Natural Psychodysleptic Compounds: Sources and Pharmacology
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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. -
Pharmacotherapeutic Considerations for Individuals with Down Syndrome Erik Hefti
Harrisburg University of Science and Technology Digital Commons at Harrisburg University Harrisburg University Faculty Works 12-8-2016 Pharmacotherapeutic Considerations for Individuals with Down Syndrome Erik Hefti Follow this and additional works at: http://digitalcommons.harrisburgu.edu/faculty-works Part of the Congenital, Hereditary, and Neonatal Diseases and Abnormalities Commons, and the Medicinal and Pharmaceutical Chemistry Commons R EVIEW O F T HERAPEUTICS Pharmacotherapeutic Considerations for Individuals with Down Syndrome Erik Hefti,* and Javier G. Blanco* Department of Pharmaceutical Sciences, The School of Pharmacy and Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, New York Down syndrome (DS; trisomy 21) is the most common survivable disorder due to aneuploidy. Individ- uals with DS may experience multiple comorbid health problems including congenital heart defects, endocrine abnormalities, skin and dental problems, seizure disorders, leukemia, dementia, and obesity. These associated conditions may necessitate pharmacotherapeutic management with various drugs. The complex pathobiology of DS may alter drug disposition and drug response in some individuals. For example, reports have documented increased rates of adverse drug reactions in patients with DS treated for leukemia and dementia. Intellectual disability resulting from DS may impact adherence to medication regimens. In this review, we highlight literature focused on pharmacotherapy for individu- als with DS. We discuss reports of altered drug disposition or response in patients with DS and explore social factors that may impact medication adherence in the DS setting. Enhanced monitoring during drug therapy in individuals with DS is justified based on reports of altered drug disposition, drug response, and other characteristics present in this population. -
Medical Review Officer Manual
Department of Health and Human Services Substance Abuse and Mental Health Services Administration Center for Substance Abuse Prevention Medical Review Officer Manual for Federal Agency Workplace Drug Testing Programs EFFECTIVE OCTOBER 1, 2010 Note: This manual applies to Federal agency drug testing programs that come under Executive Order 12564 dated September 15, 1986, section 503 of Public Law 100-71, 5 U.S.C. section 7301 note dated July 11, 1987, and the Department of Health and Human Services Mandatory Guidelines for Federal Workplace Drug Testing Programs (73 FR 71858) dated November 25, 2008 (effective October 1, 2010). This manual does not apply to specimens submitted for testing under U.S. Department of Transportation (DOT) Procedures for Transportation Workplace Drug and Alcohol Testing Programs (49 CFR Part 40). The current version of this manual and other information including MRO Case Studies are available on the Drug Testing page under Medical Review Officer (MRO) Resources on the SAMHSA website: http://www.workplace.samhsa.gov Previous Versions of this Manual are Obsolete 3 Table of Contents Chapter 1. The Medical Review Officer (MRO)........................................................................... 6 Chapter 2. The Federal Drug Testing Custody and Control Form ................................................ 7 Chapter 3. Urine Drug Testing ...................................................................................................... 9 A. Federal Workplace Drug Testing Overview.................................................................. -
Substance Abuse and Dependence
