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

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Presentation on theme: "Uppers, Downers & All Arounders Chapter 4 Downers: Opiates/Opioids & Sedative-Hypnotics."— Presentation transcript:

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

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

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

6 General Classification II.Minor Depressants 1. Over-the-counter downers a.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 20 th century –Nonmedical use declared illegal at beginning of 20 th 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 ( 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 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


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