Questions and Answers
The major effects of opioids are mediated by which 3 receptor families
Each receptor family exhibits a different specificity for the drug(s) it binds
analgesic properties of opioids are primarily mediated by the which family of receptors? (these receptors modulate responses to thermal, mechanical and chemical nociception)
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.
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mechanism of action for opioids is the inhibition of ____ and _____ to prevent action potential firing.
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Codeine undergoes metabolism and activation (demethylation) and is converted into _____
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Which is an advantage of using morphine as an analgesic?
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Which is used to reverse the coma and respiratory depression of opioid overdose?
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The biggest concern associated with the adverse effects of opioids is
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Opioid drugs are opioid receptor
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Morphine and codeine are opioids with antitussive properties, but ______ is most commonly used to treat cough symptoms.
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Naloxone and naltrexone are examples of opioid receptor
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A patient given Narcan to reverse opioid overdose is free from the risk of another episode of respiratory depression
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An example of a MODERATE/LOW opioid receptor agonist is
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What are the three receptor families commonly designated as in relation to opioids?
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Which opioid receptor primarily modulates responses to thermal, mechanical, and chemical nociception?
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True or False: Opioids inhibit calcium influx and neurotransmission of glutamate.
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What is the high-affinity metabolite of morphine that has a high affinity for the μ receptor?
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Match the following mixed agonists-antagonists with their respective drugs:
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What is the antagonist used to reverse coma and respiratory depression in opioid overdose?
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True or False: Naltrexone has actions similar to Naloxone.
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Which opioid-related drug can lead to hepatotoxicity?
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What is the difference between physical dependence and psychological dependence on opioids?
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Physical dependence, psychological dependence, and tolerance to opioids are irreversible.
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What opioid analgesic drugs are commonly used in dentistry for oral administration?
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_______ is the first choice for relief of pain in cases of inflammation in dental pain.
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What are the three major receptor families commonly designated in opioid pharmacology?
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Which receptor family primarily modulates responses to thermal, mechanical, and chemical nociception in opioid pharmacology?
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Tolerance usually does not develop to the pupil-constricting effects of morphine. (True/False)
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Naloxone is used to reverse the coma and respiratory depression of opioid ______.
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Match the following opioids with their respective categories:
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What is the antagonist of the opioid receptor?
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Why should neonates not receive morphine?
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Which of the following statements about physical dependence on opioids is true?
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Psychological dependence may contribute more to drug-seeking behavior than physical dependence.
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Physical dependence, psychological dependence, and tolerance are all ________.
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What kind of analgesic drugs are often the first choice for relief of pain originating from dental issues?
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Match the opioids with their administration route:
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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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Description
FA- intro to opioids D1 fall