in patients with bipolar I depression
    Mauricio Tohen
    University of Texas Health Science Center, Division of Mood and Anxiety Disorders, 7526 Louis Pasteur Drive, San Antonio, TX 78229 3900, USA
    Br J Psychiatry 201:376-82. 2012
    ..Atypical antipsychotics are widely used in bipolar mania. However, the efficacy of atypical antipsychotics in bipolar depression has not been comprehensively explored...
  92. ncbi Short- and long-term effects of antipsychotic drug treatment on weight gain and H1 receptor expression
    Mei Han
    Centre for Translational Neuroscience, School of Health Sciences, University of Wollongong, Northfields Avenue, Wollongong, NSW 2522, Australia
    Psychoneuroendocrinology 33:569-80. 2008
    ..The present study suggests that downregulated VMH and Arc H1 receptor expression may be a key factor contributing to olanzapine-induced obesity...
  93. ncbi Olanzapine-induced weight gain in anorexia nervosa: involvement of leptin and ghrelin secretion?
    F Brambilla
    Department of Psychiatry, University of Naples SUN, Naples, Italy
    Psychoneuroendocrinology 32:402-6. 2007
    ..Aim of this study was to determine whether in patients with Anorexia Nervosa (AN) OLA induces weight gain through the modulation of the hunger-satiety regulatory peptides leptin and ghrelin...
  94. pmc HZ166, a novel GABAA receptor subtype-selective benzodiazepine site ligand, is antihyperalgesic in mouse models of inflammatory and neuropathic pain
    Alessandra Di Lio
    Institute of Pharmacology and Toxicology, University of Zurich, Zurich, Switzerland
    Neuropharmacology 60:626-32. 2011
    ..Accordingly, pharmacological facilitation of GABAergic inhibition by spinal benzodiazepines (BDZs) has been shown to reverse pathological pain in animals as well as in human patients...
  95. pmc Negative effects of chronic oral chlorpromazine and olanzapine treatment on the performance of tasks designed to assess spatial learning and working memory in rats
    A V Terry
    Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta, GA 30912 2300, USA
    Neuroscience 156:1005-16. 2008
    ..These animal data indicate that chronic oral treatment with chlorpromazine or olanzapine can impair the performance of tasks designed to assess specific components of cognition that are affected in schizophrenia...
  96. ncbi Olanzapine pamoate for the treatment of schizophrenia
    Dieter Naber
    Klinik fur Psychiatrie und Psychotherapie, Universitatsklinikum Hamburg Eppendorf, Martinistrasse 52, Hamburg, Germany
    Expert Opin Pharmacother 12:627-33. 2011
    ..Long-acting injectable or depot atypical antipsychotics are associated with better maintenance. Olanzapine pamoate, available since 2010, is the second depot atypical antipsychotic...
  97. pmc Central nervous system delivery of the antipsychotic olanzapine induces hepatic insulin resistance
    Paulo J F Martins
    Obesity Research Center, University of Cincinnati, Cincinnati, Ohio, USA
    Diabetes 59:2418-25. 2010
    ..Recent evidence shows that OLZ alters insulin sensitivity independent of changes in body weight and composition. The present study addresses whether OLZ-induced insulin resistance is driven by its central actions...
  98. ncbi Relative positioning of diazepam in the benzodiazepine-binding-pocket of GABA receptors
    Kelly R Tan
    Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse, Switzerland
    J Neurochem 111:1264-73. 2009
    ..GABA(A) receptors are the major inhibitory neurotransmitter receptors in the brain. Some of them are targets of benzodiazepines that are widely used in clinical practice for their sedative/hypnotic, anxiolytic, muscle relaxant and ..
  99. ncbi The association between dementia and long-term use of benzodiazepine in the elderly: nested case-control study using claims data
    Chi Shin Wu
    Department of Psychiatry, Far Eastern Memorial Hospital, Taiwan
    Am J Geriatr Psychiatry 17:614-20. 2009
    The aim of this study was to examine the association between long-term benzodiazepines (BZDs) use and the risk of dementia.
