CNS ACTIVE NARCOTIC DERIVATIVE COMPOUNDS

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CNS ACTIVE NARCOTIC DERIVATIVE COMPOUNDS

• --CLASS
• SLS 1125
• --PROFFESSOR
• TERE SUAREZ
• --STUDENT
• BY INAMAI MAILE

• THIS PRESENTATION IS PRESENTED IN PART BY INAMAI
  MAILE AND WITH PERMISSION FROM WALGREENS, CVS,
  AND OTHER PHARMACEUTICAL PROVIDERS.

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OPIUM(papaver somniferum)flower of sleep
Opiums useful properties have been known for
centuries. It is believed that ancient
civilizations in Egypt and Greece used opium for
its euphoric effects. During the 1800s, laudanum
(opium dissolved in alcohol) and other opium
products were used in Great Britain and America
to treat various ailments, from teething soreness
in babies to fever and cough in children and
adults. The milky liquid from the opium poppy
plant seed pods is extracted and dried to form
opium powder. Various alkaloids from this powder
can be isolated to form opioids such as morphine,
codeine and oxycodone. The alkaloid in oxycodone
is thebaine
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Endogenous Opiates(our natural opiates)

• ENDORPHINS
• They are up to many times more potent than any
  other opiate or opioid.
• Endorphins are natural pain killing substances
  found in the human brain.
• The name comes from
• ENDOgenous (meaning within) and moRPHINe
  (morphine being a pain killer)
• ENDORPHIN. Endorphins are one of the
  neurotransmitters in the brain. Levels of
  endorphins in the brain may be changed by taking
  a number of drugs including alcohol, anabolic
  steroids and heroin and other opiates.
  Electro-acupuncture and binaural sound have been
  used to stimulate the production of endorphins . 
• Every time, or most of the time you go and eat
  something that pleases you very much, have great
  sex (orgasm), or smoke a cigarette (or any form
  of tobacco) your body will release endorphins and
  another neuro-chemical dopamine. These are the
  chemicals that make you feel exhilarated. You
  also get a quick surge of energy (a high) as the
  sugar hits your bloodstream and stimulates an
  area in the brain simply called the reward
  center for obvious reasons.
•  

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CR/ER controlled/extended release tablet abuse.
i.e. ( Oxycontin )

• When abused these CR/ER
• opiates and
• opioids,
• can be dangerously addictive. Rather than
  ingesting the pill as indicated, people who abuse
  OxyContin use other methods of administering the
  drug. To avoid the controlled-release mechanism,
  they either chew, snort or inject the medication
  to get an instant and intense "high." Frequent
  and repeated use of the drug can cause the user
  to develop a tolerance to its effects, so larger
  doses are required to elicit the desired
  sensation and the abuser gets increasingly
  addicted to the drug.

• Opiate opiate
• (plural opiates)
•  
• opium containing drug a drug such as morphine
  or heroin that contains opium or an opium
  derivative
• Opioid opioid
• (plural opioids)
• possessing some properties characteristic of
  opiate narcotics but not derived from opium
• 160mg
• Oxycontin
• tablet

