Pharmacological Classification of the Abuse-Related Discriminative
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Callistephin Enhances the Protective Effects of Isoflurane on Microglial Injury Through Downregulation of Inflammation and Apoptosis
802 MOLECULAR MEDICINE REPORTS 20: 802-812, 2019 Callistephin enhances the protective effects of isoflurane on microglial injury through downregulation of inflammation and apoptosis LILI ZHAO, SHIBIAO CHEN, TIANYIN LIU, XIUHONG WANG, HAIJIN HUANG and WEICHENG LIU Department of Anesthesiology, The First Affiliated Hospital of Nanchang University, Nanchang, Jiangxi 330006, P.R. China Received June 18, 2018; Accepted March 15, 2019 DOI: 10.3892/mmr.2019.10282 Abstract. Microglia are the major immune cells in the central enhanced the effects of isoflurane. Callistephin may therefore nervous system. Microglial activation can be beneficial or constitute a candidate drug agent that may target inflammatory detrimental depending on the stimuli and the physiopathological and growth regulatory signaling pathways, thus ameliorating environment. Microglial activation is involved in a variety certain aspects of neurodegenerative diseases. of neurodegenerative disorders. Different anesthetic agents have exhibited diverse effects on microglial activation and Introduction the engulfment process. The anthocyanin callistephin has been demonstrated to have antioxidant and anti‑inflammatory Microglial cells are the major immune cell in the central properties, and these were assessed in the present study, with a nervous system (CNS), responding against types of endog- focus on its effect on microglial activation. Mouse microglial enous and exogenous stimuli, including infection by bacteria, cells C8-4B were treated with 100 ng/µl lipopolysaccharide viruses, prions and β-amyloid plaques (1). Microglia are (LPS) and 1 ng/µl interferon-γ. Cells were subsequently treated activated upon exposure to different stimuli and, depending with 2% isoflurane, 100 µM callistephin or both. LPS promoted on the environmental context, this may be beneficial or detri- apoptosis in C8-B4 cells, and this was reduced following mental to the functionality and physiology of the CNS (2). -
Pharmacology – Inhalant Anesthetics
Pharmacology- Inhalant Anesthetics Lyon Lee DVM PhD DACVA Introduction • Maintenance of general anesthesia is primarily carried out using inhalation anesthetics, although intravenous anesthetics may be used for short procedures. • Inhalation anesthetics provide quicker changes of anesthetic depth than injectable anesthetics, and reversal of central nervous depression is more readily achieved, explaining for its popularity in prolonged anesthesia (less risk of overdosing, less accumulation and quicker recovery) (see table 1) Table 1. Comparison of inhalant and injectable anesthetics Inhalant Technique Injectable Technique Expensive Equipment Cheap (needles, syringes) Patent Airway and high O2 Not necessarily Better control of anesthetic depth Once given, suffer the consequences Ease of elimination (ventilation) Only through metabolism & Excretion Pollution No • Commonly administered inhalant anesthetics include volatile liquids such as isoflurane, halothane, sevoflurane and desflurane, and inorganic gas, nitrous oxide (N2O). Except N2O, these volatile anesthetics are chemically ‘halogenated hydrocarbons’ and all are closely related. • Physical characteristics of volatile anesthetics govern their clinical effects and practicality associated with their use. Table 2. Physical characteristics of some volatile anesthetic agents. (MAC is for man) Name partition coefficient. boiling point MAC % blood /gas oil/gas (deg=C) Nitrous oxide 0.47 1.4 -89 105 Cyclopropane 0.55 11.5 -34 9.2 Halothane 2.4 220 50.2 0.75 Methoxyflurane 11.0 950 104.7 0.2 Enflurane 1.9 98 56.5 1.68 Isoflurane 1.4 97 48.5 1.15 Sevoflurane 0.6 53 58.5 2.5 Desflurane 0.42 18.7 25 5.72 Diethyl ether 12 65 34.6 1.92 Chloroform 8 400 61.2 0.77 Trichloroethylene 9 714 86.7 0.23 • The volatile anesthetics are administered as vapors after their evaporization in devices known as vaporizers. -
