Transcript Opiates - Southeast Missouri State University

Opiates
Narcotics
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A drug that in therapeutic doses
diminishes sensibility, relieves pain, and
produces sleep, but in large doses causes
stupor, coma or convulsions; any drug
with properties similar to morphine,
identified as a narcotic drug by federal
law.
Gould’s Medical dictionary
Source
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Opium poppy
Papaver somniferum L
Papaver – Greek for poppy
Somniferum – Latin – to dream or sleep
Grows in India, Turkey, China, Mexico, SW
Asia, Afghanistan
Harvest
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Petals fall from the opium seed pod
Approximately two weeks later unripe
pods are incised
Opium oozes out and dries in about 24
hours
Then collected by hand
Yields
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Four kilos of opium per acre
80 mgs per plant
10 kilos of opium yield about 1 kilo of
morphine and morphine to heroin is a 1 to
1 conversion
Opium derivatives
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Opium
Morphine
Codeine
Thebaine
Semi – Synthetic Derivatives
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Heroin – diacetylmorphine
Eythylmorphine –Dionine
Dihydrocodeine – Paracodin
Hydromorpone – Dilaudid
Dihydrocodeinone – Kycodan
Oxycodone - Percodan
Synthetics
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Meperidine – Demorol
Methadone – Methadon, Dolophine
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Earliest recorded use of opiates, circa
1500 BC in the Ebers papyrus
Pharmacology book (Biruni 1000 AD)
describing opiate dependence
Early 16th century, Paracelsus created
laudanum, a mixture of wine and opium
Dr. Thomas Sydenham (The English Hippocrates)
modified laudanum mixture, John Bell Hood
Morphine was isolated by Frederich Serturner in
1806
Codeine (poppy head) was isolated in 1832
English developed trade with China in the 19th
century through the East India Company
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English developed trade with China in the 19th
century through the East India Company
China had the problem of increasing opium
addiction and banned the importation of opium
This lead to the Opium War in 1840 to 1842 in
which England took control of Hong Kong
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1853 the hypodermic needle was invented
U. S. Civil War lead to the “Soldier’s
Disease”
Heroin was transformed in 1874, thought
to be 3X more powerful than morphine
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Influx of Chinese laborers caused an
increase in opium smoking
1890 Heroin was marketed by the
Germans, may be derived from the
German heroisch meaning heroic, dynamic
or powerful
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Opiate abuse developed in the mid-19th
century
Harrison Act in 1914 (drugs secured by a
physician)
WWII heroin use increased in the “lower
classes”
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1960’s saw an increase in the use of
heroin as well as other drugs
Vietnam war created the opportunity for
increased use of heroin among U.S.
military personnel
In the 1970’s “black tar” from Mexico
became available
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Current use includes upper – middle class
use with purity of heroin increasing (40 to
60 %)
Effects of Opium Derivatives
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Primarily an analgesic
Constricted pupils, DRE
Depressed respiration
Constipation
Nausea
Drowsiness
Euphoria
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Apathy
Decreased sexual drive
Tolerance
Physical dependency
Dosage form and use (heroin)
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White powder
Brown powder
Black tar – smoked
Snorted
Injected
Skin popping
Smoked
Chemical Characteristics
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Raw opium contains 10% morphine and
small amounts of codeine
Heroin is produced by the addition of 2
acetyl molecules thus producing
diacetylmorphine
Fentanyl (pain reliever) resulted in
improved anesthesia
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Narcotic antagonists (Naloxone) can
reverse overdoses
Mechanism of Action
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Leu-enkephalin and met–enkephhalin act
like morphine
Endorphins found in brain tissue
Midbrain (pain reception site) interaction
Endorphins are released by the pituitary
and perhaps act in the spinal column but
have an unsubstantiated effect on the
brain
Dependence Potential
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Tolerance develops with narcotic drugs
Psychological dependence
Behavior reinforcement of needle usage
Withdrawal
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Peaks in 24 to 36 hours
Lasts 3 to 5 days
Tearing of the eyes
Runny nose
Sweating
Dilated pupils
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Loss of appetite
Gooseflesh “Cold Turkey”
Restlessness
Irritability
Tremor, convulsions
Insomnia
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Depression
Nausea and vomiting
Cramps and diarrhea
Muscle spasms – Kicking the habit
Toxicity Potential
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Acute toxicity effects,
Respiration
Decreased mental ability
Nausea/vomiting
Chronic Toxicity
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Sores at injection sites
HIV/AIDS
Hepatitis
No long-term change in tissues or organs
Treatment
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Narcotic antagonists
Methadone
LAAM (L-alpha-acetyl-methadol)
Buprenorphine
Heroin/morphine maintenance
Rapid opioid detoxification
Delancy Street
Questions?