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Pharmacology and Abuse of Cocaine, Amphetamines, Ecstasy and Related Designer Drugs: A comprehensive review on their mode of action, treatment of abuse and intoxication
Pharmacology and Abuse of Cocaine, Amphetamines, Ecstasy and Related Designer Drugs: A comprehensive review on their mode of action, treatment of abuse and intoxication Summary:By Enno Freye
Finally - a book that covers all aspects of the illicit use of cocaine, amphetamines, ecstasy and/or designer drugs such as GHB, written by two experts in their field. The use of these drugs remains a continuous threat in health and medical care delivery, and this book will be an essential asset to the physician who may have to face the evaluation of patients whose use of these drugs compromises an effective treatment plan for other health issues. The book has been conceived to fill the void in existing physician reference materials, and provides a comprehensive review of the theoretical knowledge and scope of pharmacotherapy in individuals who are hooked on a psychoactive substance. While detailed scientific information is obtainable in other major articles, the book's straightforward format and style, along with its illustrations, will make for easy reading as emphasis is put on information specifically related to drugs that occur most abused in today’s society. The information provided is based on clinical practice rather than pure experimental data, which will give the physician more effective tools useful in their daily practice. Many mechanisms of action of abuse are described in detail and references are provided to direct the reader to further sources for additional information. As a special feature, the book incorporates uncluttered tables and charts, which result in immediate clarification of the mode of action on the central nervous system and the reason for misuse, thus avoiding usual long and fatiguing text in common reference books. The book aims to give the reader a clear and concise plan on what to do when being faced with an overdose situation. A well-organized Table of Contents rapidly leads the reader from general pharmacological issues to the specific overdose syndrome and its management. Additionally, significant emphasis is placed on the practical do's and don’ts for physicians, with special reference to the predictive signs of aberrant drug-related behavior and the identification of the drug diverter by using urine drug screening. Table of Contents Introduction...................................................................................................... 1Incidence of Illicit Use of Cocaine and Other Drugs......................................... 1 Part I How It All Started with Cocaine...................................................... 5 Botanical Characteristics of Coca Leaves.......................................................... 7 Production of the Coca Leaf........................................................................... 9 Cocaine: History of Use................................................................................... 13 Coca Consumption with Wine........................................................................... 15 Coca in Refreshing Beverages........................................................................... 15 Regulatories for Use of Cocaine........................................................................ 16 Popularity of Cocaine as a Drug for Medical Treatment............................. 19 Use of Cocaine as a Local Anesthetic................................................................ 21 The Different Forms of Cocaine........................................................................ 25 The Different Types of Alkaloids in Coca...................................................... 27 The Making of Cocaine in the Jungle............................................................ 29 Steps Refining Coca Paste to Cocaine Base...................................................... 31 Trafficking of Cocaine: The Legal Approach.................................................... 33 Profit Making and Trafficking of Cocaine: The Illegal Approach..................... 33 Smuggling of Cocaine........................................................................................ 35 Diluting or “Cutting” of Cocaine................................................................... 36 Ascertaining the Purity of Cocaine and the Cutting Agent................................ 37 Economics of Cocaine....................................................................................... 40 Freebase Cocaine: High Bioavailability with Increase in Potency.............. 43 Freebasing of Cocaine: The Ether Wash Method.............................................. 44 Freebasing of Cocaine: The Baking Soda Method............................................ 47 Pharmacology of Cocaine................................................................................ 49 Pharmaceutical Cocaine..................................................................................... 49 Physicochemical Properties of Cocaine......................................................... 50 Decomposition of Cocaine............................................................................. 51 Cocaine, as a Local Anesthetic: Mechanism of Action................................. 51 Cocaine’s CNS Effects: Mechanism of Action.............................................. 54 Emotional Effects of Cocaine........................................................................ 58 Addictive Properties of Cocaine: Mode of Action......................................... 61 Psychological Dependence................................................................................ 63 Cocaine Intoxication: Strategy for Treatment.............................................. 65 Phase of Early Stimulation................................................................................. 66 Phase of Advanced Stimulation......................................................................... 66 The Depressive Phase........................................................................................ 66 Basics in Treatment of Cocaine Overdose (OD)........................................... 