(12) United States Patent (10) Patent No.: US 8,603,526 B2 Tygesen Et Al
USOO8603526B2 (12) United States Patent (10) Patent No.: US 8,603,526 B2 Tygesen et al. (45) Date of Patent: Dec. 10, 2013 (54) PHARMACEUTICAL COMPOSITIONS 2008. O152595 A1 6/2008 Emigh et al. RESISTANT TO ABUSE 2008. O166407 A1 7/2008 Shalaby et al. 2008/0299.199 A1 12/2008 Bar-Shalom et al. 2008/0311205 A1 12/2008 Habib et al. (75) Inventors: Peter Holm Tygesen, Smoerum (DK); 2009/0022790 A1 1/2009 Flath et al. Jan Martin Oevergaard, Frederikssund 2010/0203129 A1 8/2010 Andersen et al. (DK); Karsten Lindhardt, Haslev (DK); 2010/0204259 A1 8/2010 Tygesen et al. Louise Inoka Lyhne-versen, Gentofte 2010/0239667 A1 9/2010 Hemmingsen et al. (DK); Martin Rex Olsen, Holbaek 2010, O291205 A1 11/2010 Downie et al. (DK); Anne-Mette Haahr, Birkeroed 2011 O159100 A1 6/2011 Andersen et al. (DK); Jacob Aas Hoellund-Jensen, FOREIGN PATENT DOCUMENTS Frederikssund (DK); Pemille Kristine Hoeyrup Hemmingsen, Bagsvaerd DE 20 2006 014131 1, 2007 (DK) EP O435,726 8, 1991 EP O493513 7, 1992 EP O406315 11, 1992 (73) Assignee: Egalet Ltd., London (GB) EP 1213014 6, 2002 WO WO 89,09066 10, 1989 (*) Notice: Subject to any disclaimer, the term of this WO WO91,040 15 4f1991 patent is extended or adjusted under 35 WO WO95/22962 8, 1995 U.S.C. 154(b) by 489 days. WO WO99,51208 10, 1999 WO WOOOf 41704 T 2000 WO WO 03/024426 3, 2003 (21) Appl. No.: 12/701,429 WO WOO3,O24429 3, 2003 WO WOO3,O24430 3, 2003 (22) Filed: Feb. -
1,1,1-Trichloroethane (CASRN 71-55-6) | IRIS
Integrated Risk Information System (IRIS) U.S. Environmental Protection Agency Chemical Assessment Summary National Center for Environmental Assessment 1,1,1-Trichloroethane; CASRN 71-55-6 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data, as outlined in the IRIS assessment development process. Sections I (Health Hazard Assessments for Noncarcinogenic Effects) and II (Carcinogenicity Assessment for Lifetime Exposure) present the conclusions that were reached during the assessment development process. Supporting information and explanations of the methods used to derive the values given in IRIS are provided in the guidance documents located on the IRIS website. STATUS OF DATA FOR 1,1,1-Trichloroethane File First On-Line 03/31/1987 Category (section) Assessment Available? Last Revised Oral RfD (I.A.) Acute Oral RfD (I.A.1.) qualitative discussion 09/28/2007 Short-term Oral RfD (I.A.2.) qualitative discussion 09/28/2007 Subchronic Oral RfD (I.A.3.) yes 09/28/2007 Chronic Oral RfD (I.A.4.) yes 09/28/2007 Inhalation RfC (I.B.) Acute Inhalation RfC (I.B.1.) yes 09/28/2007 Short-term Inhalation RfC (I.B.2.) yes 09/28/2007 Subchronic Inhalation RfC (I.B.3.) yes 09/28/2007 1 Integrated Risk Information System (IRIS) U.S. Environmental Protection Agency Chemical Assessment Summary National Center for Environmental Assessment Category (section) Assessment Available? Last Revised Chronic Inhalation RfC (I.B.4.) yes 09/28/2007 Carcinogenicity Assessment (II.) yes 09/28/2007 I. Health Hazard Assessments for Noncarcinogenic Effects I.A. -
An Overview on “Stages of Anesthesia and Some Novel General Anesthetics Drug”
