Development Document for Interim Final Effluent Guidelines & Prop
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Comparison of the Antiischaemic and Antianginal Effects of Nicorandil and Amlodipine in Patients with Symptomatic Stable Angina Pectoris: the SWAN Study
Journal of Clinical and Basic Cardiology An Independent International Scientific Journal Journal of Clinical and Basic Cardiology 1999; 2 (2), 213-217 Comparison of the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris: the SWAN study The SWAN Study Group Homepage: www.kup.at/jcbc Online Data Base Search for Authors and Keywords Indexed in Chemical Abstracts EMBASE/Excerpta Medica Krause & Pachernegg GmbH · VERLAG für MEDIZIN und WIRTSCHAFT · A-3003 Gablitz/Austria ORIGINAL PAPERS, CLINICAL The SWAN study J Clin Basic Cardiol 1999; 2: 213 Comparison of the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris: the SWAN study The SWAN Study Group1 This multicentre, double-blind, randomised study compared the antiischaemic and antianginal effects of nicorandil and amlodipine in patients with symptomatic stable angina pectoris. Nicorandil is a new coronary and balanced peripheral vasodilating agent that operates through two mechanisms of action: activation of ATP-dependent K-channels and stimulation of guanylate cyclase. A total of 121 patients with symptomatic stable angina pectoris were randomised to receive nicorandil 10 mg twice daily (bd) or amlodipine 5 mg once daily (od) for 8 weeks (optional dosage increase after 2-4 weeks to 20 mg bd and 10 mg od, respec- tively). Symptom-limited exercise tolerance tests were performed at baseline, and after 2 and 8 weeks treatment, respectively. In addition, the number of anginal attacks, nitroglycerin (NTG) usage, blood pressure (BP), heart rate (HR) and adverse events were recorded, and a subjective assessment of quality of life performed. -
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. -
Current Status of Local Penile Therapy
International Journal of Impotence Research (2002) 14, Suppl 1, S70–S81 ß 2002 Nature Publishing Group All rights reserved 0955-9930/02 $25.00 www.nature.com/ijir Current status of local penile therapy F Montorsi1*, A Salonia1, M Zanoni1, P Pompa1, A Cestari1, G Guazzoni1, L Barbieri1 and P Rigatti1 1Department of Urology, University Vita e Salute – San Raffaele, Milan, Italy Guidelines for management of patients with erectile dysfunction indicate that intraurethral and intracavernosal injection therapies represent the second-line treatment available. Efficacy of intracavernosal injections seems superior to that of the intraurethral delivery of drugs, and this may explain the current larger diffusion of the former modality. Safety of these two therapeutic options is well established; however, the attrition rate with these approaches is significant and most patients eventually drop out of treatment. Newer agents with better efficacy-safety profiles and using user-friendly devices for drug administration may potentially increase the long-term satisfaction rate achieved with these therapies. Topical therapy has the potential to become a first- line treatment for erectile dysfunction because it acts locally and is easy to use. At this time, however, the crossing of the barrier caused by the penile skin and tunica albuginea has limited the efficacy of the drugs used. International Journal of Impotence Research (2002) 14, Suppl 1, S70–S81. DOI: 10.1038= sj=ijir=3900808 Keywords: erectile dysfunction; local penile therapy; topical therapy; alprostadil Introduction second patient category might be represented by those requesting a fast response, which cannot be obtained by sildenafil; however, sublingual apomor- Management of patients with erectile dysfunction phine is characterized by a fast onset of action and has been recently grouped into three different may represent an effective solution for these 1 levels. -
Transport of Dangerous Goods