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Morphine/ analogues

• morphine the standard for which all opiates are
  referenced

• From Vicodin to Dilaudid

Below is an opiate antagonist notice how close
it resembles morphine.
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Natural occurring (opioids)(opium alkaloids
opioids)
OPIUM POPPY
Morphine
Codeine
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Semi-Synthetics (opioids)
HYDROCODONE CIII VICODIN
DIACYTYLMORPHINE SULFATE/HCl CI HEROIN
CI ILLEGAL/ NO MEDICAL USE IN U.S. CII HIGH
POTENTIAL FOR ABUSE/DIVERSION CIII MODERATE
ADDICTION / ABUSE POTENTIAL DIVERSION CIV LOW
TO MODERATE
HYDROMORPHONE/ OXYMORPHONE CII DILAUDID
NUMORPHAN
OXYCODONE CII PERCOCET
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FULL SYNTHETICS (OPIATES)
DEMEROL MEPERIDINE HCl
DARVON CIV PROPOXYPHENE
ACTIQ CII FENTANYL CITRATE
INAMAI MAILE SLS 1125
DOLOPHINE CII METHADONE
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A Little Background
Most opiates are agonist opioids. These are some
of the most effective pain relievers available.
Unlike other analgesics, opioid agonists have an
increasing analgesic effect with increased doses.
Meaning that the more you take, the better you
feel. Other non opioid analgesics, like
-(aspirin) BAYER or Bayer company
origianally synthesized Heroin as an alternative
to morphine thinking it would be a non-addictive
substitute, they were wrong, it is 3 times as
strong as morphine. It was sold over the counter
until right after the 1900s when they started
seeing the first addicts in the
us. -(acetaminophen) TYLENOL, have a
threshold to their effectiveness which means you
can only take so much until it is no longer
effective for your pain. This is why chronic pain
patients use medications like OxyContin for
such chronic pain conditions like Cancer, Lupus,
etc. Once opioid agonists enters the body, it
works by stimulating certain opioid receptors
that are located throughout the central nervous
system, in the brain and along the spinal cord.
When the oxycodone binds to the opioid receptors,
a variety of physiologic responses can occur,
ranging from pain relief to slowed breathing to
euphoria, which is a false sense of well being or
a high.
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In historyOh how wrong we were
Above is tax stamp for morphine and or heroin and
to the right is a poster for Glyco-Heroin,
which was used by our forefathers in the early to
late 19th century, and sold over the counter just
like Robitussin is sold today.
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New Drug or Mixtures under study

• Purdue Pharma, L.P.
• Palladone TM
• NEWS-On January of this year
• The Food and Drug Administration (FDA) has
  approved Palladone
• (hydromorphone hydrochloride) capsules for the
  management of
• persistent moderate to severe pain in patients
  extended 24 hour opiate relief
• Other names for hydromorphone
• (street k4, k8, sliders) (pharmacyDilaudid by
  Knoll pharmaceuticals)
• Availability 12 mg, 16 mg, 24 mg, 32mg
• (hydromorphone hydrochloride extended-release)
  Capsules as of 11/04

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• Purdue Pharma Issues Correction of Erroneous News
  Reports on Palladone (hydromorphone HCl
  extended-release) Capsules (CII)
• Stamford, CT - September 29, 2004 - Some media
  reports on the U.S. Food and Drug
  Administration's approval of Purdue Pharma L.P.'s
  Palladone (hydromorphone HCl extended-release)
  Capsules (CII) erroneously implied that Purdue
  stated that Palladone has a time-release
  function that should make it more difficult,
  though not impossible, to misuse. Purdue Pharma
  did not say, and does not claim, that Palladone
  is abuse-resistant or more difficult to misuse.
  Palladone contains the potent Schedule II opioid
  agonist, hydromorphone. Schedule II opioid
  agonists (which include hydromorphone, fentanyl,
  methadone, morphine, oxycodone, and oxymorphone)
  have the highest potential for abuse.
• The professional prescribing information for
  Palladone Capsules contains the following boxed
  warning
• FOR USE IN OPIOID-TOLERANT PATIENTS ONLY

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Pros and Cons to Weigh

• PRO----------------------
• BLOCKS PAIN FOR PEOPLE FROM CHRONIC BACK PAIN TO
  SEVERE CANCER
• NARCOTICS HAVE A PLACE IN MEDICINE, A VERY
  IMPORTANT PLACE
• IF USED AS PRESCRIBED FOR REAL PAIN, DEPENDENCE
  ON THE OPIATE USUALLY DOES NOT OCCUR.

• CON----------------------
• FROM NORMAL TO ADDICT IN WEEKS, SOMETIMES WITHOUT
  KNOWING IT.
• SOMETIMES DIVERTED AND OVERPRESCRIBED OR STOLEN
  AND ABUSED
• YOU, I, YOUR LAWER, DOCTOR, MOTHER, CAN BECOME
  ADDICTED. AND OFTEN DO, WHEN NOT USED AS
  PRESCRIBED OR ILLICITLY.

