Podcast
Questions and Answers
What is the primary purpose of opioid agonists?
What is the primary purpose of opioid agonists?
- To treat cough and diarrhea
- To increase the production of endorphins
- To stimulate the release of GABA
- To control acute or chronic pain (correct)
What is the effect of endorphins on inhibitory neurons?
What is the effect of endorphins on inhibitory neurons?
- They inhibit the release of GABA
- They stimulate the release of dopamine
- They activate the mu, kappa, and delta receptors (correct)
- They decrease the production of serotonin
What is the goal when treating pain with opioids?
What is the goal when treating pain with opioids?
- To increase the dose of opioids rapidly
- To use short-acting opioids at the highest dose possible
- To use short-acting opioids at the lowest effective dose for a few days (correct)
- To switch to exogenous opioids immediately
What is the role of GABA in the brain?
What is the role of GABA in the brain?
What is the origin of exogenous opioids like heroin and morphine?
What is the origin of exogenous opioids like heroin and morphine?
What is the effect of exercise on endorphins?
What is the effect of exercise on endorphins?
What is the primary risk of combining opioids with other central nervous system depressants?
What is the primary risk of combining opioids with other central nervous system depressants?
Why are opioids contraindicated in patients with head injury?
Why are opioids contraindicated in patients with head injury?
What is the primary cause of death from opioid overdose?
What is the primary cause of death from opioid overdose?
What is the purpose of combining naloxone with buprenorphine in the treatment of opioid use disorder?
What is the purpose of combining naloxone with buprenorphine in the treatment of opioid use disorder?
What is the primary mechanism of action of opioids in the gastrointestinal tract?
What is the primary mechanism of action of opioids in the gastrointestinal tract?
What is the primary mechanism of action of opioids in the biliary tract?
What is the primary mechanism of action of opioids in the biliary tract?
What is the primary risk of using opioids during pregnancy?
What is the primary risk of using opioids during pregnancy?
What is the primary mechanism of action of opioids in the central nervous system?
What is the primary mechanism of action of opioids in the central nervous system?
What is the primary role of methadone in the treatment of opioid use disorder?
What is the primary role of methadone in the treatment of opioid use disorder?
What is the primary mechanism of action of partial agonists like buprenorphine?
What is the primary mechanism of action of partial agonists like buprenorphine?
What is the result of dopamine release in the brain?
What is the result of dopamine release in the brain?
Which of the following opioids acts as a full agonist but does not cause euphoria?
Which of the following opioids acts as a full agonist but does not cause euphoria?
What is the effect of endorphins binding to opioid receptors?
What is the effect of endorphins binding to opioid receptors?
Which of the following opioids is a mixed agonist-antagonist?
Which of the following opioids is a mixed agonist-antagonist?
What is the effect of norepinephrine and serotonin release in pain processing regions of the brain?
What is the effect of norepinephrine and serotonin release in pain processing regions of the brain?
Which opioid receptor is buprenorphine an antagonist at?
Which opioid receptor is buprenorphine an antagonist at?
What is the effect of tramadol when given with a full agonist?
What is the effect of tramadol when given with a full agonist?
What is the benefit of methadone in treating opioid use disorder?
What is the benefit of methadone in treating opioid use disorder?
What is the mechanism of action of codeine and hydrocodone as an antitussive?
What is the mechanism of action of codeine and hydrocodone as an antitussive?
What is the effect of fentanyl as an anesthetic medication?
What is the effect of fentanyl as an anesthetic medication?
Which opioid receptor agonist is most likely to cause severe respiratory depression?
Which opioid receptor agonist is most likely to cause severe respiratory depression?
What is the primary mechanism of action of opioids in reducing pain perception?
What is the primary mechanism of action of opioids in reducing pain perception?
Why are opioids contraindicated in people with head trauma?
Why are opioids contraindicated in people with head trauma?
What is the main reason why opioids should be avoided during pregnancy?
What is the main reason why opioids should be avoided during pregnancy?
Which of the following opioids is a partial agonist?
Which of the following opioids is a partial agonist?
What is the significance of the constipated man statue in the park?
What is the significance of the constipated man statue in the park?
What is the primary effect of opioids on neurotransmitters in the central nervous system?
What is the primary effect of opioids on neurotransmitters in the central nervous system?
Which of the following opioids is classified as a full agonist?
Which of the following opioids is classified as a full agonist?
What is the significance of the ice cream vendor in the park?
What is the significance of the ice cream vendor in the park?
Why are opioids contraindicated in people with biliary colic?
Why are opioids contraindicated in people with biliary colic?
What is the effect of opioids on inhibitory neurons in the central nervous system?
What is the effect of opioids on inhibitory neurons in the central nervous system?
What is the significance of the woman's pregnancy in the garden?
What is the significance of the woman's pregnancy in the garden?
What is the primary function of inhibitory neurons in the brain tissue?
What is the primary function of inhibitory neurons in the brain tissue?
What happens to the release of neurotransmitters like dopamine, serotonin, and norepinephrine when endorphins bind to opioid receptors?
What happens to the release of neurotransmitters like dopamine, serotonin, and norepinephrine when endorphins bind to opioid receptors?
Why are opioids used to treat diarrhea?
Why are opioids used to treat diarrhea?
What is the source of exogenous opioids like heroin and morphine?
What is the source of exogenous opioids like heroin and morphine?
What is the goal when using opioids to control pain?
What is the goal when using opioids to control pain?
What is the effect of exercise on the release of endorphins in the brain?
What is the effect of exercise on the release of endorphins in the brain?
What is the outcome of norepinephrine and serotonin release in the thalamus, brainstem, and spinal cord?
What is the outcome of norepinephrine and serotonin release in the thalamus, brainstem, and spinal cord?
Which opioid receptor does buprenorphine act as a partial agonist at?