66 Advanced Treatment of Cocaine OD............................................................. 67 Selective Approach to Cocaine OD............................................................... 67 Avoiding Procedures in Cocaine OD............................................................. 68 Special Pathologies in Chronic Cocaine Use.................................................. 69 The Toxic Cocaine Delirium.............................................................................. 69 Cocaine and Myocardial Infarction................................................................... 70 Treatment of Cocaine-Related Myocardial Ischemia (MI)............................ 71 Secondary Prevention of Cocaine-Related MI............................................... 72 Cocaine-Related Rhabdomyolysis..................................................................... 73 Cocaine and Cerebrovascular Ischemia/Hemorrhage........................................ 74 Summary of Advanced Treatment in Cocaine OD....................................... 75 Treatment of Tachyarrhythmia........................................................................... 75 Treatment of Ventricular fibrillation.................................................................. 75 Treatment of Hypertension................................................................................ 76 Treatment of Hyperthermia................................................................................ 76 Treatment of Seizures........................................................................................ 76 Lethal Doses of Cocaine.................................................................................... 77 Chronic Toxicity of Cocaine use..................................................................... 79 Summary of Acute-Chronic Effects of Cocaine............................................ 83 Duration of Withdrawal Symptoms Following Cocaine Abuse......................... 85 Cocaine Use in Pregnancy............................................................................... 87 Treatment Options in Cocaine Abuse................................................................ 88 Detoxification................................................................................................ 88 Cocaine-free environment............................................................................ 89 Hospitalization or outpatient therapy........................................................... 89 Pharmacological therapy.............................................................................. 89 Use of antidepressants to relieve post-Cocaine depression........................ 92 Non-pharmacological Treatmenet of Cocaine Addiction.............................. 96 New Options in the Treatment of Cocaine Dependency............................... 99 The Antiepileptic Gamma Vinyl-GABA (GVG)............................................... 99 Disulfiram (Antabuse®)..................................................................................... 100 Use of an Anti-cocaine Vaccine......................................................................... 102 Vaccination of the Cocaine User........................................................................ 102 Newer Dopamine Reuptake Inhibitors............................................................... 103 GBR-12909 (Vanoxerine).............................................................................. 103 Venlafaxine (Effexor®) and Ecopipam.......................................................... 103 Outlook Regarding Therapy in Cocaine Abuse................................................. 104 References......................................................................................................... 105 Part II Methamphetamine-an Old Aquaintance in New Clothes............. 109 History of Methamphetamine............................................................................ 109 From Amphetamine to Methamphetamine........................................................ 110 Mode of Action of Methamphetamine........................................................... 115 Interaction of Methamphetamine with other Stimulants................................... 117 Pharmacology of Methamphetamine............................................................. 119 Prescribing Methamphetamine.......................................................................... 122 Chemistry of Methamphetamine........................................................................ 123 Crystal Methamphetamine............................................................................. 125 Addictive Properties of Methamphetamine....................................................... 125 Treatment Options in Methamphetamine Addiction and Withdrawal............................................................................................... 131 Medical Treatment in Methamphetamine Related Depression.......................... 132 Non-Medical Treatment in Methamphetamine Related Depression.................. 132 Treatment Preventing Methamphetamine Relapse............................................ 132 Amphetamine Derivatives as Appetite Suppressants................................... 135 References......................................................................................................... 137 Part III MDMA (Ecstasy): from Psychotherapy to a Street Drug of Abuse............................................................... 139 History of MDMA............................................................................................. 139 Incidence of Illicit Use of Ecstasy................................................................... 143 Medical Use of Ecstasy in Assisting Psychotherapy......................................... 143 Pharmacology of Ecstasy (MDMA)................................................................ 147 Pharmacological Effects of MDMA in Man.................................................. 151 Onset of Action and Duration of Action............................................................ 151 The Psychological Effects of MDMA............................................................... 151 Entactogenesis (“Touching Within”)............................................................. 152 Empathogenesis............................................................................................. 152 Enhancement of Senses.................................................................................. 