9 Substance Abuse and Dependence CHAPTER CHAPTER OUTLINE CLASSIFICATION OF SUBSTANCE-RELATED THEORETICAL PERSPECTIVES 310–316 Residential Approaches DISORDERS 291–296 Biological Perspectives Psychodynamic Approaches Substance Abuse and Dependence Learning Perspectives Behavioral Approaches Addiction and Other Forms of Compulsive Cognitive Perspectives Relapse-Prevention Training Behavior Psychodynamic Perspectives SUMMING UP 325–326 Racial and Ethnic Differences in Substance Sociocultural Perspectives Use Disorders TREATMENT OF SUBSTANCE ABUSE Pathways to Drug Dependence AND DEPENDENCE 316–325 DRUGS OF ABUSE 296–310 Biological Approaches Depressants Culturally Sensitive Treatment Stimulants of Alcoholism Hallucinogens Nonprofessional Support Groups TRUTH or FICTION T❑ F❑ Heroin accounts for more deaths “Nothing and Nobody Comes Before than any other drug. (p. 291) T❑ F❑ You cannot be psychologically My Coke” dependent on a drug without also being She had just caught me with cocaine again after I had managed to convince her that physically dependent on it. (p. 295) I hadn’t used in over a month. Of course I had been tooting (snorting) almost every T❑ F❑ More teenagers and young adults die day, but I had managed to cover my tracks a little better than usual. So she said to from alcohol-related motor vehicle accidents me that I was going to have to make a choice—either cocaine or her. Before she than from any other cause. (p. 297) finished the sentence, I knew what was coming, so I told her to think carefully about what she was going to say. It was clear to me that there wasn’t a choice. I love my T❑ F❑ It is safe to let someone who has wife, but I’m not going to choose anything over cocaine. -
Hallucinogens and Dissociative Drugs
Long-Term Effects of Hallucinogens See page 5. from the director: Research Report Series Hallucinogens and dissociative drugs — which have street names like acid, angel dust, and vitamin K — distort the way a user perceives time, motion, colors, sounds, and self. These drugs can disrupt a person’s ability to think and communicate rationally, or even to recognize reality, sometimes resulting in bizarre or dangerous behavior. Hallucinogens such as LSD, psilocybin, peyote, DMT, and ayahuasca cause HALLUCINOGENS AND emotions to swing wildly and real-world sensations to appear unreal, sometimes frightening. Dissociative drugs like PCP, DISSOCIATIVE DRUGS ketamine, dextromethorphan, and Salvia divinorum may make a user feel out of Including LSD, Psilocybin, Peyote, DMT, Ayahuasca, control and disconnected from their body PCP, Ketamine, Dextromethorphan, and Salvia and environment. In addition to their short-term effects What Are on perception and mood, hallucinogenic Hallucinogens and drugs are associated with psychotic- like episodes that can occur long after Dissociative Drugs? a person has taken the drug, and dissociative drugs can cause respiratory allucinogens are a class of drugs that cause hallucinations—profound distortions depression, heart rate abnormalities, and in a person’s perceptions of reality. Hallucinogens can be found in some plants and a withdrawal syndrome. The good news is mushrooms (or their extracts) or can be man-made, and they are commonly divided that use of hallucinogenic and dissociative Hinto two broad categories: classic hallucinogens (such as LSD) and dissociative drugs (such drugs among U.S. high school students, as PCP). When under the influence of either type of drug, people often report rapid, intense in general, has remained relatively low in emotional swings and seeing images, hearing sounds, and feeling sensations that seem real recent years. -
The Cannabinoid Receptor Agonist WIN 55,212-2 Attenuates the Effects Induced by Quinolinic Acid in the Rat Striatum
Neuropharmacology 51 (2006) 1004e1012 www.elsevier.com/locate/neuropharm The cannabinoid receptor agonist WIN 55,212-2 attenuates the effects induced by quinolinic acid in the rat striatum A. Pintor a, M.T. Tebano a, A. Martire a, R. Grieco a, M. Galluzzo a, M.L. Scattoni b,A.Pe`zzola a, R. Coccurello c, F. Felici a, V. Cuomo d, D. Piomelli e, G. Calamandrei b, P. Popoli a,* a Department of Drug Research and Evaluation, Central Nervous System Pharmacology Division, Istituto Superiore di Sanita`, Viale Regina Elena, 299, 00161 Rome, Italy b Department of Cell Biology and Neuroscience, Istituto Superiore di