Which opioid receptor does buprenorphine act as a partial agonist at?
What is the effect of dopamine release in the ventral tegmental area, nucleus accumbens, and prefrontal cortex?
What is the effect of dopamine release in the ventral tegmental area, nucleus accumbens, and prefrontal cortex?
What is the effect of opioid stimulation on the GI tract?
What is the effect of opioid stimulation on the GI tract?
Which opioid is used to relax uterine muscles and inhibit contractions during labor?
Which opioid is used to relax uterine muscles and inhibit contractions during labor?
Why are opioids contraindicated in patients with head injury?
Why are opioids contraindicated in patients with head injury?
What is the primary mechanism of action of opioids in reducing pain perception?
What is the primary mechanism of action of opioids in reducing pain perception?
What is the primary cause of death from opioid overdose?
What is the primary cause of death from opioid overdose?
What is the effect of giving a partial agonist with a full agonist?
What is the effect of giving a partial agonist with a full agonist?
What is the effect of opioids on the biliary tract?
What is the effect of opioids on the biliary tract?
Which opioid receptor is butorphanol a partial agonist at?
Which opioid receptor is butorphanol a partial agonist at?
What is the benefit of methadone in treating opioid use disorder?
What is the benefit of methadone in treating opioid use disorder?
What is the advantage of using methadone in treating opioid use disorder?
What is the advantage of using methadone in treating opioid use disorder?
Which opioid is used to treat diarrhea?
Which opioid is used to treat diarrhea?
What is the effect of combining opioids with other CNS depressants?
What is the effect of combining opioids with other CNS depressants?
What is the primary mechanism of action of full agonists like morphine?
What is the primary mechanism of action of full agonists like morphine?
What is the effect of buprenorphine on opioid receptors?
What is the effect of buprenorphine on opioid receptors?
What is the primary risk of using opioids during pregnancy?
What is the primary risk of using opioids during pregnancy?
What is the effect of opioid withdrawal?
What is the effect of opioid withdrawal?
What is the benefit of tapering off opioid use?
What is the benefit of tapering off opioid use?
Study Notes
Opioid Agonists
- Opioid agonists are medications used to control acute or chronic pain and treat diarrhea and cough
- They bind to opioid receptors in the brain, spinal cord, and gastrointestinal tract
- Classified into:
- Full agonists (e.g., morphine, fentanyl, meperidine, codeine, hydrocodone) - more potent but have more severe side effects
- Partial agonists (e.g., buprenorphine, butorphanol, pentazocine, tramadol) - weaker effect, used to manage moderate pain
Mechanism of Action
- Endorphins bind to opioid receptors, blocking GABA release, allowing dopamine, serotonin, and norepinephrine to flood the thalamus, brainstem, and spinal cord, reducing pain perception
- Activate mu, kappa, and delta receptors, resulting in a calming sensation and decreased sensitivity to pain
Full Agonists
- Morphine, fentanyl, meperidine, codeine, hydrocodone, and oxycodone
- Strongest analgesics available, used to control severe pain
- Fentanyl is the most potent and used as an anesthetic due to rapid onset and short duration of action
- Meperidine can be used to relax uterine muscles and inhibit contractions during labor, but can produce respiratory depression in the baby
- Codeine is a weaker full agonist, used to treat moderate pain and relieve cough
Partial Agonists
- Buprenorphine, butorphanol, pentazocine, and tramadol
- Used to manage moderate pain
- Buprenorphine is a partial agonist at the mu receptor, but an antagonist at the kappa receptor, and is used to decrease withdrawal symptoms in opioid use disorder
- Butorphanol is a partial agonist at the kappa receptor, but an antagonist at the mu receptor
- Pentazocine is a partial agonist at the mu and kappa receptors
Side Effects and Contraindications
-
Nausea, vomiting, dysphoria, pinpoint pupils, constipation, biliary colic
-
Respiratory depression, coma, and cardiac depression in severe cases
-
Contraindicated in head trauma, pregnancy, and with other medications that cause sedation### Opioids
-
Opioids are not potent enough to cause an overdose or trigger euphoria, making them a safer alternative to methadone.
Side Effects
- Stimulation of opioid receptors in the central nervous system can cause euphoria or dysphoria (unhappiness and dissatisfaction).
- Stimulation of opioid receptors in the GI tract causes a decrease in motility and constipation.
- Stimulation of opioid receptors in the biliary tract increases motility, worsening pain during biliary colic.
- Other side effects include:
- Pinpoint pupils (pupillary constriction)
- Flushing
- Nausea
Opioid Overdose
- Can cause cardiac and central nervous system depression, leading to arrhythmias and coma.
- Respiratory depression is the most common cause of death from opioid use, due to decreased activity in the medulla.
- CO2 retention leads to dilation of blood vessels, including those in the brain, causing cerebral vasodilation and increased intracranial pressure.
- Contraindicated in patients with head injuries due to increased susceptibility to increased intracranial pressure.
- Opioids should be avoided during pregnancy, as they can cause dependence in the baby.
Withdrawal Symptoms
- Experienced by chronic users who stop treatment, including:
- Anxiety
- Agitation
- Confusion
- Sweating
- Skin crawling feeling
- Severe withdrawal symptoms can be managed with methadone and buprenorphine combined with naloxone.
Mnemonic for Opioids
- Full agonists:
- Morphine
- Meperidine
- Oxycodone
- Partial agonists:
- Buprenorphine
- Naloxone
- Butorphanol
- Pentazocine
- Tramadol
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Description
Learn how endorphins interact with neurotransmitters like dopamine, serotonin, and norepinephrine to regulate pain sensitivity in the brain and spinal cord. Understand the role of GABA and the reward pathway in this process. Test your knowledge of neurochemistry and pain management!
