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Opioidy

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Questions and Answers

What is the primary purpose of opioid agonists?

To control acute or chronic pain

What is the effect of endorphins on inhibitory neurons?

They activate the mu, kappa, and delta receptors

What is the goal when treating pain with opioids?

To use short-acting opioids at the lowest effective dose for a few days

What is the role of GABA in the brain?

<p>It prevents the release of neurotransmitters</p> Signup and view all the answers

What is the origin of exogenous opioids like heroin and morphine?

<p>They come from outside the body, from the opium poppy</p> Signup and view all the answers

What is the effect of exercise on endorphins?

<p>It releases endorphins, which activate opioid receptors</p> Signup and view all the answers

What is the primary risk of combining opioids with other central nervous system depressants?

<p>Additive CNS depression</p> Signup and view all the answers

Why are opioids contraindicated in patients with head injury?

<p>Increased intracranial pressure</p> Signup and view all the answers

What is the primary cause of death from opioid overdose?

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

What is the purpose of combining naloxone with buprenorphine in the treatment of opioid use disorder?

<p>To reduce the risk of opioid overdose</p> Signup and view all the answers

What is the primary mechanism of action of opioids in the gastrointestinal tract?

<p>Decreased motility</p> Signup and view all the answers

What is the primary mechanism of action of opioids in the biliary tract?

<p>Increased motility</p> Signup and view all the answers

What is the primary risk of using opioids during pregnancy?

<p>Risk of dependence in the baby</p> Signup and view all the answers

What is the primary mechanism of action of opioids in the central nervous system?

<p>Stimulation of opioid receptors</p> Signup and view all the answers

What is the primary role of methadone in the treatment of opioid use disorder?

<p>To treat opioid use disorder</p> Signup and view all the answers

What is the primary mechanism of action of partial agonists like buprenorphine?

<p>Partial stimulation of opioid receptors</p> Signup and view all the answers

What is the result of dopamine release in the brain?

<p>A calming sensation that feels really good</p> Signup and view all the answers

Which of the following opioids acts as a full agonist but does not cause euphoria?

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

What is the effect of endorphins binding to opioid receptors?

<p>Blockage of inhibitory neuron from releasing GABA</p> Signup and view all the answers

Which of the following opioids is a mixed agonist-antagonist?

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

What is the effect of norepinephrine and serotonin release in pain processing regions of the brain?

<p>Decreased sensitivity to pain</p> Signup and view all the answers

Which opioid receptor is buprenorphine an antagonist at?

<p>Kappa receptor</p> Signup and view all the answers

What is the effect of tramadol when given with a full agonist?

<p>It decreases the overall effect of the full agonist</p> Signup and view all the answers

What is the benefit of methadone in treating opioid use disorder?

<p>It blocks the euphoric feeling that comes from taking other opioids</p> Signup and view all the answers

What is the mechanism of action of codeine and hydrocodone as an antitussive?

<p>The mechanism is unknown</p> Signup and view all the answers

What is the effect of fentanyl as an anesthetic medication?

<p>It has a rapid onset and short duration of action</p> Signup and view all the answers

Which opioid receptor agonist is most likely to cause severe respiratory depression?

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

What is the primary mechanism of action of opioids in reducing pain perception?

<p>Stopping inhibitory neurons from releasing inhibitory neurotransmitters</p> Signup and view all the answers

Why are opioids contraindicated in people with head trauma?

<p>Because they can increase intracranial pressure</p> Signup and view all the answers

What is the main reason why opioids should be avoided during pregnancy?

<p>Because they can cause fetal harm</p> Signup and view all the answers

Which of the following opioids is a partial agonist?

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

What is the significance of the constipated man statue in the park?

<p>It represents dysphoria</p> Signup and view all the answers

What is the primary effect of opioids on neurotransmitters in the central nervous system?

<p>Increase the release of dopamine, norepinephrine, and serotonin</p> Signup and view all the answers

Which of the following opioids is classified as a full agonist?

