Endothelial Dysfunction in Heart Failure and Ischemic Heart Disease: Rationale for the Clinical Use of Mononitrates
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Tolerance and Resistance to Organic Nitrates in Human Blood Vessels
\ö-\2- Tolerance and Resistance to Organic Nitrates in Human Blood Vessels Peter Radford Sage MBBS, FRACP Thesis submit.ted for the degree of Doctor of Philosuphy Department of Medicine University of Adelaide and Cardiology Unit The Queen Elizabeth Hospital I Table of Gontents Summary vii Declaration x Acknowledgments xi Abbreviations xil Publications xtil. l.INTRODUCTION l.L Historical Perspective I i.2 Chemical Structure and Available Preparations I 1.3 Cellular/biochemical mechanism of action 2 1.3.1 What is the pharmacologically active moiety? 3 1.3.2 How i.s the active moiety formed? i 4 1.3.3 Which enzyme system(s) is involved in nitrate bioconversi<¡n? 5 1.3.4 What is the role of sulphydryl groups in nitrate action? 9 1.3.5 Cellular mechanism of action after release of the active moiety 11 1.4 Pharmacokinetics t2 1.5 Pharmacological Effects r5 1.5.1 Vascular effects 15 l.5.2Platelet Effects t7 1.5.3 Myocardial effects 18 1.6 Clinical Efhcacy 18 1.6.1 Stable angina pectoris 18 1.6.2 Unstable angina pectoris 2t 1.6.3 Acute myocardial infarction 2l 1.6.4 Congestive Heart Failure 23 ll 1.6.5 Other 24 1.7 Relationship with the endothelium and EDRF 24 1.7.1 EDRF and the endothelium 24 1.7.2 Nitrate-endothelium interactions 2l 1.8 Factors limiting nitrate efficacy' Nitrate tolerance 28 1.8.1 Historical notes 28 1.8.2 Clinical evidence for nitrate tolerance 29 1.8.3 True/cellular nitrate tolerance 31 1.8.3.1 Previous studies 31 | .8.3.2 Postulated mechanisms of true/cellular tolerance JJ 1.8.3.2.1 The "sulphydryl depletion" hypothesis JJ 1.8.3.2.2 Desensitization of guanylate cyclase 35 1 8.i.?..3 Impaired nitrate bioconversion 36 1.8.3.2.4'Ihe "superoxide hypothesis" 38 I.8.3.2.5 Other possible mechanisms 42 1.8.4 Pseudotolerance ; 42 1.8.4. -
21 CFR Ch. I (4–1–05 Edition)
§ 250.102 21 CFR Ch. I (4–1–05 Edition) health, inhalers containing meth- any use other than management of an- amphetamine or methamphetamine gina pectoris, or that is represented to salts (d-desoxyephedrine, or dl-desoxy- be efficacious for any other purpose by ephedrine, or their salts), as well as reason of its containing such drug, will amphetamine inhalers should be re- be regarded by the Food and Drug Ad- stricted to prescription sale and should ministration as misbranded and subject be labeled with the statement ‘‘Rx to regulatory proceedings, unless such only.’’ recommendations are covered by the approval of a new-drug application [40 FR 14033, Mar. 27, 1975, as amended at 67 FR 4906, Feb. 1, 2002] based on a showing of safety and effec- tiveness. § 250.102 Drug preparations intended (d) Any such drug in long-acting dos- for human use containing certain age form is regarded as a new drug that ‘‘coronary vasodilators’’. requires an approved new-drug applica- (a)(1) The Food and Drug Administra- tion before marketing. tion finds that the following ‘‘coronary (e) Any of the drugs listed in para- vasodilators’’ are extensively regarded graph (a)(2) of this section is regarded by physicians as safe and useful as em- as a new drug that requires an ap- ployed under medical supervision for proved new-drug application. Articles the management of angina pectoris in for which new-drug approvals are now some patients: in effect should be covered by supple- mental new-drug applications as nec- Amyl nitrite. essary to provide for labeling revisions Erythrityl tetranitrate. -
Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany). -
Health Reports for Mutual Recognition of Medical Prescriptions: State of Play
The information and views set out in this report are those of the author(s) and do not necessarily reflect the official opinion of the European Union. Neither the European Union institutions and bodies nor any person acting on their behalf may be held responsible for the use which may be made of the information contained therein. Executive Agency for Health and Consumers Health Reports for Mutual Recognition of Medical Prescriptions: State of Play 24 January 2012 Final Report Health Reports for Mutual Recognition of Medical Prescriptions: State of Play Acknowledgements Matrix Insight Ltd would like to thank everyone who has contributed to this research. We are especially grateful to the following institutions for their support throughout the study: the Pharmaceutical Group of the European Union (PGEU) including their national member associations in Denmark, France, Germany, Greece, the Netherlands, Poland and the United Kingdom; the European Medical Association (EMANET); the Observatoire Social Européen (OSE); and The Netherlands Institute for Health Service Research (NIVEL). For questions about the report, please contact Dr Gabriele Birnberg ([email protected] ). Matrix Insight | 24 January 2012 2 Health Reports for Mutual Recognition of Medical Prescriptions: State of Play Executive Summary This study has been carried out in the context of Directive 2011/24/EU of the European Parliament and of the Council of 9 March 2011 on the application of patients’ rights in cross- border healthcare (CBHC). The CBHC Directive stipulates that the European Commission shall adopt measures to facilitate the recognition of prescriptions issued in another Member State (Article 11). At the time of submission of this report, the European Commission was preparing an impact assessment with regards to these measures, designed to help implement Article 11. -
United States Patent 19 11) Patent Number: 5,665,766 Byrne Et Al
US005665766A United States Patent 19 11) Patent Number: 5,665,766 Byrne et al. 45 Date of Patent: Sep. 9, 1997 54 ESTER OF AN ORGANIC NTRATE AND A FOREIGN PATENT DOCUMENTS SALCYTLATE 044.9426 10/1991 European Pat. Off.. 75 Inventors: William Byrne, Dublin; Andrew WO 92/O1668 2/1992 WIPO. Rynne, Clane, both of Ireland WO 92/16506 10/1992 WIPO . OTHER PUBLICATIONS 73 Assignee: Cal International Limited, Dublin, reland European HeartJournal, vol. 12. Sup.A. 1991, pp. 2-4 "Why Use a Nitrate in 1990'. 21 Appl. No.: 374,650 European Heart Journal, vol. 9, Supp. A 1988, pp. 45-49 22 PCT Filled: Jul. 26, 1993 "Mechanisms For The In Vivo Antiplatelet Effects of Isos orbide Dinitrate'. 86 PCT No.: PCT/E93/00040 Eur, J. Clin. Pharmacology, vol. 25, 1983, pp. 779-782 $371 Date: Jan. 30, 1995 "Pharmacological Internaction Between Nitroglycerin and Asprin After Acute and Chronic Aspirin Treatment of S 102(e) Date: Jan. 30, 1995 Healthy Subjects". 