opioids intro
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Questions and Answers

The major effects of opioids are mediated by which 3 receptor families

  • beta-endorphin, delta, kappa
  • dynorphin, enkephalin, mu
  • mu, kappa, delta (correct)
  • beta-endorphin, mu, delta

    • Each receptor family exhibits a different specificity for the drug(s) it binds

  • true (correct)
  • false

    • analgesic properties of opioids are primarily mediated by the which family of receptors? (these receptors modulate responses to thermal, mechanical and chemical nociception)

  • beta-endorphin
  • mu (correct)
  • kappa
  • delta

    • Mu receptors are the main receptors responsible for analgesic effects, but the ______ receptor in the dorsal horn also contribute to analsgia by modulating the response to chemical and thermal nociception.

    <p>kappa</p> Signup and view all the answers

    mechanism of action for opioids is the inhibition of ____ and _____ to prevent action potential firing.

    <p>Calcium, glutamate</p> Signup and view all the answers

    Codeine undergoes metabolism and activation (demethylation) and is converted into _____

    <p>morphine</p> Signup and view all the answers

    Which is an advantage of using morphine as an analgesic?

    <p>90% of the drug is metabolized/excreted from the body after 24 hours</p> Signup and view all the answers

    Which is used to reverse the coma and respiratory depression of opioid overdose?

    <p>Naloxone</p> Signup and view all the answers

    The biggest concern associated with the adverse effects of opioids is

    <p>respiratory depression</p> Signup and view all the answers

    Opioid drugs are opioid receptor

    <p>agonists</p> Signup and view all the answers

    Morphine and codeine are opioids with antitussive properties, but ______ is most commonly used to treat cough symptoms.

    <p>codeine</p> Signup and view all the answers

    Naloxone and naltrexone are examples of opioid receptor

    <p>antagonists</p> Signup and view all the answers

    A patient given Narcan to reverse opioid overdose is free from the risk of another episode of respiratory depression

    <p>false</p> Signup and view all the answers

    An example of a MODERATE/LOW opioid receptor agonist is

    <p>codeine</p> Signup and view all the answers

    What are the three receptor families commonly designated as in relation to opioids?

    <p>μ (mu), κ (kappa), and δ (delta)</p> Signup and view all the answers

    Which opioid receptor primarily modulates responses to thermal, mechanical, and chemical nociception?

    <p>μ (mu) receptor</p> Signup and view all the answers

    True or False: Opioids inhibit calcium influx and neurotransmission of glutamate.

    <p>True</p> Signup and view all the answers

    What is the high-affinity metabolite of morphine that has a high affinity for the μ receptor?

    <p>Morphine 6 Glucuronide</p> Signup and view all the answers

    Match the following mixed agonists-antagonists with their respective drugs:

    <p>Buprenorphine = Mixed agonists-antagonists Pentazocine = Mixed agonists-antagonists Nalbuphine = Mixed agonists-antagonists Butorphanol = Mixed agonists-antagonists</p> Signup and view all the answers

    What is the antagonist used to reverse coma and respiratory depression in opioid overdose?

    <p>Naloxone</p> Signup and view all the answers

    True or False: Naltrexone has actions similar to Naloxone.

    <p>True</p> Signup and view all the answers

    Which opioid-related drug can lead to hepatotoxicity?

    <p>Naltrexone</p> Signup and view all the answers

    What is the difference between physical dependence and psychological dependence on opioids?

    <p>Physical dependence involves changes at the cellular level, while psychological dependence involves drug-seeking behavior.</p> Signup and view all the answers

    Physical dependence, psychological dependence, and tolerance to opioids are irreversible.

    <p>False</p> Signup and view all the answers

    What opioid analgesic drugs are commonly used in dentistry for oral administration?

    <p>codeine, hydrocodone, oxycodone</p> Signup and view all the answers

    _______ is the first choice for relief of pain in cases of inflammation in dental pain.

    <p>Nonopioid analgesic drugs with anti-inflammatory efficacy (e.g., aspirin, ibuprofen)</p> Signup and view all the answers

    What are the three major receptor families commonly designated in opioid pharmacology?

    <p>μ (mu), κ (kappa), δ (delta)</p> Signup and view all the answers

    Which receptor family primarily modulates responses to thermal, mechanical, and chemical nociception in opioid pharmacology?

    <p>μ (mu)</p> Signup and view all the answers

    Tolerance usually does not develop to the pupil-constricting effects of morphine. (True/False)

    <p>True</p> Signup and view all the answers

    Naloxone is used to reverse the coma and respiratory depression of opioid ______.

    <p>overdose</p> Signup and view all the answers

    Match the following opioids with their respective categories:

    <p>Codeine = Opioid agonist Buprenorphine = Mixed agonist-antagonist Naloxone = Antagonist Morphine = Opioid agonist</p> Signup and view all the answers

    What is the antagonist of the opioid receptor?

    <p>Naloxone</p> Signup and view all the answers

    Why should neonates not receive morphine?

    <p>low conjugating capacity</p> Signup and view all the answers

    Which of the following statements about physical dependence on opioids is true?

    <p>Can exist without psychological dependence</p> Signup and view all the answers

    Psychological dependence may contribute more to drug-seeking behavior than physical dependence.