Rohit Jaysing Bhor. et al. /Asian Journal of Research in Chemistry and Pharmaceutical Sciences. 5(4), 2017, 132-140. Review Article ISSN: 2349 – 7106 Asian Journal of Research in Chemistry and Pharmaceutical Sciences Journal home page: www.ajrcps.com AN OVERVIEW ON “STAGES OF ANESTHESIA AND SOME NOVEL GENERAL ANESTHETICS DRUG” Rohit Jaysing Bhor *1 , Bhadange Shubhangi 1, C. J. Bhangale 1 1* Department of Pharmaceutical Chemistry, PRES’s College of Pharmacy Chincholi, Tal-Sinner, Dist-Nasik, Maharashtra, India. ABSTRACT Anesthesia is a painless performance of medical producers. There are both major and minor risks of anesthesia. Anesthesia is a state of temporary induced loss of sensation or awareness. It gives analgesia i.e. relief from pain or prevention of pain and paralysis. General anaesthesia is a medically induced state of unconsciousness. It gives loss of protective reflux. It is carried out to allow medical procedures or medical surgery. It can be classified into 3 types like Intravenous Anesthetics Drug; Miscellaneous Drug; and Inhalational anesthetic Drug. Sodium thiopental is an ultra-short-acting barbiturate and has been used commonly in the induction phase of anesthesia. Methohexital is an example of barbiturates derivatives. It is classified as short-acting, and has a rapid onset of action. KEYWORDS Anesthesia, Sodium thiopental, Methohexital and Propofol. Author for Correspondence: INTRODUCTON Anesthesia is a state of temporary induced loss of sensation or awareness. It gives analgesia i.e. relief 1 Rohit Jaysing Bhor, from pain or prevention of pain and paralysis . A patient under the effects of anesthetic drug is known Department of Pharmaceutical Chemistry, as anesthetized. -
Visualizing Anesthesia-Induced Vasodilation of Cerebral Vasculature Using Multi-Exposure Speckle Imaging
bioRxiv preprint doi: https://doi.org/10.1101/2020.06.26.174227; this version posted June 29, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY 4.0 International license. Visualizing anesthesia-induced vasodilation of cerebral vasculature using multi-exposure speckle imaging Colin T. Sullendera, Lisa M. Richardsa, Fei Heb, Lan Luanb,c, Andrew K. Dunna,* aDepartment of Biomedical Engineering, University of Texas at Austin, 107 W. Dean Keeton Street Stop C0800, Austin, Texas, 78712, United States bDepartment of Electrical and Computer Engineering, Rice University, 6100 Main Street, Houston, TX, 77005, United States cDepartment of Bioengineering, Rice University, 6100 Main Street, Houston, TX, 77005, United States Abstract. Anesthetized animal models are used extensively during neurophysiological and behavioral studies despite systemic effects from anesthesia that undermine both accurate interpretation and translation to awake human physi- ology. In this paper, we characterize the impact of isoflurane on cerebral blood flow (CBF) during the induction of general anesthesia in awake mice using multi-exposure speckle imaging (MESI). We highlight the large anatomical changes caused by the vasodilatory inhalant with wide-field imagery and quantify the cortical hemodynamics with MESI across multiple subjects and imaging sessions. Compared to the awake state, we measured, on average, an 18% increase in surface vessel diameter accompanied by a 135% increase in vascular flux and 92% increase in parenchyma perfusion. These large alterations to the cortical vasculature and CBF are unrepresentative of normal physiology and provide further evidence that neuroscience experiments would benefit from transitioning to un-anesthetized awake animal models. -
