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Opiates

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Opiates are natural and synthetic compounds that come from or are copied from ... was 2% or less for fentanyl, hydromorphone, meperidine, methadone, and tramadol. ... – PowerPoint PPT presentation

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Title: Opiates


1
Opiates
  • Chapter 10

2
Opiates/Opioids
  • Opiates
  • alkaloids found in the opium poppy (Papaver
    somniferum)
  • Gk. opion poppy juice
  • Opioids
  • compounds with opiate-like actions, including,
    but not confined to opiates (e.g., synthetic,
    endogenous opioids)

3
Opiates/Opiods
  • Opiates are natural and synthetic compounds that
    come from or are copied from OPIUM the resin of
    the opium poppy
  • Natural Narcotics
  • Opium
  • Extracts Morphine Codeine
  • Semisynthetic Narcotics
  • Slight changes to chemical composition of
    morphine
  • Heroin
  • Synthetic Narcotics - Produce opiate-like
    responses
  • Methadone, Talwin, Darvon, Demerol
  • BUPRENORPHINE Partial agonist

4
History of Opium
  • Native to many regions
  • Middle East in areas bordering Mediterranean
  • Laos, Thailand, Afghanistan
  • Mexico Colombia
  • Use dates back 6000 years to Sumerians
  • Egyptians used it medically 3500 years ago
  • Common use among Islamic peoples for medical
    recreational purposes

5
History of Opium
  • Arab traders took to India China
  • Western Europe learned about it from Arabs during
    crusades
  • 1680 Laudanum Opium tincture (alcohol)
  • Next 200 years, primary consumption of opium is
    as drink
  • 18th century - development of opium smoking in
    China
  • China - first laws against Opium use in 1729
  • Dependence problem recognized

6
Opium the West
  • Western societies
  • Used opium as aspirin
  • Cheaper than liquor
  • No negative public opinion
  • No real problem with cops
  • Used to soothe infants children
  • Teething, colic, or to keep them quiet
  • Females used it more than males
  • Greater addicted

7
Opium and the West
  • Collision of cultures
  • Chinese building railroad
  • 1875 - San Francisco outlawed opium dens opium
    smoking
  • Laws targeted not at opium (laudanum legal), but
    at Chinese
  • Federal laws prohibiting opium smoking
    followed

8
Difference in Opium Use
  • Major difference between opium use in China
    West was method of consumption
  • Laudanum
  • Identified with Victorian Era
  • Opening of respectable parlors
  • Chinese smoked it
  • Identified with Opium Dens
  • Ideal of lazy Chinese
  • Seen as degrading dirty vice

9
Morphine the West
  • 1803 - morphine separated from opium
  • Increased dependence potential
  • Morphine 10 X opium potency
  • Morpheus, the Greek God of dreams
  • 1856 - development of hypodermic needle
  • Use became widespread
  • Doctors began injecting opium solutions (thought
    to sidestep addiction, thought to be purer
    safer )
  • Used during Civil War for injuries (dependency
    known as soldiers disease)

10
Heroin From Bad to Worse
  • In 1874, British chemist altered morphine into
    heroin
  • Unnoticed until rediscovered in 1898 (Bayer)
  • 3-4 X more potent than morphine
  • Thought to be safer than morphine
  • Sold by Bayer - beginning in lieu of codeine as
    medicine for coughs, bronchitis, tuberculosis
  • Heroin also began to replace morphine in addicted
    individuals

11
Opiates in US Early 1900s
  • Harrison Act of 1914
  • No ban on opiates, but doctors had to register
    with IRS
  • Decreased prescriptions
  • Users not seen as victims but as weak
  • Heroin drug of choice in black market
  • Shift of users from women to white urban adult
    males

12
Opiates Use in 1960s
  • Three Major Social Developments
  • Crackdown caused shortage of heroin increased
    smuggling price
  • Increased levels of crime
  • Increased used by urban minorities
  • Drug culture
  • Vietnam War
  • Many veterans came back hooked

13
Opiates Use in 1980 -Today
  • Fentanyl China White
  • Surgical anesthetic prescription painkiller
  • 10 to 10,000 X stronger than heroin
  • Growing illegal market growing deaths
  • Heroin Schedule I
  • Morphine Schedule II
  • Vast majority of therapeutic opiates are
    synthetic
  • Huge illegal market and trade with large
    dependence problem in U.S. and abroad

14
Opiates Today - OxyContin
  • Killers
  • OC
  • OXY
  • Oxycotton
  • Hillbilly Heroin
  • Cotton
  • Blue

15
Non-medical Use
  • Studies indicate that the nonmedical use of
    prescription medications is increasing in the
    U.S. among adolescents and young adults.
  • The nonmedical use of prescription medications is
    associated with higher rates of tobacco, alcohol
    and other drug use
  • 5 of 12 to 17 year olds reported nonmedical use
    of scheduled pain medications
  • 12 of 18 to 25 year olds reported nonmedical use
    of scheduled pain medications.