ST/SG/AC.10/1/Rev.16 (Vol.I) Recommendations on the TRANSPORT OF DANGEROUS GOODS Model Regulations Volume I Sixteenth revised edition UNITED NATIONS New York and Geneva, 2009 NOTE The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the Secretariat of the United Nations concerning the legal status of any country, territory, city or area, or of its authorities, or concerning the delimitation of its frontiers or boundaries. ST/SG/AC.10/1/Rev.16 (Vol.I) Copyright © United Nations, 2009 All rights reserved. No part of this publication may, for sales purposes, be reproduced, stored in a retrieval system or transmitted in any form or by any means, electronic, electrostatic, magnetic tape, mechanical, photocopying or otherwise, without prior permission in writing from the United Nations. UNITED NATIONS Sales No. E.09.VIII.2 ISBN 978-92-1-139136-7 (complete set of two volumes) ISSN 1014-5753 Volumes I and II not to be sold separately FOREWORD The Recommendations on the Transport of Dangerous Goods are addressed to governments and to the international organizations concerned with safety in the transport of dangerous goods. The first version, prepared by the United Nations Economic and Social Council's Committee of Experts on the Transport of Dangerous Goods, was published in 1956 (ST/ECA/43-E/CN.2/170). In response to developments in technology and the changing needs of users, they have been regularly amended and updated at succeeding sessions of the Committee of Experts pursuant to Resolution 645 G (XXIII) of 26 April 1957 of the Economic and Social Council and subsequent resolutions. -
Cardiovascular Drugs and Therapies NITRATES COMPARISON CHART
Cardiovascular Drugs and Therapies NITRATES COMPARISON CHART Isosorbide Generic Nitroglycerin Nitroglycerin Nitroglycerin Nitroglycerin Dinitrate Isosorbide Isosorbide Name Intravenous Patch Ointment Sublingual Sublingual Dinitrate 5-Mononitrate Trade Name TRIDIL, NITRODUR, NITROL NITROLINGUAL generics generics (for IMDUR, generics TRANSDERM- Pumpspray, immediate generics NITRO, RHO-NITRO release) MINITRAN, Pumpspray, SR: no longer TRINIPATCH NITROLINGUAL available Metered dose spray NITROSTAT sublingual tablet Dosage 100 mg/250 mL 0.2 mg/h 30 g/30 inches SL spray: SL tablet: 5mg Immediate SR tablet: Forms premixed bottle 0.4 mg/h ointment 0.4 mg/ dose release 60 mg SR - UHN 0.6 mg/h SL tablet: tablet: Note: 0.84 mL 0.8 mg/h 0.3 mg, 0.6 mg 10 mg *Non- alcohol per 100 mL 30 mg formulary at solution UHN 100 mcg/mL 200 mcg/mL 400 mcg/mL 10 mg/10 mL vial - UHN 50 mg/10 mL vial - UHN CARDIOVASCULAR PHARMACOTHERAPY HANDBOOK All contents copyright © University Health Network. All rights reserved Cardiovascular Drugs and Therapies NITRATES COMPARISON CHART Isosorbide Generic Nitroglycerin Nitroglycerin Nitroglycerin Nitroglycerin Dinitrate Isosorbide Isosorbide Name Intravenous Patch Ointment Sublingual Sublingual Dinitrate 5-Mononitrate Dosing Starting and 0.2 to 0.8 ½ inch to 1 inch SL spray: SL tablet: Immediate 60-240 mg SR Usual dose target doses mg/h once tid-qid; remove 0.4 mg prn; 5-10 mg q2-4h release: once daily range are determined daily. for 8-10 hours dose may be for prophylaxis 10-45 mg tid by clinical per 24-hour repeated after of acute angina on qid situation and 12-14 hour period; 5 minutes for schedule the number and patch-free response to interval e.g., ON 0600, total of 3 doses (e.g. -
The Availability of Organic Nitrates from Intravenous Administration Systems
THE AVAILABILITY OF ORGANIC NITRATES FROM INTRAVENOUS ADMINISTRATION SYSTEMS by Paul Adrian Cossum B.Sc., M.P.S. submitted in partial fulfilment of the requirements for the degree of Master of Pharmacy UNIVERSITY OF TASMANIA - HOBART JUNE 1981 SUMMARY Nitroglycerin aind isosorbide dinitrate are two drugs which are infused intravenously during the treatment of ischaemic heart disease. The availability of these two drugs in solutions infused from plastic infusion bags or glass infusion bottles through plastic giving sets has been investigated. During simulated infusions the concentration of nitroglycerin and isosorbide dinitrate appearing in the effluent of the • giving set tubing was found to be much less than the concentration of the drug solution initially contained in the plastic infusion bag or glass infusion bottle. It was found that each component of the plastic infusion equipment sorbed the drugs to a significant extent and that the rate of disappearance of drugs from solutions stored in each component was in the rank order: giving set tubing > giving set burette > plastic infusion bag. There was no significant loss of either drug from solutions stored in glass bottles. The influence of formulation factors and storage conditions on the sorption of nitroglycerin, isosorbide dinitrate and another organic nitrate compound., ethylene glycol dinitrate, by plastic infusion equipment was studied. The extent of loss during simulated infusions was also found to be dependent on flow rate of drug solution through the giving set. The sorption of nitroglycerin and isosorbide dinitrate has clinical and pharmacokinetic significance. Losses of nitroglycerin and isosorbide dinitrate associated with their infusion through plastic Lnfusion equipment were minimised by infusing drug solutions from a glass syringe through high density polyethylene tubing. -
