List of Psychotropic Substances Under International Control
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Metabolic-Hydroxy and Carboxy Functionalization of Alkyl Moieties in Drug Molecules: Prediction of Structure Influence and Pharmacologic Activity
molecules Review Metabolic-Hydroxy and Carboxy Functionalization of Alkyl Moieties in Drug Molecules: Prediction of Structure Influence and Pharmacologic Activity Babiker M. El-Haj 1,* and Samrein B.M. Ahmed 2 1 Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, University of Science and Technology of Fujairah, Fufairah 00971, UAE 2 College of Medicine, Sharjah Institute for Medical Research, University of Sharjah, Sharjah 00971, UAE; [email protected] * Correspondence: [email protected] Received: 6 February 2020; Accepted: 7 April 2020; Published: 22 April 2020 Abstract: Alkyl moieties—open chain or cyclic, linear, or branched—are common in drug molecules. The hydrophobicity of alkyl moieties in drug molecules is modified by metabolic hydroxy functionalization via free-radical intermediates to give primary, secondary, or tertiary alcohols depending on the class of the substrate carbon. The hydroxymethyl groups resulting from the functionalization of methyl groups are mostly oxidized further to carboxyl groups to give carboxy metabolites. As observed from the surveyed cases in this review, hydroxy functionalization leads to loss, attenuation, or retention of pharmacologic activity with respect to the parent drug. On the other hand, carboxy functionalization leads to a loss of activity with the exception of only a few cases in which activity is retained. The exceptions are those groups in which the carboxy functionalization occurs at a position distant from a well-defined primary pharmacophore. Some hydroxy metabolites, which are equiactive with their parent drugs, have been developed into ester prodrugs while carboxy metabolites, which are equiactive to their parent drugs, have been developed into drugs as per se. -
Participant Handbook
LOWNDES COUNTY DUI COURT PARTICIPANT HANDBOOK STATE COURT OF LOWNDES COUNTY 327 NORTH ASHLEY STREET VALDOSTA, GA 31601 PHONE: 229-671-2895 FAX: 229-671-3441 Lowndes County DUI Court Team: Ellen S. Golden Judge, State Court Cynthia Welch Assistant Solicitor-General Gee Edwards Defense Attorney Stacey Bass Court Coordinator Kayla Porter Probation Officer Laci Rankhorn Treatment Provider Jason Reeves Surveillance Officer Revised 3/1/19 1 | P a g e TABLE OF CONTENTS TABLE OF CONTENTS...........................................................................................................................2 INTRODUCTION TO THE LOWNDES COUNTY STATE COURT DUI COURT.......................... 4 TREATMENT OVERVIEW.................................................................................................................... 6 I. PHASES OF THE DUI COURT PROGRAM........................................................................................7 Phase 1 – (approximately 17 weeks)....................................................................................................7 Phase 2 – (approximately 17 weeks)................................................................................................... 8 Phase 3 – (approximately 17 weeks)................................................................................................... 9 Phase 4 Aftercare- (approximately 3 months)....................................................................................9 Phase Progression......................................................................................................................... -
The Stimulants and Hallucinogens Under Consideration: a Brief Overview of Their Chemistry and Pharmacology
Drug and Alcohol Dependence, 17 (1986) 107-118 107 Elsevier Scientific Publishers Ireland Ltd. THE STIMULANTS AND HALLUCINOGENS UNDER CONSIDERATION: A BRIEF OVERVIEW OF THEIR CHEMISTRY AND PHARMACOLOGY LOUIS S. HARRIS Dcparlmcnl of Pharmacology, Medical College of Virginia, Virginia Commonwealth Unwersity, Richmond, VA 23298 (U.S.A.) SUMMARY The substances under review are a heterogenous set of compounds from a pharmacological point of view, though many have a common phenylethyl- amine structure. Variations in structure lead to marked changes in potency and characteristic action. The introductory material presented here is meant to provide a set of chemical and pharmacological highlights of the 28 substances under con- sideration. The most commonly used names or INN names, Chemical Abstract (CA) names and numbers, and elemental formulae are provided in the accompanying figures. This provides both some basic information on the substances and a starting point for the more detailed information that follows in the individual papers by contributors to the symposium. Key words: Stimulants, their chemistry and pharmacology - Hallucinogens, their chemistry and pharmacology INTRODUCTION Cathine (Fig. 1) is one of the active principles of khat (Catha edulis). The structure has two asymmetric centers and exists as two geometric isomers, each of which has been resolved into its optical isomers. In the plant it exists as d-nor-pseudoephedrine. It is a typical sympathomimetic amine with a strong component of amphetamine-like activity. The racemic mixture is known generically in this country and others as phenylpropanolamine (dl- norephedrine). It is widely available as an over-the-counter (OTC) anti- appetite agent and nasal decongestant. -
