Local Anesthetics

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Questions and Answers

What physiochemical property of local anesthetics is described as the most important by Barash?

  • Vasoactive properties
  • Protein binding
  • Lipid solubility (correct)
  • pKa

How does the percentage of a local anesthetic in its neutral, non-protonated form relate to its pKa value?

  • No relationship
  • Exponential relationship
  • Directly proportional
  • Inversely proportional (correct)

Which characteristic of a local anesthetic molecule would lead to rapid entry into the lipid bilayer but potential sequestration?

  • Profound lipophilicity (correct)
  • High pKa
  • Low protein binding
  • Low lipid solubility

What property is associated with the rapid penetration of the lipid membrane by a local anesthetic?

<p>Low pKa (B)</p> Signup and view all the answers

How does increased lipid solubility affect the onset of action of a local anesthetic?

<p>Delays onset of action (A)</p> Signup and view all the answers

What factor is primarily responsible for increasing the duration of action of a local anesthetic?

<p>Increased lipid solubility (B)</p> Signup and view all the answers

Which type of nerve fibers would be affected first with differential blockade?

<p>Aδ sensory (A)</p> Signup and view all the answers

Which factor has the GREATEST influence on the amount of local anesthetic in the systemic circulation?

<p>Site of injection (A)</p> Signup and view all the answers

Which local anesthetic has the SLOWEST rate of metabolism by hepatic enzymes?

<p>Bupivacaine (D)</p> Signup and view all the answers

What is the relationship between protein binding and plasma concentration of local anesthetics?

<p>Protein binding is inversely proportional to plasma concentration (B)</p> Signup and view all the answers

Which local anesthetic has the FASTEST rate of metabolism by plasma cholinesterase?

<p>Chloroprocaine (A)</p> Signup and view all the answers

Which property of local anesthetics is considered the most important physiochemical property according to the text?

<p>Lipid solubility (D)</p> Signup and view all the answers

What effect does increased protein binding have on the duration of action of local anesthetics?

<p>Increased duration of action (A)</p> Signup and view all the answers

In relation to onset speed, what is the impact of increasing the dose/concentration of local anesthetics?

<p>Speeds up the onset speed (B)</p> Signup and view all the answers

Which local anesthetic is highlighted as an exception due to its vasoconstrictive properties?

<p>Cocaine (A)</p> Signup and view all the answers

How does increasing the lipophilicity of a local anesthetic impact the time to release the drug from lipid depots?

<p>Increases the time (C)</p> Signup and view all the answers

Which factor most reliably correlates with the pKa of a local anesthetic according to the text?

<p>Onset speed (D)</p> Signup and view all the answers

Which pharmacologic property correlates with a decrease in drug duration?

<p>Decreased lipid solubility (C)</p> Signup and view all the answers

What effect does increased myelination have on nerve conduction?

<p>Increases conduction speed (C)</p> Signup and view all the answers

What is the mechanism behind disrupting impulse conduction by local anesthetics?

<p>Preventing sodium influx (D)</p> Signup and view all the answers

In Tonic Inhibition, slower firing fibers are less susceptible to blockade due to what characteristic?

<p>Increased action potentials per unit time (A)</p> Signup and view all the answers

Which nerve type is MOST susceptible to blockade by local anesthetics?

<p>C sensory fibers (C)</p> Signup and view all the answers

What condition increases the action potential frequency, making fibers more susceptible to blockade?

<p>Tissue injury (A)</p> Signup and view all the answers

What is the clinical sequence of nerve blockade when increasing local anesthetic concentrations?

<p>Aα motor first, B preganglionic sympathetic last. (C)</p> Signup and view all the answers

Which fiber type is considered least susceptible to blockade by local anesthetics?

<p>C sensory fibers. (C)</p> Signup and view all the answers

What factor can prolong lidocaine metabolism and elimination the most?

<p>Renal dysfunction (C)</p> Signup and view all the answers

Which local anesthetic has a chemistry that can potentially produce methemoglobinemia at high doses?

<p>Benzoicaine (C)</p> Signup and view all the answers

Historically, which local anesthetic was primarily used in spinal anesthesia but is now rare outside dental applications?

<p>Procaine (C)</p> Signup and view all the answers

Which local anesthetic is mainly used topically in ophthalmology and provides a profound motor and sensory block?

<p>Tetracaine (D)</p> Signup and view all the answers

What is the primary purpose of adding vasoconstrictors to local anesthetics?

<p>To decrease the rate of vascular absorption (C)</p> Signup and view all the answers

Which local anesthetic is known for its intense vasoconstriction properties and is primarily used in nasopharyngeal procedures?

<p>Cocaine (D)</p> Signup and view all the answers

Where are vasoconstrictors commonly added to local anesthetics?

<p>To decrease systemic absorption (D)</p> Signup and view all the answers

Which local anesthetic has a slow onset and short duration, and was historically used mainly in spinal anesthesia?

<p>Procaine (B)</p> Signup and view all the answers

Chloroprocaine (Nesacaine) is primarily used for epidural analgesia conversion to anesthesia.

<p>True (A)</p> Signup and view all the answers

Benzoicaine (Hurricaine) has a duration of 60-90 minutes.

<p>False (B)</p> Signup and view all the answers

Mepivacaine (Carbocaine) has a slower onset compared to lidocaine.

<p>False (B)</p> Signup and view all the answers

Adding vasoconstrictors to local anesthetics decreases the density of blockade.

<p>False (B)</p> Signup and view all the answers

Local anesthetics like lidocaine are primarily used for chronic neuropathic pain management.

<p>True (A)</p> Signup and view all the answers

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Local Anesthetics (SPR2024) PDF
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