Sanita`, Viale Regina Elena, 299, 00161 Rome, Italy c Institute of Neuroscience, EBRI Foundation, Rome, Italy d Department of Pharmacology and General Physiology, University ‘‘La Sapienza’’, Rome, Italy e Department of Pharmacology and Center for Drug Discovery, University of California, Irvine, CA, USA Received 7 April 2006; received in revised form 15 May 2006; accepted 16 June 2006 Abstract The ability of CB1 receptors to regulate the release of glutamate in the striatum, together with the finding that, in experimental models of Huntington disease (HD), both endocannabinoid levels and CB1 receptor densities are reduced, has prompted the investigation on the neuropro- tective role of the cannabinoids in HD. Quinolinic acid (QA) is an excitotoxin that, when injected in the rat striatum reproduces many features of HD and that acts by stimulating glutamate outflow. The aim of the present study was to test the ability of the cannabinoid receptor agonist WIN 55,212-2 to prevent the effects induced by QA in the rat striatum. -
Adverse Reactions to Hallucinogenic Drugs. 1Rnstttutton National Test
DOCUMENT RESUME ED 034 696 SE 007 743 AUTROP Meyer, Roger E. , Fd. TITLE Adverse Reactions to Hallucinogenic Drugs. 1rNSTTTUTTON National Test. of Mental Health (DHEW), Bethesda, Md. PUB DATP Sep 67 NOTE 118p.; Conference held at the National Institute of Mental Health, Chevy Chase, Maryland, September 29, 1967 AVATLABLE FROM Superintendent of Documents, Government Printing Office, Washington, D. C. 20402 ($1.25). FDPS PRICE FDPS Price MFc0.50 HC Not Available from EDRS. DESCPTPTOPS Conference Reports, *Drug Abuse, Health Education, *Lysergic Acid Diethylamide, *Medical Research, *Mental Health IDENTIFIEPS Hallucinogenic Drugs ABSTPACT This reports a conference of psychologists, psychiatrists, geneticists and others concerned with the biological and psychological effects of lysergic acid diethylamide and other hallucinogenic drugs. Clinical data are presented on adverse drug reactions. The difficulty of determining the causes of adverse reactions is discussed, as are different methods of therapy. Data are also presented on the psychological and physiolcgical effects of L.S.D. given as a treatment under controlled medical conditions. Possible genetic effects of L.S.D. and other drugs are discussed on the basis of data from laboratory animals and humans. Also discussed are needs for futher research. The necessity to aviod scare techniques in disseminating information about drugs is emphasized. An aprentlix includes seven background papers reprinted from professional journals, and a bibliography of current articles on the possible genetic effects of drugs. (EB) National Clearinghouse for Mental Health Information VA-w. Alb alb !bAm I.S. MOMS Of NAM MON tMAN IONE Of NMI 105 NUNN NU IN WINES UAWAS RCM NIN 01 NUN N ONMININI 01011110 0. -
DEMAND REDUCTION a Glossary of Terms
UNITED NATIONS PUBLICATION Sales No. E.00.XI.9 ISBN: 92-1-148129-5 ACKNOWLEDGEMENTS This document was prepared by the: United Nations International Drug Control Programme (UNDCP), Vienna, Austria, in consultation with the Commonwealth of Health and Aged Care, Australia, and the informal international reference group. ii Contents Page Foreword . xi Demand reduction: A glossary of terms . 1 Abstinence . 1 Abuse . 1 Abuse liability . 2 Action research . 2 Addiction, addict . 2 Administration (method of) . 3 Adverse drug reaction . 4 Advice services . 4 Advocacy . 4 Agonist . 4 AIDS . 5 Al-Anon . 5 Alcohol . 5 Alcoholics Anonymous (AA) . 6 Alternatives to drug use . 6 Amfetamine . 6 Amotivational syndrome . 6 Amphetamine . 6 Amyl nitrate . 8 Analgesic . 8 iii Page Antagonist . 8 Anti-anxiety drug . 8 Antidepressant . 8 Backloading . 9 Bad trip . 9 Barbiturate . 9 Benzodiazepine . 10 Blood-borne virus . 10 Brief intervention . 11 Buprenorphine . 11 Caffeine . 12 Cannabis . 12 Chasing . 13 Cocaine . 13 Coca leaves . 14 Coca paste . 14 Cold turkey . 14 Community empowerment . 15 Co-morbidity . 15 Comprehensive Multidisciplinary Outline of Future Activities in Drug Abuse Control (CMO) . 15 Controlled substance . 15 Counselling and psychotherapy . 16 Court diversion . 16 Crash . 16 Cross-dependence . 17 Cross-tolerance . 17 Custody diversion . 17 Dance drug . 18 Decriminalization or depenalization . 18 Demand . 18 iv Page Demand reduction . 19 Dependence, dependence syndrome . 19 Dependence liability . 20 Depressant . 20 Designer drug . 20 Detoxification . 20 Diacetylmorphine/Diamorphine . 21 Diuretic . 21 Drug . 21 Drug abuse . 22 Drug abuse-related harm . 22 Drug abuse-related problem . 22 Drug policy . 23 Drug seeking . 23 Drug substitution . 23 Drug testing . 24 Drug use . -
