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INVESTIGATION of NATURAL PRODUCT SCAFFOLDS for the DEVELOPMENT of OPIOID RECEPTOR LIGANDS by Katherine M
INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS By Katherine M. Prevatt-Smith Submitted to the graduate degree program in Medicinal Chemistry and the Graduate Faculty of the University of Kansas in partial fulfillment of the requirements for the degree of Doctor of Philosophy. _________________________________ Chairperson: Dr. Thomas E. Prisinzano _________________________________ Dr. Brian S. J. Blagg _________________________________ Dr. Michael F. Rafferty _________________________________ Dr. Paul R. Hanson _________________________________ Dr. Susan M. Lunte Date Defended: July 18, 2012 The Dissertation Committee for Katherine M. Prevatt-Smith certifies that this is the approved version of the following dissertation: INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS _________________________________ Chairperson: Dr. Thomas E. Prisinzano Date approved: July 18, 2012 ii ABSTRACT Kappa opioid (KOP) receptors have been suggested as an alternative target to the mu opioid (MOP) receptor for the treatment of pain because KOP activation is associated with fewer negative side-effects (respiratory depression, constipation, tolerance, and dependence). The KOP receptor has also been implicated in several abuse-related effects in the central nervous system (CNS). KOP ligands have been investigated as pharmacotherapies for drug abuse; KOP agonists have been shown to modulate dopamine concentrations in the CNS as well as attenuate the self-administration of cocaine in a variety of species, and KOP antagonists have potential in the treatment of relapse. One drawback of current opioid ligand investigation is that many compounds are based on the morphine scaffold and thus have similar properties, both positive and negative, to the parent molecule. Thus there is increasing need to discover new chemical scaffolds with opioid receptor activity. -
2020 Kansas Statutes
2020 Kansas Statutes 65-4105. Substances included in schedule I. (a) The controlled substances listed in this section are included in schedule I and the number set forth opposite each drug or substance is the DEA controlled substances code that has been assigned to it. (b) Any of the following opiates, including their isomers, esters, ethers, salts, and salts of isomers, esters and ethers, unless specifically excepted, whenever the existence of these isomers, esters, ethers and salts is possible within the specific chemical designation: (1) Acetyl fentanyl (N-(1-phenethylpiperidin-4-yl)-N- phenylacetamide) 9821 (2) Acetyl-alpha-methylfentanyl (N-[1-(1-methyl-2-phenethyl)-4-piperidinyl]-N- phenylacetamide) 9815 (3) Acetylmethadol 9601 (4) Acryl fentanyl (N-(1-phenethylpiperidin-4-yl)-N-phenylacrylamide; acryloylfentanyl) 9811 (5) AH-7921 (3,4-dichloro-N-[(1-dimethylamino)cyclohexylmethyl]benzamide) 9551 (6) Allylprodine 9602 (7) Alphacetylmethadol 9603(except levo-alphacetylmethadol also known as levo- alpha-acetylmethadol, levomethadyl acetate or LAAM) (8) Alphameprodine 9604 (9) Alphamethadol 9605 (10) Alpha-methylfentanyl (N-[1-(alpha-methyl-beta-phenyl)ethyl-4-piperidyl] propionanilide; 1-(1-methyl-2-phenylethyl)-4-(N-propanilido) piperidine) 9814 (11) Alpha-methylthiofentanyl (N-[1-methyl-2-(2-thienyl)ethyl-4-piperidinyl]-N- phenylpropanamide) 9832 (12) Benzethidine 9606 (13) Betacetylmethadol 9607 (14) Beta-hydroxyfentanyl (N-[1-(2-hydroxy-2-phenethyl)-4-piperidinyl]-N- phenylpropanamide) 9830 (15) Beta-hydroxy-3-methylfentanyl (other -
ESTIMATED WORLD REQUIREMENTS of NARCOTIC DRUGS in GRAMS for 2019 (As of 10 January 2019 )
