1. Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 40 Drug Abuse IV: Major Drugs of Abuse Other Than Alcohol and Nicotine

2. 2Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 3Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 4Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 5Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 6Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 7Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Oxycodone  Treatment of acute toxicity  Classic triad Respiratory depression, coma, pinpoint pupils Respiratory depression, coma, pinpoint pupils  Naloxone (Narcan)  Nalmefene (Revex)

8. 8Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 9Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Opioid Detoxification  Detoxification  Methadone substitution Long-acting oral opioid Long-acting oral opioid Most commonly used agent Most commonly used agent Approximately 10 days Approximately 10 days  Clonidine-assisted withdrawal  Rapid and ultrarapid withdrawal

10. 10Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 11Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Sequelae of Compulsive Opioid Use  Few direct detrimental effects  Treatment programs vs. street drugs and subculture  Accidental overdose

12. 12Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. General CNS Depressants  Barbiturates, benzodiazepines, alcohol, and other agents  Benzodiazepines have unique properties

13. 13Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 14Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 15Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 16Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 17Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Cocaine  Cocaine  Cocaine hydrochloride White powder White powder Diluted for sale Diluted for sale Taken intranasally Taken intranasally  Cocaine base: commonly called “crack” Also called “crystals” or “rocks” Also called “crystals” or “rocks” Heated for use Heated for use Taken by IV injection Taken by IV injection

18. 18Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 19Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Methamphetamines  Other adverse effects  Tolerance, dependence, and withdrawal  Treatment  Bupropion (Wellbutrin, Zyban)  Modafinil (Provigil, Alertec)

20. 20Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 21Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Marijuana  Psychoactive substance  Delta-9-tetrahydrocannabinol (THC)  Routes  Smoking 60% of THC content absorbed, effects begin in minutes and peak within 20–30 minutes 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 Majority of THC is inactivated by first-pass effect

22. 22Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Marijuana  Increased production of prostaglandin E 2  Behaviors Euphoria Euphoria Sedation Sedation Hallucinations Hallucinations  Therapeutic uses Antiemetic Antiemetic Appetite stimulant Appetite stimulant Neuropathic pain Neuropathic pain

23. 23Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Marijuana  Effects  Low to moderate dose  High dose  Long-term use

24. 24Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 25Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Marijuana  Reproduction  Males and females affected  Altered brain structure  Hippocampal volume left hemisphere  Tolerance and dependence

26. 26Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Therapeutic Use Marijuana  Approved uses for cannabinoids  Unapproved uses for cannabinoids  Medical research on marijuana  Legal status of medical marijuana

27. 27Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 28Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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 Thinking Feelings Feelings Perception Perception Relationship to environment Relationship to environment

29. 29Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 30Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 31Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Dissociative Drugs  Phencyclidine (PCP)  Effects Low to moderate doses, high doses Low to moderate doses, high doses  Toxicity  Ketamine  Similar to PCP in structure, mechanism, and effects  Shorter duration of effects

32. 32Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 33Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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 Low doses: mild LSD-like psychologic effects Higher doses: amphetamine-like effects Higher doses: amphetamine-like effects  Promotes release of neurotransmitters  Usually taken orally; also snorted, injected, or taken by rectal suppository

34. 34Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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. 35Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Inhalants  Term can refer to many drugs; common characteristic is administration by inhalation  Anesthetics  Volatile nitrites  Organic solvents

36. 36Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 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