PSYCHEDELIC DRUGS (P.L) 1. Terminology “Hallucinogens
PSYCHEDELIC DRUGS (p.l) 1. Terminology “hallucinogens” – induce hallucinations, although sensory distortions are more common “psychotomimetics” – to minic psychotic states, although truly most drugs in this class do not do so “phantasticums”or “psychedelics” – alter sensory perception (Julien uses “psychedelics”) alterations in perception, cognition, and mood, in presence of otherwise clear ability to sense” may increase sensory awareness, increase clarity, decrease control over what is sensed/experienced “self-A” may feel a passive observer of what “self-B” is experiencing often accompanied by a sense of profound meaningfulness, of divine or cosmic importance (limbic system?) these drugs can be classified by what NT they mimic: anti-ACh, agonists for NE, 5HT, or glutamate (See p. 332, Table 12.l in Julien, 9th Ed.) 2. The Anti-ACh Psychedelics e.g. scopolamine (classified as an ACh blocker) high affinity, no efficacy plant product: Belladonna or “deadly nightshade” (Atropa belladonna) Datura stramonium (jimson weed, stinkweed) Mandragora officinarum (mandrake plant) pupillary dilation (2nd to atropine) PSYCHEDELIC DRUGS (p.2) 2. Anti-ACh Psychedelics (cont.) pharmacological effects: e.g. scopolamine (Donnatal) clinically used to tx motion sickness, relax smooth muscles (gastric cramping), mild sedation/anesthetic effect PNS effects --- dry mouth relaxation of smooth muscles decreased sweating increased body temperature blurred vision dry skin pupillary dilation tachycardia, increased BP CNS effects --- drowsiness, mild euphoria profound amnesia fatigue decreased attention, focus delirium, mental confusion decreased REM sleep no increase in sensory awareness as dose increases --- restlessness, excitement, hallucinations, euphoria, disorientation at toxic dose levels --- “psychotic delirium”, confusion, stupor, coma, respiratory depression so drug is really an intoxicant, amnestic, and deliriant 3. -
SALVIA DIVINORUM and SALVINORIN a (Street Names: Maria Pastora, Sage of the Seers, Diviner’S Sage, Salvia, Sally-D, Magic Mint) March 2020
Drug Enforcement Administration Diversion Control Division Drug & Chemical Evaluation Section SALVIA DIVINORUM AND SALVINORIN A (Street Names: Maria Pastora, Sage of the Seers, Diviner’s Sage, Salvia, Sally-D, Magic Mint) March 2020 Introduction: from Mexico and Central and South America. The Internet Salvia divinorum is a perennial herb in the mint family is used for the promotion and distribution of Salvia divinorum. native to certain areas of the Sierra Mazateca region of It is sold as seeds, plant cuttings, whole plants, fresh and Oaxaca, Mexico. The plant, which can grow to over three dried leaves, extract-enhanced leaves of various strengths feet in height, has large green leaves, hollow square stems (e.g., 5x, 10x, 20x, 30x), and liquid extracts purported to and white flowers with purple calyces, can also be grown contain salvinorin A. These products are also sold at local successfully outside of this region. Salvia divinorum has shops (e.g., head shops and tobacco shops). been used by the Mazatec Indians for its ritual divination and healing. The active constituent of Salvia divinorum has been User Population: identified as salvinorin A. Currently, neither Salvia divinorum According to the National Survey on Drug Use and nor any of its constituents, including salvinorin A, are Health (NSDUH), published by SAMHSA, it is estimated that controlled under the federal Controlled Substances Act 5.3 million persons, aged 12 or older, used Salvia divinorum (CSA). in their lifetime in 2016 in comparison to 5.1 million persons a year ago in 2015 and 1.8 million persons a decade ago in Licit Uses: 2006. -