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Localization of opiate binding sites When a
person injects heroin or morphine, it too,
travels quickly to the brain. Point to the areas
where opiates concentrate. The VTA, nucleus
accumbens, caudate nucleus and thalamus are
highlighted. The opiates bind to opiate receptors
that are concentrated in areas within the reward
system. Indicate that the action of opiates in
the thalamus contributes to their ability to
produce analgesia.
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Opiates binding to opiate receptors in the
nucleus accumbens increased dopamine
release Show how opiates activiate the reward
system using the nucleus accumbens as an example.
Explain that the action is a little more
complicated than cocaine's because more than two
neurons are involved. Point out that 3 neurons
participate in opiate action the dopamine
terminal, another terminal (on the right)
containing a different neurotransmitter (probably
GABA for those that would like to know), and the
post-synaptic cell containing dopamine receptors.
Show that opiates bind to opiate receptors
(green) on the neighboring terminal and this
sends a signal to the dopamine terminal to
release more dopamine.
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Increased cAMP produced in post-synaptic cell In
a closer view, again, show how this affects the
function of the post-synaptic cell. Since there
is more dopamine released, there is increased
activation of dopamine receptors, similar to the
effect of cocaine. This causes increased
production of cAMP inside the post-synaptic cell
which alters the normal activity of the neuron.
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Slide 20 Summary opiate binding in nucleus
accumbens and activation of the reward
pathway Show the "big picture". As a result of
opiate actions in the nucleus accumbens (point to
the sprinkles of opiates in the nuc. acc.), there
are increased impulses leaving the nucleus
accumbens to activate the reward system (point to
the frontal cortex). As with cocaine, continued
use of opiates makes the body rely on the
presence of the drug to maintain rewarding
feelings and other normal behaviors. The person
is no longer able to feel the benefits of natural
rewards (food, water, sex) and can't function
normally without the drug present.
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TREATMENTS ARE ACTUALLY OPIATES OR CLOSELY
RESEMBLE OPIATES THEMSELVES

• Naloxone Buprenex Methadone
• Antagonist Mixed ant/ago Agonist

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Dolophine(methadone HCl)how it came to be.
Dolophine

• During World War II, the Nazis needed a
  substitute for morphine because they had lost
  control of the primary opium-producing countries.
  This resulted in the development of methadone--a
  purely synthetic opioid.
• Methadone is also known as "Dolophine". This has
  been taken to mean that the drug was named after
  Adolf Hitler. It is a stretch, however Adoloph.
  There are clearly a couple of problems with this
  connection. First, Hitler's first name is
  "Adolf", not "Adoloph". Second, methadone wasn't
  even called Dolophine until it was brought to the
  United States--after the war was over and Hitler
  was long dead.
• The name "Dolophine", rather than being any kind
  of homage to the führer, seems to be derived from
  the Latin word "dolor" which means pain.

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Summary

• Opioid Narcotic pain reliever derived from
  opium.
• Opiate - Narcotic pain reliever not from opium.
• Agonist Pain releiver (narcotic-opiate/opioid )
• Antagonist Drug used to reverse the action of
  an agonist
• Mixed Agonist/antagonist Drug that has some
  opiate qualities but also blocks euphoria or a
  high and lowers addiction potential.
• There are 3 types of Narcotic drugs
• Natural made completely or isolated from opium.
  
• (Morphine, Codeine and, Thebaine - a precursor
  for semi-synthetics)
• Semi-synthetic made in the laboratory via
  synthesis of natural and man made, or
  petro-chemicals.
• ( Vicodin , Dilaudid / Pallidone )
• Synthetic Completely synthesized in a
  laboratory from raw materials, man made.
• ( Demerol, Methadone, and Fentanyl )

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