ESTIMATED WORLD REQUIREMENTS OF NARCOTIC DRUGS IN GRAMS FOR 2019 (as of 10 January 2019 ) Afghanistan Cannabis 50 Codeine 50 000 Cannabis resin 1 Dextropropoxyphene 10 000 Coca leaf 1 Diphenoxylate 5 000 Cocaine 15 Fentanyl 1 Codeine 650 000 Methadone 20 000 Codeine -N-oxide 1 Morphine 8 000 Dextromoramide 1 Pethidine 90 000 Dextropropoxyphene 200 000 Pholcodine 40 000 Difenoxin 1 Albania Dihydrocodeine 1 Cocaine 1 Diphenoxylate 1 Codeine 1 189 000 Dipipanone 1 Fentanyl 300 Ecgonine 2 Heroin 1 Ethylmorphine 1 Methadone 7 000 Etorphine 1 Morphine 7 800 Fentanyl 17 000 Oxycodone 2 000 Heroin 1 Pethidine 2 700 Hydrocodone 10 000 Pholcodine 1 500 Hydromorphone 4 000 Remifentanil 9 Ketobemidone 1 Sufentanil 2 Levorphanol 1 Algeria Methadone 100 000 Alfentanil 350 Morphine 1 550 000 Codeine 2 500 000 Morphine -N-oxide 1 Etorphine 1 Nicomorphine 1 Fentanyl 500 Norcodeine 1 Methadone 4 000 Normethadone 1 Morphine 9 000 Normorphine 1 Oxycodone 4 000 Opium 10 Pethidine 3 000 Oripavine 1 Pholcodine 1 500 000 Oxycodone 60 000 Remifentanil 1 Oxymorphone 1 Sufentanil 30 Pethidine 50 000 Andorra Phenoperidine 1 Cannabis 2 000 Pholcodine 1 Fentanyl 100 Piritramide 1 Methadone 1 000 Remifentanil 20 000 Morphine 500 Sufentanil 10 Oxycodone 2 000 Thebacon 1 Pethidine 500 Thebaine 70 000 Remifentanil 4 Tilidine 1 Angola Armenia Alfentanil 20 Codeine 3 000 Codeine 21 600 Fentanyl 40 Dextromoramide 188 Methadone 13 500 Dextropropoxyphene 200 Morphine 7 500 Dihydrocodeine 500 Thebaine 15 Diphenoxylate 300 Trimeperidine 1 500 Fentanyl 63 Aruba* Methadone 2 000 -
Pain Management After Elective Shoulder Surgery: a Randomized Quantitative Study Comparing Hydromorphone with Piritramide
Case Report J Anest & Inten Care Med Volume 9 Issue 4 - October 2019 Copyright © All rights are reserved by Hermann Prossinger DOI: 10.19080/JAICM.2019.09.555768 Pain Management After Elective Shoulder Surgery: A Randomized Quantitative Study Comparing Hydromorphone With Piritramide Boesmueller S1, Gerstorfer I1, Steiner M1, Prossinger H2*, Fialka C1 and Steltzer H1, 3 1AUVA Meidling, Austria 2Department for Evolutionary Anthropology, University of Vienna, Austria 3Sigmund Freud University, Austria Submission: September 25, 2019; Published: October 11, 2019 *Corresponding author: Hermann Prossinger, Department for Evolutionary Anthropology, Faculty of Life Sciences, University of Vienna, Vienna, Austria Abstract Background: Postoperative pain management plays an important role in elective shoulder surgery. Several methods have been investigated so far. The aim of this randomized quantitative study is to compare two frequently used postoperative pain regimes (hydromorphone versus piritramide) regarding onset and duration after the effectiveness of the single-shot interscalene block has diminished. Methods: All patients who underwent elective shoulder surgery at our institution agreed to participate in this study. Upon admission patients were assigned membership to group A (hydromorphone) or group B (piritramide) according to the patient number (which ensured randomization). Pain assessment was performed using the numeric rating scale (NRS). For statistical analyses the techniques of maximum likelihood (ML) estimation were used. Results: Of the 48 patients aged 18–89 years included in this study, 25 were in group A and 23 in group B. Of these 48, 21 in each group registered pain levels above threshold at least once. Shoulder surgery was performed 45 times in an arthroscopic and 3 times in an open technique. -
Evidence Review F: Opioids for Pain Relief After Caesarean Birth
