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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. -
The Use of Nitrous Oxide Gas for Lower Gastrointestinal Endoscopy Sophie Welchman, Sean Cochrane, Gary Minto, Stephen Lewis
Systematic review: The use of nitrous oxide gas for lower gastrointestinal endoscopy Sophie Welchman, Sean Cochrane, Gary Minto, Stephen Lewis To cite this version: Sophie Welchman, Sean Cochrane, Gary Minto, Stephen Lewis. Systematic review: The use of nitrous oxide gas for lower gastrointestinal endoscopy. Alimentary Pharmacology and Therapeutics, Wiley, 2010, 32 (3), pp.324. 10.1111/j.1365-2036.2010.04359.x. hal-00552574 HAL Id: hal-00552574 https://hal.archives-ouvertes.fr/hal-00552574 Submitted on 6 Jan 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. Alimentary Pharmacology & Therapeutic Systematic review: The use of nitrous oxide gas for lower gastrointestinal endoscopy ForJournal: Alimentary Peer Pharmacology Review & Therapeutics Manuscript ID: APT-0287-2010.R1 Manuscript Type: Systematic Review Date Submitted by the 13-May-2010 Author: Complete List of Authors: Welchman, Sophie; Derriford Hospital, Surgery Cochrane, Sean; Derriford Hospital, Gastroenterology Minto, Gary; Derriford Hospital, Anaesthesia Lewis, stephen; Derriford Hospital, -
Federal Register/Vol. 85, No. 36/Monday, February 24, 2020
10466 Federal Register / Vol. 85, No. 36 / Monday, February 24, 2020 / Notices Controlled substance Drug code Schedule Alphamethadol ................................................................................................................................................................. 9605 I Benzethidine .................................................................................................................................................................... 9606 I Betacetylmethadol ........................................................................................................................................................... 9607 I Clonitazene ...................................................................................................................................................................... 9612 I Diampromide ................................................................................................................................................................... 9615 I Diethylthiambutene .......................................................................................................................................................... 9616 I Dimethylthiambutene ....................................................................................................................................................... 9619 I Ketobemidone ................................................................................................................................................................. -
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 -
Prescription Regulations Summary Chart Who Hold an Approval to Prescribe Methadone from Their
Products included in the Triplicate Prescription Program* This is a reference list provided for convenience. While all generic medication names appear, only sample brand names are provided and it should not be viewed as an all-inclusive listing of all trade names of drugs included in the Triplicate Prescription Program. BUPRENORPHINE METHADONE BuTrans, Suboxone** Metadol, Methadose - May only be prescribed by physicians Prescription regulations summary chart who hold an approval to prescribe methadone from their BUTALBITAL PREPARATIONS provincial regulatory body*** Summary of federal and provincial laws governing prescription drug ordering, Fiorinal, Fiorinal C ¼ & C ½, Pronal, Ratio-Tecnal, records, prescription requirements, and refills Ratio-Tecnal C ¼ & C ½, Trianal, Trianal C ½ METHYLPHENIDATE Biphentin®, Foquest®, and Concerta® brands are excluded Revised 2019 BUTORPHANOL from TPP prescr ip t i o n p a d req u ir e m e n t s (generic versions Butorphanol NS, PMS-Butorphanol, Torbutrol (Vet), of these products require a triplicate presc ription) Torbugesic (Vet) Apo-Methyphenidate, PHL-Methylphenidate, PMS- Prescription regulations DEXTROPROPOXYPHENE Methylphenidate, PMS-Methylphenidate ER, Ratio- None identified Methylphenidate, Ritalin, Ritalin SR, Sandoz- According to the Standards of Practice for Pharmacists and Pharmacy Technicians: Methylphenidate SR, Teva-Methylphenidate ER-C FENTANYL/SUFENTANIL/ALFENTANIL 6.4 Neither a pharmacist nor a pharmacy technician may dispense a drug or blood product under a Alfentanil Injection, -