152 Abuse Liability and Psychomotor Performance................................................ 153 The Physical Effects of MDMA........................................................................ 153 Cardiovascular Effects of MDMA................................................................. 154 Neuroendocrine Effects of MDMA............................................................... 154 Ocular Effects of MDMA.............................................................................. 155 Lethal Effects of MDMA............................................................................... 155 Effects in Chronic Use of MDMA................................................................. 155 Chronic MDMA Use and Neurotoxicity............................................................ 156 Pharmacokinetics of MDMA.......................................................................... 161 Primary Metabolism of MDMA........................................................................ 161 Secondary Metabolism of MDMA.................................................................... 163 Interactions and Overdose with MDMA............................................................ 164 Acute Intoxication with MDMA........................................................................ 165 Hyperthermia................................................................................................. 166 Cardiovascular Effects................................................................................... 166 Cerebrovascular Effects................................................................................. 167 Neuroendocrine Effects.................................................................................. 167 Hepatotoxicity................................................................................................ 168 Psychopathology............................................................................................ 168 Treatment of MDMA-Related Toxicity............................................................. 168 Hyperthermia................................................................................................. 169 Cardiovascular Treatment.............................................................................. 170 Cerebrovascular Treatment............................................................................ 170 Neurologic Treatment.................................................................................... 171 Appendix Analogues of MDMA and Related Compounds....................... 173 MDA (3,4-methylenedioxyamphetamine)......................................................... 173 MDE or MDEA (N-ethyl-methylenedioxyamphetamine)................................. 173 MMDA (3-methoxy-4,5-methylenedioxyamphetamine)................................... 173 2-Methoxy-3,4-methylenedioxyphenethylamine............................................... 174 MBDB (N-methyl-1-(1,3-benzodioxol-5-yl)-N-methylbutan-2-amine)............ 174 References......................................................................................................... 175 Part IV Designer Drugs and their Abuse.................................................... 181 History of Designer Drugs............................................................................... 183 Well-Known Designer Drugs of the Past Years................................................. 186 Gamma-Hydroxybutyric (GHB) Acid........................................................... 191 History of GHB.................................................................................................. 191 Medical Use of g-Hydroxybutyrate.................................................................... 192 Pharmacokinetics of GHB................................................................................. 194 The Pharmacology of g-Hydroxybutyric Acid (GHB).................................. 195 Mode of Action of GHB.................................................................................... 195 Dose-Related CNS Effects of GHB............................................................... 197 Cardiovascular Effects of GHB..................................................................... 197 Respiratory Effects of GHB........................................................................... 198 Neuroendocrine Effects of GHB.................................................................... 198 Sleep Pattern Following GHB........................................................................ 198 Use of GHB in Clinical Medicine.................................................................... 199 GHB for Sedation and Anesthesia..................................................................... 199 GHB for Cerebral Protection............................................................................. 199 GHB in Narcolepsy and Insomnia..................................................................... 200 GHB in Alcohol and Opiate Withdrawal........................................................... 200 Metabolism of g-Hydroxybutyrate(GHB).......................................................... 201 Abuse Potential and Intoxication with GHB................................................. 203 Incidence of Adverse Effects in GHB Intoxication........................................... 203 Principles in GHB Intoxication.......................................................................... 204 Effects of Acute GHB Intoxication.................................................................... 205 Cardiovascular Effects with GHB Intoxication............................................. 205 Respiratory Effects with GHB Intoxication................................................... 205 Psychotic Effects with GHB Intoxication...................................................... 206 Ocular Effects with GHB Intoxication........................................................... 206 Metabolic Effects with GHB Intoxication..................................................... 206 Gastrointestinal Effects with GHB Intoxication............................................ 206 Body Temperature in GHB Intoxication........................................................ 206 Muscular Disorders in GHB Intoxication...................................................... 207 Miscellaneous Effects in GHB Intoxication.................................................. 