Amphetamines: Structure- Activity Relationships
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A Quick Guide to Drugs and Alcohol
A QUICK GUIDE TO Drugs & Alcohol THIRD EDITION by the National Drug and Alcohol Research Centre (NDARC) Drug Info is a partnership between the State Library of New South Wales and NSW Health. www.druginfo.sl.nsw.gov.au Disclaimer The contents of this book are intended for information purposes only. Every efort has been made to ensure that the information is correct at the time of publication. Drug Info does not ofer any information in this book as a tool for treatment, counselling or legal advice. Drug Info recommends that prior to making any decision based on any information in this book, you should obtain independent professional legal or medical advice. Websites and information about service providers referred to in the publication have been selected to provide relevant and up-to-date information as at the date of publication. Drug Info accepts no responsibility for the content of websites and does not endorse any specifc services ofered by providers. A Quick Guide to Drugs & Alcohol, third edition, September 2017 Published by Drug Info, State Library of NSW © Copyright Library Council of NSW and NSW Ministry of Health, 2017 ISBN 0 7313 7239 5 (print) ISBN 0 7313 7240 9 (online) Printed in Australia by SEED Print, using Spicers Paper Monza Recycled Satin 350 gsm and Impress Matt 115 gsm. Monza Recycled contains 99% recycled fbre and is FSC® Mix Certifed, Impress Matt is FSC® Mix Certifed. P&D-4660-9/2017 ECSTASY E, pills, eccy, XTC, MDMA, pingas, Adam, X 7 Ecstasy is a derivative of methamphetamine (the active ingredient is 3, 4-methylenedioxymethamphetamine, abbreviated to MDMA). -
Pharmacology and Toxicology of Amphetamine and Related Designer Drugs
Pharmacology and Toxicology of Amphetamine and Related Designer Drugs U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES • Public Health Service • Alcohol Drug Abuse and Mental Health Administration Pharmacology and Toxicology of Amphetamine and Related Designer Drugs Editors: Khursheed Asghar, Ph.D. Division of Preclinical Research National Institute on Drug Abuse Errol De Souza, Ph.D. Addiction Research Center National Institute on Drug Abuse NIDA Research Monograph 94 1989 U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service Alcohol, Drug Abuse, and Mental Health Administration National Institute on Drug Abuse 5600 Fishers Lane Rockville, MD 20857 For sale by the Superintendent of Documents, U.S. Government Printing Office Washington, DC 20402 Pharmacology and Toxicology of Amphetamine and Related Designer Drugs ACKNOWLEDGMENT This monograph is based upon papers and discussion from a technical review on pharmacology and toxicology of amphetamine and related designer drugs that took place on August 2 through 4, 1988, in Bethesda, MD. The review meeting was sponsored by the Biomedical Branch, Division of Preclinical Research, and the Addiction Research Center, National Institute on Drug Abuse. COPYRIGHT STATUS The National Institute on Drug Abuse has obtained permission from the copyright holders to reproduce certain previously published material as noted in the text. Further reproduction of this copyrighted material is permitted only as part of a reprinting of the entire publication or chapter. For any other use, the copyright holder’s permission is required. All other matieral in this volume except quoted passages from copyrighted sources is in the public domain and may be used or reproduced without permission from the Institute or the authors. -
Effects of Chronic Administration of Sibutramine on Body Weight, Food