87 PCT Pub. No.: WO94/03421 J. Cardiovascular Pharmacology, vol. 5. No. 5, 1983, pp. 874-877 "Influence of Aspirin on the Hemodynamic Effects PCT Pub. Date: Feb. 17, 1994 of Sublingual Nitroglycerin". Foreign Application Priority Data AN 100 : 12587 Kim et al., "Pharmaceutical Studies on the 30 Estimation of Chloramphinzol with Antipyretics”. Yahihak Jul. 30, 1992 (E) Ireland ................................... 92.2474 Hoech, 27(3), 207-13. Abstract Only 1983. 51) Int. Cl. ............... A61K 31/34; CO7D 493/00 Primary Examiner-Marianne M. Cintins 52 U.S. Cl. ......................... 514/470; 514/475; 514/533; Assistant Examiner-Keith MacMillan 514/548; 549/464 Attorney, Agent, or Firm-Jacobson, Price, Holman & 58 Field of Search .................................... -
Title 16. Crimes and Offenses Chapter 13. Controlled Substances Article 1
TITLE 16. CRIMES AND OFFENSES CHAPTER 13. CONTROLLED SUBSTANCES ARTICLE 1. GENERAL PROVISIONS § 16-13-1. Drug related objects (a) As used in this Code section, the term: (1) "Controlled substance" shall have the same meaning as defined in Article 2 of this chapter, relating to controlled substances. For the purposes of this Code section, the term "controlled substance" shall include marijuana as defined by paragraph (16) of Code Section 16-13-21. (2) "Dangerous drug" shall have the same meaning as defined in Article 3 of this chapter, relating to dangerous drugs. (3) "Drug related object" means any machine, instrument, tool, equipment, contrivance, or device which an average person would reasonably conclude is intended to be used for one or more of the following purposes: (A) To introduce into the human body any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (B) To enhance the effect on the human body of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; (C) To conceal any quantity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state; or (D) To test the strength, effectiveness, or purity of any dangerous drug or controlled substance under circumstances in violation of the laws of this state. (4) "Knowingly" means having general knowledge that a machine, instrument, tool, item of equipment, contrivance, or device is a drug related object or having reasonable grounds to believe that any such object is or may, to an average person, appear to be a drug related object. -
Nitric Oxide Releasing Chelating Agents and Their
Europäisches Patentamt *EP001060174B1* (19) European Patent Office Office européen des brevets (11) EP 1 060 174 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.7: C07D 401/12, A61K 31/44 of the grant of the patent: 22.09.2004 Bulletin 2004/39 (86) International application number: PCT/GB1998/003840 (21) Application number: 98962567.8 (87) International publication number: (22) Date of filing: 18.12.1998 WO 1999/033823 (08.07.1999 Gazette 1999/27) (54) NITRIC OXIDE RELEASING CHELATING AGENTS AND THEIR THERAPEUTIC USE STICKSTOFFOXID FREISETZENDE CHELATBILDNER UND IHRE THERAPEUTISCHE VERWENDUNG CHELATEURS LIBERANT DE L’OXYDE NITRIQUE ET LEUR EMPLOI A DES FINS THERAPEUTIQUES (84) Designated Contracting States: (74) Representative: AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU Hammett, Audrey Grace Campbell et al MC NL PT SE Amersham plc Amersham Place (30) Priority: 23.12.1997 GB 9727226 Little Chalfont, Bucks. HP7 9NA (GB) 13.03.1998 GB 9805450 (56) References cited: (43) Date of publication of application: EP-A- 0 292 761 WO-A-93/20806 20.12.2000 Bulletin 2000/51 WO-A-95/12394 WO-A-96/31217 WO-A-96/39409 WO-A-97/49390 (73) Proprietor: Amersham Health AS US-A- 5 250 550 0401 Oslo (NO) • MOORADIAN D L ET AL: "NITRIC OXIDE (NO) (72) Inventors: DONOR MOLECULES: EFFECT OF NO • TOWART, Robertson RELEASE RATE ON VASCULAR SMOOTH Stoke Poges SL2 4PT (GB) MUSCLE CELL PROLIFERATION IN VITRO" • KARLSSON, Jan, Olof, Gustav JOURNAL OF CARDIOVASCULAR N-1450 Nesoddtangen (NO) PHARMACOLOGY, vol. -