  100. ncbi Is benzodiazepine use a risk factor for cognitive decline and dementia? A literature review of epidemiological studies
    Helene Verdoux
    EA 3676, Universite Victor Segalen Bordeaux 2, Bordeaux, France
    Psychol Med 35:307-15. 2005
    ..The aim of the present review was to examine findings from prospective studies carried out in general population samples exploring whether exposure to benzodiazepines is associated with an increased risk of incident cognitive decline.
  101. ncbi The clinical dilemma--prescribing in pregnancy
    Roshelle Ramkisson
    Bolton, Salford and Trafford Mental Health NHS Trus, England
    Psychiatr Danub 20:88-90. 2008
    ..We present two cases where a choice had to be made as to whether to prescribe Olanzapine during pregnancy, with different results...

Research Grants65

  1. Efficacy of GABAA a5 receptor inverse agonists in learning impaired rats
    EARL MICHAEL GIBBS; Fiscal Year: 2010
    ..Patients with learning disorders and those suffering from complications due to neurodegenerative diseases will greatly benefit as PWZ-029 moves another step closer to the clinic. ..
  2. Design and Synthesis of Anxioselective Anxiolytics
    James M Cook; Fiscal Year: 2010
    ..The 1,4-benzodiazepines, employed to treat anxiety disorders as well as sleep disorders exhibit anxiolytic, anticonvulsant, muscle ..
  3. Oxidative Stress: A Recipe for Anxiety
    Samina Salim; Fiscal Year: 2012
    ..These people have anxiety disorders. The mainstays of treatment are benzodiazepines and selective serotonin reuptake inhibitors (SSRIs)...
  4. GABA chaperoning of epilepsy-associated GABAA receptor mutants.
    Nancy J Leidenheimer; Fiscal Year: 2012
    ..2009) and is the target of several classes of therapeutic agents including benzodiazepines, barbiturates and anesthetics (Whiting, 2003)...
  5. Pharmacological Management of Delirium
    Malaz Boustani; Fiscal Year: 2013
    ..Older adults with delirium receive potentially harmful medications such as anticholinergics and benzodiazepines and are more prone to falls, injuries, pressure ulcers and restraints than their counterparts with no ..
  6. Structural Rearrangements in GABA-A Receptors
    CYNTHIA M CZAJKOWSKI; Fiscal Year: 2012
    ..of synaptic inhibition in the brain and are modulated by a variety of clinically important drugs, such as benzodiazepines, barbiturates, steroids, anesthetics and anti-convulsants...
  7. Altering Sedation Paradigms to Improve Brain Injury and Survival in Severe Sepsis
    Pratik Pandharipande; Fiscal Year: 2013
    ..The gamma-aminobutyric acid (GABA)-ergic benzodiazepines, in particular, have been shown to increase brain dysfunction, promote infection, and prolong MV...
  8. The Role of Amygdala GABAergic Transmission in Fear and Anxiety
    Scott A Heldt; Fiscal Year: 2011
    ..by the fact that patients suffering from anxiety disorders are commonly treated by the administration of benzodiazepines (BZs), which mediate their actions via GABAA receptors (GABAARs)...
  9. Constructing inhibitory synapses
    Stephen J Moss; Fiscal Year: 2013
    ..We will evaluate if deficits in paired pulse inhibition are reversed by antipsychotics and subtype-selective benzodiazepines. We will also assess if blocking GABAAR clustering in the cortex induces other schizophrenia-related ..
  10. GENETIC VULNERABILITY TO DRUGS OF ABUSE
    Kari J Buck; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Abuse of prescribed and other sedative drugs (e.g., benzodiazepines, barbiturates and ethanol) is among the top five health problems in the U.S...
  11. Neurosteroid-BZ combinations: Strategy for reducing abuse and sedation
    James K Rowlett; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Benzodiazepines (BZs) are prescribed widely as anxiolytics, hypnotics, muscle relaxants, and anticonvulsants...
