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Opiates

Opiates. 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. Gould’s Medical dictionary. Source.

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Opiates

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  1. Opiates

  2. 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. • Gould’s Medical dictionary

  3. 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

  4. 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

  5. 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

  6. Opium derivatives • Opium • Morphine • Codeine • Thebaine

  7. Semi – Synthetic Derivatives • Heroin – diacetylmorphine • Eythylmorphine –Dionine • Dihydrocodeine – Paracodin • Hydromorpone – Dilaudid • Dihydrocodeinone – Kycodan • Oxycodone - Percodan

  8. Synthetics • Meperidine – Demorol • Methadone – Methadon, Dolophine

  9. 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

  10. 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

  11. 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

  12. 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

  13. 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

  14. 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”

  15. 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

  16. Current use includes upper – middle class use with purity of heroin increasing (40 to 60 %)

  17. Effects of Opium Derivatives • Primarily an analgesic • Constricted pupils, DRE • Depressed respiration • Constipation • Nausea • Drowsiness • Euphoria

  18. Apathy • Decreased sexual drive • Tolerance • Physical dependency

  19. Dosage form and use (heroin) • White powder • Brown powder • Black tar – smoked • Snorted • Injected • Skin popping • Smoked

  20. 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

  21. Narcotic antagonists (Naloxone) can reverse overdoses

  22. Mechanism of Action • 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

  23. Dependence Potential • Tolerance develops with narcotic drugs • Psychological dependence • Behavior reinforcement of needle usage

  24. Withdrawal • Peaks in 24 to 36 hours • Lasts 3 to 5 days • Tearing of the eyes • Runny nose • Sweating • Dilated pupils

  25. Loss of appetite • Gooseflesh “Cold Turkey” • Restlessness • Irritability • Tremor, convulsions • Insomnia

  26. Depression • Nausea and vomiting • Cramps and diarrhea • Muscle spasms – Kicking the habit

  27. Toxicity Potential • Acute toxicity effects, • Respiration • Decreased mental ability • Nausea/vomiting

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

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

  30. Questions?

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