(12) United States Patent (10) Patent No.: US 9,636.405 B2 Tamarkin Et Al
USOO9636405B2 (12) United States Patent (10) Patent No.: US 9,636.405 B2 Tamarkin et al. (45) Date of Patent: May 2, 2017 (54) FOAMABLE VEHICLE AND (56) References Cited PHARMACEUTICAL COMPOSITIONS U.S. PATENT DOCUMENTS THEREOF M (71) Applicant: Foamix Pharmaceuticals Ltd., 1,159,250 A 1 1/1915 Moulton Rehovot (IL) 1,666,684 A 4, 1928 Carstens 1924,972 A 8, 1933 Beckert (72) Inventors: Dov Tamarkin, Maccabim (IL); Doron 2,085,733. A T. 1937 Bird Friedman, Karmei Yosef (IL); Meir 33 A 1683 Sk Eini, Ness Ziona (IL); Alex Besonov, 2,586.287- 4 A 2/1952 AppersonO Rehovot (IL) 2,617,754. A 1 1/1952 Neely 2,767,712 A 10, 1956 Waterman (73) Assignee: EMY PHARMACEUTICALs 2.968,628 A 1/1961 Reed ... Rehovot (IL) 3,004,894. A 10/1961 Johnson et al. (*) Notice: Subject to any disclaimer, the term of this 3,062,715. A 1 1/1962 Reese et al. tent is extended or adiusted under 35 3,067,784. A 12/1962 Gorman pa 3,092.255. A 6/1963 Hohman U.S.C. 154(b) by 37 days. 3,092,555 A 6/1963 Horn 3,141,821 A 7, 1964 Compeau (21) Appl. No.: 13/793,893 3,142,420 A 7/1964 Gawthrop (22) Filed: Mar. 11, 2013 3,144,386 A 8/1964 Brightenback O O 3,149,543 A 9/1964 Naab (65) Prior Publication Data 3,154,075 A 10, 1964 Weckesser US 2013/0189193 A1 Jul 25, 2013 3,178,352. -
Ehealth DSI [Ehdsi V2.2.2-OR] Ehealth DSI – Master Value Set
MTC eHealth DSI [eHDSI v2.2.2-OR] eHealth DSI – Master Value Set Catalogue Responsible : eHDSI Solution Provider PublishDate : Wed Nov 08 16:16:10 CET 2017 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 1 of 490 MTC Table of Contents epSOSActiveIngredient 4 epSOSAdministrativeGender 148 epSOSAdverseEventType 149 epSOSAllergenNoDrugs 150 epSOSBloodGroup 155 epSOSBloodPressure 156 epSOSCodeNoMedication 157 epSOSCodeProb 158 epSOSConfidentiality 159 epSOSCountry 160 epSOSDisplayLabel 167 epSOSDocumentCode 170 epSOSDoseForm 171 epSOSHealthcareProfessionalRoles 184 epSOSIllnessesandDisorders 186 epSOSLanguage 448 epSOSMedicalDevices 458 epSOSNullFavor 461 epSOSPackage 462 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 2 of 490 MTC epSOSPersonalRelationship 464 epSOSPregnancyInformation 466 epSOSProcedures 467 epSOSReactionAllergy 470 epSOSResolutionOutcome 472 epSOSRoleClass 473 epSOSRouteofAdministration 474 epSOSSections 477 epSOSSeverity 478 epSOSSocialHistory 479 epSOSStatusCode 480 epSOSSubstitutionCode 481 epSOSTelecomAddress 482 epSOSTimingEvent 483 epSOSUnits 484 epSOSUnknownInformation 487 epSOSVaccine 488 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 3 of 490 MTC epSOSActiveIngredient epSOSActiveIngredient Value Set ID 1.3.6.1.4.1.12559.11.10.1.3.1.42.24 TRANSLATIONS Code System ID Code System Version Concept Code Description (FSN) 2.16.840.1.113883.6.73 2017-01 A ALIMENTARY TRACT AND METABOLISM 2.16.840.1.113883.6.73 2017-01 -
Potentially Explosive Chemicals*