The Cardiovascular and Respiratory Effects of Isoflurane-Nitrous Oxide Anaesthesia
THE CARDIOVASCULAR AND RESPIRATORY EFFECTS OF ISOFLURANE-NITROUS OXIDE ANAESTHESIA WILLIAM M. DOLAN, M.D.S, WENDELL C. STEVENS, M.D.,O EDMOND I. EGER, II, M.D.,* TnOlX~AS H. CROMWELL, M.D,, c* MICHAEL J. HALSEY, PH.D.,C* THOMAS F. SHAKESPEAlqE, Ik~.D.,c* AND RONALD D. MILLER, M.D. c* INTRODUCTION ISOFLURAnE (Forane| 1 chloro-2-2-2 trifluoroethyl, difluoromethyl ether), is a halogenated ether currently being evaluated for use as an inhalational anaesthetic. Its favourable properties include non-flammability, 1 relatively low blood and fat solubilities (blood-gas and oil-gas partitions of 1.4 and 99, respectively), 1,2 mole- cular stability resulting in resistance to dehydrohalogenation and hepatic meta- bolism, 1,~ lack of sensitization of the heart to catecholamines, 4 and favourable depression of neuromuscular function and potentiation of muscle relaxants. ~ However, isoflurane can produce profound depression of ventilation and blood pressure. ~ Since the concurrent use of nitrous oxide with halothane attenuates the hypotension and ventilatory depression caused by halothane, s,'~,l~ we asked whether nitrous oxide would produce similar changes towards awake values dur- ing isoflurane anaesthesia. METHODS We studied the cardiovascular and respiratory effects of anaesthesia with iso- flurane and 70 per cent nitrous oxide in eight healthy, unpremedicated volun- teers. The volunteers were 25 --4- 1 (SD) years of age and were informed of the purposes, procedures, and hazards of the study. The protocol was approved by the Committee on Human Experimentation of the University of California, San Francisco. A normal medical history, physical examination, chest roentgenogram, complete blood count, serum glutamic oxaloacetic transanainase and lactic de- hydrogenase were required before a volunteer was accepted for anaesthesia. -
Synthetic Method for Fluoromethylation Of
Europäisches Patentamt *EP001286941B1* (19) European Patent Office Office européen des brevets (11) EP 1 286 941 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.7: C07C 43/12, C07C 41/16, of the grant of the patent: C07C 41/22, C07C 41/28, 20.07.2005 Bulletin 2005/29 C07C 41/52, C07C 43/313 (21) Application number: 01939633.2 (86) International application number: PCT/US2001/017348 (22) Date of filing: 30.05.2001 (87) International publication number: WO 2001/092193 (06.12.2001 Gazette 2001/49) (54) SYNTHETIC METHOD FOR FLUOROMETHYLATION OF HALOGENATED ALCOHOLS VERFAHREN ZUR FLUORMETHYLIERUNG VON HALOGENIERTEN ALKOHOLEN PROCEDE DE SYNTHESE DE FLUOROMETHYLATION D’ALCOOLS HALOGENES (84) Designated Contracting States: (72) Inventors: AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU • BIENIARZ, Christopher MC NL PT SE TR Highland Park, IL 60035 (US) Designated Extension States: • RAMAKRISHNA, Kornepati, V. RO SI Libertyville, IL 60048 (US) (30) Priority: 01.06.2000 US 587421 (74) Representative: Modiano, Guido, Dr.-Ing. et al Modiano, Josif, Pisanty & Staub, (43) Date of publication of application: Baaderstrasse 3 05.03.2003 Bulletin 2003/10 80469 München (DE) (73) Proprietor: Abbott Laboratories (56) References cited: Abbott Park, IL 60064-6050 (US) EP-A- 0 822 172 GB-A- 1 250 928 Note: Within nine months from the publication of the mention of the grant of the European patent, any person may give notice to the European Patent Office of opposition to the European patent granted. Notice of opposition shall be filed in a written reasoned statement. -
Physiologically-Based Pharmacokinetic Modelling of Infant