Exp. Anim. 49(4), 239–249, 2000 Effects of Chronic Administration of Sibutramine on Body Weight, Food Intake and Motor Activity in Neonatally Monosodium Glutamate-Treated Obese Female Rats: Relationship of Antiobesity Effect with Monoamines Terutake NAKAGAWA1), Kiyoharu UKAI1), Tadashi OHYAMA1), Yutaka GOMITA2), and Hitoshi OKAMURA3) 1)Central Research Institute, Kaken Pharmaceutical Co. Ltd., 14 Shinomiya, Minamikawara-cho, Yamashina-ku, Kyoto 607-8042, 2)Department of Hospital Pharmacy, Okayama University Medical School, Shikada-cho 2–5–1, Okayama 700-8558, and 3)Department of Anatomy, Kobe University School of Medicine, 7–5–1 Chuohoku Kusunoki-cho, Kobe 650-0017, Japan Abstract: When the hypothalamic ventromedial nucleus and arcuate nucleus were destroyed in rats by treatment with monosodium glutamate in the neonatal stage, increase in the Lee index (body weight 1/3/body length) and in retroperitoneal fat as well as decreases in spontaneous motor activity, food consumption and growth hormone secretion function associated with hypothalamic low body length obesity (monosodium glutamate- treated obesity; MSG-OB) were observed as these rats grew. Treatment with sibutramine at 3 and 10 mg/kg p.o. once a day continuously for 14 days improved these parameters, and the degree of improvement was dose related. The plasma lipid values in MSG-OB rats, which were the same as those in normal rats, were decreased by consecutive administration of sibutramine. Levels of hypothalamic monoamines (MAs) such as norepinephrine, 5-HT (serotonin) and dopamine and their metabolites DOPAC, HVA and 5- HIAA were decreased in MSG-OB rats, and further decrease in them, though slight, was observed with consecutive daily administration of sibutramine, probably as a result of the feedback attributable to an increase in MA in synapses caused by inhibition of MA uptake by sibutramine. -
Insights Into the Mechanisms of Action Ofthe MAO Inhibitors Phenelzine and Tranylcypromine
Insights into the Mechanisms of Action of the MAO Inhibitors Phenelzine and Tranylcypromine: A Review Glen B. Baker, Ph.D., Ronald T. Coutts, Ph.D., D.Sc., Kevin F. McKenna, M.D., and Rhonda L. Sherry-McKenna, B.Sc. Neurochemical Research Unit, Department of Psychiatry and Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta Submitted: July 10, 1992 Accepted: October 7, 1992 Although the non-selective monoamine oxidase inhibitors phenelzine and tranylcypromine have been used for many years, much still remains to be understood about their mechanisms of action. Other factors, in addition to the inhibition of monoamine oxidase and the subsequent elevation of brain levels of the catecholamines and 5-hydroxytryptamine, may contribute to the overall pharma- cological profiles ofthese drugs. This review also considers the effects on brain levels of amino acids and trace amines, uptake and release of neurotransmitter amines at nerve terminals, receptors for amino acids and amines, and enzymes other than monoamine oxidase, including enzymes involved in metabolism of other drugs. The possible contributions of metabolism and stereochemistry to the actions of these monoamine oxidase inhibitors are discussed. Key Words: amino acids, monoamine oxidase, neurotransmitter amines, phenelzine, tranylcypromine, uptake Despite the fact that the non-selective monoamine oxidase nerve endings (Baker et al 1977; Raiteri et al 1977) and/or (MAO) inhibitors phenelzine (PLZ) and tranylcypromine may act as neuromodulators through direct actions on recep- (TCP) (see Fig. 1) have been used clinically for many years, tors for the catecholamines and/or 5-HT (Jones 1983; much remains to be learned about theirmechanisms ofaction. -
Effects of in Vitro Amitriptyline, Fluoxetine, Tranylcypromine and Venlafaxine on Saphenous Vein Grafts
ORIGINAL ARTICLE Braz J Cardiovasc Surg 2019;34(3):290-6 Effects of in vitro Amitriptyline, Fluoxetine, Tranylcypromine and Venlafaxine on Saphenous Vein Grafts Melek Akinci1, MD; Cetin Hakan Karadag2, MD; Serhat Huseyin3, MD; Cagatay Oltulu4, MD; Suat Canbaz3, MD; Ozgur Gunduz2, MD; Ruhan Deniz Topuz2, MD DOI: 10.21470/1678-9741-2018-0338 Abstract Objective: In this study, we aimed to examine the effects of (Log M) was 74.6%, the response at -6.32 (Log M) was 75.5%. amitriptyline, fluoxetine, tranylcypromine and venlafaxine on While the relaxation response at -6.46 (Log M) of fluoxetine was saphenous vein grafts in coronary artery bypass graft surgeries. 