Analytical Methods for Determination of Benzodiazepines. a Short Review
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WHO Drug Information Vol. 12, No. 3, 1998
WHO DRUG INFORMATION VOLUME 12 NUMBER 3 • 1998 RECOMMENDED INN LIST 40 INTERNATIONAL NONPROPRIETARY NAMES FOR PHARMACEUTICAL SUBSTANCES WORLD HEALTH ORGANIZATION • GENEVA Volume 12, Number 3, 1998 World Health Organization, Geneva WHO Drug Information Contents Seratrodast and hepatic dysfunction 146 Meloxicam safety similar to other NSAIDs 147 Proxibarbal withdrawn from the market 147 General Policy Issues Cholestin an unapproved drug 147 Vigabatrin and visual defects 147 Starting materials for pharmaceutical products: safety concerns 129 Glycerol contaminated with diethylene glycol 129 ATC/DDD Classification (final) 148 Pharmaceutical excipients: certificates of analysis and vendor qualification 130 ATC/DDD Classification Quality assurance and supply of starting (temporary) 150 materials 132 Implementation of vendor certification 134 Control and safe trade in starting materials Essential Drugs for pharmaceuticals: recommendations 134 WHO Model Formulary: Immunosuppressives, antineoplastics and drugs used in palliative care Reports on Individual Drugs Immunosuppresive drugs 153 Tamoxifen in the prevention and treatment Azathioprine 153 of breast cancer 136 Ciclosporin 154 Selective serotonin re-uptake inhibitors and Cytotoxic drugs 154 withdrawal reactions 136 Asparaginase 157 Triclabendazole and fascioliasis 138 Bleomycin 157 Calcium folinate 157 Chlormethine 158 Current Topics Cisplatin 158 Reverse transcriptase activity in vaccines 140 Cyclophosphamide 158 Consumer protection and herbal remedies 141 Cytarabine 159 Indiscriminate antibiotic -
Uso Adecuado De BZD En Insomnio Y Ansiedad.Pdf
Vol. 6 Nº 1 · OCTUBRE 2014 BOLETÍN CANARIO DE USO RACIONAL DEL MEDICAMENTO DEL SCS Uso adecuado de BENZODIAZEPINAS en insomnio y ansiedad. SUMARIO PERFIL FARMACOLÓGICO DE LAS BZD (Tabla 1). - INTRODUCCIÓN 1 - PERFIL FARMACOLÓGICO DE LAS BENZODIAZEPINAS 1 No todas las BZD son iguales, ni tienen las mismas indicaciones. - BENZODIAZEPINAS EN EL INSOMNIO 2 Conocer algunos aspectos sobre su perfil farmacológico es esencial para realizar una prescripción adecuada y segura. - BENZODIAZEPINAS EN LA ANSIEDAD 4 - RECOMENDACIONES PARA SUSPENDER 5 Por lo general las BZD se absorben muy bien por vía oral, mientras TRATAMIENTOS CON BZD que la vía intramuscular presenta una absorción lenta e irregular, por - BIBLIOGRAFÍA 7 lo que no suele ser muy recomendada. En situaciones de emergencia (convulsiones) es preferible utilizar la vía endovenosa. INTRODUCCIÓN Inicio de acción y vida media: el inicio de acción es distinto según el principio activo y constituye un criterio fundamental en la selección de Las benzodiazepinas (BZD) son psicofármacos que actúan aumentan- las BZD. Puede ser: de inicio rápido (0,5-1 h), de utilidad en el insomnio do la acción del ácido gammaaminobutírico (GABA), principal neuro- de conciliación y en crisis de ansiedad; de inicio intermedio (1-3 h) o transmisor inhibidor del sistema nervioso central. Tienen indicaciones de inicio lento (> 3 h), preferibles en insomnio de mantenimiento o terapéuticas diversas, y auque su uso más habitual es en el tratamien- despertar precoz y en la ansiedad generalizada. to de la ansiedad e insomnio, también se utilizan en la inducción a la anestesia, en el tratamiento de las crisis comiciales, en el síndrome La vida media de las BZD es otro de los criterios de selección y puede 5 de abstinencia alcohólica, como tratamiento coadyuvante de de dolor ser : corta (< 6 h); intermedia (6-24 h) y larga (> 24 h). -
Ionization Energies of Benzodiazepines Salvatore Millefiori, Andrea Alparone
