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Questions and Answers
Which of the following is considered a naturally occurring opiate?
Which of the following is considered a naturally occurring opiate?
What percentage of morphine is found in opium?
What percentage of morphine is found in opium?
Which of the following compounds is NOT classified as a narcotic analgesic?
Which of the following compounds is NOT classified as a narcotic analgesic?
Which of the following statements about thebaine is true?
Which of the following statements about thebaine is true?
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What is the primary source of naturally occurring opiates?
What is the primary source of naturally occurring opiates?
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What characteristic distinguishes naloxone from naltrexone?
What characteristic distinguishes naloxone from naltrexone?
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Which medicinal application of opiates has a historical precedent dating back to ancient practices?
Which medicinal application of opiates has a historical precedent dating back to ancient practices?
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What was the primary composition of laudanum as introduced by Paracelsus in 1520?
What was the primary composition of laudanum as introduced by Paracelsus in 1520?
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Which of the following effects does tolerance develop towards when consuming opiates?
Which of the following effects does tolerance develop towards when consuming opiates?
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What led to the addiction of Thomas DeQuincy in the 1800s?
What led to the addiction of Thomas DeQuincy in the 1800s?
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Which of the following opiates is known to be derived from morphine and is over 10 times more potent?
Which of the following opiates is known to be derived from morphine and is over 10 times more potent?
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What is a primary reason users prefer fentanyl over heroin in street use?
What is a primary reason users prefer fentanyl over heroin in street use?
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Which synthetic opiate is used to treat chronic pain and is as potent as morphine for analgesic effects?
Which synthetic opiate is used to treat chronic pain and is as potent as morphine for analgesic effects?
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Which of the following is NOT a common method of administration for fentanyl?
Which of the following is NOT a common method of administration for fentanyl?
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Which opiate is specifically derived from thebaine?
Which opiate is specifically derived from thebaine?
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What is the primary active compound found in opium, which constitutes about 10% of it?
What is the primary active compound found in opium, which constitutes about 10% of it?
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What is a typical withdrawal effect associated with opiates?
What is a typical withdrawal effect associated with opiates?
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Which of the following opiates is known to have both analgesic effects and potential for dependence?
Which of the following opiates is known to have both analgesic effects and potential for dependence?
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What type of tolerance develops rapidly with daily opiate use?
What type of tolerance develops rapidly with daily opiate use?
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Which of the following withdrawal symptoms intensifies to a peak within 36 to 72 hours?
Which of the following withdrawal symptoms intensifies to a peak within 36 to 72 hours?
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Which mechanism is responsible for the development of pharmacokinetic tolerance?
Which mechanism is responsible for the development of pharmacokinetic tolerance?
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Which opiate is considered to potentially have a longer duration of psychological dependence compared to physical dependence?
Which opiate is considered to potentially have a longer duration of psychological dependence compared to physical dependence?
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In terms of physical withdrawal, which symptom is most immediately associated with craving?
In terms of physical withdrawal, which symptom is most immediately associated with craving?
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Which statement accurately describes the general timeline for the onset of withdrawal symptoms?
Which statement accurately describes the general timeline for the onset of withdrawal symptoms?
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What effect does tolerance not typically develop to?
What effect does tolerance not typically develop to?
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What is the expected duration for withdrawal symptoms to resolve completely?
What is the expected duration for withdrawal symptoms to resolve completely?
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Which of the following is primarily mediated through mu opiate receptors?
Which of the following is primarily mediated through mu opiate receptors?
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What type of user experiences little tolerance due to intermittent use?
What type of user experiences little tolerance due to intermittent use?
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Which opiate is primarily metabolized into morphine after administration?
Which opiate is primarily metabolized into morphine after administration?
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What is the estimated half-life of LAAM (levo-alpha-acetylmethadol)?
What is the estimated half-life of LAAM (levo-alpha-acetylmethadol)?
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Through which route can opiates NOT be administered?
Through which route can opiates NOT be administered?
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Which pharmacological action is NOT associated with opiates?
Which pharmacological action is NOT associated with opiates?
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What is the impact of tolerance on opiate effects?
What is the impact of tolerance on opiate effects?
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Infants born to addicted mothers typically exhibit which of the following?
Infants born to addicted mothers typically exhibit which of the following?
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Which receptor type is most understood in relation to opiate pharmacology?
Which receptor type is most understood in relation to opiate pharmacology?
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What determines the power of the Governor in Council related to drug regulation?
What determines the power of the Governor in Council related to drug regulation?
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Which of the following compounds has a long half-life and is not an immediate metabolite of other opiates?