lifetime
16
Nonmedical Use of Prescription
Medications, Ages 12-25
Percent Using in Past Year
NSDUH, 2005
17
Annual Prevalence by Gender
Monitoring the Future, 2005 12th grade
18
Past Year Nonmedical Use

reporting medical use

  • p chi-square tests Source McCabe, Teter,
    Boyd, 2006

19
Specific Prescription Opioids Used Nonmedically
(Past Year)

The past year use was 2 or less for fentanyl,
hydromorphone, meperidine, methadone, and
tramadol.
SLS, 2005
Source McCabe, Cranford, Boyd Teter,
2007"Addict Behav 2006\7
20
Gender Differences in Motives for nonmedical Use
of Prescription Opioids


SLS, 2005 check all that apply
pSource McCabe Cranford, Boyd Teter, Add
Behaviors, 2007
21
Absorption, Distribution, Metabolism Excretion
  • Most opiates poorly absorbed through GI tract
    (except codeine)
  • Effective nasally and through lungs
  • Opium frequently smoked, heroin snorted
  • Most effective IV (heroin 100 times more potent
    IV than orally)

22
Absorption, distribution excretion
  • In bloodstream, distributed throughout body
  • accumulating in kidney, lung, liver, spleen,
    muscle brain
  • Opiates and blood brain barrier
  • Morphine does not cross BBB well
  • only 20 of circulating enters brain
  • 30-60 min to reach significant brain
    concentrations

23
Absorption, distribution excretion
  • Heroin more lipid soluble, so penetrates BBB
    better
  • - Heroin converted to morphine once it crosses
    the BBB

24
Absorption, distribution excretion
  • All have somewhat different pharmacological
    effects
  • Differ in potency, duration of action oral
    effectiveness
  • Heroin more potent than morphine when injected,
    but same when taken orally

25
Mechanism of Action
  • Act via the endogenous opiate system
  • 1960s - discovery of the opiate antagonist
    naloxone
  • 1973 - discovery of "opiate receptors in brain
  • Led to discovery of several endogenous opiates
    in 1975
  • Endorphin
  • Enkephalin
  • Dynorphin

26
Opioid receptors
  • Subtype
  • Mu (µ)
  • Delta (?)
  • Kappa (?)
  • Subtypes have subtypes

27
Pharmacological Actions
  • Primary sites of action - CNS and GI tract
  • Abuse of opiate use due to
  • Analgesia (best for dull continuous pain, not
    sharp)
  • Due to CNS not PNS effects
  • Euphoria (dream-like state with intense visions)
  • Relieves negative mood states

28
Medical Use
  • Analgesia
  • Sedation - markedly differs between individuals
  • poor sedative in general
  • Anti-diarrheal agents
  • extremely effective for dysentery (1800s)
  • were the only effective agents in that time

29
Analgesia
  • Spinal actions
  • inhibit incoming pain signals

Opioid receptor
12.8
30
Reinforcing effects
  • All classical opioid drugs of abuse have a
    preference for µ sites (e.g., morphine, heroin,
    methadone, fentanyl etc.)
  • µ compounds
  • Increase DA cell firing
  • Increase DA release in NA
  • Kappa compounds have opposite effect
  • Dynorphin likes kappa receptors

31
Side Effects
  • Vomiting
  • very common with first dose
  • Respiratory depression
  • Decrease sensitivity to CO2
  • Occurs at low doses - those common for analgesia
  • Increase dose - increase depression
  • Most common cause of death in overdose
  • Biliary Constriction

32
Side Effects
  • Body temperature
  • Resetting of body temperature thermostat
  • with limited use, lowers temperature by about 1
    degree
  • can persist for a month
  • Sex hormones
  • Inhibited
  • Males - decreased testosterone levels, decreased
    sex drive
  • Females - decreased estrogen

33
Side Effects
  • Cardiovascular effects
  • increased skin blood flow - gives them a warm
    feeling
  • Blood pressure decrease upon standing - faint
  • Pinpoint pupils
  • Signs of overdose
  • Seizures

34
Tolerance Dependence
  • Develops fast with repeated use
  • More rapidly and to greater degree as potency
    increases
  • Constipation and biliary constriction not subject
    to tolerance
  • Cross-tolerance based on receptor affinity
  • Neuroadaptation to numerous brain areas leads to
    dependence

35
Withdrawal
  • Withdrawal - onset related half-life of opiate.
  • 6-8 hrs drug seeking behavior, restless,
    anxious
  • 8-12 hrs Pupils dilated, reactive to light
    increased pulse rate, blood pressure, yawning
    chills rhinorrhea lacrimation gooseflesh
    sweating restless sleep
  • 48-72 hrs (peak) All of the above plus
    muscular weakness, aches (cramps) and twitches
    nausea, vomiting and diarrhea temperature and
    respiration rate elevated heart rate and blood
    pressure elevated dehydration.
  • Withdrawal managed in a number of ways
  • Cold Turkey
  • Medically managed
  • Ultra-rapid Detox

36
Methadone Maintenance
  • Methadone used as a replacement for heroin and
    other opiates in dependent individuals
  • Longer half-life
  • Slower, less intense effects no euphoria
  • Can be taken orally no needles
  • Cheap
  • Blocks heroin effect
  • Methadone withdrawal 24-48 hrs after last dose
  • withdrawal symptoms reported to be less intense
  • however, much greater duration
  • can take months to clear all withdrawal symptoms

37
Buprenorphine
  • Partial Agonist
  • Low levels agonist
  • High levels antagonist
  • Can be managed by physician
  • Taken sublingually every 24-48 hours
  • Can bridge the gap between methadone and nothing
    or used long-term
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