Electronic properties of neuroleptics: ionization energies of benzodiazepines Salvatore Millefiori, Andrea Alparone To cite this version: Salvatore Millefiori, Andrea Alparone. Electronic properties of neuroleptics: ionization energies of benzodiazepines. Journal of Molecular Modeling, Springer Verlag (Germany), 2010, 17 (2), pp.281- 287. 10.1007/s00894-010-0723-7. hal-00590996 HAL Id: hal-00590996 https://hal.archives-ouvertes.fr/hal-00590996 Submitted on 6 May 2011 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. Editorial Manager(tm) for Journal of Molecular Modeling Manuscript Draft Manuscript Number: JMMO1191R1 Title: Electronic properties of neuroleptics: ionization energies of benzodiazepines Article Type: Original paper Keywords: Benzodiazepines; vertical ionization energies; vertical electron affinities; DFT calculations; electron propagator theory calculations. Corresponding Author: Prof. Salvatore Millefiori, Corresponding Author's Institution: First Author: Salvatore Millefiori Order of Authors: Salvatore Millefiori; Andrea Alparone Abstract: Abstract. Vertical ionization energies (VIEs) of medazepam and nordazepam and of their molecular subunits have been calculated with the electron propagator method in the P3/CEP-31G* approximation. Vertical electron affinities (VEAs) have been obtained with a ΔSCF procedure at the DFT-B3LYP/6-31+G* level of theory. Excellent correlations have been achieved between IEcalc and IEexp allowing reliable assignment of the ionization processes. -
(12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn Et Al
US 2004O224012A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn et al. (43) Pub. Date: Nov. 11, 2004 (54) TOPICAL APPLICATION AND METHODS Related U.S. Application Data FOR ADMINISTRATION OF ACTIVE AGENTS USING LIPOSOME MACRO-BEADS (63) Continuation-in-part of application No. 10/264,205, filed on Oct. 3, 2002. (76) Inventors: Pichit Suvanprakorn, Bangkok (TH); (60) Provisional application No. 60/327,643, filed on Oct. Tanusin Ploysangam, Bangkok (TH); 5, 2001. Lerson Tanasugarn, Bangkok (TH); Suwalee Chandrkrachang, Bangkok Publication Classification (TH); Nardo Zaias, Miami Beach, FL (US) (51) Int. CI.7. A61K 9/127; A61K 9/14 (52) U.S. Cl. ............................................ 424/450; 424/489 Correspondence Address: (57) ABSTRACT Eric G. Masamori 6520 Ridgewood Drive A topical application and methods for administration of Castro Valley, CA 94.552 (US) active agents encapsulated within non-permeable macro beads to enable a wider range of delivery vehicles, to provide longer product shelf-life, to allow multiple active (21) Appl. No.: 10/864,149 agents within the composition, to allow the controlled use of the active agents, to provide protected and designable release features and to provide visual inspection for damage (22) Filed: Jun. 9, 2004 and inconsistency. US 2004/0224012 A1 Nov. 11, 2004 TOPCAL APPLICATION AND METHODS FOR 0006 Various limitations on the shelf-life and use of ADMINISTRATION OF ACTIVE AGENTS USING liposome compounds exist due to the relatively fragile LPOSOME MACRO-BEADS nature of liposomes. Major problems encountered during liposome drug Storage in vesicular Suspension are the chemi CROSS REFERENCE TO OTHER cal alterations of the lipoSome compounds, Such as phos APPLICATIONS pholipids, cholesterols, ceramides, leading to potentially toxic degradation of the products, leakage of the drug from 0001) This application claims the benefit of U.S. -
Understanding Benzodiazephine Use, Abuse, and Detection
Siemens Healthcare Diagnostics, the leading clinical diagnostics company, is committed to providing clinicians with the vital information they need for the accurate diagnosis, treatment and monitoring of patients. Our comprehensive portfolio of performance-driven systems, unmatched menu offering and IT solutions, in conjunction with highly responsive service, is designed to streamline workflow, enhance operational efficiency and support improved patient care. Syva, EMIT, EMIT II, EMIT d.a.u., and all associated marks are trademarks of General Siemens Healthcare Diagnostics Inc. All Drugs other trademarks and brands are the Global Division property of their respective owners. of Abuse Siemens Healthcare Product availability may vary from Diagnostics Inc. country to country and is subject 1717 Deerfield Road to varying regulatory requirements. Deerfield, IL 60015-0778 Please contact your local USA representative for availability. www.siemens.com/diagnostics Siemens Global Headquarters Global Siemens Healthcare Headquarters Siemens