Which of the following compounds has a long half-life and is not an immediate metabolite of other opiates?
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How do opiates primarily mimic endorphins in the body?
How do opiates primarily mimic endorphins in the body?
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What effect do mu receptors have on respiratory function?
What effect do mu receptors have on respiratory function?
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Which receptors are primarily involved in mediating euphoria?
Which receptors are primarily involved in mediating euphoria?
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What physiological effect occurs as a result of the activation of kappa receptors?
What physiological effect occurs as a result of the activation of kappa receptors?
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Which of the following statements about the tolerance effects of opioids is correct?
Which of the following statements about the tolerance effects of opioids is correct?
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What is a common psychological effect experienced with first-time opiate use?
What is a common psychological effect experienced with first-time opiate use?
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What impact do opiates have on gastrointestinal function?
What impact do opiates have on gastrointestinal function?
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What mechanism mediates analgesic effects at the spinal cord?
What mechanism mediates analgesic effects at the spinal cord?
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What happens to levels of sex hormones with the use of opiates?
What happens to levels of sex hormones with the use of opiates?
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In addition to pain relief, what other primary effect do opioids have on the central nervous system?
In addition to pain relief, what other primary effect do opioids have on the central nervous system?
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What is one of the mechanisms by which opiates inhibit pain signaling?
What is one of the mechanisms by which opiates inhibit pain signaling?
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What unique aspect made laudanum significant in the history of opiates?
What unique aspect made laudanum significant in the history of opiates?
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Which of the following opiates is known for having agonist properties, differing from naloxone?
Which of the following opiates is known for having agonist properties, differing from naloxone?
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What is a documented reason for the high potency of some opiates over others?
What is a documented reason for the high potency of some opiates over others?
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What is the primary pharmacological action that opiates utilize to develop tolerance?
What is the primary pharmacological action that opiates utilize to develop tolerance?
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What is a common withdrawal symptom associated with opiate cessation?
What is a common withdrawal symptom associated with opiate cessation?
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What is a common characteristic of heroin compared to its parent compound morphine?
What is a common characteristic of heroin compared to its parent compound morphine?
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Which of the following routes of administration is NOT commonly associated with fentanyl?
Which of the following routes of administration is NOT commonly associated with fentanyl?
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Which opiate is known to have a potency more than 10 times that of morphine?
Which opiate is known to have a potency more than 10 times that of morphine?
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What is considered a primary reason users prefer fentanyl over heroin?
What is considered a primary reason users prefer fentanyl over heroin?
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Tolerance to which of the following effects does NOT develop with regular opiate use?
Tolerance to which of the following effects does NOT develop with regular opiate use?
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Which synthetic opiate is used to treat chronic pain and has similar analgesic effects to morphine?
Which synthetic opiate is used to treat chronic pain and has similar analgesic effects to morphine?
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Which of the following statements regarding the metabolism of opiates is true?
Which of the following statements regarding the metabolism of opiates is true?
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What is a notable feature of withdrawal from opiates?
What is a notable feature of withdrawal from opiates?
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What is a key characteristic of heroin's pharmacokinetics once ingested?
What is a key characteristic of heroin's pharmacokinetics once ingested?
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Which route of administration has the quickest onset of opiate effects?
Which route of administration has the quickest onset of opiate effects?
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Which opiate is recognized for its long half-life, making it effective for chronic pain management?
Which opiate is recognized for its long half-life, making it effective for chronic pain management?
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What type of receptor action is primarily associated with the euphoric effects of opiates?
What type of receptor action is primarily associated with the euphoric effects of opiates?
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Which of the following describes the effect that does not typically develop tolerance in opiate users?
Which of the following describes the effect that does not typically develop tolerance in opiate users?
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What is the primary metabolic pathway for codeine in the body?
What is the primary metabolic pathway for codeine in the body?
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What withdrawal symptom is most likely to peak within 36 to 72 hours after cessation of opiate use?
What withdrawal symptom is most likely to peak within 36 to 72 hours after cessation of opiate use?
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Which of the following pharmacological actions of opiates contributes to decreased neuronal firing?
Which of the following pharmacological actions of opiates contributes to decreased neuronal firing?
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Which opiate-derived compound is known for being over ten times more potent than morphine?
Which opiate-derived compound is known for being over ten times more potent than morphine?
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What is one common psychological effect experienced with the initial use of opiates?
What is one common psychological effect experienced with the initial use of opiates?
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Which receptor type is primarily linked to the analgesic effects of opiates at the spinal cord level?
Which receptor type is primarily linked to the analgesic effects of opiates at the spinal cord level?
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What is a significant gastrointestinal effect of opiate use?
What is a significant gastrointestinal effect of opiate use?
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Which of the following statements correctly reflects the onset of tolerance to opiates?
Which of the following statements correctly reflects the onset of tolerance to opiates?
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What is one consequence of chronic opiate use in terms of sex hormone levels?
What is one consequence of chronic opiate use in terms of sex hormone levels?
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Which mechanism mediates the inhibition of pain signals via opiates at the spinal cord?
Which mechanism mediates the inhibition of pain signals via opiates at the spinal cord?
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Which natural opiate has been historically significant, dating back to ancient medicinal practices?
Which natural opiate has been historically significant, dating back to ancient medicinal practices?
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What is a notable effect of kappa receptors activation in the central nervous system?
What is a notable effect of kappa receptors activation in the central nervous system?
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How quickly do opiates typically metabolize in the body?
How quickly do opiates typically metabolize in the body?
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What is a primary reason some users develop a psychological dependence on certain opiates?
What is a primary reason some users develop a psychological dependence on certain opiates?
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What is the relationship between opiate use and psychological dependence?
What is the relationship between opiate use and psychological dependence?
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Which opiate mechanism leads to the dulling of emotional pain?
Which opiate mechanism leads to the dulling of emotional pain?
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What effect does tolerance develop towards in opiate consumption?
What effect does tolerance develop towards in opiate consumption?
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How quickly do withdrawal symptoms typically peak after cessation of opiate use?
How quickly do withdrawal symptoms typically peak after cessation of opiate use?
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Which statement about the physical tolerance of opiates is true?
Which statement about the physical tolerance of opiates is true?
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What is a characteristic symptom of opiate withdrawal?
What is a characteristic symptom of opiate withdrawal?
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How does the onset of tolerance differ among varying patterns of opiate use?
How does the onset of tolerance differ among varying patterns of opiate use?
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Which pharmacokinetic mechanism is responsible for increased tolerance?
Which pharmacokinetic mechanism is responsible for increased tolerance?
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What significant physiological change is associated with opiate use in infants born to addicted mothers?
What significant physiological change is associated with opiate use in infants born to addicted mothers?
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What distinguishes the onset and duration of withdrawal from psychological dependence?
What distinguishes the onset and duration of withdrawal from psychological dependence?
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Morphine is the only naturally occurring opiate with significant analgesic properties.
Morphine is the only naturally occurring opiate with significant analgesic properties.
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Fentanyl is 30 to 50 times more potent than morphine.
Fentanyl is 30 to 50 times more potent than morphine.
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Hydromorphone is derived from codeine and is less potent than morphine.
Hydromorphone is derived from codeine and is less potent than morphine.
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Thebaine has analgesic effects that are weaker compared to other traditional opiates.
Thebaine has analgesic effects that are weaker compared to other traditional opiates.
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Tolerance to the euphoric effects of opiates develops more quickly than tolerance to their analgesic effects.
Tolerance to the euphoric effects of opiates develops more quickly than tolerance to their analgesic effects.
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Withdrawal symptoms from opiates typically resolve within 24 hours.
Withdrawal symptoms from opiates typically resolve within 24 hours.
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Buprenorphine is a synthetic opiate that exhibits both agonist and antagonist properties.
Buprenorphine is a synthetic opiate that exhibits both agonist and antagonist properties.
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Oxycodone is derived from morphine and has effects that are more potent than morphine.
Oxycodone is derived from morphine and has effects that are more potent than morphine.
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Laudanum was first introduced as a medicinal drink by a physician named Paracelsus in 1520.
Laudanum was first introduced as a medicinal drink by a physician named Paracelsus in 1520.
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Naltrexone is primarily used to stimulate the mu receptors in the body.
Naltrexone is primarily used to stimulate the mu receptors in the body.
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By the 1800s, laudanum was widely found in numerous patented medicines with varying names and formulations.
By the 1800s, laudanum was widely found in numerous patented medicines with varying names and formulations.
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Thomas DeQuincy became addicted to opium after using it primarily for alleviating respiratory issues.
Thomas DeQuincy became addicted to opium after using it primarily for alleviating respiratory issues.
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The effects of tolerance to opiates develop rapidly with continuous use and are observed in various physiological reactions.
The effects of tolerance to opiates develop rapidly with continuous use and are observed in various physiological reactions.
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The opiate known as LAAM has a shorter half-life than methadone.
The opiate known as LAAM has a shorter half-life than methadone.
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Codeine is inactive until it is metabolized into morphine and other metabolites.