68.02%, the response at -6.02 (Log M) was 72.12%. While the Methods: 59 patients (40 males and 19 females; mean age relaxation response of tranylcypromine at -7.53 (Log M) was 65.1 years, distribution: 45-84 years) who had coronary artery 61.13%, the response at -7.23 (Log M) was 65.53%. While the bypass graft surgery between February 2014 and May 2016 were relaxation response of venlafaxine at -6.21 (Log M) was 29.98%, included in the study. After the saphenous vein grafts with intact the response at -5.90 (Log M) was 32.96%. and denuded endothelium were precontracted with 3×10-6M Conclusion: The maximum relaxation at minimum and phenylephrine, amitriptyline, fluoxetine and tranylcypromine maximum therapeutic concentrations was obtained with were cumulatively added to isolated organ baths in the range of amitriptyline, fluoxetine and tranylcypromine, and the minimum 10-11-3x10-5M, while venlafaxine was added in the range of 10-9- relaxation was obtained with venlafaxine. -
A Review of Serotonin Toxicity Data: Implications for the Mechanisms of Antidepressant Drug Action P
ARTICLE IN PRESS REVIEW A Review of Serotonin Toxicity Data: Implications for the Mechanisms of Antidepressant Drug Action P. Ken Gillman Data now exist from which an accurate definition for serotonin toxicity (ST), or serotonin syndrome, has been developed; this has also lead to precise, validated decision rules for diagnosis. The spectrum concept formulates ST as a continuum of serotonergic effects, mediated by the degree of elevation of intrasynaptic serotonin. This progresses from side effects through to toxicity; the concept emphasizes that it is a form of poisoning, not an idiosyncratic reaction. Observations of the degree of ST precipitated by overdoses of different classes of drugs can elucidate mechanisms and potency of drug actions. There is now sufficient pharmacological data on some drugs to enable a prediction of which ones will be at risk of precipitating ST, either by themselves or in combinations with other drugs. This indicates that some antidepressant drugs, presently thought to have serotonergic effects in animals, do not exhibit such effects in humans. Mirtazapine is unable to precipitate serotonin toxicity in overdose or to cause serotonin toxicity when mixed with monoamine oxidase inhibitors, and moclobemide is unable to precipitate serotonin toxicity in overdose. Tricyclic antidepressants (other than clomipramine and imipramine) do not precipitate serotonin toxicity and might not elevate serotonin or have a dual action, as has been assumed. Key Words: Serotonin toxicity, monoamine oxidase inhibitors, se- do not, and cannot, cause ST (Gillman 2003c; Isbister and Whyte lective serotonin reuptake inhibitors, tricyclic antidepressants, mir- 2003). Such erroneous reports are still being published in tazapine, moclobemide prominent journals (Haddow et al 2004) and continue to main- tain the confused and inaccurate understanding of this toxidrome (Gillman 2005b; Isbister and Buckley 2005). -
PQA Measure Specifications ______
PQA Measure Specifications ______________________________________________________________________________ Table DDI-A: Target Medications and Precipitant Medications Table DDI-A Category Target Drug or Drug Class (Step 1) Precipitant Drug or Drug Class (Step 2) A Benzodiazepines: alprazolam, midazolam, triazolam Azole antifungal agents: ketoconazole, itraconazole, fluconazole, posaconazole, voriconazole B carbamazepine Clarithromycin, erythromycin, telithromycin C cyclosporine Rifamycins: rifampin, rifabutin, rifapentine D digoxin clarithromycin, erythromycin, azithromycin, telithromycin E Ergot alkaloids: ergotamine, dihydroergotamine clarithromycin, erythromycin, telithromycin F Estrogen/progestin oral contraceptives: Rifamycins: rifampin, rifabutin, rifapentine desogestrel-ethinyl estradiol, drospirenone-ethinyl estradiol, estradiol valerate-dienogest, ethinyl estradiol-ethynodiol, ethinyl estradiol-levonorgestrel, ethinyl estradiol-norethindrone, ethinyl estradiol- norgestimate, ethinyl estradiol-norgestrel, mestranol- norethindrone G MAO Inhibitors: isocarboxazid, linezolid, phenelzine, Sympathomimetics: amphetamines, atomoxetine, rasagiline, selegiline, tranylcypromine, sibutramine benzphetamine, dextroamphetamine, diethylpropion, isometheptene, methamphetamine, methylphenidate, phendimetrazine, phentermine, phenylephrine, pseudoephedrine, tapentadol, dexmethylphenidate, lisdexamfetamine Serotonergic Agents: buspirone, citalopram, cyclobenzaprine, desvenlafaxine, dextromethorphan, duloxetine, escitalopram, fluoxetine, fluvoxamine, -
