Pharmacology of Acetylcholine Blockers
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Pharmacology of Acetylcholine Blockers

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Questions and Answers

What is a common postoperative complaint associated with succinylcholine use?

  • Nausea
  • Muscle pain (correct)
  • Excessive sweating
  • Dehydration
  • In which patient population is succinylcholine more likely to cause hyperkalemia?

  • Patients with diabetes
  • Patients with severe burns (correct)
  • Elderly patients
  • Pregnant women
  • Which adverse effect can result from fasciculations caused by succinylcholine?

  • Increased blood pressure
  • Regurgitation (correct)
  • Hypoglycemia
  • Liver failure
  • Which inhaled anesthetic specifically prolongs neuromuscular blockade when used with succinylcholine?

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

    What is a very early sign of malignant hyperthermia associated with succinylcholine use?

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

    How should the dosing of nondepolarizing blockers be adjusted for older patients?

    <p>Reduce the dose</p> Signup and view all the answers

    Why might patients with severe burns be less responsive to nondepolarizing neuromuscular blockers?

    <p>Proliferation of extra-junctional nicotinic receptors</p> Signup and view all the answers

    Which types of drugs may also potentiate the action of neuromuscular blockers?

    <p>Aminoglycoside antibiotics and antiarrhythmic drugs</p> Signup and view all the answers

    Which of the following are examples of non-depolarizing neuromuscular blockers?

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

    What is the primary action of non-depolarizing neuromuscular blockers?

    <p>Block acetylcholine receptors</p> Signup and view all the answers

    Which of the following compounds is known to inhibit acetylcholine release?

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

    Which characteristic of neuromuscular blockers means that their effects can be reversed by increasing acetylcholine levels?

    <p>Surmountable blockade</p> Signup and view all the answers

    Which of the following is classified as a muscle action spasmolytic agent?

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

    Which neurotransmitter is cleaved by cholinesterase to reverse the effects of neuromuscular blockers?

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

    Which non-depolarizing neuromuscular blocker is noted for having the fastest onset time?

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

    What is the primary mechanism by which succinylcholine induces muscle relaxation?

    <p>It acts as a nicotinic agonist at the neuromuscular end plate.</p> Signup and view all the answers

    Which of the following substances is a known inhibitor of acetylcholine synthesis?

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

    Which drug is metabolized by plasma cholinesterase?

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

    What is a possible side effect of high blood levels of laudanosine?

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

    Cisatracurium is preferred over atracurium in clinical practice primarily because it:

    <p>Forms less laudanosine.</p> Signup and view all the answers

    What happens to the effect of succinylcholine during continuous infusion?

    <p>It transitions to a phase II block characterized by repolarization.</p> Signup and view all the answers

    Which non-depolarizing neuromuscular blocker has a duration of action less than 35 minutes?

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

    What type of muscle block is caused by succinylcholine during its initial action?

    <p>Continuous depolarization with fasciculations</p> Signup and view all the answers

    What distinguishes atracurium from other neuromuscular blockers?

    <p>It undergoes rapid spontaneous breakdown.</p> Signup and view all the answers

    Study Notes

    Acetylcholine Blockers

    • Depolarizing Agents: Include Suxamethonium (Succinylcholine) and Decamethonium.
    • Non-Depolarizing Agents:
      • Isoquinoline Derivatives: Tubocurarine, Atracurium, Cisatracurium, Metocurine, Doxacurium, Mivacurium.
      • Steroid Derivatives: Pancuronium, Vecuronium, Pipecuronium, Rocuronium.
      • Others: Gallamine.

    Mechanisms of Non-Depolarizing Blockers

    • Non-depolarizing drugs act as surmountable blockers at the skeletal muscle end plate by competing with acetylcholine (ACh) at the receptor.
    • Their effects can be reversed with cholinesterase inhibitors.
    • Larger muscles recover more rapidly from neuromuscular blockade compared to smaller muscles.

    Pharmacokinetics of Non-Depolarizing Blockers

    • Administered parenterally and highly polar, unable to cross the blood-brain barrier.
    • Duration of action varies:
      • Drugs metabolized by plasma cholinesterase (e.g., Mivacurium) have shorter effects (10-20 min).
      • Renal elimination leads to longer durations (up to 35 min) for drugs like Metocurine, Pancuronium, and Tubocurarine.
    • Atracurium undergoes Hofmann elimination, which may lead to seizure risk due to laudanosine.

    Depolarizing Neuromuscular Blocking Drugs

    • Mechanism of Action: Succinylcholine acts as a nicotinic agonist, leading to continuous depolarization, muscle relaxation, and paralysis.
    • Phase Effects: Continuous infusion shifts from Phase I (depolarization) to Phase II (repolarization resistance).

    Specific Effects of Succinylcholine

    • Common side effects include postoperative muscle pain and potential hyperkalemia, especially in high-risk patients.
    • Fasciculations can increase intragastric pressure, which may lead to regurgitation and aspiration risks.

    Drug Interactions

    • Inhaled anesthetics like isoflurane can potentiate and prolong neuromuscular blockade.
    • Potential for malignant hyperthermia is associated with succinylcholine; initial symptom is trismus (jaw muscle contraction).
    • Certain antibiotics and antiarrhythmic medications may also enhance effects of neuromuscular blockers.

    Patient Sensitivity

    • Older adults (>75 years) and myasthenia gravis patients are more sensitive to non-depolarizing blockers; dosing adjustments are necessary.
    • Patients with severe burns or upper motor neuron diseases show reduced responsiveness due to increased extra-junctional nicotinic receptors.

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    Description

    This quiz covers various drugs that inhibit the action of acetylcholine, including depolarizing and non-depolarizing agents. Test your knowledge on specific drug classes such as isoquinoline and steroid derivatives. Understand their mechanisms and clinical uses in pharmacology.

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