Tatp) Precursors and Synthetic By-Products
University of Central Florida STARS Electronic Theses and Dissertations, 2004-2019 2009 The Forensic Analysis Of Triacetone Triperoxide (tatp) Precursors And Synthetic By-products Kimberly Painter University of Central Florida Part of the Chemistry Commons, and the Forensic Science and Technology Commons Find similar works at: https://stars.library.ucf.edu/etd University of Central Florida Libraries http://library.ucf.edu This Masters Thesis (Open Access) is brought to you for free and open access by STARS. It has been accepted for inclusion in Electronic Theses and Dissertations, 2004-2019 by an authorized administrator of STARS. For more information, please contact [email protected]. STARS Citation Painter, Kimberly, "The Forensic Analysis Of Triacetone Triperoxide (tatp) Precursors And Synthetic By- products" (2009). Electronic Theses and Dissertations, 2004-2019. 4047. https://stars.library.ucf.edu/etd/4047 THE FORENSIC ANALYSIS OF TRIACETONE TRIPEROXIDE (TATP) PRECURSORS AND SYNTHETIC BY-PRODUCTS by KIMBERLY LYNNE PAINTER B.S. University of South Carolina, 2007 A thesis submitted in partial fulfillment of the requirements for the degree of Master of Science in the Department of Chemistry in the College of Sciences at the University of Central Florida Orlando, Florida Fall Term 2009 © 2009 Kimberly L. Painter ii ABSTRACT Triacetone Triperoxide (TATP) is a primary high explosive that can be synthesized using commercially available starting materials and has grown in use among terrorists over the past several years. Additives present in the precursors were investigated to see if they carry through the TATP synthesis and can be detected in the final product potentially aiding in the identification of the source. -
Use of Sildenafil in Patients with Cardiovascular Disease
Arq Bras Cardiol GuimarãesReview et al volume 73, (nº6), 1999 Sildenafil in patients with cardiovascular disease Use of Sildenafil in Patients with Cardiovascular Disease Armênio Costa Guimarães, Marcus Vinícius Bolívar Malachias, Otávio Rizzi Coelho, Emílio Cesar Zilli, Rafael Leite Luna Introduction of phosphodiesterase inhibitors. The erectile action of sildenafil combines increase in arterial flow with reduction Erectile dysfunction, formerly called impotence, is the in the venous flow of cavernous body of penis. Sildenafil inability of the male to achieve or maintain penile erection and leads to relaxation of smooth muscle of penile arteries and thus engage in coitus1. It is common among patients with trabeculae surrounding the sinusoidal spaces, resulting in cardiovascular diseases or their risk factors. This dysfunc- a greater engorgement of cavernous body. The trabeculae tion occurs mainly among individuals with coronary artery of engorged sinusoidal spaces compress the penile disease, after episodes of acute ischemic syndrome, hyper- venules against the tunica albuginea, reducing venous tensive patients underpharmacologic treatment, and among flow, contributing to maintenance of engorgement of patients with heart failure. In approximately 85% of these ca- cavernous body8. Relaxation of this smooth muscle ses, the fear of a cardiac event during coitus constitutes an results from a decrease in intracellular calcium mediated important factor for erectile dysfunction 2-4. by accumulation of the second messenger, the cyclic Discovery of sildenafil citrate has represented a great de- guanosine monophosphate (cGMP), whose production velopment in the treatment of erectile dysfunction; it may results from activation of guanyl cyclase by nitric oxide benefit, among many others, those patients with cardiovascu- produced by the stimulus of endothelial cells generated lar diseases or with their risk factors 5. -
REVATIO (Sildenafil Citrate) – Product Monograph Page 52 of 55 PART