National Institute for Health and Care Excellence FINAL Caesarean birth [F] Opioids for pain relief after caesarean birth NICE guideline NG192 Evidence review March 2021 Final This evidence review was developed by the National Guideline Alliance which is a part of the Royal College of Obstetricians and Gynaecologists FINAL Contents Disclaimer The recommendations in this guideline represent the view of NICE, arrived at after careful consideration of the evidence available. When exercising their judgement, professionals are expected to take this guideline fully into account, alongside the individual needs, preferences and values of their patients or service users. The recommendations in this guideline are not mandatory and the guideline does not override the responsibility of healthcare professionals to make decisions appropriate to the circumstances of the individual patient, in consultation with the patient and/or their carer or guardian. Local commissioners and/or providers have a responsibility to enable the guideline to be applied when individual health professionals and their patients or service users wish to use it. They should do so in the context of local and national priorities for funding and developing services, and in light of their duties to have due regard to the need to eliminate unlawful discrimination, to advance equality of opportunity and to reduce health inequalities. Nothing in this guideline should be interpreted in a way that would be inconsistent with compliance with those duties. NICE guidelines cover health and care in England. Decisions on how they apply in other UK countries are made by ministers in the Welsh Government, Scottish Government, and Northern Ireland Executive. -
Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate. -
Problems of Drug Dependence 1980 Proceedings of the 42Nd Annual Scientific Meeting the Committee on Problems of Drug Dependence
National Institute on Drug Abuse MONOGRAPH SERIES Problems of Drug Dependence 1980 Proceedings of the 42nd Annual Scientific Meeting The Committee on Problems of Drug Dependence, Inc. U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES • Public Health Service • Alcohol, Drug Abuse, and Mental Health Administration Problems of Drug Dependence, 1980 Proceedings of the 42nd Annual Scientific Meeting, The Committee on Problems of Drug Dependence, Inc. Editor: Louis S. Harris, Ph.D. NIDA Research Monograph 34 February 1981 DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service Alcohol, Drug Abuse, and Mental Health Administration National Institute on Drug Abuse Division of Research 5600 Fishers Lane Rockville, Maryland 20857 For sale by the Superintendent of Documents, U.S. Government Printing Office Washington, D.C. 20402 The NIDA Research Monograph series is prepared by the Division of Research of the National Institute on Drug Abuse. Its primary objective is to provide critical reviews of research problem areas and techniques, the content of state-of-the-art conferences, integrative research reviews and significant original research. Its dual publication emphasis is rapid and targeted dissemination to the scientific and professional community. Editorial Advisory Board Avram Goldstein, M.D. Addiction Research Foundation Palo Alto, California Jerome Jaffe, M.D. College of Physicians and Surgeons Columbia University, New York Reese T. Jones, M.D. Langley Porter Neuropsychiatric Institute University of California San Francisco, California William McGlothlin, Ph.D. Deportment of Psychology, UCLA Los Angeles, California Jack Mendelson, M.D. Alcohol and Drug Abuse Research Center Harvard Medical School McLean Hospital Belmont, Massachusetts Helen Nowlis, Ph.D. Office of Drug Education, DHHS Washington, D.C Lee Robins, Ph.D. -
Chromatography Including Electrophoresis and Other Separation Methods
15SIO 06£ i 36 j 6 VOL. 610 NO.2 JUNE 12, 1992 THIS ISSUE COMPLETES VOL. 610 Bibliography Section JOURNAL OF CHROMATOGRAPHY INCLUDING ELECTROPHORESIS AND OTHER SEPARATION METHODS EDITORS U. A. Th. Brinkman (Amsterdam) R. W. Giese (Boston, MA) J. K. Haken (Kensington, N.S.W.) K. Macek (Prague) L. R. Snyder (Orinda, CA) EDITORS. SYMPOSIUM VOLUMES. E. Heftmann (Orinda. CAl. Z. Deyl (Prague) EDITORIAL BOARD D. W. Armstrong (Rollo. MO) W. A. Aue (Holifo,) P. Botek (8.00) A. A. Boulton (Saskatoon) P. W. Cmr (Minneopolis. MN) N. H. C. Cooke (San Ramon. CAl V. A. Davankov (Moscow) Z. Deyl (Progue) S. Dilli (Kl~nsington. N.S.W.) F. Ern! (Basle) M. B. Evans (Hatfield) J. L. Glojcl, (N. Billerico. MA) G. A. Guiochon (Knoxville, TN) P. R. Haddod (Kensington. N.S.W.) I. M. Hais (Hradec Kralove) W. S. Hancock (San FranCISCo. CAl S. Hjerten (Uppsalo) Cs. Horvinh (New Haven. CT) J. F. K. Huber (Vienna) K.