An Inventory of Literature on the Relation Between Drug Use, Impaired Driving and Traffic Accidents
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(12) Patent Application Publication (10) Pub. No.: US 2012/0190743 A1 Bain Et Al
US 2012O190743A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0190743 A1 Bain et al. (43) Pub. Date: Jul. 26, 2012 (54) COMPOUNDS FOR TREATING DISORDERS Publication Classification OR DISEASES ASSOCATED WITH (51) Int. Cl NEUROKININ 2 RECEPTORACTIVITY A6II 3L/23 (2006.01) (75) Inventors: Jerald Bain, Toronto (CA); Joel CD7C 69/30 (2006.01) Sadavoy, Toronto (CA); Hao Chen, 39t. ii; C Columbia, MD (US); Xiaoyu Shen, ( .01) Columbia, MD (US) A6IPI/00 (2006.01) s A6IP 29/00 (2006.01) (73) Assignee: UNITED PARAGON A6IP II/00 (2006.01) ASSOCIATES INC., Guelph, ON A6IPI3/10 (2006.01) (CA) A6IP 5/00 (2006.01) A6IP 25/00 (2006.01) (21) Appl. No.: 13/394,067 A6IP 25/30 (2006.01) A6IP5/00 (2006.01) (22) PCT Filed: Sep. 7, 2010 A6IP3/00 (2006.01) CI2N 5/071 (2010.01) (86). PCT No.: PCT/US 10/48OO6 CD7C 69/33 (2006.01) S371 (c)(1) (52) U.S. Cl. .......................... 514/552; 554/227; 435/375 (2), (4) Date: Apr. 12, 2012 (57) ABSTRACT Related U.S. Application Data Compounds, pharmaceutical compositions and methods of (60) Provisional application No. 61/240,014, filed on Sep. treating a disorder or disease associated with neurokinin 2 4, 2009. (NK) receptor activity. Patent Application Publication Jul. 26, 2012 Sheet 1 of 12 US 2012/O190743 A1 LU 1750 15OO 1250 OOO 750 500 250 O O 20 3O 40 min SampleName: EM2OO617 Patent Application Publication Jul. 26, 2012 Sheet 2 of 12 US 2012/O190743 A1 kixto CFUgan <tro CFUgan FIG.2 Patent Application Publication Jul. -
The National Drugs List
^ ^ ^ ^ ^[ ^ The National Drugs List Of Syrian Arab Republic Sexth Edition 2006 ! " # "$ % &'() " # * +$, -. / & 0 /+12 3 4" 5 "$ . "$ 67"5,) 0 " /! !2 4? @ % 88 9 3: " # "$ ;+<=2 – G# H H2 I) – 6( – 65 : A B C "5 : , D )* . J!* HK"3 H"$ T ) 4 B K<) +$ LMA N O 3 4P<B &Q / RS ) H< C4VH /430 / 1988 V W* < C A GQ ") 4V / 1000 / C4VH /820 / 2001 V XX K<# C ,V /500 / 1992 V "!X V /946 / 2004 V Z < C V /914 / 2003 V ) < ] +$, [2 / ,) @# @ S%Q2 J"= [ &<\ @ +$ LMA 1 O \ . S X '( ^ & M_ `AB @ &' 3 4" + @ V= 4 )\ " : N " # "$ 6 ) G" 3Q + a C G /<"B d3: C K7 e , fM 4 Q b"$ " < $\ c"7: 5) G . HHH3Q J # Hg ' V"h 6< G* H5 !" # $%" & $' ,* ( )* + 2 ا اوا ادو +% 5 j 2 i1 6 B J' 6<X " 6"[ i2 "$ "< * i3 10 6 i4 11 6! ^ i5 13 6<X "!# * i6 15 7 G!, 6 - k 24"$d dl ?K V *4V h 63[46 ' i8 19 Adl 20 "( 2 i9 20 G Q) 6 i10 20 a 6 m[, 6 i11 21 ?K V $n i12 21 "% * i13 23 b+ 6 i14 23 oe C * i15 24 !, 2 6\ i16 25 C V pq * i17 26 ( S 6) 1, ++ &"r i19 3 +% 27 G 6 ""% i19 28 ^ Ks 2 i20 31 % Ks 2 i21 32 s * i22 35 " " * i23 37 "$ * i24 38 6" i25 39 V t h Gu* v!* 2 i26 39 ( 2 i27 40 B w< Ks 2 i28 40 d C &"r i29 42 "' 6 i30 42 " * i31 42 ":< * i32 5 ./ 0" -33 4 : ANAESTHETICS $ 1 2 -1 :GENERAL ANAESTHETICS AND OXYGEN 4 $1 2 2- ATRACURIUM BESYLATE DROPERIDOL ETHER FENTANYL HALOTHANE ISOFLURANE KETAMINE HCL NITROUS OXIDE OXYGEN PROPOFOL REMIFENTANIL SEVOFLURANE SUFENTANIL THIOPENTAL :LOCAL ANAESTHETICS !67$1 2 -5 AMYLEINE HCL=AMYLOCAINE ARTICAINE BENZOCAINE BUPIVACAINE CINCHOCAINE LIDOCAINE MEPIVACAINE OXETHAZAINE PRAMOXINE PRILOCAINE PREOPERATIVE MEDICATION & SEDATION FOR 9*: ;< " 2 -8 : : SHORT -TERM PROCEDURES ATROPINE DIAZEPAM INJ. -
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. -
Download Product Insert (PDF)
PRODUCT INFORMATION Chlormezanone Item No. 25716 CAS Registry No.: 80-77-3 Formal Name: 2-(4-chlorophenyl)tetrahydro-3-methyl-4H- O 1,3-thiazin-4-one, 1,1-dioxide Synonyms: (±)-Chlormezanone, NSC 169108 N MF: C11H12ClNO3S FW: 273.7 Purity: ≥98% S OO UV/Vis.: λmax: 228 nm Supplied as: A crystalline solid Cl Storage: -20°C Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Chlormezanone is supplied as a crystalline solid. A stock solution may be made by dissolving the chlormezanone in the solvent of choice. Chlormezanone is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of chlormezanone in these solvents is approximately 2, 20, and 10 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of chlormezanone can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of chlormezanone in PBS, pH 7.2, is approximately 0.1 mg/ml. We do not recommend storing the aqueous solution for more than one day. Description Chlormezanone is a centrally acting muscle relaxant.1 It induces paralysis in mice, guinea pigs, dogs, cats, and monkeys (EC50s = 133, <200, 100-250, 50, and 50 mg/kg, respectively). Chlormezanone increases ataxia induced by pentobarbital and alcohol in mice and blocks the crossed extensor reflex of the spine without affecting the knee-jerk reflex in cats. -
(12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig. -
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 -
Cochrane Library