207 Withdrawal and Tolerance Following Use of GHB........................................... 207 Treatment Following GHB Intoxication............................................................ 208 First-Line Treatment in GHB Overdose........................................................ 208 Cardiovascular Withdrawal Treatment Following GHB Overdose................ 209 Benzylpiperazine (BZP) as a Designer Drug................................................. 211 Pharmacology of Benzylpiperazine (BZP)........................................................ 211 Addictive Effects of Benzylpiperazine.............................................................. 212 Natural Products with Abuse Potential.......................................................... 215 Datura a Hallucinogenic.................................................................................... 215 Toxicity of Datura Stramonium...................................................................... 217 Overdose of Datura............................................................................................ 217 Dimethyltryptamine (DMT) a Psychedelic.................................................... 219 The Mushroom Psilocybin with Psychedelic Properties.............................. 221 Toxicity of Psilocybine...................................................................................... 221 Pharmacological Effects of Psilocybine............................................................ 221 Ibogaine, Psychedelic Molecule with Anti-addictive Properties.................. 225 Pharmacology of Ibogaine................................................................................. 226 Peyote, a Mescaline-Containing Cactus......................................................... 227 Behavioral Effects Produced by Mescaline....................................................... 227 LSD, a Semisynthetic Psychedelic Drug........................................................ 229 Pharmacology of LSD........................................................................................ 229 Research with LSD............................................................................................ 230 The Legal Status of LSD.................................................................................... 231 5-MeO-DIPT, a Psychedelic Structurally Related to Psiloc(yb)in............... 233 Pharmacology of 5-MeO-DIPT......................................................................... 233 Legal Status of 5-MeO-DIPT............................................................................. 234 References......................................................................................................... 235 Part V How to Demask the Patient with an Aberrant Drug Use.............. 243 Stigma of Persons with a Potential Drug Addictive Behavior........................... 243 The Alcohol Addictive Patient........................................................................... 244 Signs of Alcohol Co-abuse in Addiction....................................................... 244 Positive Signs and Symptoms of Hard Drug Abuse...................................... 247 Signs and Symptoms for Abusive Drug Behavior............................................. 247 Urine Drug Screening (UDS): Identifying the Person with Illicit Use........ 251 Prerequisites for Use of UDS............................................................................. 251 Types of Urine Drug Testing........................................................................... 253 Half-Life of Detection and Cut-Offs in Urine Drug Screening......................... 255 Interpretation of Positive Urine Drug Tests (UDT)........................................... 256 Considerations When Having a Positive Urine Drug Test............................. 256 Considerations When Having a Negative Urine Drug Test........................... 260 Type of Tests for Urine Drug Testing (UDT)................................................. 261 The Dip Test....................................................................................................... 261 The Drop Test.................................................................................................... 261 How to Interpret the Results.......................................................................... 261 Identification of the Methadone Metabolite in Substitution Therapy................ 262 Single Test Strips............................................................................................... 265 Test-Cup for Permanent Storage........................................................................ 266 Detecting Manipulations of Urine Samples in UDT.......................................... 267 Analysis of Saliva, Hair and Sweat for Drug Testing................................... 269 Hair Analysis for the Detection of Abused Drugs and Medications................. 269 Analysis of Sweat for Abused Drugs and Medications..................................... 271 SmartClip® Test for Saliva Testing............................................................... 272 OraLab® Test for Saliva Testing................................................................... 274 OraTube® for Fluid Testing........................................................................... 274 DRUGWIPE® 5+ for Drug Testing of Saliva................................................ 275 Dräger Drug Test 5000................................................................................... 278 Trace Wipe Test for Identification of Cocaine Smuggling or Abuse............. 279 Professional Equipment for Drug Analysis of Liquids / Powder / Tablet............................................................................................... 279 Drug Testing in Vapor.................................................................................... 282 References......................................................................................................... 283 Appendix Common Street Names of Cocaine and Methamphetamine used as a Jargon............................................................................................... 287 Index.................................................................................................................. 297 Please select one mirror to download
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