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Opium Poppy. Opium Poppy: Papaver somniferum. Member of the Papaveraceae, poppy family Large showy annual with conspicuous flowers (white, pink, red, purple) Fruit is a capsule that produces latex with several potent alkaloids

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opium poppy papaver somniferum
Opium Poppy: Papaver somniferum
  • Member of the Papaveraceae, poppy family
  • Large showy annual with conspicuous flowers (white, pink, red, purple)
  • Fruit is a capsule that produces latex with several potent alkaloids
  • Latex is collected from cut capsules (latex oozes out and dries – dried latex scraped off) - dried latex called opium
slide4

Fresh capsule of opium poppy

Cut capsule showing latex exuding from cut

opium poppy5
Opium Poppy
  • Native to the Mediterranean area
  • Oldest evidence of poppy use was existence of a poppy capsule found with religious artifacts from a cave in Spain that are dated 7500 years old
  • Evidence of spread in Europe from 3000 to 5000 years ago
  • Reasons for use at these sites unknown
ancient medical use
Ancient medical use
  • Poppy was revered by several ancient societies for its analgesic properties and its ability to induce sleep
  • Opium latex has a long history of use for pain relieve and inducing sleep among Babylonia, Egyptian, Greek, and Roman civilizations
    • Opium eaten, drunk, and smoked
    • Most common method was to dissolve opium in alcohol – opium wine
mediterranean societies
Mediterranean societies
  • Writings of Hippocrates, Theophrastus, Dioscorides, and Galen show evidence of the widespread use of opium
  • In eastern Mediterranean it seems that poppy also became valued for its narcotic use
  • Ancient goddess of Crete is depicted wearing a crown with 3 poppy capsules
opium alkaloids
Opium Alkaloids
  • Many alkaloids have been identified in opium latex (opiates) - maybe as many as 50
  • Morphine and codeine most important
  • Morphine first alkaloid identified from any plant in 1806 and the pain relieving properties soon recognized
  • Morphine (like raw opium) is strongly addictive and because of this its general medical use declined in 20th century
  • Still drug of choice for cases of severe pain
morphine
Morphine
  • Morphine affects the central nervous system but also induces drowsiness and can depress respiration - overdose can cause death through respiratory failure
  • Cause has high physical dependency
  • Has relatively low oral activity
  • Became drug of choice to treat war injuries during Civil War - created many addicts
codeine
Codeine
  • Codeine most widely used opiate
  • Only 1/5 as strong as morphine and still addictive
  • Effective in oral medication and often used in combination with non-opiate compounds
  • Codeine is especially effective in cough syrups because it suppresses the coughing reflex
heroin
Heroin
  • In 1898, Bayer Pharmaceuticals introduced heroin which they thought was a non-addictive opiate and more effective than morphine and codeine
  • Heroin is a semi-synthetic derivative of morphine - diacetyl morphine
  • Widely available in over the counter tonics and cough syrups from 1898 to 1914 - mail order catalogs, etc
heroin13
Heroin
  • Within a few years over 1 million people addicted to heroin in US alone
  • Soon realized that it was actually more addictive than morphine - actually six times more addictive
  • In US use of heroin is illegal placed under Harrison Act of 1914
  • Heroin still used medicinally in other countries
  • Heroin addiction a major problem worldwide
mode of action
Mode of action
  • Opiates bind to opiate receptors in membrane of neurons of the brain and spinal column (ID’d in 1970s)
  • The natural ligands that normally bind to these receptors are endorphins and enkephalins (small peptides)
  • These peptides are released at synapses on neurons involved in transmitting pain signals to the brain
opiate receptors
Opiate receptors
  • When enkephalins bind to the opiate receptors they inhibit neurons from transmitting pain signal - pain signal does not reach brain
  • Inhibit release of neurotransmitter “Substance P”
  • Substance P used by the sensory neurons involved in the perception of chronic and/or intense pain
opiate receptors19
Opiate receptors
  • Peptides and receptors form a complex neurotransmitter system that plays a major role in controlling pain, euphoria, and motivation
  • Also involved in other biological events - stress responses, immune regulation, respiration, endocrine responses
  • Different classes of opiate receptors
opiate receptors20
Opiate receptors
  • Three (or 4) classes of opiate receptors - with subtypes of each
  • Opioids exert their effects by activating one or more of these receptors
  • Pain relief involves activation of one type receptors in the brain and another in the spinal cord
  • Other receptors are are involved in respiratory depression and euphoria
opiate receptors21
Opiate receptors
  • m (mu) receptors - analgesia, euphoria
  • k (kappa) receptors - sedation, spinal cord analgesia
  • d (delta) receptors - Antitussive (coughing) properties, emesis (vomiting), and anticholinergic (constipation)
  • sigma (?) receptors cardiac stimulation
opiates22
Opiates
  • Morphine and the other opiates bind these same receptors
  • Morphine especially binds to m receptors
  • Explains why opiates are excellent pain killers
  • However, they are also highly addictive