Cochrane Library Cochrane Database of Systematic Reviews Sedation of children undergoing dental treatment (Review) Ashley PF, Chaudhary M, Lourenço-Matharu L Ashley PF, Chaudhary M, Lourenço-Matharu L. Sedation of children undergoing dental treatment. Cochrane Database of Systematic Reviews 2018, Issue 12. Art. No.: CD003877. DOI: 10.1002/14651858.CD003877.pub5. www.cochranelibrary.com Sedation of children undergoing dental treatment (Review) Copyright © 2018 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. Cochrane Trusted evidence. Informed decisions. Library Better health. Cochrane Database of Systematic Reviews T A B L E O F C O N T E N T S HEADER......................................................................................................................................................................................................... 1 ABSTRACT..................................................................................................................................................................................................... 1 PLAIN LANGUAGE SUMMARY....................................................................................................................................................................... 2 SUMMARY OF FINDINGS.............................................................................................................................................................................. 3 BACKGROUND............................................................................................................................................................................................. -
Withdrawing Benzodiazepines in Primary Care
PC\/ICU/ ADTiriC • CNS Drugs 2009,-23(1): 19-34 KtVltW MKIIWLC 1172-7047/I»/O(X)1«119/S4W5/C1 © 2009 Adis Dato Intocmation BV. All rights reserved. Withdrawing Benzodiazepines in Primary Care Malcolm Luder} Andre Tylee^ and ]ohn Donoghue^ 1 Institute of Psychiatry, King's College London, London, England 2 John Moores University, Liverpool, Scotland Contents Abstract ' 19 1. Benzodiazepine Usage 22 2. Interventions 23 2.1 Simple interventions 23 2.2 Piiarmacoiogicai interventions 25 2.3 Psychoiogical Interventions 26 2.4 Meta-Anaiysis ot Various interventions 27 3. Outcomes 28 4. Practicai Issues 29 5. Otiier Medications 30 5.1 Antidepressants 30 5.2 Symptomatic Treatments 30 6. Conciusions 31 Abstract The use of benzodiazepine anxiolytics and hypnotics continues to excite controversy. Views differ from expert to expert and from country to country as to the extent of the problem, or even whether long-term benzodiazepine use actually constitutes a problem. The adverse effects of these drugs have been extensively documented and their effectiveness is being increasingly questioned. Discontinua- tion is usually beneficial as it is followed by improved psychomotor and cognitive functioning, particularly in the elderly. The potential for dependence and addic- tion have also become more apparent. The licensing of SSRIs for anxiety disorders has widened the prescdbers' therapeutic choices (although this group of medications also have their own adverse effects). Melatonin agonists show promise in some forms of insomnia. Accordingly, it is now even more imperative that long-term benzodiazepine users be reviewed with respect to possible discon- tinuation. Strategies for discontinuation start with primary-care practitioners, who are still the main prescdbers. -
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. -
The Effects of Clobazam Upon Critical Flicker Fusion Thresholds: a Review
Drug Development Research Supplement 157-66 (1982) The Effects of Clobazam Upon Critical Flicker Fusion Thresholds: A Review A.C. Parrott Department of Psychology, University of Leeds, Leeds, England ABSTRACT Parrott, A.C.: The effects of clobazam upon critical flicker fusion thresholds: a review. Drug Dev. Res. S1:057-066,1982. The effects of the 1,5-bentodiazepinederivative clobazam upon critical flicker fusion (CFF) values in normal subjects is reviewed. All studies reviewed were double-blind and placebo controlled. Single acute doses of 10 or 20 mg did not lead to significant CFF changes, whereas repeated doses of 20 mg clobazam a day for 4 days produced a significant elevation in CFF thresholds. Possible pharmacokinetic reasons for this CFF elevation after repeated doses are discussed. Equivalent investigations of clobazam at higher dose levels (30 to 60 mg) showed a similar difference in the effects of acute versus repeated doses; single acute doses led to significant CFF decrements, while repeated administrations led to similar clobazam and placebo CFF levels. The patterns of CFF changes with this 13- benzodiazepine anxiolytic agent seems to be different from the CFF changes generally reported with the 1,Cbenzodiazepine anxiolytic agents (generally CFF reductions), and suggests possible central nervous system alerting affects after repeated administration at the lower dose levels. Key words: critical flicker fusion, clobazam, benzodlazeplnes, arousal, anxlety INTRODUCTION Critical flicker fusion (CFF) threshold values have been investigated in psychopharmaco- logical investigations involving a wide variety of psychotropic agents. Smith and Misiac [1976] in their review of the effects upon CFF of acute single doses of psychotropic agents, concluded that the direction of the CFF change was clearly related to the nature of the psychotropic agent. -
Customs Tariff - Schedule
CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2020 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels.