G.P. Ellis (9).Pdf
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Anticonvulsants
ALZET® Bibliography References on the Administration of Anticonvulsive Agents Using ALZET Osmotic Pumps 1. Carbamazepine Q5784: K. Deseure, et al. Differential drug effects on spontaneous and evoked pain behavior in a model of trigeminal neuropathic pain. J Pain Res 2017;10(279-286 ALZET Comments: Carbamazepine, baclofen, clomipramine; DMSO, PEG, Ethyl Alcohol, Acetone; SC; Rat; 2ML1; Controls received mp w/ vehicle; animal info (7 weeks old); dimethyl sulfoxide, propylene glycol, ethyl alcohol, and acetone at a ratio of 42:42:15:1; post op. care (morphine 5 mg/day); behavioral testing (Facial grooming); Therapeutic indication (Trigeminal neuralgia, neuropathic pain); Dose (30 mg/day carbamazepine (the first-line drug treatment for trigeminal neuralgia), 1.06 mg/day baclofen, 4.18 mg/day clomipramine, and 5 mg/day morphine);. Q0269: S. M. Cain, et al. High resolution micro-SPECT scanning in rats using 125I beta-CIT: Effects of chronic treatment with carbamazepine. Epilepsia 2009;50(8):1962-1970 ALZET Comments: Carbamazepine; DMSO; propylene glycol; ethyl alcohol; acetone; SC; Rat; 2ML2; 14 days; Controls received mp w/ vehicle; animal info (adult, male, Sprague-Dawley, 160-270 g); functionality of mp verified by serum drug levels; 42% DMSO used; identified 3 mg/kg/day as the highest dose that could be reliably administered via minipumps over a 14-day period at 37 degrees Celsius, pg. 1969. P5195: H. C. Doheny, et al. A comparison of the efficacy of carbamazepine and the novel anti-epileptic drug levetiracetam in the tetanus toxin model of focal complex partial epilepsy. British Journal of Pharmacology 2002;135(6):1425-1434 ALZET Comments: Carbamazepine; levetiracetam; DMSO; Propylene glycol; ethanol, saline; IP; Rat; 7 days; Controls received mp/ vehicle; functionality of mp verified by drug serum levels; dose-response (text p.1428); carbamazepine was dissolved in 42.5% DMSO/42% Propylene glycol/15% ethanol. -
(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. -
United States Patent (19) (11) 4,310,524 Wiech Et Al
United States Patent (19) (11) 4,310,524 Wiech et al. 45 Jan. 12, 1982 (54) TCA COMPOSITION AND METHOD FOR McMillen et al., Fed. Proc., 38,592 (1979). RAPD ONSET ANTDEPRESSANT Sellinger et al., Fed. Proc., 38,592 (1979). THERAPY Pandey et al., Fed. Proc., 38,592 (1979). 75) Inventors: Norbert L. Wiech; Richard C. Ursillo, Primary Examiner-Stanley J. Friedman both of Cincinnati, Ohio Attorney, Agent, or Firm-Millen & White 73) Assignee: Richardson-Merrell, Inc., Wilton, Conn. (57 ABSTRACT A method is provided for treating depression in a pa (21) Appl. No.: 139,498 tient therefrom and requiring rapid symptomatic relief, (22 Filed: Apr. 11, 1980 which comprises administering to said patient concur 51) Int. Cl. .................... A61K 31/33; A61K 31/135 rently (a) an effective antidepressant amount of a tricy clic antidepressant or a pharmaceutically effective acid (52) ...... 424/244; 424/330 addition salt thereof, and (b) an amount of an a-adrener 58) Field of Search ................................ 424/244, 330 gic receptor blocking agent effective to achieve rapid (56) References Cited onset of the antidepressant action of (a), whereby the PUBLICATIONS onset of said antidepressant action is achieved within Chemical Abst., vol. 66-72828m, (1967), Kellett. from 1 to 7 days. Chemical Abst, vol. 68-94371a, (1968), Martelli et al. A pharmaceutical composition is also provided which is Chemical Abst., vol. 74-86.048j, (1971), Dixit et al. especially adapted for use with the foregoing method. Holmberg et al., Psychopharm., 2,93 (1961). Svensson, Symp. Med. Hoechst., 13, 245 (1978). 17 Claims, No Drawings 4,310,524 1. -
1 'New/Designer Benzodiazepines'
1 ‘New/Designer Benzodiazepines’: an analysis of the literature and psychonauts’ trip reports 2 Laura Orsolini*1,2,3, John M. Corkery1, Stefania Chiappini1, Amira Guirguis1, Alessandro Vento4,5,6,7, 3 Domenico De Berardis3,8,9, Duccio Papanti1, and Fabrizio Schifano1 4 5 1 Psychopharmacology, Drug Misuse and Novel Psychoactive Substances Research Unit, School of Life and Medical 6 Sciences, University of Hertfordshire, Hatfield, AL10 9AB, Herts, UK. 7 2 Neomesia Mental Health, Villa Jolanda Hospital, Jesi, Italy. 8 3 Polyedra, Teramo, Italy. 9 4 NESMOS Department (Neurosciences, Mental Health and Sensory Organs), Sapienza University – Rome, School of 10 Medicine and Psychology; Sant’Andrea Hospital, Rome, Italy 11 5 School of psychology - G. Marconi Telematic University, Rome, Italy 12 6 Addictions Observatory (ODDPSS), Rome, Italy 13 7 Mental Health Department - ASL Roma 2, Rome, Italy 14 8 Department of Neuroscience, Imaging and Clinical Science, Chair of Psychiatry, University of “G. D’Annunzio”, Chieti, 15 Italy. 16 9 NHS, Department of Mental Health, Psychiatric Service of Diagnosis and Treatment, Hospital “G. Mazzini”, ASL 4 17 Teramo, Italy. 18 19 Corresponding author: 20 Laura Orsolini, Psychopharmacology, Drug Misuse and Novel Psychoactive Substances Research Unit, School of Life 21 and Medical Sciences, University of Hertfordshire, Hatfield, AL10 9AB, Herts, UK; Villa Jolanda Hospital, Neomesia 22 Mental Health, Villa Jolanda, Italy; Polyedra, Teramo, Italy; E-mail address: [email protected]. Tel.: (+39) 392 23 3244643. 24 25 Conflicts of Interest 26 The authors declare that this research was conducted in the absence of any commercial or financial relationships 27 that could be construed as a potential conflict of interest. -
Antidepressant Potential of Nitrogen-Containing Heterocyclic Moieties: an Updated Review
Review Article Antidepressant potential of nitrogen-containing heterocyclic moieties: An updated review Nadeem Siddiqui, Andalip, Sandhya Bawa, Ruhi Ali, Obaid Afzal, M. Jawaid Akhtar, Bishmillah Azad, Rajiv Kumar Department of ABSTRACT Pharmaceutical Chemistry, Depression is currently the fourth leading cause of disease or disability worldwide. Antidepressant is Faculty of Pharmacy, Jamia Hamdard approved for the treatment of major depression (including paediatric depression), obsessive-compulsive University, Hamdard disorder (in both adult and paediatric populations), bulimia nervosa, panic disorder and premenstrual Nagar, New Delhi - dysphoric disorder. Antidepressant is a psychiatric medication used to alleviate mood disorders, such as 110 062, India major depression and dysthymia and anxiety disorders such as social anxiety disorder. Many drugs produce an antidepressant effect, but restrictions on their use have caused controversy and off-label prescription a Address for correspondence: risk, despite claims of superior efficacy. Our current understanding of its pathogenesis is limited and existing Dr. Sandhya Bawa, E-mail: sandhyabawa761@ treatments are inadequate, providing relief to only a subset of people suffering from depression. Reviews of yahoo.com literature suggest that heterocyclic moieties and their derivatives has proven success in treating depression. Received : 08-02-11 Review completed : 15-02-11 Accepted : 17-02-11 KEY WORDS: Antidepressant, depression, heterocyclic epression is a chronic, recurring and potentially life- monoamine oxidase inhibitors (MAOIs, e.g. Nardil®) tricyclic D threatening illness that affects up to 20% of the population antidepressants (TCAs, e.g. Elavil). They increases the synaptic across the globe.[1] The etiology of the disease is suboptimal concentration of either two (5-HT and NE) or all three (5-HT, concentrations of the monoamine neurotransmitters serotonin NE and dopamine (DA)) neurotransmitters. -
Drugs for Primary Prevention of Atherosclerotic Cardiovascular Disease: an Overview of Systematic Reviews
Supplementary Online Content Karmali KN, Lloyd-Jones DM, Berendsen MA, et al. Drugs for primary prevention of atherosclerotic cardiovascular disease: an overview of systematic reviews. JAMA Cardiol. Published online April 27, 2016. doi:10.1001/jamacardio.2016.0218. eAppendix 1. Search Documentation Details eAppendix 2. Background, Methods, and Results of Systematic Review of Combination Drug Therapy to Evaluate for Potential Interaction of Effects eAppendix 3. PRISMA Flow Charts for Each Drug Class and Detailed Systematic Review Characteristics and Summary of Included Systematic Reviews and Meta-analyses eAppendix 4. List of Excluded Studies and Reasons for Exclusion This supplementary material has been provided by the authors to give readers additional information about their work. © 2016 American Medical Association. All rights reserved. 1 Downloaded From: https://jamanetwork.com/ on 09/28/2021 eAppendix 1. Search Documentation Details. Database Organizing body Purpose Pros Cons Cochrane Cochrane Library in Database of all available -Curated by the Cochrane -Content is limited to Database of the United Kingdom systematic reviews and Collaboration reviews completed Systematic (UK) protocols published by by the Cochrane Reviews the Cochrane -Only systematic reviews Collaboration Collaboration and systematic review protocols Database of National Health Collection of structured -Curated by Centre for -Only provides Abstracts of Services (NHS) abstracts and Reviews and Dissemination structured abstracts Reviews of Centre for Reviews bibliographic -
Self-Measured Compared to Office
Systematic Review for the 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults: Supplemental Tables and Figures Part 1: Self-Measured Compared to Office-Based Measurement of Blood Pressure in the Management of Adults With Hypertension Table 1.1 Electronic search terms used for the current meta-analysis (Part 1 – Self-Measured Compared to Office-Based Measurement of Blood Pressure in the Management of Adults With Hypertension). PubMed Search (Blood Pressure Monitoring, Ambulatory [mesh] OR self care [mesh] OR telemedicine [mesh] OR patient participation [tiab] OR ambulatory [tiab] OR kiosk [tiab] OR kiosks [tiab] OR self-monitor* [tiab] OR self-measure* [tiab] OR self-care* [tiab] OR self-report* [tiab] OR telemonitor* [tiab] OR tele-monitor* [tiab] OR home monitor* [tiab] OR telehealth [tiab] OR tele-health [tiab] OR telemonitor* [tiab] OR tele-monitor* [tiab] OR telemedicine [tiab] OR patient-directed [tiab] OR Blood pressure monitoring “patient directed” [tiab] OR HMBP [tiab] OR SMBP [tiab] OR home [tiab] OR white coat [tiab] OR concept + Self Care concept ((patient participation [ot] OR ambulatory [ot] OR kiosk [ot] OR kiosks [ot] OR self-monitor* [ot] OR self-measure* [ot] OR self-care* [ot] OR self-report* [ot] OR telemonitor* [ot] OR tele-monitor* [ot] OR home monitor* [ot] OR telehealth [ot] OR tele-health [ot] OR telemonitor* [ot] OR tele- monitor* [ot] OR telemedicine [ot] OR patient-directed [tiab] OR “patient directed” [tiab] -
A Review of the Evidence of Use and Harms of Novel Benzodiazepines
ACMD Advisory Council on the Misuse of Drugs Novel Benzodiazepines A review of the evidence of use and harms of Novel Benzodiazepines April 2020 1 Contents 1. Introduction ................................................................................................................................. 4 2. Legal control of benzodiazepines .......................................................................................... 4 3. Benzodiazepine chemistry and pharmacology .................................................................. 6 4. Benzodiazepine misuse............................................................................................................ 7 Benzodiazepine use with opioids ................................................................................................... 9 Social harms of benzodiazepine use .......................................................................................... 10 Suicide ............................................................................................................................................. 11 5. Prevalence and harm summaries of Novel Benzodiazepines ...................................... 11 1. Flualprazolam ......................................................................................................................... 11 2. Norfludiazepam ....................................................................................................................... 13 3. Flunitrazolam .......................................................................................................................... -
2-Adrenergic Receptor Is Determined by Conformational Equilibrium in the Transmembrane Region
ARTICLE Received 21 Mar 2012 | Accepted 2 Aug 2012 | Published 4 Sep 2012 DOI: 10.1038/ncomms2046 Efficacy of theβ 2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region Yutaka Kofuku1,2, Takumi Ueda1, Junya Okude1, Yutaro Shiraishi1, Keita Kondo1, Masahiro Maeda3, Hideki Tsujishita3 & Ichio Shimada1,4 Many drugs that target G-protein-coupled receptors (GPCRs) induce or inhibit their signal transduction with different strengths, which affect their therapeutic properties. However, the mechanism underlying the differences in the signalling levels is still not clear, although several structures of GPCRs complexed with ligands determined by X-ray crystallography are available. Here we utilized NMR to monitor the signals from the methionine residue at position 82 in neutral antagonist- and partial agonist-bound states of β2-adrenergic receptor (β2AR), which are correlated with the conformational changes of the transmembrane regions upon activation. We show that this residue exists in a conformational equilibrium between the inverse agonist- bound states and the full agonist-bound state, and the population of the latter reflects the signal transduction level in each ligand-bound state. These findings provide insights into the multi-level signalling of β2AR and other GPCRs, including the basal activity, and the mechanism of signal transduction mediated by GPCRs. 1 Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo 7-3-1, Bunkyo-ku, Tokyo 113-0033, Japan. 2 Japan Biological Informatics Consortium (JBIC), Tokyo 135-0064, Japan. 3 Shionogi Co., Ltd., Discovery Research Laboratories, Osaka 561-0825, Japan. 4 Biomedicinal Information Research Center (BIRC), National Institute of Advanced Industrial Science and Technology (AIST), Aomi 2-41-6, Koto-ku, Tokyo 135-0064, Japan. -
The Organic Chemistry of Drug Synthesis
THE ORGANIC CHEMISTRY OF DRUG SYNTHESIS VOLUME 3 DANIEL LEDNICER Analytical Bio-Chemistry Laboratories, Inc. Columbia, Missouri LESTER A. MITSCHER The University of Kansas School of Pharmacy Department of Medicinal Chemistry Lawrence, Kansas A WILEY-INTERSCIENCE PUBLICATION JOHN WILEY AND SONS New York • Chlchester • Brisbane * Toronto • Singapore Copyright © 1984 by John Wiley & Sons, Inc. All rights reserved. Published simultaneously in Canada. Reproduction or translation of any part of this work beyond that permitted by Section 107 or 108 of the 1976 United States Copyright Act without the permission of the copyright owner is unlawful. Requests for permission or further information should be addressed to the Permissions Department, John Wiley & Sons, Inc. Library of Congress Cataloging In Publication Data: (Revised for volume 3) Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." Includes bibliographical references and index. 1. Chemistry, Pharmaceutical. 2. Drugs. 3. Chemistry, Organic—Synthesis. I. Mitscher, Lester A., joint author. II. Title. [DNLM 1. Chemistry, Organic. 2. Chemistry, Pharmaceutical. 3. Drugs—Chemical synthesis. QV 744 L473o 1977] RS403.L38 615M9 76-28387 ISBN 0-471-09250-9 (v. 3) Printed in the United States of America 10 907654321 With great pleasure we dedicate this book, too, to our wives, Beryle and Betty. The great tragedy of Science is the slaying of a beautiful hypothesis by an ugly fact. Thomas H. Huxley, "Biogenesis and Abiogenisis" Preface Ihe first volume in this series represented the launching of a trial balloon on the part of the authors. In the first place, wo were not entirely convinced that contemporary medicinal (hemistry could in fact be organized coherently on the basis of organic chemistry. -
