Opioid Overdose Effects and Treatment
59 Questions
5 Views
3.7 Stars

Opioid Overdose Effects and Treatment

This quiz covers the effects of opioid overdose on respiration, pupil size, and treatment options. Learn about the symptoms and duration of opioid overdose.

Created by
@SleekDramaticIrony

Questions and Answers

Which of the following is a characteristic of meperidine in elderly patients?

Less protein binding and greater sensitivity to the drug

What is a unique feature of meperidine's use in clinical settings?

It can be used intrathecally due to its blockade of sodium channels

What is a potential complication of prolonged infusions of meperidine?

Normeperidine toxicity

What is a characteristic of fentanyl that distinguishes it from morphine?

<p>Greater potency and quicker onset of action due to its lipid solubility</p> Signup and view all the answers

Where does fentanyl redistribute rapidly after administration?

<p>Fat and lungs</p> Signup and view all the answers

What is the primary treatment for opioid-induced apnea?

<p>Mechanical ventilation and an opioid antagonist</p> Signup and view all the answers

Which of the following opioids has the shortest duration of action and should be administered with a longer-acting analgesic to prevent acute hyperalgesia ?

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

What is the effect of hypercarbia on morphine's effects?

<p>Increases cerebral blood flow and morphine effects</p> Signup and view all the answers

What is the primary effect of normeperidine, a metabolite of meperidine?

<p>CNS stimulation</p> Signup and view all the answers

What is the primary route of elimination for morphine metabolites?

<p>Urinary excretion - Renal failure impairs elimination of morphine metabolites which are active</p> Signup and view all the answers

What is the relative potency of meperidine compared to morphine?

<p>1/10 the potency of morphine</p> Signup and view all the answers

What is the characteristic of opioid agonist-antagonists at μ receptors?

<p>They produce limited responses or no effect</p> Signup and view all the answers

What is an advantage of opioid agonist-antagonists?

<p>They produce limited depression of ventilation and have low abuse potential</p> Signup and view all the answers

What is a disadvantage of opioid agonist-antagonists?

<p>They reduce the analgesic effect of previously administered agonists</p> Signup and view all the answers

What is the effect of opioid antagonists on opioid agonists?

<p>They displace opioid agonists from the μ receptor</p> Signup and view all the answers

Which of the following is an opioid agonist-antagonist?

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

What is the characteristic of opioid agonist-antagonists at κ and δ receptors?

<p>They produce limited responses</p> Signup and view all the answers

What is the duration of action of Naloxone?

<p>30-40 minutes</p> Signup and view all the answers

What is the primary indication for Nalmefene?

<p>Long acting treatment of opioid overdose</p> Signup and view all the answers

What are common side effects of neuraxial opioids?

<p>All of the above</p> Signup and view all the answers

What is a potential effect of neuraxial opioids on gastric function?

<p>Delayed gastric emptying</p> Signup and view all the answers

What is a potential complication of neuraxial opioid injection?

<p>Spinal cord injury from preservative-containing solutions such as those found in morphine</p> Signup and view all the answers

Why does morphine have a slow onset of action?

<p>Due to its poor lipid solubility and high degree of ionization</p> Signup and view all the answers

What is unique about the metabolite of morphine, morphine-6-glucuronide?

<p>It has analgesic effects and a greater duration of action than morphine</p> Signup and view all the answers

What effect does hyperventilation have on morphine ionization?

<p>Increase in ionization due to increasing the pH of the blood causing morphine to become more water soluble</p> Signup and view all the answers

What is the result of morphine administered with nitrous oxide?

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

How are opioids metabolized in the body?

<p>Oxidized by the liver via CP450 enzymes and excreted through the kidneys</p> Signup and view all the answers

What is a complication of neuraxial morphine related to its poor lipid solubility?

<p>Respiratory depression due to its increased rostral migration to the respiratory centers in the brain</p> Signup and view all the answers

What is the result of binding of opioid to opioid GPCR in nociceptive pathways?

<p>Neuronal hyperpolarization and decreased neuronal activity</p> Signup and view all the answers

When an opioid binds to a GPCR, what is the resulting order of events to cause decreased neuronal activity in nociceptive pathways?

