Opioid Overdose Effects and Treatment
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Questions and Answers

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

  • No change in protein binding or sensitivity
  • Less sensitivity to the drug
  • Increased protein binding
  • Less protein binding and greater sensitivity to the drug (correct)

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

  • It can be used orally for chronic pain
  • It is effective in treating diarrhea
  • It is a potent cough suppressant
  • It can be used intrathecally due to its blockade of sodium channels (correct)

    • What is a potential complication of prolonged infusions of meperidine?

  • Respiratory depression
  • Tachyphylaxis
  • Normeperidine toxicity (correct)
  • Hypertension

    • 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.

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