  12. Rational polytherapy in the treatment of cholinergic seizures
    Claude G Wasterlain; Fiscal Year: 2013
    ..self-sustaining, independent of their original cholinergic trigger, and refractory to standard treatment (benzodiazepines), and represent an unresolved problem and potentially a very serious military and terrorist threat...
  13. Effectiveness of Mandatory Prescription Drug Monitoring
    Guohua Li; Fiscal Year: 2012
    ..of unintentional overdose morbidity and mortality are attributable to nonmedical use of opioid analgesics and benzodiazepines obtained from diversion and 'doctor shopping...
  14. In vitro screening of novel therapeutic agents for the treatment of alcohol abuse
    S John Mihic; Fiscal Year: 2010
    ..polyamines, metals and benzodiazepines) there is a strong rationale to support the idea that small compounds can be identified that antagonize the ..
  15. Genetic Epidemiology of Opioid Dependence in Bulgaria
    Alexandre A Todorov; Fiscal Year: 2010
    ..g., nicotine, alcohol, benzodiazepines) and mental disorders (e.g., childhood conduct disorder, ASPD, major depressive disorder, suicidality)...
  16. The Regulation of GABAA Receptor Cell Surface Stability
    Stephen Moss; Fiscal Year: 2009
    ..These receptors are also targets for several clinically important drug classes, including benzodiazepines, barbiturates, neurosteroids and general anesthetic...
  17. Regulation of voltage-gated calcium channels during chronic BZ treatment in rats
    DAMIEN EUGENE EARL; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Benzodiazepines (BZs) enhance inhibitory gamma-aminobutyric acid type A receptors (GABARs) in the central nervous system and are clinically used to treat insomnia, anxiety, and seizure disorders...
  18. Functional Imaging of Tremor Circuits and Mechanisms of Treatment Response.
    Fatta B Nahab; Fiscal Year: 2013
    ..Treatment of ET focuses on pharmacological agents of various mechanisms (e.g. b-blockers, anticonvulsants, benzodiazepines) and rarely deep brain stimulation of the Vim thalamus...
  19. Neurosteroid Treatment for OP Intoxication
    Doodipala Samba Reddy; Fiscal Year: 2013
    ..Current anticonvulsant countermeasures (benzodiazepines) for nerve intoxication do not sufficiently protect the brain from SE, a prolonged seizure activity lasting ..
  20. The role of ubiquitination in regulating GABA(A) receptor functional expression
    Stephen J Moss; Fiscal Year: 2010
    ..key sites of synaptic inhibition in the brain and are critical drug targets for therapeutic agents including benzodiazepines, barbiturates, general anesthetics and neurosteroids...
  21. Molecular genetic dissection of central amygdala microcircuitry underlying fear a
    David J Anderson; Fiscal Year: 2013
    ..that activation of PKC-4 neurons is required for the behavioral effects of anxiolytic drugs, such as benzodiazepines. These studies should begin to provide a functional dissection of the amygdala at the level of granularity of ..
  22. Effectiveness of Feeding Tubes Among Person with Advanced Cognitive Impairment
    Joan M Teno; Fiscal Year: 2010
    ..prevention and healing of pressure ulcers), risks (use of restraints, prescription of antipsychotics or benzodiazepines, and transitions to the ER and acute care hospital), and health care expenditures...
  23. Amygdalar neuropeptides and anxiety
    Marlene A Wilson; Fiscal Year: 2012
    ..neural basis of heightened anxiety states seen in chronic pain patients or during withdrawal from opiates, benzodiazepines, and alcohol...
  24. Pharmacotherapy to counterACT parathion-induced NMJ dysfunction
    Steven B Bird; Fiscal Year: 2013
    ..requires resuscitation with the use of atropine, followed by administration of oximes to reactivate AChE, and benzodiazepines to mitigate neurological complications...