<p>GPCR activation → inhibition of adenylate cyclase → decrease in cAMP → decreased Ca conductance and increased outward flow of K → decreased neuronal activity</p> Signup and view all the answers

What is tolerance?

<p>Receptor desensitization resulting in decreased number of receptors</p> Signup and view all the answers

What is dependence in the context of opioid use?

<p>The capacity to experience withdrawal when opioids are tapered or when an opioid reversal agent is given</p> Signup and view all the answers

What is the role of NMDA glutamate receptors in the context of opioid use?

<p>They are involved in the development of opioid tolerance and increased pain sensitivity</p> Signup and view all the answers

What can increased camp production in tolerance lead to?

<p>Dependence and withdrawal symptoms</p> Signup and view all the answers

What effect do opioids have on cerebral blood flow and ICP in the event of normal PaCO2?

<p>Decrease cerebral blood flow and possibly ICP</p> Signup and view all the answers

What is the result of hyperpolarization at the opioid receptor?

<p>Interruption of the presynaptic NT release of Ach, dopamine, NE, and substance P</p> Signup and view all the answers

What effects do opioids have on the cardiovascular system?

<p>Decreased sympathetic tone</p> Signup and view all the answers

What is a potential consequence of histamine release in opioids?

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

What are the respiratory consequences of opioid administration?

<p>Chest wall/muscle rigidity</p> Signup and view all the answers

What is a possible mechanism behind chest wall rigidity in opioid administration?

<p>Inhibition of GABA resulting increased muscle tone</p> Signup and view all the answers

Where are mu receptors predominantly located?

<p>Brain and spinal cord</p> Signup and view all the answers

What are the common side effects of neuraxial opioid use?

<p>Urticaria, nausea, and pruritis secondary to histamine release</p> Signup and view all the answers

What causes nausea and vomiting after opioid administration?

<p>Stimulation of the CTZ and stimulation of dopaminergic receptors</p> Signup and view all the answers

What are significant side effects of meperidine?

<p>All of the above</p> Signup and view all the answers

Rank the following opioids from most potent to least potent: morphine, fentanyl, and sufentanil.

<p>Sufentanil, fentanyl, morphine</p> Signup and view all the answers

As compared to fentanyl, what is unique about sufentanil?

<p>It produces longer analgesia and less respiratory depression than fentanyl</p> Signup and view all the answers

How is sufentanil similar to fentanyl?

<p>Rapid effect site equilibration time</p> Signup and view all the answers

Alfentanil has a longer context sensitive half time than sufentanil

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

What is unique about the context-sensitive half-time of fentanyl?

<p>Prolonged infusions (&gt;2 hours) lead to saturation of inactive tissues and increases in Context Sensitive Half Time greater than sufentanil</p> Signup and view all the answers

What is the reason for the prolonged elimination half-time of fentanyl?

<p>High lipid solubility and sequestration in peripheral tissues</p> Signup and view all the answers

Compared to fentanyl, alfentanil is:

<p>1/5 as potent</p> Signup and view all the answers

What is the reason for the onset of action for alfentanil being shorter than either fentanyl or sufentanil?

<p>Rapid effect site equilibration (1.4 minutes)</p> Signup and view all the answers

What is the effect of a low pKa on alfentanil's ability to cross the blood-brain barrier?

<p>It allows 90% of the drug to exist in the nonionized state, enabling greater penetration of the blood-brain barrier despite lower lipid solubility</p> Signup and view all the answers

What are the disadvantages of alfentanil?

<p>Interindividual variability of alfentanil pharmacokinetics varies 10-fold</p> Signup and view all the answers

Alfentanil provoke less post-operative nausea and vomiting (PONV) than equipotent doses of fentanyl or sufentanil

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

Remifentanil is equipotent to fentanyl

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

What is the effect site equilibration time of remifentanil similar to?

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

How is Remifentanil metabolized in the body?

<p>It undergoes hydrolysis by non-specific plasma and tissue esterase to inactive metabolites</p> Signup and view all the answers

What is the dose of remifentanil based on?

