Pharmacology Chapter 20: Local Anesthetics
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Questions and Answers

What is a common systemic toxicity effect of local anesthetics?

  • Allergic reaction
  • Cardiovascular depression
  • Neurotoxicity (correct)
  • Respiratory failure
  • Which of the following is a characteristic of ester-type local anesthetics?

  • They are more likely to cause allergic reactions
  • They are more stable than amide-type local anesthetics
  • They are more potent than amide-type local anesthetics
  • They are metabolized by pseudocholinesterase in the plasma (correct)
  • What is the primary mechanism by which local anesthetics interact with voltage-gated Na+ channels?

  • They block the pore of the Na+ channel
  • They inhibit the inactivation of the Na+ channel
  • They bind to the alpha subunit of the Na+ channel (correct)
  • They alter the gating mechanisms of the Na+ channel
  • Which of the following local anesthetics is known for its high lipid solubility and potential for systemic toxicity?

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

    What is the primary factor that determines the duration of action of local anesthetics?

    <p>The rate of metabolism of the local anesthetic</p> Signup and view all the answers

    Which of the following is a characteristic of chiral forms of local anesthetics?

    <p>They have different pharmacodynamic properties</p> Signup and view all the answers

    Study Notes

    Local Anesthetics

    • Local anesthetics are a group of structurally related compounds that share a principal mechanism of action: blocking voltage-gated sodium channels, resulting in reversible interruption of nerve signal transduction.

    Historical Perspective

    • Cocaine, the first local anesthetic, was isolated from leaves of the coca plant, Erythroxylum coca, by Albert Niemann in 1860.

    Chemical Structure and Physicochemical Properties

    • Local anesthetics can be classified into two classes: ester-type and amide-type.

    Pharmacodynamics

    • Local anesthetics bind to voltage-gated Na+ channels and block depolarizing Na+ current through these channels.

    Mechanism of Nerve Block

    • Local anesthetics interrupt nerve signal transduction by blocking voltage-gated sodium channels, resulting in reversible nerve block.

    Pharmacokinetics

    • Local anesthetics undergo absorption, distribution, and metabolism, and can cause systemic toxicity, including lipid rescue, neurotoxicity, and other tissue toxicity.

    Specific Local Anesthetics

    • Amide local anesthetics include lidocaine and prilocaine.

    Local Anesthetics

    • Local anesthetics are a group of structurally related compounds that share a principal mechanism of action: blocking voltage-gated sodium channels, resulting in reversible interruption of nerve signal transduction.

    Historical Perspective

    • Cocaine, the first local anesthetic, was isolated from leaves of the coca plant, Erythroxylum coca, by Albert Niemann in 1860.

    Chemical Structure and Physicochemical Properties

    • Local anesthetics can be classified into two classes: ester-type and amide-type.

    Pharmacodynamics

    • Local anesthetics bind to voltage-gated Na+ channels and block depolarizing Na+ current through these channels.

    Mechanism of Nerve Block

    • Local anesthetics interrupt nerve signal transduction by blocking voltage-gated sodium channels, resulting in reversible nerve block.

    Pharmacokinetics

    • Local anesthetics undergo absorption, distribution, and metabolism, and can cause systemic toxicity, including lipid rescue, neurotoxicity, and other tissue toxicity.

    Specific Local Anesthetics

    • Amide local anesthetics include lidocaine and prilocaine.

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    Description

    This quiz covers the pharmacological aspects of local anesthetics, including their mechanism of action and effects on nerve signal transduction.

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