·P. Hupe (Woldbronn) T. W. Hutchens (Houston. IX) J. Jonak (B.oo) P. Jandera (Pardubice) B. L. Kmger (B05<on. MA) J. J. Kirkland (Wilmington. DE) E. sz. Kovats (Lausanne) A. J. P. Mortin (Cambridge) L. W. McLoughlin (Chestnut Hill. MA) E. D. Morgan (Keele) J. O. Pearson (KrJlamazoo, MI) H. Poppe (Amsterdam) F. E. Regnier (West Lafayette. IN) P. G. Righetti (Milan) P. Sclloenmakers (Eindhoven) R. Schwarzenbach (Dubendor!) R. E. Shoup (West Lafayette. IN) A. M. Siouf!i (Mo,seille) D. J. Strydom (Boston. MA) N. Tonaka (Kyoto) S. Terabe (Hyogo) K. K. Unger (Mainz) R. Verpoorle (Leiden) Gy. -
7.5 Mg/Ml Solution for Injection Piritramide Read All of This Leafle
PACKAGE LEAFLET: INFORMATION FOR THE USER Piritramide [MAH] 7.5 mg/ml solution for injection Piritramide Read all of this leaflet carefully before you start using this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet: 1. What Piritramide [MAH] is and what it is used for 2. What you need to know before you are given Piritramide [MAH] 3. How to use Piritramide [MAH] 4. Possible side effects 5. How to store Piritramide [MAH] 6. Contents of the pack and other information 1. WHAT PIRITRAMIDE [MAH] IS AND WHAT IT IS USED FOR Piritramide [MAH] contains the active substance piritramide. It belongs to a group of medicines called opioid analgesics (strong painkillers). Piritramide [MAH] is used to relieve severe to strongest pain. 2. WHAT YOU NEED TO KNOW BEFORE YOU ARE GIVEN PIRITRAMIDE [MAH] Do not use Piritramide [MAH]: - If you are allergic to piritramide or any of the other ingredients of this medicine (listed in section 6). - If you suffer from severely impaired consciousness from which you cannot be roused even by external stimuli. - If you have problems with breathing (respiratory depression). Warnings and precautions Talk to your doctor or pharmacist before you are given Piritramide [MAH] - If you have suffer from seizures (such as epileptic fits) - If you suffer from alcoholism - If you have head injuries - If you have an increased brain pressure - If you have an enlarged prostate (prostatic hypertrophy) - If you are in shock - If you have a severely slowed heart beat (bradycardia) or irregular heart beat (bradyarrhythmia). -
Quality Issues in Caring for Older People
Doctoral Thesis - Tesis Doctoral Quality issues in caring for older people: • Appropriateness of transition from long-term care facilities to acute hospital care • Potentially inappropriate medication: development of a European list Anna Renom Guiteras Prof. Gabriele Meyer Prof. Ramón Miralles Basseda Martin Luther University Halle-Wittenberg Universitat Autònoma de Barcelona Halle (Saale) & Barcelona, Catalonia University of Witten/Herdecke Spain Witten Germany Programa de doctorat en Medicina Departament de Medicina, Facultat de Medicina Universitat Autònoma de Barcelona Barcelona, 2015 13 Contents 15 1. Introduction • Research context • Background of the research topics • Pesetaio of the ailes 23 2. Summary and discussion of the results 31 3. Conclusions 37 4. References 47 5. Articles • Article 1: Renom-Guiteras A, Uhrenfeldt L, Meyer G, Mann E. Assessment tools for determining appropriateness of admission to acute care of persons transferred from long-term care facilities: a systematic review. BMC Geriatr. 2014;14:80 • Article 2: Renom-Guiteras A, Meyer G, Thürmann PA. The EU(7)-PIM list: a list of potentially inappropriate medications for older people consented by experts from seven European countries. Eur J Clin Pharmacol. 2015;71(7):861-75 77 6. Annexes • Annex 1.1 (article 1) - Additional file 1: Studies dealing with assessment tools for determining appropriateness of hospital admissions among residents of LTC facilities. • Annex 1.2 (article 1) - Additional file 2: Characteristics of the assessment tools for determining appropriateness of hospital admissions among residents of LTC facilities. • Annex 2.1 (article 2) - Appendix 1: Complete EU(7)-PIM list • Annex 2.2 (article 2) - Appendix 2: Questionable Potentially Inappropriate Medications (Questionable PIM): results of the Delphi survey. -