<p>Lean body weight</p> Signup and view all the answers

Study Notes

Opioids

  • Depression of respiration leading to apnea, and symmetric miosis leading to mydriasis (hypoxemia) are common effects of opioid overdose, which can be treated with mechanical ventilation and an opioid antagonist.
  • Onset of opioid overdose is most rapid with opioids with the shortest duration of action.

Withdrawal Symptoms

  • Symptoms of opioid withdrawal include abdominal cramps, nausea, vomiting, diarrhea, lacrimation, coryza, restlessness, and insomnia.

Specific Opioid Agonists

  • Morphine:
    • Pharmacokinetics: good IM absorption, onset of action 15-30 minutes, duration @ 4 hours, peak brain concentrations lag behind peak plasma concentrations, high degree of ionization, and poor lipid solubility.
    • Metabolism and elimination: conjugation with glucuronic acid in liver and kidney, excretion in urine (slight fraction in bile), active metabolite morphine-6-glucuronide has analgesic effects and a greater duration of action than morphine.
  • Meperidine:
    • Structurally similar to fentanyl, sufentanil, alfentanil, remifentanil, and local anesthetics, with mild atropine-like anti-spasmodic effects on smooth muscle.
    • Approximately 1/10 the potency of morphine.
    • Metabolism and elimination: hepatic metabolism produces normeperidine by demethylation (90%), normeperidine has an elimination half-life of 15 hours (normal) to 35 hours (renal failure), and is a CNS stimulant.
    • Clinical uses: can be used intrathecally due to blockade of sodium channels, decreases post-operative shivering, kappa opioid receptor stimulation, alpha2 agonist activity, but is not useful for treatment of diarrhea and is not a cough suppressant.
    • Side effects: tachycardia secondary to atropine-like effects, negative inotropy & decreased myocardial contractility, delirium & seizures, ventilatory depression, and mydriasis.

Fentanyl

  • Pharmacokinetics: greater lipid solubility, onset of action is more rapid, and potency is greater than morphine.
  • Short duration of action reflects rapid redistribution to inactive tissues (fat and skeletal muscle).
  • Pulmonary uptake approaches 75% of an initial dose.

Opioid Agonist-Antagonists

  • These drugs bind to μ receptors and produce limited responses (partial agonist) or no effect (competitive antagonists).
  • Features: production of analgesia with limited depression of ventilation and low abuse potential, ceiling effect above which further agonist effects do not appear.
  • Disadvantages: reduction in the analgesic effect of previously administered agonists, and dysphoric reactions.

Opioid Antagonists

  • These agents bind to the μ receptor and exert no agonist activity, displacing opioid agonists from the μ receptor.
  • Agents: naloxone, naltrexone, nalmefene, methylnaltrexone, and alvimopan.

Naloxone

  • Binds to all three opioid receptors.
  • Promptly reverses opioid-induced analgesia and respiratory depression.
  • Short duration of action (30-40 minutes) may necessitate redosing if used to treat the effects of a long-acting opioid.
  • Uses: post-op ventilatory depression, neonatal respiratory depression secondary to maternal opioid use, treatment of deliberate/accidental opioid overdose, and detection of suspected opioid dependence.

Neuraxial Opioids

  • Most side effects are dose-dependent.
  • Pruritus is localized to the face, neck, and thorax.
  • Urinary retention is more common in males.
  • Depression of ventilation reflects systemic absorption of opioid.
  • Rate is approximately 1%.
  • Delayed depression more commonly associated with neuraxial morphine.
  • Sedation tends to be dose-related and is most common with sufentanil.
  • Reactivation of herpes simplex labialis virus (cold sores) 2-5 days after epidural morphine.
  • Maternal administration of epidural opioids during labor may produce depression of ventilation in newborns.
  • Neuraxial opioids may delay gastric emptying.
  • Inhibition of shivering and heat loss.
  • Spinal cord injury from injection of preservative-containing solutions.

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Quiz Team

More Quizzes Like This

Use Quizgecko on...
Browser
Browser