AAS Open Research AAS Open Research 2018, 1:16 Last updated: 21 MAY 2018 RESEARCH ARTICLE Physiologically-based pharmacokinetic modelling of infant exposure to efavirenz through breastfeeding [version 1; referees: 1 approved with reservations] Adeniyi Olagunju 1,2, Rajith K. R. Rajoli 2, Shakir A. Atoyebi1, Saye Khoo2, Andrew Owen2, Marco Siccardi2 1Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria 2Department of Molecular and Clinical Pharmacology, University of Liverpool, Liverpool, L69 3GF, UK v1 First published: 14 May 2018, 1:16 (doi: 10.12688/aasopenres.12860.1) Open Peer Review Latest published: 14 May 2018, 1:16 (doi: 10.12688/aasopenres.12860.1) Referee Status: Abstract Background: Very little is known about the level of infant exposure to many drugs commonly used during breastfeeding. The aim of this study was to Invited Referees develop a physiologically-based pharmacokinetic (PBPK) model for predicting 1 infant exposure to maternal efavirenz through breastmilk. Methods: A breastfeeding PBPK model combining whole-body maternal and version 1 infant sub-models was constructed from drug-specific and system parameters published report affecting drug disposition using mathematical descriptions. The model was 14 May 2018 validated against published data on the pharmacokinetics of efavirenz in nursing mother-infant pairs. Further simulations were conducted to assess 1 Jeffrey W. Fisher, US Food and Drug exposure in the context of the 400 mg reduced dose of efavirenz as well as Administration, USA best- and worse-case scenarios. Results: The model adequately described efavirenz pharmacokinetics, with over 80% of observed data points (203 matched breast milk and plasma pairs) Discuss this article within the predictive interval. -
Federal Register/Vol. 71, No. 34/Tuesday, February 21, 2006
Federal Register / Vol. 71, No. 34 / Tuesday, February 21, 2006 / Notices 8859 DEPARTMENT OF HEALTH AND DEPARTMENT OF HEALTH AND of the Public Health Service Act to HUMAN SERVICES HUMAN SERVICES conduct directly or by grants or contracts, research, experiments, and Office of the National Coordinator; Office of the National Coordinator; demonstrations relating to occupational American Health Information American Health Information safety and health and to mine health. Community Chronic Care Workgroup Community Consumer Empowerment The BSC shall provide guidance to the Meeting Workgroup Meeting Director, NIOSH on research and prevention programs. Specifically, the ACTION: Announcement of meeting. ACTION: Announcement of meeting. board shall provide guidance on the institute’s research activities related to SUMMARY: SUMMARY: This notice announces the This notice announces the developing and evaluating hypotheses, third meeting of the American Health third meeting of the American Health Information Community Consumer systematically documenting findings Information Community Chronic Care and disseminating results. The board Workgroup in accordance with the Empowerment Workgroup in accordance with the Federal Advisory shall evaluate the degree to which the Federal Advisory Committee Act (Pub. activities of NIOSH: (1) Conform to L. 92–463, 5 U.S.C., App.) Committee Act (Pub. L. 92–463, 5 U.S.C., App.) appropriate scientific standards, (2) DATES: March 22, 2006 from 1 p.m. to address current, relevant needs, and (3) DATES: March 20, 2006 from 1 p.m. to 5 p.m. produce intended results. 5 p.m. ADDRESSES: Hubert H. Humphrey Matters to be Discussed: Agenda items ADDRESSES: Hubert H. Humphrey Building (200 Independence Ave., SW., include a report from the Director, Building (200 Independence Ave., SW., Washington, DC 20201), Conference NIOSH; progress report by BSC working Washington, DC 20201), Conference Room 705A. -
