Uppers, Downers & All Arounders

1. Uppers, Downers & All Arounders Chapter 4 Downers: Opiates/Opioids & Sedative-Hypnotics

3. General Classification • Downers induce: • Sedation • Muscle Relaxation • Drowsiness • Coma by depressing the Central Nervous System • Works more on the sites throughout the body than uppers (which generally stimulate the Neurochemicals

4. General Classification • Major Depressants • Opiates/opioids • Used to treat acute pain, diarrhea, coughs and other ailments • Abused for the euphoric affect • For Physical & emotional relief • Suppression of withdrawal effects • Sedative-hypnotics • Synthesized drugs designed to treat anxiety and insomnia • Can cause tissue dependence • Alcohol (Chapter 5)

5. General Classification • Minor Depressants 1.Skeletal muscle relaxants • Synthetically designed to depress areas in the brain responsible for muscle coordination and activity • Prescribed for muscle tension and pain 2. Antihistamines • Synthetic drugs used to treat allergies, ulcers, shock, rashes and motion sickness • Produces drowsiness • Blocks the release of histamine • Can induce depression • Abused for depressant effects

6. General Classification • Minor Depressants 1. Over-the-counter downers • Nytol, Sominex: marked as sleep aids and sedatives 2. Lookalike downers: • Looked like prescription downers • Rarely found, except in magazine ads for legal downers

7. Opiates/Opioids • Oldest and best-domented of psychoactive drugs • Discovery of neurotransmitters/own body’s natural painkillers: • endorphins & enkephalins changed scientists understanding of opiates/opioids • & field of addiction

8. Opiates/Opioids • Opium is processed from milky fluid of the opium poppy plant producing • Morphine, codeine & thebaine • Semi-synthetic opiates include: • Heroin • Vicodin • OxyContin • Percodan • Dilaudid • Fully synthetic opiate-like drugs include • Demerol • Darvon • Methadone • Antagonist that block effects are naloxone & natrexone

9. Opiates/Opioids • Some opioids (opium, morphine, codeine, thebaine) are refined directly from the milk of the opium poppy. Heroin, oxycodone Percodan, OxyContin, Dilaudid) are semisynthetic, which means that a refinement of the opium poppy is manipulated in the laboratory. • Some opioids (e.g., methadone, Demerol, Darvon) are completely synthetic. (p. 142)

10. Opiates/Opioids • History of Use • Used by ancient Sumerians, Egyptians & Chinese as medicine, pleasure and poison • Opium originally chewed, eaten and drunk in liquids • Bitter taste limited addiction • Used throughout Middle Ages • Smoking opium: • increased nonmedical use • Increased intensity of effects • Multiplied its abuse potential • Actively promoted by British in China • Introduced to U.S. by Chinese immigrants

11. Opiates/Opioids • Refinement of Morphine, codeine & heroin from opium increasing its strength • Codeine only 1/5 strength of morphine • Used in cough syrups & other drugs • Heroin was refined from morphine • IV use began in 1853 with invention of hypodermic needle • Patent medicines introduced mid-1880s • Used in tonic • Physician induced addiction was common

12. Opiates/Opioids • Snorting was popular method of taking heroin • More than half of addicts that enter treatment began by snorting • 20th century • Nonmedical use declared illegal at beginning of 20th century • Pur Food and Drug Act 1906 and Harrison Narcotics Act in 1914 • Est. 3.5 million Americans use prescription opiates/opioids monthly • Est 120,00 to 800,000 heroin users in U.S. • 5-10 milion regular users world wide • U.S. consumes only 3% • Afghanistan produces 70% of world supply • China White (Golden Triangle in Asia) • Black Mexican Tar • Colombian cartels

13. HEROIN • Block of refined heroin weighing 1 kilogram. • This block of heroin was processed in the jungles of the Golden Triangle (Myanmar [Burma], Northern Thailand, and Laos) and packaged for easy smuggling. Golden Triangle heroin, known as “China White,” is extremely pure. (pp. 145–147) • Picture of Mexican “tar” heroin. • “Tar” heroin is most prevalent in the western United States. It is often 40–80% pure but also has more plant impurities. A small chunk the size of a match (2–5 doses) sells for $20–25. It dissolves easily in water for injection. (p. 146).