  25. Structural investigation of a GABA receptor subtype
    DEREK CLAXTON; Fiscal Year: 2013
    ..Specifically, binding of commonly prescribed benzodiazepines, such as diazepam, enhances the observed Cl- conductance of receptors composed of 1/2/3 subunit isoforms...
  26. Neuroactive Steroid GABAA Receptor Positive Modulators for Fragile X Syndrome
    Albert J Robichaud; Fiscal Year: 2013
    ..Importantly, benzodiazepines, which do not bind to this type of receptor, have limited utility in patients with FXS because they are less ..
  27. Early Life Seizures and Development of Gabaergic Inhibition in the Human Brain
    Laura A Jansen; Fiscal Year: 2013
    ..The most frequently used anticonvulsant medications in this age group, the barbiturates and the benzodiazepines, act by enhancement of current through neuronal GABAA receptors...
  28. Novel Neuromuscular Protection to CounterACT Organophosphorus (OP) Poisoning
    Steven B Bird; Fiscal Year: 2012
    ..requires resuscitation with the use of atropine, followed by administration of oximes to reactivate AChE, and benzodiazepines to mitigate neurological complications...
  29. Regulation of GABAA Receptors by PKCe
    Robert O Messing; Fiscal Year: 2013
    ..regulates GABAA receptors by phosphorylating GABAA2 subunits at Ser-327, which reduces their sensitivity to benzodiazepines and ethanol...
  30. GABA(A) Receptor Modulation via the beta subunit
    Andrew Jenkins; Fiscal Year: 2010
    ..GABAA receptors also are important therapeutic targets for benzodiazepines and general anesthetics. Receptor function is also modulated by neurosteroids and many abused hypnotic drugs...
  31. Role of Parabrachial Nucleus Benzodiazepines in Gustatory Coding and Behavior
    David W Pittman; Fiscal Year: 2012
    ..Prior studies showed that benzodiazepines (BZDs;GABAA receptor agonists) potently increase consumption by enhancing palatability, and a key site of ..
  32. GABA Channel Activation Domains and Mechanisms
    David S Weiss; Fiscal Year: 2013
    ..Furthermore, GABA receptors are targets for a host of therapeutic and endogenous modulators such as benzodiazepines, barbiturates, and neurosteroids...
  33. Canine Status Epilepticus: A Translational Platform for Human Therapeutic Trials
    Ilo E Leppik; Fiscal Year: 2011
    ..Current guidelines for treatment incorporate drugs developed 30 to 70 or more years ago (phenytoin, benzodiazepines), which are not successful in more than 1/3 to 1/2 of cases (4)...
  34. Long-Term Chamomile Therapy of Generalized Anxiety Disorder
    Jun J Mao; Fiscal Year: 2013
    ..Generalized anxiety disorder (GAD) is a chronic, recurrent form of the disorder. Although benzodiazepines and serotonin reuptake inhibitors have become the mainstay therapy of GAD, these drugs are often associated ..
  35. GABA Modulation and Negative Affect in Psychosis
    Stephan F Taylor; Fiscal Year: 2010
    ..Pharmacotherapy of negative affects, particularly anxiety, often augments GABAergic function with benzodiazepines (BDZ)...
  36. The Effect of Alcohol Induced Insomnia on Cognitive Function and Cortical Replay
    William Bailey Glen; Fiscal Year: 2012
    ..sleep enhancers which similar clinical efficacy but fewer side-effects compared to traditional benzodiazepines. Of particular importance, zolpidem shows minimal risk of physical dependency, has limited effect on normal ..
  37. Sedation Management in Pediatric Patients with Acute Respiratory Failure
    MARTHA AQ CURLEY; Fiscal Year: 2013
    ..c] a Nurse-Implemented Goal-Directed Comfort Algorithm that guides moment-to-moment titration of opioids and benzodiazepines, and [d] team feedback on sedation management performance...
