Opiates

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Opiates
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Narcotics

• 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.
• Goulds Medical dictionary

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Source

• Opium poppy
• Papaver somniferum L
• Papaver Greek for poppy
• Somniferum Latin to dream or sleep
• Grows in India, Turkey, China, Mexico, SW Asia,
  Afghanistan

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Harvest

• 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

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Yields

• 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

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Opium derivatives

• Opium
• Morphine
• Codeine
• Thebaine

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Semi Synthetic Derivatives

• Heroin diacetylmorphine
• Eythylmorphine Dionine
• Dihydrocodeine Paracodin
• Hydromorpone Dilaudid
• Dihydrocodeinone Kycodan
• Oxycodone - Percodan

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Synthetics

• 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

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• 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 Soldiers 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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• 1960s 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 1970s 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 )

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Effects of Opium Derivatives

• Primarily an analgesic
• Constricted pupils, DRE
• Depressed respiration
• Constipation
• Nausea
• Drowsiness
• Euphoria

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• Apathy
• Decreased sexual drive
• Tolerance
• Physical dependency

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Dosage form and use (heroin)

• White powder
• Brown powder
• Black tar smoked
• Snorted
• Injected
• Skin popping
• Smoked

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Chemical Characteristics

• 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

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Mechanism of Action

• Leu-enkephalin and metenkephhalin 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

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Dependence Potential

• Tolerance develops with narcotic drugs
• Psychological dependence
• Behavior reinforcement of needle usage

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Withdrawal

• 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

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Toxicity Potential

• Acute toxicity effects,
• Respiration
• Decreased mental ability
• Nausea/vomiting

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Chronic Toxicity

• Sores at injection sites
• HIV/AIDS
• Hepatitis
• No long-term change in tissues or organs

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Treatment

• Narcotic antagonists
• Methadone
• LAAM (L-alpha-acetyl-methadol)
• Buprenorphine
• Heroin/morphine maintenance
• Rapid opioid detoxification
• Delancy Street

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Questions?