IMPORTANT: PLEASE READ PART III: CONSUMER INFORMATION o nitroglycerin (sprays, ointments, skin patches or pastes, and tablets that are swallowed or dissolved in PrREVATIO® the mouth) (sildenafil tablets, Upjohn Standard) o isosorbide mononitrate and isosorbide dinitrate 20 mg sildenafil as (sildenafil citrate) (tablets that are swallowed, chewed, or dissolved in the mouth) (sildenafil injection, Upjohn Standard) If you are not sure if any of your medicines contain nitrates, 0.8 mg/mL sildenafil as (sildenafil citrate) or if you do not understand what nitrates are, ask your doctor or pharmacist. If you take REVATIO with any nitrate- READ THIS FOR SAFE AND EFFECTIVE USE OF YOUR containing medicine or any nitrate, your blood pressure could MEDICINE. suddenly drop to a life-threatening level. You could get Read this carefully before you start taking REVATIO and each dizzy, faint, or even have a heart attack or stroke. time you get a refill. This leaflet is a summary and will not tell have loss of vision in one or both eyes from an eye disease you everything about this drug. Talk to your healthcare called non-arteritic anterior ischaemic optic neuropathy professional about your medical condition and treatment and ask (NAION) if there is any new information about REVATIO. ® take drugs like ketoconazole (Nizoral ), itraconazole (Sporanox®), ritonavir (Kaletra®) ABOUT THIS MEDICATION have pulmonary hypertension secondary to sickle cell anaemia (abnormality of the red blood cells) What the medication is used for: have severe liver disease REVATIO (sildenafil citrate) is used to treat pulmonary arterial have a recent history of stroke or heart attack or life- hypertension (high blood pressure in the blood vessels between the threatening arrhythmia (a heart rhythm disorder) heart and the lungs) in adults (18 years of age or older). -
The Nitric Oxide Donor, Isosorbide Dinitrate, Induces a Cephalic
The nitric oxide donor, isosorbide dinitrate, induces a cephalic cutaneous hypersensitivity, associated with sensitization of the medullary dorsal horn Running Title: nitric oxide donors induced central sensitization José Maria Ramos Flores, Laurent Devoize, Amélie Descheemaeker, Jean-Louis Molat, Philippe Luccarini, Radhouane Dallel To cite this version: José Maria Ramos Flores, Laurent Devoize, Amélie Descheemaeker, Jean-Louis Molat, Philippe Luc- carini, et al.. The nitric oxide donor, isosorbide dinitrate, induces a cephalic cutaneous hypersensi- tivity, associated with sensitization of the medullary dorsal horn Running Title: nitric oxide donors induced central sensitization: Nitric oxide donors induced central sensitization. Neuroscience, Else- vier - International Brain Research Organization, 2017, 10.1016/j.neuroscience.2016.12.028. inserm- 01458345 HAL Id: inserm-01458345 https://www.hal.inserm.fr/inserm-01458345 Submitted on 6 Feb 2017 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. The nitric oxide donor, isosorbide dinitrate, induces a cephalic cutaneous hypersensitivity, associated with sensitization of the medullary dorsal horn José María Flores Ramos1, Laurent Devoize1,2, Amélie Descheemaeker1, Jean-Louis Molat1, Philippe Luccarini1, Radhouane Dallel1,2 1Clermont Université, Université d’Auvergne, Neuro-Dol, BP 10448, F-63000, Clermont- Ferrand & Inserm U1107, F-63100 Clermont-Ferrand, France; 2CHU Clermont-Ferrand, Service d’Odontologie, F-63100 Clermont-Ferrand, France. -
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 -
Fast Dissolving Sublingual Strips: a Novel Approach for the Delivery Of
Pharmaceutical Sciences December 2019, 25(4), 311-318 doi: 10.15171/PS.2019.34 https://ps.tbzmed.ac.ir/ Research Article Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate Marziyeh Fathi1 , Mitra Alami-Milani2,3, Sara Salatin1,3, Sharahm Sattari4, Hassan Montazam5, Farhad Fekrat3, Mitra Jelvehgari2,6* 1Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz, Iran. 2Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran. 3Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran. 4Nikookari Ophtalmology Center, Tabriz University of Medical Sciences, Tabriz, Iran. 5Islamic Azad University of Bonab Unit, Bonab, Iran. 6Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. A r t i c l e I n f o A B S T R A C T Article History: Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In Received: 19 November 2018 addition, oral ISDN is available in immediate and sustained release formulations and the Revised: 6 April 2019 Accepted: 12 April 2019 bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are ePublished: 20 December 2019 developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation Keywords: for sublingual delivery of ISDN. -Film -Sublingual Methods: In the present study, sublingual films were prepared by the solvent casting -Isosorbide dinitrate technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and -HPMC 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10).