Protocol Gebruik Van Klassieke MAO-Remmers
Protocol Gebruik van klassieke MAO-remmers1 De basis van dit protocol is gelegd door Dr. Marc.J. Blom, psychiater, verbonden aan het PsyQ te Den Haag, waarna deze verder is uitgebouwd met hulp van de expertise van onderstaande (behandel) deskundigen, onder leiding van Prof. Dr. W.A. Nolen. Dr. T.K. Birkenhäger, psychiater, verbonden aan het Erasmus MC te R’dam, Dr. W. van den Broek, psychiater, verbonden aan het Erasmus MC te R’dam, Dr. G.W.K. Hugenholtz, zhs-apotheker, verbonden aan het Diakonessenhuis Utrecht-Zeist-Doorn, Dr. R.M. Kok, psychiater, verbonden aan Altrecht geestelijke gezondheidszorg te Zeist, Prof. Dr. W.A. Nolen, psychiater, Universitair Medisch Centrum Groningen (UMCG), Mw. Drs. P. Kölling, psychiater, verbonden aan het Medisch Spectrum Twente te Enschede, Dr. J.P. van der Post, psychiater, Klin. Farmacoloog, verbonden aan GGZ Rivierduinen te Leiden. Dr. P.F.J. Schulte, psychiater, voorzitter geneesmiddelencommissie GGZ-NHN. Daleco Pharma b.v. heeft bij het tot stand komen van dit protocol een faciliterende rol vervuld en heeft er vervolgens zorg voor gedragen dat dit protocol onder de aandacht van belanghebbenden is gebracht, o.a. via haar website www.dalecopharma.nl 1 Waar in dit protocol gesproken wordt over een MAO-remmer, wordt in alle gevallen een klassieke, d.w..z. niet-selectieve, irreversibele MAO-remmer (tranylcypromine of fenelzine) bedoeld. Versie mei 2009 Inleiding ....................................................................................................................................... 3 Indicatie -
212102Orig1s000
CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 212102Orig1s000 OTHER REVIEW(S) Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research | Office of Surveillance and Epidemiology (OSE) Epidemiology: ARIA Sufficiency Date: June 29, 2020 Reviewer: Silvia Perez-Vilar, PharmD, PhD Division of Epidemiology I Team Leader: Kira Leishear, PhD, MS Division of Epidemiology I Division Director: CAPT Sukhminder K. Sandhu, PhD, MPH, MS Division of Epidemiology I Subject: ARIA Sufficiency Memo for Fenfluramine-associated Valvular Heart Disease and Pulmonary Arterial Hypertension Drug Name(s): FINTEPLA (Fenfluramine hydrochloride, ZX008) Application Type/Number: NDA 212102 Submission Number: 212102/01 Applicant/sponsor: Zogenix, Inc. OSE RCM #: 2020-953 The original ARIA memo was dated June 23, 2020. This version, dated June 29, 2020, was amended to include “Assess a known serious risk” as FDAAA purpose (per Section 505(o)(3)(B)) to make it consistent with the approved labeling. The PMR development template refers to the original memo, dated June 23, 2020. Page 1 of 13 Reference ID: 46331494640015 EXECUTIVE SUMMARY (place “X” in appropriate boxes) Memo type -Initial -Interim -Final X X Source of safety concern -Peri-approval X X -Post-approval Is ARIA sufficient to help characterize the safety concern? Safety outcome Valvular Pulmonary heart arterial disease hypertension (VHD) (PAH) -Yes -No X X If “No”, please identify the area(s) of concern. -Surveillance or Study Population X X -Exposure -Outcome(s) of Interest X X -Covariate(s) of Interest X X -Surveillance Design/Analytic Tools Page 2 of 13 Reference ID: 46331494640015 1. -
(12) Patent Application Publication (10) Pub. No.: US 2015/0202317 A1 Rau Et Al
US 20150202317A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0202317 A1 Rau et al. (43) Pub. Date: Jul. 23, 2015 (54) DIPEPTDE-BASED PRODRUG LINKERS Publication Classification FOR ALPHATIC AMNE-CONTAINING DRUGS (51) Int. Cl. A647/48 (2006.01) (71) Applicant: Ascendis Pharma A/S, Hellerup (DK) A638/26 (2006.01) A6M5/9 (2006.01) (72) Inventors: Harald Rau, Heidelberg (DE); Torben A 6LX3/553 (2006.01) Le?mann, Neustadt an der Weinstrasse (52) U.S. Cl. (DE) CPC ......... A61K 47/48338 (2013.01); A61 K3I/553 (2013.01); A61 K38/26 (2013.01); A61 K (21) Appl. No.: 14/674,928 47/48215 (2013.01); A61M 5/19 (2013.01) (22) Filed: Mar. 31, 2015 (57) ABSTRACT The present invention relates