KHAT Latest Revision: June 11, 2005
KHAT Latest Revision: June 11, 2005 O CH3 NH2 Cathinone OH CH3 NH2 Cathine N CH3 H3C N 3,6-dimethyl-2,5-diphenylpyrazine (dimer of Cathinone) 1. SYNONYMS CFR: Cathinone Cathine CAS #: Cathinone Hydrochloride: 71031-15-7 Cathine Hydrochloride: 2153-98-2 Cathine Base: 492-39-7 Other Names: Catha edulis Kat Mutsawhari Mutsawari Mdimamadzi Musitate Mirungi Miraa Ol meraa Tumayot Liruti Ikwa Arabian Tea 2. CHEMICAL AND PHYSICAL DATA Khat is used as a stimulant or as a medicine in parts of Africa and the Arabian Peninsula. The plant is thought to have been in cultivation before the coffee plant; historical references date the use of the plant to the fourteenth century. Peter Forsskal, a physician and botanist, collected khat specimens in an expedition organized by the King of Denmark in the eighteenth century. Forsskal assigned the name Catha edulis to the plant. The effects produced by the drug include excitation, hypersensitivity, anorexia, insomnia, euphoria, increased respiration, and hyperthermia. These effects closely parallel the effects of d-amphetamine. Khat is a bush or tree that grows naturally in the humid mountainous regions (elevations of 5000 to 6500 feet) of East and South Africa. The trees can grow naturally to over 60 ft; however, cultivated khat trees are pruned and their height to kept to approximately 16 feet. Khat also grows to a height of 3 feet as a small bush in arid regions. Like opium, the alkaloid content of khat will vary with the soil, climatic conditions, and cultivation. Khat belongs to the genus Catha edulis. It is recognized that the genus consists of only one species; however, the plant exhibits extreme polymorphism. -
The In¯Uence of Medication on Erectile Function
International Journal of Impotence Research (1997) 9, 17±26 ß 1997 Stockton Press All rights reserved 0955-9930/97 $12.00 The in¯uence of medication on erectile function W Meinhardt1, RF Kropman2, P Vermeij3, AAB Lycklama aÁ Nijeholt4 and J Zwartendijk4 1Department of Urology, Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands; 2Department of Urology, Leyenburg Hospital, Leyweg 275, 2545 CH The Hague, The Netherlands; 3Pharmacy; and 4Department of Urology, Leiden University Hospital, P.O. Box 9600, 2300 RC Leiden, The Netherlands Keywords: impotence; side-effect; antipsychotic; antihypertensive; physiology; erectile function Introduction stopped their antihypertensive treatment over a ®ve year period, because of side-effects on sexual function.5 In the drug registration procedures sexual Several physiological mechanisms are involved in function is not a major issue. This means that erectile function. A negative in¯uence of prescrip- knowledge of the problem is mainly dependent on tion-drugs on these mechanisms will not always case reports and the lists from side effect registries.6±8 come to the attention of the clinician, whereas a Another way of looking at the problem is drug causing priapism will rarely escape the atten- combining available data on mechanisms of action tion. of drugs with the knowledge of the physiological When erectile function is in¯uenced in a negative mechanisms involved in erectile function. The way compensation may occur. For example, age- advantage of this approach is that remedies may related penile sensory disorders may be compen- evolve from it. sated for by extra stimulation.1 Diminished in¯ux of In this paper we will discuss the subject in the blood will lead to a slower onset of the erection, but following order: may be accepted. -
The 2014 Prohibited List International Standard