  38. Drugs of Abuse and Memory Span
    JOSEPH MARK GALIZIO; Fiscal Year: 2012
    ..compounds that are thought to have amnestic effects on olfactory memory using the span procedure including benzodiazepines (chlordiazepoxide, midazolam), NMDA antagonists (dizocilpine, ketamine), opiates (morphine), psychostimulants ..
  39. Sedation Strategy and Cognitive Outcome after Critical Illness in Early Childhood
    R Scott Watson; Fiscal Year: 2013
    ..of these young patients requires the use of sedating medications, most commonly combinations of opioids and benzodiazepines. Unfortunately, sedative use also carries risk...
  40. THE ROLE OF EPSILON SUBUNIT IN GABAA RECEPTOR FUNCTION
    David C Perry; Fiscal Year: 2010
    ..On the other hand anticonvulsant benzodiazepines and anesthetics that increase GABAA receptor activity are anticonvulsant...
  41. Regulation of GABAA Receptor Cell Surface Expression
    Nancy J Leidenheimer; Fiscal Year: 2010
    ..to binding GABA, the receptor is allosterically modulated by a variety of therapeutic agents, such as benzodiazepines (BZ) and barbiturates, that bind to distinct sites on the receptor...
  42. Pharmacepidemiology in the elderly: medications pneumonia risk and confounding
    Sascha Dublin; Fiscal Year: 2011
    ..First, she will investigate associations between use of specific medications-acid-suppressing medications, benzodiazepines, angiotensin-converting enzyme inhibitors (ACEIs), and statins-and risk of pneumonia, a common and serious ..
  43. Non-invasive Blood Alcohol Sensor for Emergency Room Applications
    MANAL BESHAY; Fiscal Year: 2013
    ..for quantitative (high/mid/low) measurement of six drugs of abuse (opiates, cocaine, amphetamines, THC, benzodiazepines, barbiturates), and develop the portable readout system...
  44. Molecular mechanism for the synaptic localization of GABA(A)Rs.
    James Martenson; Fiscal Year: 2013
    ..group of hetero-pentameric ion channels, are the target of both clinically relevant and abused drugs, such as benzodiazepines, barbiturates, inhaled anesthetics and ethanol...
  45. DISCRIMINATIVE EFFECTS OF BENZODIAZEPINE WITHDRAWAL
    Lisa R Gerak; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): Benzodiazepines are extremely important in the treatment of disorders, such as anxiety, insomnia and ethanol withdrawal. Unfortunately, these drugs have abuse and dependence liability...
  46. Gabapentin Treatment of Benzodiazepine Dependence
    John J Mariani; Fiscal Year: 2013
    ..The most commonly prescribed sedative-hypnotic agents are the benzodiazepines. Chronic use induces pharmacodynamic tolerance in the GABA neurotransmitter system and individuals with ..
  47. Evolution of cytochrome p450s for the diversification of drug scaffolds
    ERIC MICHAEL BRUSTAD; Fiscal Year: 2011
    ..to generate a panel of catalysts that site-selectively hydroxylate three privileged drug scaffolds: the benzodiazepines, the arylindoles, and the dihydropyridines...
  48. ANESTHETIC MECHANISMS AND GABA-A RECEPTOR STRUCTURE
    MYLES AKABAS; Fiscal Year: 2001
    ..Many drugs used in the induction of general anesthesia, including benzodiazepines, volatile and intravenous anesthetics and barbiturates potentiate GABA-induced currents...
  49. ANXIOLYTIC EFFECTS AND ABUSE OF BZ RECEPTOR LIGANDS
    James K Rowlett; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Benzodiazepines (BZs) are prescribed widely for the treatment of anxiety and sleep disorders...
  50. TREATMENT OF STATUS EPILEPTICUS
    Jaideep Kapur; Fiscal Year: 2013
    ..Many patients in SE do not respond to benzodiazepines, which are the only established treatment of this neurological emergency...
  51. Biosynthesis of Pyrrolo[1,4]benzodiazepines, potent antitumor antibiotics
    Steven E Rokita; Fiscal Year: 2012
    ..Pyrrolo[1,4]benzodiazepines, a class of potent antitumor antibiotics found in actinomycetes, are sequence selective DNA alkylating agents...