References to Argentina
References to Argentina Part 1 RECENT STATISTICS AND TREND ANALYSIS OF ILLICIT DRUG MARKETS A. EXTENT OF ILLICIT DRUG USE AND HEALTH CONSEQUENCES The Americas (pages 12 to 14 WDR 13) In the Americas, a high prevalence of most illicit drugs, essentially driven by estimates in North America, was observed, with the prevalence of cannabis (7.9 per cent) and cocaine (1.3 per cent) being particularly high in the region. South America, Central America and the Caribbean The annual prevalence of cocaine use in South America (1.3 per cent of the adult population) is comparable to levels in North America, while it remains much higher than the global average in Central America (0.6 per cent) and the Caribbean (0.7 per cent). Cocaine use has increased significantly in Brazil, Costa Rica and, to lesser extent, Peru while no change in its use was reported in Argentina. The use of cannabis in South America is higher (5.7 per cent) than the global average, but lower in Central America and Caribbean (2.6 and 2.8 per cent respectively). In South America and Central America the use of opioids (0.3 and 0.2 per cent, respectively) and Ecstasy (0.1 per cent each) also remain well below the global average. While opiates use remains low, countries such as Colombia report that heroin use is becoming increasingly common among certain age groups and socio-economic classes.30 Part 2 NEW PSYCHOACTIVE SUBSTANCES C. THE RECENT EMERGENCE AND SPREAD OF NEW PSYCHOACTIVE SUBSTANCES (page 67 WDR 13) Spread at the global level Number of countries reporting the emergence of new psychoactive substances Pursuant to Commission on Narcotic Drugs resolution 55/1, entitled “Promoting international cooperation in responding to the challenges posed by new psychoactive substances”, in 2012 UNODC sent a questionnaire on NPS to all Member States, to which 80 countries and territories replied. -
Effectiveness of Bronchodilator and Corticosteroid Treatment in Patients with Chronic Obstructive Pulmonary Disease (Copd)
Journal of Pharmaceutical Science and Application Volume 2, Issue 1, Page 17-22, June 2020 E-ISSN : 2301-7708 EFFECTIVENESS OF BRONCHODILATOR AND CORTICOSTEROID TREATMENT IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) Putu Rika Veryanti1*, Ainun Wulandari1 1Department of Pharmacy, Institut Sains dan Teknologi Nasional, Jakarta, Indonesia Corresponding author email: [email protected] ABSTRACT Background: Chronic Obstructive Pulmonary Disease (COPD) is a chronic airway disease which is characterized by progressive airway obstruction. Bronchodilators and corticosteroids are the first choices of therapy in COPD patients. The goal therapy of COPD patients is to prevent respiratory failure, which can impact on death. But nowadays, the mortality rate due to COPD continues to increase. WHO predicts mortality from COPD in the year 2030 will be ranked third in the world. This high mortality can be caused by the ineffectiveness of therapy given. Objective: The aim of this study is to find out the effectiveness of bronchodilator and corticosteroid treatments in COPD patients. Methods: An observational study conducted retrospectively in the 2018 period at Fatmawati Central General Hospital. The effectiveness of therapy was assessed from the patient's clinical condition, blood gas values (PaO2 & PaCO2) and the average length of stay (AvLOS). Results: COPD was mostly suffered by males (83,33%), and the highest age for COPD was in the range of 45 years and above (90%). Bronchodilator that commonly prescribed were albuterol (30.08%), ipratropium bromide (12.2%), fenoterol hydrobromide (10.57%), terbutaline sulfate (8.13%), theophylline (1.63%) and aminophylline (5.69%), while the corticosteroids were budesonide (17.07%), methylprednisolone (9.76%) and dexamethasone (4.88%).