The World Anti-Doping Code THE 2014 PROHIBITED LIST INTERNATIONAL STANDARD Version 2.0 (revised 2014 version) The official text of the Prohibited List shall be maintained by WADA and shall be published in English and French. In the event of any conflict between the English and French versions, the English version shall prevail. This List shall come into effect on 1 September 2014 The revised 2014 Prohibited List 17 May 2014 THE 2014 PROHIBITED LIST WORLD ANTI-DOPING CODE Valid 1 September 2014 In accordance with Article 4.2.2 of the World Anti-Doping Code, all Prohibited Substances shall be considered as “Specified Substances” except Substances in classes S1, S2, S4.4, S4.5, S6.a, and Prohibited Methods M1, M2 and M3. SUBSTANCES AND METHODS PROHIBITED AT ALL TIMES (IN- AND OUT-OF-COMPETITION) PROHIBITED SUBSTANCES S0. NON-APPROVED SUBSTANCES Any pharmacological substance which is not addressed by any of the subsequent sections of the List and with no current approval by any governmental regulatory health authority for human therapeutic use (e.g drugs under pre-clinical or clinical development or discontinued, designer drugs, substances approved only for veterinary use) is prohibited at all times. S1. ANABOLIC AGENTS Anabolic agents are prohibited. 1. Anabolic Androgenic Steroids (AAS) a. Exogenous* AAS, including: 1-androstenediol (5α-androst-1-ene-3β,17β-diol ); 1-androstenedione (5α- androst-1-ene-3,17-dione); bolandiol (estr-4-ene-3β,17β-diol ); bolasterone; boldenone; boldione (androsta-1,4-diene-3,17-dione); calusterone; clostebol; -
NTP-CERHR Expert Panel Report on the Reproductive and Developmental Toxicity of Amphetamine and Methamphetamine
Published 2005 Wiley-Liss, Inc.w Birth Defects Research (Part B) 74:471–584 (2005) NTP-CERHR Expert Panel Report on the Reproductive and Developmental Toxicity Of Amphetamine and Methamphetamine Mari Golub,1 Lucio Costa,2 Kevin Crofton,3 Deborah Frank,4 Peter Fried,5 Beth Gladen6 Rogene Henderson,7 Erica Liebelt,8 Shari Lusskin,9 Sue Marty,10 Andrew Rowland11 John Scialli12 and Mary Vore13 1California Environment Protection Agency, Sacramento, California 2University of Washington, Seattle, Washington 3U.S. Environmental Protection Agency, Research Triangle Park, North Carolina 4Boston Medical Center, Boston, Massachusetts 5Carleton University, Ottawa, Ontario 6National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 7Lovelace Respiratory Research Institute, Albuquerque, New Mexico 8University of Alabama at Birmingham School of Medicine, Birmingham, Alabama 9New York University School of Medicine, New York, New York 10The Dow Chemical Company, Midland, Michigan 11University of New Mexico, Albuquerque, New Mexico 12Phoenix, Arizona 13University of Kentucky, Lexington, Kentucky PREFACE studies indexed before December 31, 2004. References were also identified from databases such as REPRO- The National Toxicology Program (NTP) and the TOXs, HSDB, IRIS, and DART and from report National Institute of Environmental Health Sciences bibliographies. (NIEHS) established the NTP Center for the Evaluation This evaluation resulted from the efforts of a 13- of Risks to Human Reproduction (CERHR) in June 1998. member panel of government and non-government The purpose of the Center is to provide timely, unbiased, scientists that culminated in a public expert panel scientifically sound evaluations of human and experi- meeting held January 10–12, 2005. This report is a mental evidence for adverse effects on reproduction and product of the Expert Panel and is intended to (1) development caused by agents to which humans may be interpret the strength of scientific evidence that exposed. -
(19) United States (12) Patent Application Publication (10) Pub
US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist. -
Abecarnil/Allobarbital 959 Pharmacopoeias
Abecarnil/Allobarbital 959 Pharmacopoeias. In Eur. (see p.vii). acamprosate’s action including inhibition of neuronal hyper- maleate in the treatment of anxiety disorders, hiccups, and nau- Ph. Eur. 6.2 (Acamprosate Calcium). A white or almost white excitability by antagonising excitatory amino acids such as sea and vomiting. Acepromazine, as the base, has also been giv- powder. Freely soluble in water; practically insoluble in alcohol glutamate. en in preparations for the management of insomnia. and in dichloromethane. A 5% solution in water has a pH of 5.5 1. Wilde MI, Wagstaff AJ. Acamprosate: a review of its pharmacol- Preparations to 7.0. ogy and clinical potential in the management of alcohol depend- ence after detoxification. Drugs 1997; 53: 1038–53. Proprietary Preparations (details are given in Part 3) Adverse Effects 2. Anonymous. Acamprosate for alcohol dependence? Drug Ther Denm.: Plegicil; Turk.: Plegicil. The main adverse effect of acamprosate is dosage-related diar- Bull 1997; 35: 70–2. Multi-ingredient: Fr.: Noctran. rhoea; nausea, vomiting, and abdominal pain occur less frequent- 3. Mason BJ. Treatment of alcohol-dependent outpatients with acamprosate: a clinical review. J Clin Psychiatry 2001; 62 (suppl ly. Other adverse effects have included pruritus, and occasionally 20): 42–8. a maculopapular rash; bullous skin reactions have occurred rare- 4. Overman GP, et al. Acamprosate for the adjunctive treatment of Aceprometazine (rINN) ly. Depression and fluctuations in libido have also been reported. alcohol dependence. Ann Pharmacother 2003; 37: 1090–9. Hypersensitivity reactions including urticaria, angioedema, and 5. Anton RF, et al. Combined pharmacotherapies and behavioral 16-64 CB; Aceprometazina; Acéprométazine; Aceprometazi- anaphylaxis have been reported very rarely. -
