opioids intro

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.

kappa Signup and view all the answers

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

Calcium, glutamate Signup and view all the answers

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

morphine Signup and view all the answers

Which is an advantage of using morphine as an analgesic?

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

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

Naloxone Signup and view all the answers

The biggest concern associated with the adverse effects of opioids is

respiratory depression Signup and view all the answers

Opioid drugs are opioid receptor

agonists Signup and view all the answers

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

codeine Signup and view all the answers

Naloxone and naltrexone are examples of opioid receptor

antagonists 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

false Signup and view all the answers

An example of a MODERATE/LOW opioid receptor agonist is

codeine Signup and view all the answers

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

μ (mu), κ (kappa), and δ (delta) Signup and view all the answers

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

μ (mu) receptor Signup and view all the answers

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

True Signup and view all the answers

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

Morphine 6 Glucuronide Signup and view all the answers

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

Buprenorphine = Mixed agonists-antagonists Pentazocine = Mixed agonists-antagonists Nalbuphine = Mixed agonists-antagonists Butorphanol = Mixed agonists-antagonists Signup and view all the answers

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

Naloxone Signup and view all the answers

True or False: Naltrexone has actions similar to Naloxone.

True Signup and view all the answers

Which opioid-related drug can lead to hepatotoxicity?

Naltrexone Signup and view all the answers

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

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

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

False Signup and view all the answers

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

codeine, hydrocodone, oxycodone Signup and view all the answers

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

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

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

μ (mu), κ (kappa), δ (delta) Signup and view all the answers

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

μ (mu) Signup and view all the answers

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

True Signup and view all the answers

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

overdose Signup and view all the answers

Match the following opioids with their respective categories:

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

What is the antagonist of the opioid receptor?

Naloxone Signup and view all the answers

Why should neonates not receive morphine?

low conjugating capacity Signup and view all the answers

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

Can exist without psychological dependence Signup and view all the answers

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

True Signup and view all the answers

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

reversible Signup and view all the answers

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

Nonopioid analgesic drugs with anti-inflammatory efficacy Signup and view all the answers

Match the opioids with their administration route:

Codeine = Oral administration Morphine = Parenteral administration Hydrocodone = Oral administration Fentanyl = Parenteral administration 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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Description

FA- intro to opioids D1 fall

opioids intro

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.

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

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

Which is an advantage of using morphine as an analgesic?

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

The biggest concern associated with the adverse effects of opioids is

Opioid drugs are opioid receptor

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

Naloxone and naltrexone are examples of opioid receptor

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

An example of a MODERATE/LOW opioid receptor agonist is

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

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

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

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

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

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

True or False: Naltrexone has actions similar to Naloxone.

Which opioid-related drug can lead to hepatotoxicity?

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

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

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

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

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

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

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

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

Match the following opioids with their respective categories:

What is the antagonist of the opioid receptor?

Why should neonates not receive morphine?

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

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

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

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

Match the opioids with their administration route:

Study Notes

Opioids and Physical Function

Mechanism of Action

Morphine Pharmacology

Pharmacokinetics of Morphine

Adverse Effects

Antagonists

Dental Implications

Withdrawal Symptoms

Opioids and Physical Function

Mechanism of Action

Morphine Pharmacology

Pharmacokinetics of Morphine

Adverse Effects

Antagonists

Dental Implications

Withdrawal Symptoms

Studying That Suits You

Description

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