Transcript Introduction to opiates - UCLA Brain Research Institute

Opiates
By Neal Deot & Adrina Kocharian
Background on Opiates
 Opiates

derived from poppy
 Some types of Opiates
 Heroin
 Morphine
 Codeine
Background on Opiates
 What are they used for?
 Some are medically
prescribed as a longterm pain killer
 Some are non-
medically used as a
drug to get high
 What primary effect do
they have?
 Analgesia
Krokodil
UCLA Brain Institute Outreach
Introduction to Krokodil
 Consists of Desomorphine
morphine
 Desomorphine is similar to
morphine
 It was intended to be
created as another
prescription pain killer
 Had very potent and severe
effects so it was removed
from market
 In Russia it resurfaced
 Homemade krokodil
desomorphine
Legality
 Schedule 1 Drug
 Absolutely prohibited in the United States
 Controlled internationally under Single
Convention on Narcotic Drugs of 1961
So How Do People Get a Hold of It?
 Krokodil is made from
Codeine, which is legal
 It is cooked and combined
with extremely toxic
chemicals
 Red phosphorous
 Gasoline
 Hydrochloric Acid
 Paint thinner
Effects
Side Effects
High Effects
 Same drug
effects as other
opioids
 Analgesia
 Sedation
 Muscle
Relaxation
 Euphoria
Venous damage and skin and soft issue infections
Rapidly followed by tissue necrosis and
gangrene
Scaly, gray-green dead skin forms
• Thrombosis of major vessels and errosive bleeding
• Large open ulcers, and gangrene
• Respiratory depression
• Skin and soft tissue infections to bone
• Meningitis
• Rotting gums and tooth loss
• Bone infection, decayed structure of jaw and
other facial bones
• Limb rotting
• Pneumonia
• Sepsis
• Coronary artery rupture
• Sores and ulcers on forehead and skull
• Gangrenous wounds
• Speech impediments
• Motor skill impairment
• Rotting ears, nose, and lips
• Liver and kidney injury
Pharmacology
 About 10 times more potent than heroin
 Faster onset so more instant gratification
 Stronger effect than morphine and heroin
 The high typically lasts longer than heroin high
 Hard to know exact details
Mode of Action
dopamine
Inhibitory GABA
NO DOPAMINE IN SYNAPSE
Mode of Action
Inhibitory GABA
Dopamine
Krokodil
DOPAMINE IN SYNAPSE
Effects of Withdrawal
 Physical/ psychological
 Feeling horrible
physical and
psychological pain
 Anxiety
 Increased sensitivity
to pain
 Diarrhea
 Runny nose
Treatment in Addiction
 Antagonist Therapy
N
 Overdoses are
treated with a drug
called Naloxone
which blocks the
receptor to which
desomorphine
binds
 Later, patients are
maintained with
Naltrexone
N
N
Pre-Synaptic Neuron
N
Opioid
Receptor
N
N
Treatment for Addiction
B
 Subsitution Therapy
B
 Given a
medication that
binds to the same
receptor but
induces a milder
effect
 So it’s less harmful
and reduces
horrible withdrawal
= buprenorphine
B
B
Pre-Synaptic Neuron
B
Opioid
Receptor
B
B
Heroin
Background
 Artificially produced from morphine
 Gets into brain FASTER(“the rush”)
 Was used for pain relief but TOO ADDICTIVE
 Is Schedule 1 (MOST ILLEGAL)
Effects
 Extreme euphoric rush (lasts 15-45min)
 Followed by relaxation state (1-3 hours)
 Pain relief
 Cough suppressant
 Constipation

Death
 stop breathing
 dirty needle (HIV)
Mode of Action
 Slows down neuron (brain cell) firing
 Increases dopamine levels
 High + relaxed
 Depressant
Pharmacokinetics
 High begins within 30 min
 Lasts up to 5 hours
 Methods
 Injection (fastest, shortest lasting)
 Crosses blood brain barrier FAST
 Faster onset = more addictive
 Breakdowns into morphine
 Orally (slowest, longest lasting)
 Smoked
 Snorted
Withdrawal
 Strong comedown
 Anxiety and depression
 Dependence
 Receptors are desensitized so you need MORE to feel
high again
Treatment
 Naltroxone
 IMMEDIATE ACTION: prevents overdose
 Kicks morphine off the receptors
 Methadone (substitution)
 longer lasting and less comedown
 Instead of stopping use, it slows it
 Suboxone (substitution)
 feels good if ingested but bad if injected
Relevance

Robert Downey Junior (ex-user)

Philip Seymour Hoffman (death)

Chris Farley (death)