14. Effects of Opioids • Prevents the transmission of Substance “P”. • Painkilling: effects include lower anxiety, serenity, drowsiness and deadening of unwanted emotions • Pleasure: Artificially activate the reward/reinforcement center by slotting into receptor sites meant for endorphions • Heroin has strongest effects of any of the opioids on the reward pathway • Psychoactive drugs disrupts the CUT-OFF switch in the brain that says that’s enough, thereby reinforcing the desire to continue to use

15. Side effects of Opioids • Physical: • Felt in almost every part of body • Noticeable: Droopy eyelids, nodding, slurred speech • Suppression of cough center • Digestive and hormonal • Nausea and constipation • Tolerance: • Occurs when body tries to neutralize heroin • Speeds-up metabolism • Desensitizes nerve cells • Excreting drug from body • Altering the brain and body to compensate of effects of drug • Develops at different rate for different body systems

16. Side effects of Opioids • Tissue Dependence • Adaptation to the effects can alter brain chemistry temporarily or permanently • Body relies on drug to stay normal • Withdrawal • Acute withdrawal occurs 2-3 weeks after abstinence • Protracted or Post Acute Withdrawal (PAWS) can occur for months • Heroin & morphine more severe

17. Side effects of Opioids • Neonatal: Opioids cross the placenta resulting in risk of miscarriage, • placenta separation, • premature labor, • stillbirth, • Seizures • Addiction of infant: withdrawal is severe (death in some cases) • Overdose in older users can be fatal • Severe respiratory depression • Opioid antagonist: Narcan can counteract overdose but victim will still experience severe withdrawal

18. Side effects of Opioids • Dirty/Shared Needles: • Risk of adulteration • Bacteria and viral infections • (Hepatitis C, HIV/AIDS) • 50-90% of IV users carry Hep. C virus • 25% OF HIV/AIDS cases used needles • 10% of AIDS transmitted through sex • 70% of children with HIV from mothers who were IV users or had sexual contact with IV users

19. Side effects of Opioids • Abscesses & other infections • Necrotizing fasciitis • Destroys the fascia & subcutaneous tissues • Endocardistis • Infection of heart valves • Cotton Fever • Endotoxins that thrive in cotton

20. Opioids • Cost: • $20 - $200 daily depending on level of use • 60% of cost through consensual crime • 73% of heroin users are gainfully employed • Polydrug use: • Stop withdrawal symptoms • Speed to get energetic • Mixing drugs • Morphing use of multiple drugs to counter the effects of original drug • Cycling: giving up drug to lower tolerance • Sequential: using one drug then to another drug

21. Morphine & Other Opioids • Morphine: • Refined from opium • Liver converts morphine into metabolites • Can be detected in urine fro several days • Therapeutic pain control • Patient become more sensitive to pain after long-term use because the body produces fewer of its own painkillers • Down regulates opioid receptor sites

22. Morphine & Other Opioids • Codeine • Extracted from opium or refined from morpjine • Analgesic use to control coughs • Most widely prescribed and abused prescription drug • Vicodin now more prescribed (produces less nausea) • Last 3 hours in system • Detectable in urine 2 to 3 days

23. Morphine & Other Opioids • Methadone (Dolophine) • Long-lasting opiod taken to control heroin addiction • 200,000 heroin addicts involved in methadone treatment in 950 clinics • Hydromorphine (Dilaudid) • Short-acting semisynthetic opioid • Prescribed as an alternative to morphine • 7-10 times stronger than morphine • Mixed with cocaine to make speedballs

24. Morphine & Other Opioids • Oxycodone (OxyCondin, Percodan) • Much stronger than codeine, but weaker than morphine or Dilaudid • Time-released version • When crushed, time-release effect destroyed • Meperidine (Demoral, Pethidine, Mepergan) • Most widely used analgesics: 1/6 strength of morphine • Most often abused by medical professionals • Pentazocine (Talwin NX) Opioid antagonist and agonist • When combined with antihistamine gives heroin like high

25. Morphine & Other Opioids • Propoxyphene (Darvon, Darvocet) • Prescribed for mild-moderate pain • Last 4-6 hours • Can be used to detox heroin addicts • Fentanyl (Sublimaze) • Most powerful opioid (50-100 X’s as strong as morphine) • Used right after surgery for severe pain