to a prodrug or a pharmaceuti Related U.S. Application Data cally acceptable salt thereof, comprising a drug linker conju (63) Continuation of application No. 13/574,092, filed on gate D-L, wherein D being a biologically active moiety con Oct. 15, 2012, filed as application No. PCT/EP2011/ taining an aliphatic amine group is conjugated to one or more 050821 on Jan. 21, 2011. polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeu (30) Foreign Application Priority Data tically useful half-lives. The invention also relates to pharma ceutical compositions comprising said prodrugs and their use Jan. 22, 2010 (EP) ................................ 10 151564.1 as medicaments. US 2015/0202317 A1 Jul. 23, 2015 DIPEPTDE-BASED PRODRUG LINKERS 0007 Alternatively, the drugs may be conjugated to a car FOR ALPHATIC AMNE-CONTAINING rier through permanent covalent bonds. -
Revisão Pharmacological Treatment of Obesity
Pharmacological Treatment of Obesity revisão ABSTRACT Marcio C. Mancini This review offers an overview of physiological agents, current therapeu- Alfredo Halpern tics, as well as medications, which have been extensively used and those agents not currently available or non-classically considered anti-obesity drugs. As obesity — particularly that of central distribution — represents an important triggering factor for insulin resistance, its pharmacological treatment is relevant in the context of metabolic syndrome control. The authors present an extensive review on the criteria for anti-obesity man- agement efficacy, on physiological mechanisms that regulate central and/or peripheral energy homeostasis (nutrients, monoamines, and pep- tides), on β-phenethylamine pharmacological derivative agents (fenflu- ramine, dexfenfluramine, phentermine and sibutramine), tricyclic deriva- tives (mazindol), phenylpropanolamine derivatives (ephedrin, phenyl- propanolamine), phenylpropanolamine oxytrifluorphenyl derivative (flu- oxetine), a naftilamine derivative (sertraline) and a lipstatine derivative (orlistat). An analysis of all clinical trials — over ten-week long — is also presented for medications used in the management of obesity, as well as data about future medications, such as a the inverse cannabinoid agonist, rimonabant. (Arq Bras Endocrinol Metab 2006;50/2:377-389) Keywords: Obesity; Treatment; Anfepramone; Mazindol; Sibutramine; Endocrinology and Metabology Orlistat; Rimonabant Division, Hospital das Clínicas, University of São Paulo Medical -
CENTRAL NERVOUS SYSTEM DEPRESSANTS Opioid Pain Relievers Anxiolytics (Also Belong to Psychiatric Medication Category) • Codeine (In 222® Tablets, Tylenol® No
CENTRAL NERVOUS SYSTEM DEPRESSANTS Opioid Pain Relievers Anxiolytics (also belong to psychiatric medication category) • codeine (in 222® Tablets, Tylenol® No. 1/2/3/4, Fiorinal® C, Benzodiazepines Codeine Contin, etc.) • heroin • alprazolam (Xanax®) • hydrocodone (Hycodan®, etc.) • chlordiazepoxide (Librium®) • hydromorphone (Dilaudid®) • clonazepam (Rivotril®) • methadone • diazepam (Valium®) • morphine (MS Contin®, M-Eslon®, Kadian®, Statex®, etc.) • flurazepam (Dalmane®) • oxycodone (in Oxycocet®, Percocet®, Percodan®, OxyContin®, etc.) • lorazepam (Ativan®) • pentazocine (Talwin®) • nitrazepam (Mogadon®) • oxazepam ( Serax®) Alcohol • temazepam (Restoril®) Inhalants Barbiturates • gases (e.g. nitrous oxide, “laughing gas”, chloroform, halothane, • butalbital (in Fiorinal®) ether) • secobarbital (Seconal®) • volatile solvents (benzene, toluene, xylene, acetone, naptha and hexane) Buspirone (Buspar®) • nitrites (amyl nitrite, butyl nitrite and cyclohexyl nitrite – also known as “poppers”) Non-Benzodiazepine Hypnotics (also belong to psychiatric medication category) • chloral hydrate • zopiclone (Imovane®) Other • GHB (gamma-hydroxybutyrate) • Rohypnol (flunitrazepam) CENTRAL NERVOUS SYSTEM STIMULANTS Amphetamines Caffeine • dextroamphetamine (Dexadrine®) Methelynedioxyamphetamine (MDA) • methamphetamine (“Crystal meth”) (also has hallucinogenic actions) • methylphenidate (Biphentin®, Concerta®, Ritalin®) • mixed amphetamine salts (Adderall XR®) 3,4-Methelynedioxymethamphetamine (MDMA, Ecstasy) (also has hallucinogenic actions) Cocaine/Crack