Uppers, Downers

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Uppers, Downers All Arounders

• Chapter 4
• Downers Opiates/Opioids
• Sedative-Hypnotics

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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

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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)

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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

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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

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Opiates/Opioids

• Oldest and best-domented of psychoactive drugs
• Discovery of neurotransmitters/own bodys natural
  painkillers
• endorphins enkephalins changed scientists
  understanding of opiates/opioids
• field of addiction

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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

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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)

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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

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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

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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

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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. 145147)
• Picture of Mexican tar heroin.
• Tar heroin is most prevalent in the western
  United States. It is often 4080 pure but also
  has more plant impurities. A small chunk the size
  of a match (25 doses) sells for 2025. It
  dissolves easily in water for injection. (p.
  146).

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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 thats enough, thereby
  reinforcing the desire to continue to use

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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

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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

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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

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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

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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

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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

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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

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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

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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

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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

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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 Xs as strong as
  morphine)
• Used right after surgery for severe pain

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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

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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

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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 1850s used for
  sedation and hypnotic

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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

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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

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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

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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)

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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

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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

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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

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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

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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

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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