26. Morphine & Other Opioids • Designer heroin • Street versions of fentanyl • 100-20,000 Xs stronger than regular heroin • Can contain MPTP (street demerol) that destroys dopamine-producing cells that control voluntary muscular movements • Mimics Parkinson Disease • Causes condition called “frozen addict.” • Addict can lose the ability to make any physical movements

27. Morphine & Other Opioids • LAAM • Long lasting opioid used for heroin replacement therapy • Unsuitable for pain management • Naloxone (Narcan) & Natrexone (Revia) • Opioid antagonist that block effects of opioids • Effective in treating overdoses • Revia can be used to treat craving for cocaine and alcohol • Buprenorphine • Power opioid agonist at low doses and antagonist at high doses • Alternative to methadone

28. Sedatives/Hypnotics • 60 million prescriptions written in 2001 • Used for psychiatric medication for depression • Two groups of sedative/hypnotics • Benzodiazeohines • Barbituates • Calming and sleep inducing • Include Bromides introduced in 1850’s used for sedation and hypnotic

29. Sedatives/Hypnotics • Chlora hydrate: sedative or anticonvulsive • Paradehyde: to control alcohol withdrawal • Barbiturates: popular in 1940s and 50s • Low margin of safety • Meprobamate (Miltown) AKA “Mothers little helper” • Benzodiazepines discovered in 1957 • Less toxic than barbituarates

30. Benzodiazepines • Most widely used as: • anti-anxiety drugs, • Sleep aids, • Sedatives • Control seizures • Prescribed for panic attacks • Insomnia • Skeletal muscular spasms • Control seizures • Anesthetic for seizures

31. Benzodiazepines • Non Medical Use: • Often abused with other drugs • To come down off fo methamphetamine, cocaine • Substitute as heroin • To prevent alcohol withdrawal symptoms • Abusers then to be over 30 years, White, weel-educated and female • Neurotransmitter GABA • Converted by live to metabolites more strong that original drug • Tolerance develops as liver becomes more efficient in processing drug • Younger person can tolerate higher doses

32. Benzodiazepines • Tissue Dependence • Addiction develops 10-20 times the normal dosage is taken for several months • Withdrawal • Can be severe • Can involve seizures, convulsions and death • Takes several months to taper off drug • Withdrawal can come in cycles separated from 2-10 days • Symptoms may persist several months (PAWS)

33. Benzodiazepines • Overdose • Takes 700 Xs the therapeutic dose to be lethal • Symptoms include • Drowsiness • Loss of consciousness • Depressed breathing • Coma • Death if left untreated • Rohhyponal (Date Rape Drug) • Memory impairment • 1996 banned in America • Used to sexually assault someone or commit violence

34. Barbiturates • Developed in 1903 • Phenobarbital in 1913 • Effects • Long-acting, intermediate-acting, short-acting • Induce feeling of dis-inhibitory euphoria, similar to alcohol • Effects often depend on the mood of the person and setting

35. Barbiturates • Tolerance • Develops in variety of ways • Dispositional tolerance increase the efficiency of metabolism • Pharmacodynamic tolerance • Reduces nerve cell and tissue sensitivity to the drug • Tissue dependence occurs when 8-10 Xs the dosage is taken daily for 30 days

36. Barbiturates • Withdrawal • Anxiety, • Agitation, • Loss of appetite, • Vomiting • Increased heart rate • Excessive sweating • abdominal cramps • Tremors • Can result in in convulsions within 12 hours to 1 week from last dose

37. Other Sedative/Hypnotics • GHB: • Popular among bodybuilders • Has a similar effect to methaqualone or alcohol intoxication • Popular in rave clubs • Has been used a date rape drug • GBL: • Metabolized to GBH in the body • Also an ingredient in paint strippers • Methaqualone (Quaaludes, Mandrax) • Withdrawn from the market in 1984 • Counterfeit versions on market • Sought for overall sedative effect

38. Other Sedative/Hypnotics • Ethchlorynol (placidyl) • Older sedative-hypnotic “green weenies” • Synergism • Occurs when the combined effects of different drugs are greater on the individual effects • 4,000 deaths & 50,000 hospital emergency room visits per year • Cross-tolerance & Cross-dependence • Development of tolerance to other drugs when addiction of one drug increases liability to using other drugs