AG Understanding Wittelsbacherplatz 2 Siemens AG 80333 Muenchen Healthcare Sector Germany Henkestrasse 127 Benzodiazephine Use, 91052 Erlangen Germany Abuse, and Detection Telephone: +49 9131 84 - 0 www.siemens.com/healthcare www.usa.siemens.com/diagnostics Answers for life. Order No. A91DX-0701526-UC1-4A00 | Printed in USA | © 2009 Siemens Healthcare Diagnostics Inc. Syva has been R1 R2 a leading developer N and manufacturer of AB R3 X N drugs-of-abuse tests R4 for more than 30 years. R2 C Now part of Siemens Healthcare ® Diagnostics, Syva boasts a long and Benzodiazepines have as their basic chemical structure successful track record in drugs-of-abuse a benzene ring fused to a seven-membered diazepine ring. testing, and leads the industry in the All important benzodiazepines contain a 5-aryl substituent ring (ring C) and a 1,4–diazepine ring. -
Retention Behaviour of Some Benzodiazepines in Solid-Phase Extraction Using Modified Silica Adsorbents Having Various Hydrophobicities
ACADEMIA ROMÂNĂ Rev. Roum. Chim., Revue Roumaine de Chimie 2015, 60(9), 891-898 http://web.icf.ro/rrch/ RETENTION BEHAVIOUR OF SOME BENZODIAZEPINES IN SOLID-PHASE EXTRACTION USING MODIFIED SILICA ADSORBENTS HAVING VARIOUS HYDROPHOBICITIES Elena BACALUM,a Mihaela CHEREGIb,* and Victor DAVIDb,* a Research Institute from University of Bucharest – ICUB, 36-46 M. Kogalniceanu Blvd., Bucharest, 050107, Roumania b University of Bucharest, Faculty of Chemistry, Department of Analytical Chemistry, 90 Panduri Ave, Bucharest – 050663, Roumania Received April 6, 2015 The retention properties of six benzodiazepines (alprazolam, bromazepam, diazepam, flunitrazepam, medazepam, and nitrazepam) on four different solid phase extraction silica 1.0 adsorbents with various hydrophobicities (octadecylsilica, octylsilica, phenylsilica, and cyanopropylsilica) were 0.8 H O investigated. The breakthrough curves showed a significant N retention of these compounds on octadecylsilica, octylsilica, 0.6 Br N phenylsilica, excepting alprazolam that has a poor retention on 0 C/C N octadecylsilica. These results can be explained by the 0.4 PHENYL CN hydrophobic character of studied benzodiazepines (octanol- C18 0.2 C8 Bromazepam water partition constant, log Kow, being situated within the interval 1.90-4.45). A poor retention on cyanopropylsilica was 0.0 observed for all studied compounds indicating that π-π and 0 102030405060708090100 Volume (mL) polar intermolecular interactions have a less significant role in their retention on this adsorbent. Generally, the breakthrough -
Tel: 86-2985324244; Fax: 86-2985252580
medRxiv preprint doi: https://doi.org/10.1101/2020.02.27.20028605; this version posted February 27, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted medRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC 4.0 International license . Efficacy and Acceptability Comparisons of Cognitive Behavior Therapy, Drugs, and Their Combination for Panic Disorder in Adults: a Network Meta-analysis Fengjie Gao(M.M.)1,a, Hairong He(M.M.)2,a, Bin Yan(M.M.)2, Jian Yang(M.M.)2, Yajuan Fan(M.D.)1, Binbin Zhao(M.M.)1, Xiaoyan He(M.M.)1, Qingyan Ma(M.M.)1, Baijia Li(M.D.)1, Yuan Gao(M.D.)1, Li Qian(M.D.)1, Zai Yang(M.M.)1, Ce Chen(M.M.)1, Yunchun Chen(M.D.)1, Chengge Gao(M.D.)1, Feng Zhu(M.D.)5, Wei Wang(M.M.)1,*, Xiancang Ma(M.D.)1,3,4,* 1Department of Psychiatry, The First Affiliated Hospital of Xi'an Jiaotong University, 277 Yanta West Road, 710061 Xi’an, Shaanxi, China. 2Clinical Research Center, The First Affiliated Hospital of Xi'an Jiaotong University, 277 Yanta West Road, 710061 Xi’an, Shaanxi, China. 3Center for Brain Science, The First Affiliated Hospital of Xi’an Jiaotong University, 277 Yanta West Road, 710061 Xi’an, Shaanxi, China. 4Clinical Research center for Psychiatric Medicine of Shaanxi Province, The First Affiliated Hospital of Xi'an Jiaotong University, 277 Yanta West Road, 710061 Xi’an, Shaanxi, China. -
GABA Receptors
D Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews • BIOTREND Reviews Review No.7 / 1-2011 GABA receptors Wolfgang Froestl , CNS & Chemistry Expert, AC Immune SA, PSE Building B - EPFL, CH-1015 Lausanne, Phone: +41 21 693 91 43, FAX: +41 21 693 91 20, E-mail: [email protected] GABA Activation of the GABA A receptor leads to an influx of chloride GABA ( -aminobutyric acid; Figure 1) is the most important and ions and to a hyperpolarization of the membrane. 16 subunits with γ most abundant inhibitory neurotransmitter in the mammalian molecular weights between 50 and 65 kD have been identified brain 1,2 , where it was first discovered in 1950 3-5 . It is a small achiral so far, 6 subunits, 3 subunits, 3 subunits, and the , , α β γ δ ε θ molecule with molecular weight of 103 g/mol and high water solu - and subunits 8,9 . π bility. At 25°C one gram of water can dissolve 1.3 grams of GABA. 2 Such a hydrophilic molecule (log P = -2.13, PSA = 63.3 Å ) cannot In the meantime all GABA A receptor binding sites have been eluci - cross the blood brain barrier. It is produced in the brain by decarb- dated in great detail. The GABA site is located at the interface oxylation of L-glutamic acid by the enzyme glutamic acid decarb- between and subunits. Benzodiazepines interact with subunit α β oxylase (GAD, EC 4.1.1.15). It is a neutral amino acid with pK = combinations ( ) ( ) , which is the most abundant combi - 1 α1 2 β2 2 γ2 4.23 and pK = 10.43. -
Information to Users
Confirmation of urinary benzodiazepines by gas chromatography/mass spectrometry Item Type text; Thesis-Reproduction (electronic) Authors West, Robert E., 1952- Publisher The University of Arizona. Rights Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author. Download date 06/10/2021 02:51:08 Link to Item http://hdl.handle.net/10150/277228 INFORMATION TO USERS The most advanced technology has been used to photo graph and reproduce this manuscript from the microfilm master. UMI films the text directly from the original or copy submitted. Thus, some thesis and dissertation copies are in typewriter face, while others may be from any type of computer printer. The quality of this reproduction is dependent upon the quality of the copy submitted. Broken or indistinct print, colored or poor quality illustrations and photographs, print bleedthrough, substandard margins, and improper alignment can adversely affect reproduction. In the unlikely event that the author did not send UMI a complete manuscript and there are missing pages, these will be noted. Also, if unauthorized copyright material had to be removed, a note will indicate the deletion. Oversize materials (e.g., maps, drawings, charts) are re produced by sectioning the original, beginning at the upper left-hand corner and continuing from left to right in equal sections with small overlaps. Each original is also photographed in one exposure and is included in reduced form at the back of the book. -
The Misuse of Benzodiazepines Among High-Risk Opioid Users in Europe
EMBARGO — 7 JUNE 7. 6. 2018 UPDATED 11:30 Central European Time/CET (10:30 Western European Time/WET/Lisbon) Proof - 28 May 2018 not for circulation PERSPECTIVES ON DRUGS The misuse of benzodiazepines among high-risk opioid users in Europe Benzodiazepines are a widely prescribed I Introduction group of medicines with a range of clinical uses that include treating Benzodiazepines have a range of clinical uses and are among the most commonly prescribed medicines globally. anxiety, insomnia and managing alcohol They are useful in the short-term treatment of anxiety and withdrawal. This group of medicines is insomnia, and in managing alcohol withdrawal (Medicines often misused by high-risk opioid users, and Healthcare Products Regulatory Agency, 2015). Like all medicines, benzodiazepines can produce side effects. They and this is associated with considerable may also be misused, which we define as use without a morbidity and mortality. This paper prescription from a medical practitioner or, if prescribed, when describes the impact of benzodiazepines they are used outside accepted medical practice or guidelines. misuse on the health and treatment of While the misuse of benzodiazepines has been identified high-risk opioid users. as a concern for large groups in the general population, for example, among elderly people and women, this analysis focuses specifically on misuse among high-risk opioid users (1), a group of people among whom these medicines have been linked with severe treatment challenges and implicated in considerable numbers of drug-related deaths. It is important to stress that much benzodiazepine prescribing to high-risk drug users is done with legitimate therapeutic aims in mind. -