A Review of Unique Opioids and Their Conversions
A Review of Unique Opioids and Their Conversions Jacqueline Cleary, PharmD, BCACP Assistant Professor Albany College of Pharmacy and Health Sciences Adjunct Professor SAGE College of Nursing DISCLOSURES • Kaleo • Remitigate, LLC OBJECTIVES • Compare and contrast unique pharmacotherapy options for the treatment of chronic pain including: methadone, buprenoprhine, tapentadol, and tramadol • Select methadone, buprenorphine, tapentadol, or tramadol based on patient specific factors • Apply appropriate opioid conversion strategies to unique opioids • Understand opioid overdose risk surrounding opioid conversions and the use of unique opioids UNIQUE OPIOIDS METHADONE, BUPRENORPHINE, TRAMADOL, TAPENTADOL METHADONE My favorite drug because….? METHADONE- INDICATIONS • FDA labeled indications – (1) chronic pain (2) detoxification Oral soluble tablets for suspension NOT indicated for chronic pain treatment • Initial inpatient detoxification of opioids by a licensed trained provider with methadone and supportive care is appropriate • Methadone maintenance provider must have special credentialing and training as required by state Outpatient prescription must be for pain ONLY and say “for pain” on RX • Continuation of methadone maintenance from outside provider while patient is inpatient for another condition is appropriate http://cdn.atforum.com/wp-content/uploads/SAMHSA-2015-Guidelines-for-OTPs.pdf MECHANISM OF ACTION • Potent µ-opioid agonist • NMDA receptor antagonist • Norepinephrine reuptake inhibitor • Serotonin reuptake inhibitor ADVERSE EVENTS -
Kappa Opioid Receptor Regulation of Erk1/2 Map Kinase Signaling Cascade
1 KAPPA OPIOID RECEPTOR REGULATION OF ERK1/2 MAP KINASE SIGNALING CASCADE: MOLECULAR MECHANISMS MODULATING COCAINE REWARD A dissertation presented by Khampaseuth Rasakham to The Department of Psychology In partial fulfillment of the requirements for the degree of Doctor of Philosophy in the field of Psychology Northeastern University Boston, Massachusetts August, 2008 2 KAPPA OPIOID RECEPTOR REGULATION OF ERK1/2 MAP KINASE SIGNALING CASCADE: MOLECULAR MECHANISMS MODULATING COCAINE REWARD by Khampaseuth Rasakham ABSTRACT OF DISSERTATION Submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy in Psychology in the Graduate School of Arts and Sciences of Northeastern University, August, 2008 3 ABSTRACT Activation of the Kappa Opioid Receptor (KOR) modulates dopamine (DA) signaling, and Extracellular Regulated Kinase (ERK) Mitogen-Activated Protein (MAP) kinase activity, thereby potentially regulating the rewarding effects of cocaine. The central hypothesis to be tested is that the time-and drug-dependent KOR-mediated regulation of ERK1/2 MAP kinase activity occurs via distinct molecular mechanisms, which in turn may determine the modulation (suppression or potentiation) by KOR effects on cocaine conditioned place preference (CPP). Three studies were performed to test this hypothesis. Study 1 examined the effects of U50,488 and salvinorin A on cocaine reward. In these studies, mice were treated with equianalgesic doses of agonist from 15 to 360 min prior to daily saline or cocaine place conditioning. At time points corresponding with peak biological activity, both agonists produced saline-conditioned place aversion and suppressed cocaine-CPP, effects blocked by the KOR antagonist nor-BNI. However, when mice were place conditioned with cocaine 90 min after agonist pretreatment, U50,488-pretreated mice demonstrated a 2.5-fold potentiation of cocaine-CPP, whereas salvinorin A-pretreated mice demonstrated normal cocaine-CPP responses. -
Ketamine for Chronic Non- Cancer Pain: a Review of Clinical Effectiveness, Cost- Effectiveness, And
CADTH RAPID RESPONSE REPORT: SUMMARY WITH CRITICAL APPRAISAL Ketamine for Chronic Non- Cancer Pain: A Review of Clinical Effectiveness, Cost- Effectiveness, and Guidelines Service Line: Rapid Response Service Version: 1.0 Publication Date: May 28, 2020 Report Length: 28 Pages Authors: Khai Tran, Suzanne McCormack Cite As: Ketamine for Chronic Non-Cancer Pain: A Review of Clinical Effectiveness, Cost-Effectiveness, and Guidelines. Ottawa: CADTH; 2020 May. (CADTH rapid response report: summary with critical appraisal) ISSN: 1922-8147 (online) Disclaimer: The information in this document is intended to help Canadian health care decision-makers, health care professionals, health systems leaders, and policy-makers make well-informed decisions and thereby improve the quality