Codeine is inactive until it is metabolized into morphine and other metabolites.
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Oral administration of opiates results in a longer onset of effects compared to intravenous administration.
Oral administration of opiates results in a longer onset of effects compared to intravenous administration.
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The pharmacological action of opiates involves increasing the firing rate of all neurons in the central nervous system.
The pharmacological action of opiates involves increasing the firing rate of all neurons in the central nervous system.
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The onset of withdrawal symptoms after abrupt cessation of opiates peaks within 36 to 72 hours.
The onset of withdrawal symptoms after abrupt cessation of opiates peaks within 36 to 72 hours.
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Infants born to addicted mothers will exhibit withdrawal symptoms due to in utero exposure to opiates.
Infants born to addicted mothers will exhibit withdrawal symptoms due to in utero exposure to opiates.
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Fentanyl is considered to be less potent than heroin for analgesic effects.
Fentanyl is considered to be less potent than heroin for analgesic effects.
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Tolerance to opiates typically develops slowly over time, regardless of usage frequency.
Tolerance to opiates typically develops slowly over time, regardless of usage frequency.
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The regulation allowing the Governor in Council to add drugs to the Schedule is based on public health considerations.
The regulation allowing the Governor in Council to add drugs to the Schedule is based on public health considerations.
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Morphine's half-life is shorter than that of heroin.
Morphine's half-life is shorter than that of heroin.
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Laudanum was introduced by Paracelsus in 1520 as a significant opiate preparation.
Laudanum was introduced by Paracelsus in 1520 as a significant opiate preparation.
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Fentanyl is considered to be less potent than morphine for its analgesic effects.
Fentanyl is considered to be less potent than morphine for its analgesic effects.
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Opiates are primarily metabolized in the liver before they exert their effects.
Opiates are primarily metabolized in the liver before they exert their effects.
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Psychological dependence on opiates often resolves more quickly than physical dependence.
Psychological dependence on opiates often resolves more quickly than physical dependence.
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Pupil constriction tolerance typically develops rapidly with opiate use.
Pupil constriction tolerance typically develops rapidly with opiate use.
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Withdrawal symptoms from opiates can include cramping and vomiting.
Withdrawal symptoms from opiates can include cramping and vomiting.
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The analgesic effect of opiates is primarily mediated through kappa receptors.
The analgesic effect of opiates is primarily mediated through kappa receptors.
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Tolerance to the euphoric effects of opiates can develop significantly faster than tolerance to respiratory depression.
Tolerance to the euphoric effects of opiates can develop significantly faster than tolerance to respiratory depression.
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Some opiates, like buprenorphine, have been successfully used to treat both physical and psychological dependence.
Some opiates, like buprenorphine, have been successfully used to treat both physical and psychological dependence.
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With daily use of opiates, tolerance typically develops within 30 to 40 days.
With daily use of opiates, tolerance typically develops within 30 to 40 days.
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Mu receptors are primarily associated with the physiological effect of euphoria.
Mu receptors are primarily associated with the physiological effect of euphoria.
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Morphine has a strong attachment but weak effect at mu receptors.
Morphine has a strong attachment but weak effect at mu receptors.
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The effects of opiates include increased levels of sex hormones in both men and women.
The effects of opiates include increased levels of sex hormones in both men and women.
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Delta receptors do not overlap in distribution with mu receptors within the limbic system.
Delta receptors do not overlap in distribution with mu receptors within the limbic system.
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Constipation due to opiate use is primarily caused by increased peristalsis in the intestine.
Constipation due to opiate use is primarily caused by increased peristalsis in the intestine.
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Kappa receptors are found in the nucleus accumbens and the ventral tegmental area.
Kappa receptors are found in the nucleus accumbens and the ventral tegmental area.
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The initial effects of opiates on the vomiting center are typically inhibitory.
The initial effects of opiates on the vomiting center are typically inhibitory.
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Dysphoria is a common psychological effect experienced only with synthetic opiates.
Dysphoria is a common psychological effect experienced only with synthetic opiates.
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Withdrawal symptoms from opiates manifest immediately and peak within 36 to 72 hours.
Withdrawal symptoms from opiates manifest immediately and peak within 36 to 72 hours.
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Not all opiates produce euphoric effects in all users, with some experiencing strong dysphoria instead.
Not all opiates produce euphoric effects in all users, with some experiencing strong dysphoria instead.
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Study Notes
Opiates: Definitional Issues
- Opiates are naturally occurring, derived, and synthetic compounds with analgesic properties.
- <span>These substances are classified as "narcotic analgesics" due to their ability to relieve pain while often inducing a sense of sedation or euphoria in the user.</span>
Naturally Occurring Opiates
- Morphine, codeine, and thebaine are found in opium.
- Opium is the sap from the seedpods of the opium poppy.
- Morphine makes up approximately 10% of opium.
- Codeine accounts for .75 to 2.5% of opium.
- Thebaine makes up less than 1% of opium.
Opiate Derivatives/Semi-Synthetics
- Heroin is an example of an opiate derivative.
- Other examples include hydromorphone, oxycodone, oxymorphone, and hydrocodone.
Synthetic Opiates
- Meperidine and methadone are synthetic opiates.
- Other synthetic opiates include fentanyl, LAAM, and buprenorphine.
Opiate Antagonists
- Naloxone and nalorphine are useful in treating opiate overdoses.
Medical Uses
- Opioid medications are used medically for:
- Treatment of pain
- Treatment of diarrhea
- Treatment of coughs
Uses and History
- Opiates have been used medicinally for hundreds of years.
- Evidence of opiate use dates back to 1550 BC, documented in Egyptian medical scrolls.
- Galen, in the second century AD, recommended opiates for various ailments.
- In 1520, a medicinal drink called laudanum was introduced.
- Recreational use of opiates also dates back hundreds of years, with opium cakes and candy sold broadly.
- Opium dens appeared in various parts of the world starting in the 18th century.
History (Continued)
- Until the early to mid-1800s, opium use was widely socially accepted.
- Concerns about chronic opium use and social prejudice led to government efforts in the US and Britain to regulate opium use and sales starting in the mid to late 1800s.
- There were documented negative consequences of chronic use of opiates.
- Some historical accounts noted an increasing number of young people becoming addicted.
- The use of opiates was noted as an issue in the 19th century in the US, with accounts of the social problems linked to recreational use, in particular among women and young people.
Mechanism of Action (MOA)
- Opiates are administered orally, parenterally, via inhalation, or transdermally.
Distribution
- Opiates are found in high concentrations in the lungs, liver, and spleen.
- Opiates readily pass through the placental barrier.
- In the brain, opiates concentrate in the limbic system, basal ganglia, nucleus accumbens, ventral tegmental areas, periaqueductal gray area (pain area), and brain stem.
Metabolism
- Codeine and much of heroin are inactive until metabolized.
- Metabolism of opiates is rapid.
- An exception to the rapid metabolism includes some synthetic opiates such as methadone and LAAM.
Pharmacological Actions
- Opiates mimic endorphins.
- They are agonists at six types of receptors, with mu, kappa, and delta receptors being the most well-understood.
- Opiates decrease neuronal firing via two mechanisms: inhibiting calcium influx and enhancing potassium flow.
- They increase neuronal firing in some instances by preventing the inhibition of these neurons (inhibitory synapses).
CNS Effects
- Opiates exert analgesic effects.
- They depress the respiratory center, cough center, and vomiting center.
- Opiates also cause drowsiness.
- Opiates can decrease levels of sex hormones.
Effects on Eyes
- Opiates cause constriction of pupils.
- The mechanism for this effect is unknown.
Gastrointestinal Effects
- Opiates diminish peristalsis in the intestines.
- They increase muscle tone in the intestines, which can lead to constipation.
Psychological Effects
- Opiate use can cause euphoria and dysphoria.
- Concentration can decrease.
- Emotional pain can be dulled by opiate use.
Tolerance
- Tolerance develops to respiratory depression, analgesia, sedation, and euphoria.
- Pupil constriction may develop.
- Constipation does not develop as a tolerance effect.
- Tolerance develops rapidly.
- There are three types of tolerance.
Physical Dependence
- Physical dependence involves characteristic withdrawal symptoms.
- This includes restlessness and agitation, yawning, fever and chills, deep sleep, cramps, twitching of limbs, and profuse sweating.
- Symptoms intensify to a peak within 36-72 hours; the withdrawal symptoms resolve over five to ten days.
- Withdrawal from opiates is generally not considered a life-threatening event.
Psychological Dependence
- Psychological dependence is harder to treat than physical dependence.
- Methadone and synthetic opiates like LAAM and buprenorphine show some success in treating psychological dependence.
Methadone Treatment
- Factors contributing to methadone’s effectiveness include oral administration, long-acting effects, and antagonistic actions.
- These are advantages for opiate cessation.
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Description
This quiz explores the various definitions and classifications of opiates, including naturally occurring, semi-synthetics, and synthetics. Learn about their medical uses, derivatives, and specific compounds like morphine and heroin. Test your knowledge on the effects and implications of opiate usage.
