6 Questions
What is a common systemic toxicity effect of local anesthetics?
Neurotoxicity
Which of the following is a characteristic of ester-type local anesthetics?
They are metabolized by pseudocholinesterase in the plasma
What is the primary mechanism by which local anesthetics interact with voltage-gated Na+ channels?
They bind to the alpha subunit of the Na+ channel
Which of the following local anesthetics is known for its high lipid solubility and potential for systemic toxicity?
Bupivacaine
What is the primary factor that determines the duration of action of local anesthetics?
The rate of metabolism of the local anesthetic
Which of the following is a characteristic of chiral forms of local anesthetics?
They have different pharmacodynamic properties
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.
This quiz covers the pharmacological aspects of local anesthetics, including their mechanism of action and effects on nerve signal transduction.
Make Your Own Quizzes and Flashcards
Convert your notes into interactive study material.
Get started for free