    <p>True</p> Signup and view all the answers

    Physical dependence, psychological dependence, and tolerance are all ________.

    <p>reversible</p> Signup and view all the answers

    What kind of analgesic drugs are often the first choice for relief of pain originating from dental issues?

    <p>Nonopioid analgesic drugs with anti-inflammatory efficacy</p> Signup and view all the answers

    Match the opioids with their administration route:

    <p>Codeine = Oral administration Morphine = Parenteral administration Hydrocodone = Oral administration Fentanyl = Parenteral administration</p> Signup and view all the answers

    Study Notes

    Opioids and Physical Function

    • Opioids are used to reduce pain and are mediated by three receptor families: μ (mu), κ (kappa), and δ (delta)
    • μ receptors are responsible for the analgesic properties of opioids
    • κ receptors in the dorsal horn contribute to analgesia by modulating responses to chemical and thermal nociception

    Mechanism of Action

    • Opioids bind to specific receptors, activating subtypes of G protein, and phosphorylation, leading to a conformational change of the receptor
    • This inhibits calcium influx, neurotransmission, and the release of glutamate

    Morphine Pharmacology

    • Analgesia: raises pain threshold at the spinal cord level and alters the brain's perception of pain
    • Respiratory depression: reduces sensitivity of respiratory center neurons to carbon dioxide
    • Cough suppression: antitussive properties
    • Miosis: stimulation of μ and κ receptors causes pinpoint pupils
    • Emesis: direct stimulation of the chemoreceptor trigger zone in the area postrema causes vomiting

    Pharmacokinetics of Morphine

    • Absorption: significant first-pass metabolism in the liver, with slow and erratic absorption from the GI tract
    • Distribution: rapidly enters all body tissues, including the fetuses of pregnant women
    • Fate: conjugated with glucuronic acid in the liver, with the conjugates excreted primarily in urine

    Adverse Effects

    • Tolerance and physical dependence: repeated use produces tolerance to the respiratory depressant, analgesic, euphoric, and sedative effects
    • Drug-drug interactions: includes interactions with other CNS depressants, neuroleptics, tricyclic antidepressants, monoamine oxidase inhibitors, local anesthetics, and oral anticoagulants

    Antagonists

    • Naloxone: rapidly displaces all receptor-bound opioid molecules, reversing the effects of opioid overdose
    • Naltrexone: similar to naloxone, with a longer duration of action and used for rapid opioid detoxification

    Dental Implications

    • Use: opioids are not anti-inflammatory, and non-opioid analgesic drugs are often the first choice for relief of pain
    • Caution: opioid analgesics are subject to misuse and abuse, and interactions with other medications and substances can be significant
    • Genetic variation: codeine metabolism is affected by variations in the activity of cytochrome P450 2D6, which can result in different rates and degrees of conversion to morphine

    Withdrawal Symptoms

    • Symptoms of opioid withdrawal after abrupt withdrawal of equivalent doses of heroin, buprenorphine, and methadone

    Opioids and Physical Function

    • Opioids are used to reduce pain and are mediated by three receptor families: μ (mu), κ (kappa), and δ (delta)
    • μ receptors are responsible for the analgesic properties of opioids
    • κ receptors in the dorsal horn contribute to analgesia by modulating responses to chemical and thermal nociception

    Mechanism of Action

    • Opioids bind to specific receptors, activating subtypes of G protein, and phosphorylation, leading to a conformational change of the receptor
    • This inhibits calcium influx, neurotransmission, and the release of glutamate

    Morphine Pharmacology

    • Analgesia: raises pain threshold at the spinal cord level and alters the brain's perception of pain
    • Respiratory depression: reduces sensitivity of respiratory center neurons to carbon dioxide
    • Cough suppression: antitussive properties
    • Miosis: stimulation of μ and κ receptors causes pinpoint pupils
    • Emesis: direct stimulation of the chemoreceptor trigger zone in the area postrema causes vomiting

    Pharmacokinetics of Morphine

    • Absorption: significant first-pass metabolism in the liver, with slow and erratic absorption from the GI tract
    • Distribution: rapidly enters all body tissues, including the fetuses of pregnant women
    • Fate: conjugated with glucuronic acid in the liver, with the conjugates excreted primarily in urine

    Adverse Effects

    • Tolerance and physical dependence: repeated use produces tolerance to the respiratory depressant, analgesic, euphoric, and sedative effects
    • Drug-drug interactions: includes interactions with other CNS depressants, neuroleptics, tricyclic antidepressants, monoamine oxidase inhibitors, local anesthetics, and oral anticoagulants

    Antagonists

    • Naloxone: rapidly displaces all receptor-bound opioid molecules, reversing the effects of opioid overdose
    • Naltrexone: similar to naloxone, with a longer duration of action and used for rapid opioid detoxification

    Dental Implications

    • Use: opioids are not anti-inflammatory, and non-opioid analgesic drugs are often the first choice for relief of pain
    • Caution: opioid analgesics are subject to misuse and abuse, and interactions with other medications and substances can be significant
    • Genetic variation: codeine metabolism is affected by variations in the activity of cytochrome P450 2D6, which can result in different rates and degrees of conversion to morphine

    Withdrawal Symptoms

    • Symptoms of opioid withdrawal after abrupt withdrawal of equivalent doses of heroin, buprenorphine, and methadone

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