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Chapter 40

Chapter 40. Drug Abuse IV: Major Drugs of Abuse Other Than Alcohol and Nicotine. Drug Abuse IV: Major Drugs of Abuse. Heroin and other opioids General CNS depressants Psychostimulants Marijuana and related preparations Psychedelics 3,4-Methylenedioxymethamphetamine (MDMA, Ecstasy)

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Chapter 40

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  1. Chapter 40 Drug Abuse IV: Major Drugs of Abuse Other Than Alcohol and Nicotine

  2. Drug Abuse IV: Major Drugs of Abuse • Heroin and other opioids • General CNS depressants • Psychostimulants • Marijuana and related preparations • Psychedelics • 3,4-Methylenedioxymethamphetamine (MDMA, Ecstasy) • Phencyclidine • Inhalants • Anabolic steroids

  3. Heroin, Oxycodone, and Other Opioids • Major drugs of abuse • Most opioids are Schedule II • Patterns of abuse • Subjective and behavioral effects • Preferred drugs and routes of administration

  4. Heroin • Patterns of use • Greatest use among 18- to 25-year-olds • All segments of society • First exposure usually social or for pain management • Subjective and behavioral effects • Moments after IV injection, lower abdominal sensation that is similar to sexual orgasm and lasts about 45 seconds • Followed by euphoria • Initial use causes nausea and vomiting • Preferred drugs and routes of administration • Opioid of choice for street use • High lipid solubility • IV route preferred, but also smoking, nasal inhalation

  5. Meperidine • Nurses and physicians who abuse opioids often select meperidine • Highly effective in oral route (unlike injections, leaves no sign) • Minimal effect on smooth muscle: fewer problems with constipation and urinary retention

  6. Oxycodone • Opioid similar to morphine • Intended as controlled-release drug (OxyContin) • Abusers crush tablet • Snort powder or dissolve in water for IV • Entire dose absorbed immediately with high risk of death • Tolerance and physical dependence

  7. Oxycodone • Treatment of acute toxicity • Classic triad • Respiratory depression, coma, pinpoint pupils • Naloxone (Narcan) • Nalmefene (Revex)

  8. Tolerance and Physical Dependence • Tolerance • Prolonged use • Effects for which tolerance develops • Effects for which tolerance does not develop • Cross-tolerance • Physical dependence • Long-term use • Abstinence syndrome • Acute phase and second phase

  9. Opioid Detoxification • Detoxification • Methadone substitution • Long-acting oral opioid • Most commonly used agent • Approximately 10 days • Clonidine-assisted withdrawal • Rapid and ultrarapid withdrawal

  10. Drugs for Long-Term Opioid Addiction Management • Three groups of medications • Opioid agonists, opioid agonist-antagonists, and opioid antagonists • Methadone • Maintenance and suppressive therapy • Buprenorphine • Maintenance therapy and detox facilitation • Naltrexone • Discourages renewed opioid abuse

  11. Sequelae of Compulsive Opioid Use • Few direct detrimental effects • Treatment programs vs. street drugs and subculture • Accidental overdose

  12. General CNS Depressants • Barbiturates, benzodiazepines, alcohol, and other agents • Benzodiazepines have unique properties

  13. Barbiturates • Depressant effects are dose-dependent • Mild sedation to sleep to coma and death • Subjective effects similar to those of alcohol • Agents with short to intermediate duration of action have highest abuse incidence and are Schedule II • Amobarbital, pentobarbital, and secobarbital

  14. Benzodiazepines • Tolerance • Physical dependence and withdrawal techniques • Acute toxicity • Flumazenil (Romazicon) • Benzodiazepines (Schedule IV) • Much safer than barbiturates • Overdose rare when taken alone and orally • Risk increased with IV or with other depressants • Alcohol and miscellaneous CNS depressants • Methaqualone (Quaalude)

  15. Psychostimulants • CNS stimulants (Schedule II) that have a high potential for abuse • Amphetamines • Cocaine • Related substances • Can stimulate the heart, blood vessels, and other structures under sympathetic control

  16. Cocaine • Extracted from leaves of coca plant • CNS effect similar to that of amphetamines • Two forms used by abusers • Cocaine • “Crack” • Can produce local anesthesia, vasoconstriction, and cardiac stimulation

  17. Cocaine • Cocaine • Cocaine hydrochloride • White powder • Diluted for sale • Taken intranasally • Cocaine base: commonly called “crack” • Also called “crystals” or “rocks” • Heated for use • Taken by IV injection

