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Questions and Answers
Which compound accounts for the highest percentage of raw opium?
Which compound accounts for the highest percentage of raw opium?
Which of the following statements about naturally occurring opioids is true?
Which of the following statements about naturally occurring opioids is true?
What is the source of naturally occurring opioids?
What is the source of naturally occurring opioids?
How is the term 'narcotic' most accurately defined in relation to opioids?
How is the term 'narcotic' most accurately defined in relation to opioids?
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Which of the following is NOT considered an opioid?
Which of the following is NOT considered an opioid?
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What is the primary use of opioids in medical practice?
What is the primary use of opioids in medical practice?
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Which of the following compounds is most abundant in raw opium?
Which of the following compounds is most abundant in raw opium?
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What distinguishes naturally occurring opioids from synthetic compounds?
What distinguishes naturally occurring opioids from synthetic compounds?
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Which of the following is NOT a major compound derived from the opium poppy?
Which of the following is NOT a major compound derived from the opium poppy?
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What percentage range of raw opium does codeine typically account for?
What percentage range of raw opium does codeine typically account for?
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What are opioids primarily used for?
What are opioids primarily used for?
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Which of the following is a naturally occurring opioid derived from the opium poppy?
Which of the following is a naturally occurring opioid derived from the opium poppy?
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Which statement differentiates naturally occurring opioids from synthetic ones?
Which statement differentiates naturally occurring opioids from synthetic ones?
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What is the sap extracted from the opium poppy known as?
What is the sap extracted from the opium poppy known as?
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Which opioid compound is most significant in terms of its percentage content in raw opium?
Which opioid compound is most significant in terms of its percentage content in raw opium?
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Study Notes
Learning Outcomes for Opiates
- Opiates are discussed in Chapter 11 of the text
- Includes historical use, names of common natural and synthetic opiates
- Details potency, metabolism, medical uses, administration methods, pharmacological actions, effects of tolerance, withdrawal, and psychological dependence. Methadone use for treatment is included.
Opioids Overview
- Opioids are a class of naturally occurring, derived, and synthetic compounds with analgesic properties.
- Often referred to as narcotic analgesics, though this term can be confusing as it includes other dissimilar drugs.
Naturally Occurring Opioids
- Sources are derived from the opium poppy (Papaver somniferum).
- Opium is the sap extracted from the seedpods.
- Major compounds include:
- Morphine (10% of raw opium)
- Codeine (0.75-2.5% of raw opium).
- Thebaine (<1% of raw opium)
- Opium extraction:
- Incisions are made in the seedpod after the petals fall
- Milky white juice (raw opium) oozes out.
- The juice oxidizes to reddish-brown tar-like balls.
- The balls have a smell similar to new-mown hay.
- Opium production lasts for 10 days after the petals drop.
Opiate Derivatives/Semi-Synthetics
- Heroin: Derived from morphine, 3x more potent, and more lipid-soluble, increasing its ability to cross the blood-brain barrier.
- Other derivatives include:
- Hydromorphone (10x more potent than morphine)
- Oxycodone (commonly prescribed for pain)
- Oxymorphone (1.5x more potent than morphine)
- Hydrocodone (slightly more potent than morphine)
Synthetic Opioids
- Meperidine (Demerol): A less potent synthetic opioid, often used as a painkiller.
- Methadone: Used to treat chronic pain and opioid dependency, with similar analgesic effects to morphine but less euphoria. Methadone is used in opioid maintenance programs for individuals recovering from heroin addiction.
- Fentanyl: A potent synthetic opioid available in several forms (e.g., oral transmucosal lozenges, sublingual tablets, nasal sprays, transdermal patches).
Opiate Antagonists
- Naloxone (Brand Name: Narcan): Can reverse opioid effects, especially respiratory depression, within minutes. Administered intravenously (IV) or intramuscularly (IM).