  52. Behavioral Effects of Neuroactive Steroids
    Lisa R Gerak; Fiscal Year: 2013
    ..Emerging evidence suggests that the chronic effects of neuroactive steroids are different from those of benzodiazepines;such differences can be exploited to improve our understanding of GABAA receptor function, particularly ..
  53. GABAA RECEPTOR CHANNEL ALTERATION BY PROLONGED SEIZURES
    Robert MacDonald; Fiscal Year: 2003
    ..Status epilepticus in humans is treated acutely with benzodiazepines as well as barbiturates, which enhance GABAR-mediated inhibition...
  54. Sleep disturbance as a risk factor for developing chronic pain
    Clifford J Woolf; Fiscal Year: 2013
    ..neurochemical systems, we will administer three classes of hypnotic drugs that act on different systems (benzodiazepines, orexin antagonists, and gamma hydroxybutyrate)...
  55. NEOPAIN MULTICENTER TRIAL: DATA COORDINATING CENTER
    Bruce Barton; Fiscal Year: 2001
    ..practices recorded prospectively in 109 Neonatal Intensive Care Units (NICUs) showed that opioids and benzodiazepines were most commonly used, with large variations in clinical practice. No analgesia/sedation was given to 73...
  56. Anticonvulsant Pharmacotherapy for Sedative-Hypnotic Use Disorders
    John J Mariani; Fiscal Year: 2010
    ..It is estimated that approximately one-third of patients in methadone maintenance treatment abuse benzodiazepines and there are no known effective treatments...
  57. Behavioral Pharmacology and GHB Physical Dependence
    Elise M Weerts; Fiscal Year: 2010
    ..dependence and the withdrawal syndrome reportedly resembles withdrawal from classic sedative-hypnotics (benzodiazepines and alcohol)...
  58. Emotional regulation: Modeling GABA A receptor subtype specific agents in mice
    Uwe Rudolph; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): GABAA receptors are the target of clinically used benzodiazepines, which modulate multiple GABAA receptor subtypes non-selectively...
  59. BENZODIAZEPINES AND THE GABA A RECEPTOR
    JOSEPH NEALE; Fiscal Year: 1999
    ..This includes analysis of the role of the receptor subunits in mediating the physiologic effects of benzodiazepines and barbiturates...
  60. Impact of Pharmacology on Duration of Ventilation in Patients with Resp Failure
    Athena F Zuppa; Fiscal Year: 2012
    ..of mechanical ventilation, such as level of awakeness, mandated titrations and total dose of opiates and benzodiazepines. However, within each group (intervention, control) and across the entire cohort, variation in the duration ..
  61. HEPATIC COMA--GLIAL BENZODIAZEPINE RECEPTORS & STEROIDS
    Michael Norenberg; Fiscal Year: 2000
    ..implicates ammonia, astrocytes, and excessive GABAergic activity mediated by elevated levels of endogenous benzodiazepines. During the prior funding period, the investigator studied the role of astrocytes, ammonia and ..
  62. BETA-CARBOLINES: VALIUM AGONISTS AND ANTAGONISTS
    James Cook; Fiscal Year: 1992
    ..The benzodiazepines (Bz) employed to treat anxiety are a group of compounds with wide therapeutic applications as anxiolytics, ..
  63. ABUSE LIABILITY OF COMMONLY PRESCRIBED HYPNOTICS
    CRAIG RUSH; Fiscal Year: 1999
    ..e., it produces adverse effects such as impaired performance and dependence). Benzodiazepines are among the most widely prescribed psychoactive drugs...
  64. ORAL BENZODIAZEPINE SELF ADMINISTRATION
    RICHARD MEISCH; Fiscal Year: 1999
    APPLICANT'S ABSTRACT: The introduction of new short-acting benzodiazepines and partial agonists has led to an increased interest in the reinforcing effects of the benzodiazepines...