Potentially Explosive Chemicals* Chemical Name CAS # Not 1,1’-Diazoaminonaphthalene Assigned 1,1-Dinitroethane 000600-40-8 1,2,4-Butanetriol trinitrate 006659-60-5 1,2-Diazidoethane 000629-13-0 1,3,5-trimethyl-2,4,6-trinitrobenzene 000602-96-0 1,3-Diazopropane 005239-06-5 Not 1,3-Dinitro-4,5-dinitrosobenzene Assigned Not 1,3-dinitro-5,5-dimethyl hydantoin Assigned Not 1,4-Dinitro-1,1,4,4-tetramethylolbutanetetranitrate Assigned Not 1,7-Octadiene-3,5-Diyne-1,8-Dimethoxy-9-Octadecynoic acid Assigned 1,8 –dihydroxy 2,4,5,7-tetranitroanthraquinone 000517-92-0 Not 1,9-Dinitroxy pentamethylene-2,4,6,8-tetramine Assigned 1-Bromo-3-nitrobenzene 000585-79-5 Not 2,2',4,4',6,6'-Hexanitro-3,3'-dihydroxyazobenzene Assigned 2,2-di-(4,4,-di-tert-butylperoxycyclohexyl)propane 001705-60-8 2,2-Dinitrostilbene 006275-02-1 2,3,4,6- tetranitrophenol 000641-16-7 Not 2,3,4,6-tetranitrophenyl methyl nitramine Assigned Not 2,3,4,6-tetranitrophenyl nitramine Assigned Not 2,3,5,6- tetranitroso nitrobenzene Assigned Not 2,3,5,6- tetranitroso-1,4-dinitrobenzene Assigned 2,4,6-Trinitro-1,3,5-triazo benzene 029306-57-8 Not 2,4,6-trinitro-1,3-diazabenzene Assigned Not 2,4,6-Trinitrophenyl trimethylol methyl nitramine trinitrate Assigned Not 2,4,6-Trinitroso-3-methyl nitraminoanisole Assigned 2,4-Dinitro-1,3,5-trimethyl-benzene 000608-50-4 2,4-Dinitrophenylhydrazine 000119-26-6 2,4-Dinitroresorcinol 000519-44-8 2,5-dimethyl-2,5-diydroperoxy hexane 2-Nitro-2-methylpropanol nitrate 024884-69-3 3,5-Dinitrosalicylic acid 000609-99-4 Not 3-Azido-1,2-propylene glycol dinitrate -
Pharmaceutical Appendix to the Tariff Schedule 2
Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9 -
Prediction of the Crystalline Densities of Aliphatic Nitrates by Quantum Chemistry Methods
Central European Journal of Energetic Materials ISSN 1733-7178; e-ISSN 2353-1843 Copyright © 2019 Sieć Badawcza Łukasiewicz – Institute of Industrial Organic Chemistry, Poland Cent. Eur. J. Energ. Mater. 2019, 16(3): 412-432; DOI 10.22211/cejem/112306 Article is available in PDF-format, in colour, at: http://www.wydawnictwa.ipo.waw.pl/cejem/Vol-16-Number3-2019/CEJEM_00978.pdf Article is available under the Creative Commons Attribution-Noncommercial-NoDerivs 3.0 license CC BY-NC-ND 3.0. Research paper Prediction of the Crystalline Densities of Aliphatic Nitrates by Quantum Chemistry Methods Guixiang Wang,* Yimin Xu, Chuang Xue, Zhiyuan Ding, Yan Liu, Hui Liu, Xuedong Gong** Computation Institute for Molecules and Materials, Department of Chemistry, Nanjing University of Science and Technology, Nanjing 210094, China E-mails: * [email protected]; ** [email protected] Abstract: Crystal density is a basic and important parameter for predicting the detonation performance of explosives, and nitrate esters are a type of compound widely used in the military context. In this study, thirty-one aliphatic nitrates were investigated using the density functional theory method (B3LYP) in combination with six basis sets (3-21G, 6-31G, 6-31G*, 6-31G**, 6-311G* and 6-31+G**) and the semiempirical molecular orbital method (PM3). Based on the geometric optimizations at various theoretical levels, the molecular volumes and densities were calculated. Compared with the available experimental data, the densities calculated by various methods are all overestimated, and the errors of the PM3 and B3LYP/3-21G methods are larger than those of other methods. Considering the results and the computer resources required by the calculations, the B3LYP/6-31G* method is recommended for predicting the crystalline densities of organic nitrates using a fitting equation.