INFORMATION to USERS the Quality of This Reproduction Is
INFORMATION TO USERS This manuscript has been reproduced from the microfilm master. UMI films the text directly from the original or copy submitted. Thus, some thesis and dissertation copies are in typewriter face, while others may be fiom any type of computer printer. The quality of this reproduction is dependent upon the quality of the copy submitted. Broken or indistinct print, colored or poor quality illustrations and photographs, print bleedthrough, substandard margins, and improper alignment can adversely affect reproduction. In the unlikely event that the author did not send UMI a complete manuscript and there are missing pages, these will be noted. Also, if unauthorized copyright material had to be removed, a note will indicate the deletion. Oversize materials (e.g., maps, drawings, charts) are reproduced by sectioning the original, beginning at the upper left-hand comer and continuing from left to right in equal sections with small overlaps. Each original is also photographed in one eq)osure and is included in reduced form at the back of the book. Photographs included in the original manuscript have been reproduced xerographically in this copy. Higher quality 6” x 9” black and white photographic prints are available for any photographs or illustrations appearing in this copy for an additional charge. Contact UMI directly to order. UMI A Bell & Howell Information Company 300 North Zeeb Road, Ann Aibor MI 48106-1346 USA 313/761-4700 800/521-0600 PHARMACOLOGICAL EVALUATION OF TRIMETOQUINOL ANALOGS AS AFFINITY LIGANDS FOR S-ADRENERGIC RECEPTOR SYSTEMS A Dissertation Presented in Partial Fulfillment of the Requirements for the Degree of Doctor of Philosophy in the Graduate School of The Ohio State University By Ratnavali C. -
(12) United States Patent (10) Patent No.: US 7,119,196 B2 Cook Et Al
US007 119196B2 (12) United States Patent (10) Patent No.: US 7,119,196 B2 Cook et al. (45) Date of Patent: Oct. 10, 2006 (54) ANXIOLYTIC AGENTS WITH REDUCED Armin Walser, et al., “Triazolobenzo- and Triazolothienodiazepines SEDATIVE AND ATAXC EFFECTS as Potent Antagonists of Platelet Activating Factor,” “Journal of Medicinal Chemistry,” 1991, pp. 1209-1221, vol. 34, No. 3, Ameri (75) Inventors: James M. Cook, Whitefish Bay, WI can Chemistry Society. (US); Qi Huang, Moorpark, CA (US); Qi Huang, “Part One: A Chemical and Computer Assisted Approach to Pharmacophore/Receptor Models for GABAaBZ Receptor Sub Xiaohui He, San Diego, CA (US); types; Part Two: Predictive Models for GABAaBZR Subtypes Via Xioayan Li, Milwaukee, WI (US); Comparative Molecular Field Analysis.” DISSERTATION, UW Jianming Yu, Princeton, NJ (US); Milwaukee, 1998, pp. 1-296. Dongmei Han, Milwaukee, WI (US); Shu Yu, et al., “Studies in the Search for a5 Subtype Selective Snjezana Lelas, Middletown, CT (US); Agonists for GABAaBZR Sites,” “Medicinal Chemistry Research.” John F. McElroy, Wilmington, DE 1999, pp. 71-88, Birkhauser Boston. (US) Qi Huang, et al., “Pharmacophore Receptor Models for GABAa? BZR Subtypes (alB3y2, aSB3y2, and aoB3y2) via a Comprehensive (73) Assignee: Wisys Technology Foundation, Inc., Ligand Mapping Approach.” “J. Med. Chem.” 2000, pp. 71-95, Madison, WI (US) American Chemical Society. Xiaohui He, et al., “Pharmacophore/Receptor Models for GABAa? (*) Notice: Subject to any disclaimer, the term of this BZRa2B3y2, a3B3y2 and a4B3y2 Recombinant Subtypes. Induced patent is extended or adjusted under 35 Volume Analysis and Comparison to alB3y2, aSB3y2 and aoB3y2 U.S.C. 154(b) by 198 days.