Comparative Efficacy and Acceptability of Pharmacological Treatments for Insomnia in Adults: a Systematic Review and Network Meta-Analysis (Protocol)
Cochrane Database of Systematic Reviews Comparative efficacy and acceptability of pharmacological treatments for insomnia in adults: a systematic review and network meta-analysis (Protocol) De Crescenzo F, Foti F, Ciabattini M, Del Giovane C, Watanabe N, Sañé Schepisi M, Quested DJ, Cipriani A, Barbui C, Amato L De Crescenzo F, Foti F, Ciabattini M, Del Giovane C, Watanabe N, Sañé Schepisi M, Quested DJ, Cipriani A, Barbui C, Amato L. Comparative efficacy and acceptability of pharmacological treatments for insomnia in adults: a systematic review and network meta-anal- ysis. Cochrane Database of Systematic Reviews 2016, Issue 9. Art. No.: CD012364. DOI: 10.1002/14651858.CD012364. www.cochranelibrary.com Comparative efficacy and acceptability of pharmacological treatments for insomnia in adults: a systematic review and network meta- analysis (Protocol) Copyright © 2016 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. TABLE OF CONTENTS HEADER....................................... 1 ABSTRACT ...................................... 1 BACKGROUND .................................... 1 OBJECTIVES ..................................... 4 METHODS ...................................... 4 Figure1. ..................................... 5 ACKNOWLEDGEMENTS . 9 REFERENCES ..................................... 10 APPENDICES ..................................... 14 WHAT’SNEW..................................... 18 CONTRIBUTIONSOFAUTHORS . 18 DECLARATIONSOFINTEREST . 18 Comparative efficacy and acceptability of pharmacological treatments for -
International Journal of Pharma and Bio Sciences ISSN 0975-6299 1,5
Int J Pharm Bio Sci 2013 July; 4(3): (P) 345 - 370 Review Article Medicinal Chemistry International Journal of Pharma and Bio Sciences ISSN 0975-6299 1,5-BENZODIAZEPINE: A VERSATILE PHARMACOPHORE P.S. SALVE* AND D.S. MALI Department of Pharmaceutical Chemistry, KLE University’s College of Pharmacy, Belgaum, Karnataka, India. ABSTRACT Diazepines are an eminent class of drugs owing to their psychotherapeutic activities. Among these, 1,5-benzodiazepines are regarded as privileged structures due to their clinical importance and commercial success. Although immense work has been carried out on the benzodiazepine nucleus, it continues to receive a great deal of attention. Due to their vast range of biological properties the benzodiazepine nucleus has fascinated many investigators to synthesize and screen the analogues for all possible activities through all possible routes. This current review article mainly covers the various routes of synthesis utilized, the numerous solvents employed, catalysts used and the different pharmacological activities exhibited by 1,5-benzodiazepine derivatives. This review encompasses the research work that has been accomplished since the past decade. KEYWORDS: 1,5-Benzodiazepines, o-Phenylenediamines, Synthesis, Catalyst, Diazepines P.S. SALVE Department of Pharmaceutical Chemistry, KLE University’s College of Pharmacy, Belgaum, Karnataka, India. *Corresponding author This article can be downloaded from www.ijpbs.net P - 345 Int J Pharm Bio Sci 2013 July; 4(3): (P) 345 - 370 INTRODUCTION Benzodiazepines are an important class of activities.1,2 They have also been used in nitrogen containing heterocyclic compounds treatment of viral diseases3,4, cardiovascular acting mainly on the central nervous system. disorders5 and as cholecystokinin (CCK) They have attracted much attention in the field receptor antagonists.6,7The 1,5-benzodiazepine of medicine and pharmaceuticals due to their scaffold is extremely versatile and has featured broad spectrum of biological activities.