Smumedical Journal
SMU Medical Journal ISSN : 2349 – 1604 (Volume – 4, No. 1, January 2017) Review Article Indexed in SIS (USA), ASI (Germany), I2OR & i-Scholar (India), SJIF (Morocco) and Cosmos Foundation (Germany) databases. Impact Factor: 3.835 (SJIF) Analytical Aspects with Brief Overview of Depressants Sandeep Kumar1 Nand Gopal Giri2 Ashok Kumar Jaiswal3* Anil Kumar Jaiswal4 1M.Sc. (Forensic Science), LNJN NICFS, New Delhi 110085, 2Assistant Professor, Department of Chemistry, Shivaji College (University of Delhi) Raja Garden, New Delhi 110 027, 3Dept. of Forensic Medicine and toxicology, All India institute of Medical Sciences, New Delhi 110 029.4Assistant Professor, Department of Mathematics, St. Andrew’s PG College, Gorakhpur, UP. *Corresponding author Manuscript received : 30.10.2016 Manuscript accepted: 21.11.2016 Abstract Depressants are drugs that slow down the functions of the central nervous system (CNS). These drugs are used to reduce anxiety and insomnia without drowsiness. The depressants cause relaxed feeling if used in small quantity but cause unconsciousness, vomiting and even death if taken in high quantity. It affects concentration and coordination of a person by slowing down his/ her ability to respond in unexpected situations. These drugs are also attributed for their physiological and psychological effects, eventually in large dose it become lethal. The different 142 SMU Medical Journal, Volume – 4, No. – 1, January, 2017 physical and chemical features of some very often used depressants are discussed in this manuscript. Keyword: Depressant, TLC, UV spectroscopy, HPLC, GLC etc. Introduction The classical depressants are hypnotics (which induce sleep), most antianxiety medicine (diazepam or valium), muscle spasm prevent seizure, but these drugs rapidly develop dependence and tolerance which finally leads to coma and death, so use of these drugs is highly unsafe. -
WO 2012/148799 Al 1 November 2012 (01.11.2012) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2012/148799 Al 1 November 2012 (01.11.2012) P O P C T (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 9/107 (2006.01) A61K 9/00 (2006.01) kind of national protection available): AE, AG, AL, AM, A 61 47/10 (2006.0V) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, (21) International Application Number: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, PCT/US2012/034361 HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, (22) International Filing Date: KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, 20 April 2012 (20.04.2012) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, (25) Filing Language: English SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 61/480,259 28 April 201 1 (28.04.201 1) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, (71) Applicant (for all designated States except US): BOARD UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, OF REGENTS, THE UNIVERSITY OF TEXAS SYS¬ TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, TEM [US/US]; 201 West 7th St., Austin, TX 78701 (US). -
Since the Introduction of Extracorporeal Hemodialysis For
ROBERT P. DAVIS* WILLIAM B. BLYTHE ** Department of Medicine, University of North Carolina School of Medicire, MARGARET NEWTONt Chapel Hill, North Carolina LOUIS G. WELTt THE TREATMENT OF INTOXICATION WITH ETHYNYL-CYCLOHEXYL CARBAMATE (VALMIDR) BY EXTRACORPOREAL HEMODIALYSIS: A CASE REPORT Since the introduction of extracorporeal hemodialysis for the management of renal failure, its usefulness in the treatment of otherwise fatal poisoning by various chemical agents has been repeatedly demonstrated. Among these agents have been various barbiturates,' salicylates,' and bromide.' Recent experience with a case of intoxication with ethynyl-cyclohexyl carbamate (Fig. 1), a short-acting nonbarbiturate hypnotic,' provided an opportunity to demonstrate its dialyzability. Although the poisoning proved fatal in this instance, the ability to remove an appreciable quantity of the drug by hemodialysis suggests that patients with severe intoxication coming under observation earlier may be treated by this method more successfully. CASE HISTORY M.F.K., NCMH Unit No. 05-26-69 A 24-year-old single white female graduate student was brought to the Emergency Ward of the North Carolina Memorial Hospital at 9:30 p.m. on 9/25/58. She had been found comatose in her apartment shortly before with the beginning of a "suicide note" and an empty prescription bottle discovered near her body. The prescription had been refilled one week previously after a long interval for at least thirty 0.5 gram tablets of ethynyl-cyclohexyl-carbamate (ValmidR, Lilly). The patient was last heard from specifically 26 hours prior to the discovery prompted by her having missed several specific appointments throughout the day. Past medical history, obtained from friends and previous medical record, was noncontributory.