of health care services. While patients and others may access this document, the document is made available for informational purposes only and no representations or warranties are made with respect to its fitness for any particular purpose. The information in this document should not be used as a substitute for professional medical advice or as a substitute for the application of clinical judgment in respect of the care of a particular patient or other professional judgment in any decision-making process. The Canadian Agency for Drugs and Technologies in Health (CADTH) does not endorse any information, drugs, therapies, treatments, products, processes, or services. While care has been taken to ensure that the information prepared by CADTH in this document is accurate, complete, and up-to-date as at the applicable date the material was first published by CADTH, CADTH does not make any guarantees to that effect. CADTH does not guarantee and is not responsible for the quality, currency, propriety, accuracy, or reasonableness of any statements, information, or conclusions contained in any third-party materials used in preparing this document. -
Best Bets from the Manchester Royal Infirmary Edited by K Mackway-Jones
247 BEST EVIDENCE TOPIC REPORTS Emerg Med J: first published as 10.1136/emj.19.3.248 on 1 May 2002. Downloaded from Towards evidence based emergency medicine: best BETs from the Manchester Royal Infirmary Edited by K Mackway-Jones Clinical scenario Best evidence topic reports (BETs) summarise the evidence A 23 year old woman attends an emergency department hav- pertaining to particular clinical questions. They are not ing taken sixty 500 mg paracetamol tablets. Her four hour systematic reviews, but rather contain the best (highest paracetamol levels are above the treatment line. She does not level) evidence that can be practically obtained by busy want to be treated with intravenous therapy. You wonder practising clinicians. The search strategies used to find the whether oral antidote is as effective. best evidence are reported in detail in order to allow clinicians to update searches whenever necessary. The BETs published below were first reported at the Critical Three part question Appraisal Journal Club at the Manchester Royal Infirmary.1 In [patients who need an antidote for paracetamol overdose] Each BET has been constructed in the four stages that have is [intravenous therapy better than oral therapy] at [prevent- been described elsewhere.2 The BETs shown here together ing liver damage and death]? with those published previously and those currently under construction can be seen at http://www.bestbets.org.3 Six Search strategy BETs are included in this issue of the journal. Medline 1966 to 12/01 using the OVID interface. [exp acetyl- -
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. -
Recommended Methods for the Identification and Analysis of Fentanyl and Its Analogues in Biological Specimens
Recommended methods for the Identification and Analysis of Fentanyl and its Analogues in Biological Specimens MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES Laboratory and Scientific Section UNITED NATIONS OFFICE ON DRUGS AND CRIME Vienna Recommended Methods for the Identification and Analysis of Fentanyl and its Analogues in Biological Specimens MANUAL FOR USE BY NATIONAL DRUG ANALYSIS LABORATORIES UNITED NATIONS Vienna, 2017 Note Operating and experimental conditions are reproduced from the original reference materials, including unpublished methods, validated and used in selected national laboratories as per the list of references. A number of alternative conditions and substitution of named commercial products may provide comparable results in many cases. However, any modification has to be validated before it is integrated into laboratory routines. ST/NAR/53 Original language: English © United Nations, November 2017. All rights reserved. The designations employed and the presentation of 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. Mention of names of firms and commercial products does not imply the endorse- ment of the United Nations. This publication has not been formally edited. Publishing production: English, Publishing and Library Section, United Nations Office at Vienna. Acknowledgements The Laboratory and Scientific Section of the UNODC (LSS, headed by Dr. Justice Tettey) wishes to express its appreciation and thanks to Dr. Barry Logan, Center for Forensic Science Research and Education, at the Fredric Rieders Family Founda- tion and NMS Labs, United States; Amanda L.A.