What are the three Opiates?
MORPHINE, CODEINE, THEBAINE
What are the 4 Opiate Derivatives?
HEROIN, NUMOPRHAN, PERCODAN, HYDOCAN
What are the 5 Synthetic Opiates?
METHADONE, DEMEROL, DARVON, LAAM, BUPRENORPHINE
What are the acute effects of Heroin?
Almost immediate tingling sensation and a sudden feeling off warmth in lower abdomen ( when injected- MAINLINE)
Intense Euphoria
Subsequent tranquil drowsiness (uncontrollable- its like they all of a sudden lose consciousness)
Diminishment of sexual desire
What are the symptoms of Heroin Withdrawal?
Elevated body temperature
Increased blood pressure
GOOSEBUMPS (piloerection)
Tearing-Runny Nose
Diarrhea
Yawning, panting, sneezing
Spontaneous ejaculations and orgasms
Restlessness, involuntary kicking movements (basal ganglia problems)
Insomnia
Pain and Irritability
Depression and Anxiety
In 1914 the Harrison Act was made- What is it?
Morphine and Heroin were made illegal because the soldiers were getting addicted to it during the civil war.
What happened in 1803?
Friedrich W. A. Sertuner identifies morphine as the active ingredient in opium
During the mid 1900’s the principle supplier of Heroin shifted from Asia to where?
South America
Who makes 90% of the worlds Opium?
Afghanistan
How do you prepare Opium for use?
Boil
The Akaloids Dissole
Strain
Evaporate them through boiling (dehydrate them)
Paste Remains - whatever the weight of the paste is , will be sold to the Cartel, who will then turn it into heroin
Opium -to- Heroin
Extracting Morphine:
Dissolve the opium in boiling water
Precipitate other alkaloids (over 35 different)
Pour off solution containing morphine
add ammonium chloride to morphine solution
Heat to precipitate morphine
and you end up with Morphine base = Heroin Number 1 (dark brown chunks)
From Morphine to Heroin
Heroin Number 2 (heroin base)
Acetylation of Morphine add acetic acid to morphine chunks heat 2 hrs at 85 degrees Celsius Cool, dissolve in water, add sodium carbonate
NOTE: acetylation increases lipid solubility and passage into brain
Your basically just adding acetic acid to morphine and you get heroin after heating it cooling it and adding sodium carbonate
What is Heroin Number 1?
Morphine Base
What is Heroin Number 2
Heroin Base
What is Heroin Number 3?
For Smoking
What is Heroin Number 4?
For Injecting
What is Black Tar?
A New Form of Heroin found in the 1980’s
relatively pure and inexpensive (purity can vary not always pure)
From Mexico and illegal drug laboratories in the United States
What is Fetanyl?
A new form of Heroin found in the 1980s
a prescription narcotic drug, 10 to 1000 x stronger than regular heroin (powerful narcotic effect- alleviates and calms)- strongly analgesic, reduces pain
Chine White - Heroin Number 4 (snort, inject, smoke)
Who is Lou Reed?
He made a song about Heroin. He said he was married to the drug, Heroin is your wife, your life, its your lover, and being without it means your lost
Mechanisms of Action-
In the 1970’s there were early clues that brainthat endogenous opioids- that there were receptors for opiates in the brain.
Electrical stimulation of the brain led to less pain sensitivity (i.e. analgesia)
Displaceable binding of morphine to brain tissue- It binded to the brain because there is an actual receptors there for morphine. A receptor that binds with morphine- this means that our body must make morphine which led to the discovery of Endoprhines- Enkephlans- and Dynorphin- which are now known as our Opioid Peptides
What are the Four Opiate Receptors ?
Mu, Delta, Kappa, Sigma
What is Mu and what is it named after?
Mu is the first opiate receptor to be discovered. It is named after Morphine.
It is bound by morphine . Morphine was binding the the Mu receptors
ACTIONS OF HEROIN….
Heroin enters the brain (acts fairly quickly- instantaneous reaction)
Enzymes remove acetyl groups ( CONVERTS BACK INTO MORPHINE)
Back to morphine
Binds to Mu Receptors ( receptors are really for the endorphines however morphine can bind to them)
Effects: POSITIVE FEELINGS- ANALGESIA
What are the four Opioid Peptides?
Enkepphalin, Beta-Endorphin, Dynorphin, and Endomorphins
ENKEPHALIN
Opioid Peptide- was the first one discovered
Greatest affinity for Delta (receptor)
BETA- ENDORPHIN
Opioid Peptide
Binds Mu and Delta Equally
DYNORPHIN
Opioid Peptide
Kappa receptors -when stimulates can reduce Dopamine in the Nucleus accumbens
Endomorphins
Newest Discovery of Opioid Peptides
Greatest affinity for Mu
During withdrawal… what happens when we overstimulate our Kappa Receptors?
Overstimulating our Kappa Receptors reduces Dopamine in our Nucleus accumbens and leads to going to get that 1 hit.
What are the function of Opioid Peptides?
They are distributed in the emotional areas of the brain, and throughout the spinal cord (major portal of entry for any physical stimulation (pain etc))
Their functions include: Regulation of emotion, Modulation of Memory, and Analgeisa
Buprenorphine- Naloxone
Reduces craving of Opiates- allows person to go through desensitization process without cravings or less cravings