- Naltrexone: Has mild agonist effects resembling morphine-like activity, but can last longer than Naloxone. Primarily used in opioid addiction treatment.
Medical Uses of Opioids
- Pain relief (morphine is a key agent)
- Diarrhea treatment (loperamide)
- Cough suppression (codeine)
Opioids: Historical Medical Uses
- Opium was documented in Egyptian medical scrolls (Ebers Papyrus) in 1550 BC.
- Used for various conditions, including excessive crying in children.
- Galen (Greek physician) prescribed opium for multiple conditions.
Opioids: Historical Recreational Uses
- Opium use dates back to the Bronze Age.
- Widespread availability of opium cakes and candy was evident by the 2nd Century AD.
- Opium smoking became widespread in the 18th century (China) resulting in the rise of opium dens.
- Opium dens emerged globally offering specialized pipes, lamps, and paraphernalia for smoking. Opium dens catered to all social classes, with more luxurious dens for wealthier patrons.
Opioids: Historical Regulation and Social Perception
- Opium was widely accepted for medical and recreational use in the early to mid-1800s.
- Addiction issues were not viewed as a predominant medical or social problem.
- Increased regulation began in the U.S and Britain in the mid to late 1800s due to concerns about chronic use and anti-Chinese prejudice linked to opium dens. Regulation was driven by a combination of public health concerns, social perception shifts, and political considerations.
Opioids: History and Canada's Opium Act (1908 & 1911)
- The Opium Acts focused on prohibiting the importation, manufacture, and sale of opium for non-medical purposes. Medical use was restricted.
- Stricter controls (e.g., limiting sales to pharmacies) were a feature of the 1911 Act.
- The Acts restricted use to medical purposes, and manufacturing, selling, and possession of opium for smoking was prohibited.
- The 1911 Act also expanded the scope of regulation, adding substances like cocaine, morphine, and eucaine to the list of controlled substances. Legislative details are provided in the text.
Methods of Administration
- Oral: Examples (pills, capsules, liquid forms). Slower onset due to first-pass metabolism.
- Parenteral: Examples (IM, SC, IV). Injected directly into the body, bypassing the GI tract.
- Inhalation: Smoking opium, or vaporized fentanyl. Rapid absorption into the bloodstream.
- Transdermal: Examples (Fentanyl patches for chronic pain) Absorbed through the skin.
Opioids: Metabolism
- Many opioids are inactive until metabolized into their active forms in the liver.
- Metabolization is generally rapid, except for some synthetic opioids.
- Specific enzymes and half-lives are referenced for various key opioids including Heroin, Codeine, Methadone, LAAM, and Fentanyl.
Opioids: CNS Effects
- Analgesic effects (act on Mu, Delta, and Kappa receptors in the spinal cord to block pain signals).
- Euphoria, dysphoria (unpleasant feelings).
- Decreased concentration (sedative effects).
- Emotional pain dulling (acting on receptors within the limbic system and frontal lobe).
Opioids: Tolerance & Dependence
- Tolerance develops to certain effects with continued use (e.g., respiratory depression, analgesia).
- Tolerance to some effects, such as constipation or pupil constriction, does not develop. Conditions leading to different tolerances are described.
Dependence: Characteristics of Withdrawal
- Initial symptoms (restlessness, agitation, yawning, fever, chills).
- Peak symptoms (intensify and reached peak 36-72 hours after last use)
- Physical symptoms (cramps, limb twitching, profuse sweating, nausea, muscle pain, loss of body fluids, and possible hallucinations). Variations in severity are described. Life-threatening aspects of withdrawals are detailed.
- Psychological dependence is more challenging to treat than physical addiction; treatment options are mentioned.
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Description
Explore the crucial aspects of opiates as discussed in Chapter 11. This quiz delves into the history, types, potency, medical uses, and effects of opiates, including their administration methods and treatment for withdrawal. Gain a deeper understanding of both naturally occurring and synthetic opiates.