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

What is the significance of the ice cream vendor in the park?

<p>Representing the CNS, cardiovascular, and respiratory depression side effects of opioids</p> Signup and view all the answers

Why are opioids contraindicated in people with biliary colic?

<p>Because they can cause nausea and vomiting</p> Signup and view all the answers

What is the effect of opioids on inhibitory neurons in the central nervous system?

<p>They block the release of inhibitory neurotransmitters</p> Signup and view all the answers

What is the significance of the woman's pregnancy in the garden?

<p>It serves as a reminder that opioids should be avoided if possible during pregnancy</p> Signup and view all the answers

What is the primary function of inhibitory neurons in the brain tissue?

<p>To prevent nearby neurons from releasing neurotransmitters like dopamine, serotonin, and norepinephrine</p> Signup and view all the answers

What happens to the release of neurotransmitters like dopamine, serotonin, and norepinephrine when endorphins bind to opioid receptors?

<p>It decreases significantly</p> Signup and view all the answers

Why are opioids used to treat diarrhea?

<p>Because they slow down the movement of food in the gastrointestinal tract</p> Signup and view all the answers

What is the source of exogenous opioids like heroin and morphine?

<p>The opium poppy plant</p> Signup and view all the answers

What is the goal when using opioids to control pain?

<p>To use short-acting opioids at the lowest effective dose for just a few days</p> Signup and view all the answers

What is the effect of exercise on the release of endorphins in the brain?

<p>It increases the release of endorphins</p> Signup and view all the answers

What is the outcome of norepinephrine and serotonin release in the thalamus, brainstem, and spinal cord?

<p>Decreased sensitivity to pain</p> Signup and view all the answers

Which opioid receptor does buprenorphine act as a partial agonist at?

<p>Mu receptor</p> Signup and view all the answers

What is the effect of dopamine release in the ventral tegmental area, nucleus accumbens, and prefrontal cortex?

<p>A calming sensation that feels really good</p> Signup and view all the answers

What is the effect of opioid stimulation on the GI tract?

<p>Decreased motility and constipation</p> Signup and view all the answers

Which opioid is used to relax uterine muscles and inhibit contractions during labor?

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

Why are opioids contraindicated in patients with head injury?

<p>Because they can increase intracranial pressure</p> Signup and view all the answers

What is the primary mechanism of action of opioids in reducing pain perception?

<p>Blocking the release of GABA</p> Signup and view all the answers

What is the primary cause of death from opioid overdose?

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

What is the effect of giving a partial agonist with a full agonist?

<p>Decreased overall effect</p> Signup and view all the answers

What is the effect of opioids on the biliary tract?

<p>Increased motility and worsened biliary colic</p> Signup and view all the answers

Which opioid receptor is butorphanol a partial agonist at?

<p>Kappa receptor</p> Signup and view all the answers

What is the benefit of methadone in treating opioid use disorder?

<p>It can reduce opioid dependence</p> Signup and view all the answers

What is the advantage of using methadone in treating opioid use disorder?

<p>It does not cause euphoria and blocks the euphoric feeling from other opioids</p> Signup and view all the answers

Which opioid is used to treat diarrhea?

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

What is the effect of combining opioids with other CNS depressants?

<p>Additive CNS depression</p> Signup and view all the answers

What is the primary mechanism of action of full agonists like morphine?

<p>Completely inhibiting GABA release</p> Signup and view all the answers

What is the effect of buprenorphine on opioid receptors?

<p>It is a partial agonist</p> Signup and view all the answers

What is the primary risk of using opioids during pregnancy?

<p>Dependence in the baby</p> Signup and view all the answers

What is the effect of opioid withdrawal?

<p>Anxiety and agitation</p> Signup and view all the answers

What is the benefit of tapering off opioid use?

<p>It can safely eliminate opioid use</p> Signup and view all the answers

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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