Phencyclidine: an Update
Phencyclidine: An Update U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES • Public Health Service • Alcohol, Drug Abuse and Mental Health Administration Phencyclidine: An Update Editor: Doris H. Clouet, Ph.D. Division of Preclinical Research National Institute on Drug Abuse and New York State Division of Substance Abuse Services NIDA Research Monograph 64 1986 DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service Alcohol, Drug Abuse, and Mental Health Administratlon National Institute on Drug Abuse 5600 Fishers Lane Rockville, Maryland 20657 For sale by the Superintendent of Documents, U.S. Government Printing Office Washington, DC 20402 NIDA Research Monographs are prepared by the research divisions of the National lnstitute on Drug Abuse and published by its Office of Science The primary objective of the series is to provide critical reviews of research problem areas and techniques, the content of state-of-the-art conferences, and integrative research reviews. its dual publication emphasis is rapid and targeted dissemination to the scientific and professional community. Editorial Advisors MARTIN W. ADLER, Ph.D. SIDNEY COHEN, M.D. Temple University School of Medicine Los Angeles, California Philadelphia, Pennsylvania SYDNEY ARCHER, Ph.D. MARY L. JACOBSON Rensselaer Polytechnic lnstitute National Federation of Parents for Troy, New York Drug Free Youth RICHARD E. BELLEVILLE, Ph.D. Omaha, Nebraska NB Associates, Health Sciences Rockville, Maryland REESE T. JONES, M.D. KARST J. BESTEMAN Langley Porter Neuropsychiatric lnstitute Alcohol and Drug Problems Association San Francisco, California of North America Washington, D.C. DENISE KANDEL, Ph.D GILBERT J. BOTV N, Ph.D. College of Physicians and Surgeons of Cornell University Medical College Columbia University New York, New York New York, New York JOSEPH V. -
Misuse and Abuse of Opioid Analgesics – the Role of the Internet
Misuse and Abuse of Opioid Analgesics – the Role of the Internet H. Siemann, J. Schnell, N. Scherbaum LVR Hospital Essen, Clinic for Dependent Behavior and Addiction Medicine University of Duisburg-Essen, Germany Misuse and Abuse of Opioid Analgesics – the Role of the Internet 09/18/2009 Opioid Analgesics • Prescription Drugs – Tramadol, Tilidine, Codeine, Loperamide – Easy to prescribe • Schedule III Drugs according to the German Narcotics Act (BtmG) – Morphine, Methadone, Fentanyl, Buprenorphine, Oxycodone – Special conditions to be fulfilled for a valid presciption Holger Siemann ([email protected]) 2 Misuse and Abuse of Opioid Analgesics – the Role of the Internet 09/18/2009 Prescription Rate Holger Siemann ([email protected]) 3 Misuse and Abuse of Opioid Analgesics – the Role of the Internet 09/18/2009 Non-Scheduled Opioids • Tramadol – Pain management (post-surgery treatment, injury treatment) • Tilidine + Naloxone (Valoron N®) – Higher analgesic potency – Prevention of parenteral drug abuse by combination with the µ-receptor antagonist Naloxone Holger Siemann ([email protected]) 4 Misuse and Abuse of Opioid Analgesics – the Role of the Internet 09/18/2009 Aim of the Study • To assess the role of the internet regarding the abuse of prescription opioids – Role as a trading platform – Role as an information system Holger Siemann ([email protected]) 5 Misuse and Abuse of Opioid Analgesics – the Role of the Internet 09/18/2009 Methods • Analysis of the first 50 websites provided by the leading search engine Google for