Lectures Covering Concentrated Topics in Emergency Medicine (Tems)
Lectures covering concentrated Topics in Emergency Medicine (TEMs) Section Week Title Topics Toxicology 007 External Decontamination and External decontamination Patient Stabilization Initial approach Airway management Patient control Drug interactions Anatomical distortion Advanced life support Alterations to standard therapy Prolonged resuscitation Organ donation Focused assessment History Vital signs Physical examination 008 Minimizing Absorption, Minimizing absorption Enhancing Elimination, and Syrup of ipecac Ancillary Testing Gastric lavage Activated charcoal Cathartics Whole-bowel irrigation Enhancing elimination Chelation Multidose charcoal Hemodialysis and peritoneal dialysis Hemoperfusion Exchange transfusion Ancillary testing Toxicology screens Serum Urine Serum quantitation 009 Insecticides [17.01.20(b)] DEET Diquat and Paraquat Metaldehyde Methylbromide and other fumigants Nicotine Organophosphates [17.01.33] and carbamates Pyrethrins, pyrethroids, and organohalides 010 Rodenticides [17.01.20(c)] Anticoagulant [17.01.05] 4-hydroxycoumarins Indanediones Nonanticoagulant [excluding heavy metals] α-naphthylthiourea Boric acid Bromethalin Cholecalciferol Elemental phosphorus Fluroacetamide PNU Strychnine [17.01.37] 011 Hydrocarbons [17.01.23] Aliphatic Aromatic General Toluene Xylene Halogenated General Carbon tetrachloride Methylene chloride Trichloroethylene Pine Oil and Turpentine Polychlorinated biphenyls and related substances 012 Caustic & Corrosive Agents Ingestions Acid [17.01.14(a)] Alkali [17.01.14(b)] Other Disc batteries -
BYSTOLIC Safely and Effectively
HIGHLIGHTS OF PRESCRIBING INFORMATION • Patients with severe hepatic impairment (Child-Pugh >B) These highlights do not include all the information needed to (4) use BYSTOLIC safely and effectively. See full prescribing • Hypersensitive to any component of this product (4) information for BYSTOLIC. -------------WARNINGS AND PRECAUTIONS---------- BYSTOLIC® (nebivolol) tablets, for oral use • Acute exacerbation of coronary artery disease upon cessation of therapy: Do not abruptly discontinue. (5.1) Initial U.S. Approval: 2007 • Diabetes: Monitor glucose as β-blockers may mask symptoms of hypoglycemia. (5.5) ------------RECENT MAJOR CHANGES------------------ Indications and Usage (1.1) 12/2011 -----------------ADVERSE REACTIONS----------------- Most common adverse reactions (6.1): --------------INDICATIONS AND USAGE--------------- • Headache, fatigue BYSTOLIC is a beta-adrenergic blocking agent indicated for To report SUSPECTED ADVERSE REACTIONS, Contact the treatment of hypertension, to lower blood pressure. Forest Laboratories, Inc. at 1-800-678-1605 or FDA at Lowering blood pressure reduces the risk of fatal and nonfatal 1-800-FDA-1088 or www.fda.gov/medwatch. cardiovascular events, primarily strokes and myocardial infarctions. (1.1) ----------------DRUG INTERACTIONS------------------ • CYP2D6 enzyme inhibitors may increase nebivolol levels. ------------DOSAGE AND ADMINISTRATION---------- (7.1) Can be taken with and without food. Individualize to the • Reserpine or clonidine may produce excessive reduction needs of the patient and monitor during up-titration. (2) of sympathetic activity. (7.2) • Hypertension: Most patients start at 5 mg once daily. • Both digitalis glycosides and β-blockers slow Dose can be increased at 2-week intervals up to 40 mg. atrioventricular conduction and decrease heart rate. (2.1) Concomitant use can increase the risk of bradycardia.