  18. Methamphetamines • In abuse, usually taken orally, snorted, smoked, or IV • Also called “ice” or “crystal meth” • Form of dextroamphetamine • Smoked, snorted, or inserted into rectum • Effects • Arousal, euphoria, sense of increased physical strength and mental capacity • Hallucinations, psychotic state, sympathomimetic actions

  19. Methamphetamines • Other adverse effects • Tolerance, dependence, and withdrawal • Treatment • Bupropion (Wellbutrin, Zyban) • Modafinil (Provigil, Alertec)

  20. Marijuana • Cannabis sativa (hemp) • Marijuana and hashish are derivatives • Common names: “grass,” “weed,” “pot” • Most commonly used illicit drug in the United States • 95 million Americans have tried marijuana at least once

  21. Marijuana • Psychoactive substance • Delta-9-tetrahydrocannabinol (THC) • Routes • Smoking • 60% of THC content absorbed, effects begin in minutes and peak within 20–30 minutes • Oral • Majority of THC is inactivated by first-pass effect

  22. Marijuana • Increased production of prostaglandin E2 • Behaviors • Euphoria • Sedation • Hallucinations • Therapeutic uses • Antiemetic • Appetite stimulant • Neuropathic pain

  23. Marijuana • Effects • Low to moderate dose • High dose • Long-term use

  24. Marijuana • Effects • Low to moderate dose • High-dose • Long-term use • Schizophrenia • Cardiovascular • Dose-related increase in heart rate • Respiratory • Acute: bronchodilation • Chronic: airway constriction

  25. Marijuana • Reproduction • Males and females affected • Altered brain structure • Hippocampal volume left hemisphere • Tolerance and dependence

  26. Therapeutic Use Marijuana • Approved uses for cannabinoids • Unapproved uses for cannabinoids • Medical research on marijuana • Legal status of medical marijuana

  27. Therapeutic Use Marijuana • Comparison of marijuana with alcohol • Aggressive behavior is rare with marijuana use • Loss of judgment is less with marijuana • Increased appetite with marijuana: fewer problems with nutritional deficiencies • Marijuana produces increased toxic psychosis, dissociative phenomena, and paranoia, more so than with alcohol

  28. Psychedelics • Lysergic acid diethylamide (LSD) • Acts on serotonin receptors of brain • Routes: oral, IV, smoked • Alters the following (as otherwise occurs only in dreams): • Thinking • Feelings • Perception • Relationship to environment

  29. Other Psychedelic Drugs • Subjective and behavioral effects are similar to those of LSD • None approved for medical use • Salvia • Mescaline • From peyote cactus • Psilocybin • Psilocin • Dimethyltryptamine

  30. Dissociative Drugs • Phencyclidine (PCP) and ketamine • Original use: surgical anesthetics • Recreational use: distort sight and sound and produce dissociation • Act in the cerebral cortex and limbic system • PCP synthesized/manufactured easily by amateurs • Routes: oral, intranasal, IV, smoking • Ketamine

  31. Dissociative Drugs • Phencyclidine (PCP) • Effects • Low to moderate doses, high doses • Toxicity • Ketamine • Similar to PCP in structure, mechanism, and effects • Shorter duration of effects

  32. Dextromethorphan • OTC cough suppressant • Low dose for antitussive: no psychologic effects • At doses 5–10 times higher, produces euphoria, disorientation, paranoia, altered sense of time, and hallucinations • Also used in combination cold products • Highly abused by adolescents and teenagers OTC = over-the-counter.

  33. 3,4- Methylenedioxymethamphetamine • Common names: MDMA, Ecstasy • Complex drug with stimulant and psychedelic properties • Structurally related to methamphetamine (stimulant) and mescaline (hallucinogen) • Low doses: mild LSD-like psychologic effects • Higher doses: amphetamine-like effects • Promotes release of neurotransmitters • Usually taken orally; also snorted, injected, or taken by rectal suppository

  34. MDMA, Ecstasy • Adverse effects • Can injure serotonergic neurons, stimulate the heart, and dangerously raise body temperature • Neurologic effects • Seizures, spasmodic jerking, jaw clenching, teeth grinding • Confusion, anxiety, paranoia, panic

  35. Inhalants • Term can refer to many drugs; common characteristic is administration by inhalation • Anesthetics • Volatile nitrites • Organic solvents

  36. Anabolic Steroids • Androgens • Taken to enhance athletic performance • Increase muscle mass and strength • Massive doses that are often used have high risk for adverse effects • Most are classified as Schedule III drugs

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