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Local Anesthetics

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38 Questions

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

Lipid solubility

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

Inversely proportional

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

Profound lipophilicity

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

Low pKa

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

Delays onset of action

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

Increased lipid solubility

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

Aδ sensory

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

Site of injection

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

Bupivacaine

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

Protein binding is inversely proportional to plasma concentration

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

Chloroprocaine

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

Lipid solubility

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

Increased duration of action

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

Speeds up the onset speed

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

Cocaine

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

Increases the time

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

Onset speed

Which pharmacologic property correlates with a decrease in drug duration?

Decreased lipid solubility

What effect does increased myelination have on nerve conduction?

Increases conduction speed

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

Preventing sodium influx

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

Increased action potentials per unit time

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

C sensory fibers

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

Tissue injury

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

Aα motor first, B preganglionic sympathetic last.

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

C sensory fibers.

What factor can prolong lidocaine metabolism and elimination the most?

Renal dysfunction

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

Benzoicaine

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

Procaine

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

Tetracaine

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

To decrease the rate of vascular absorption

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

Cocaine

Where are vasoconstrictors commonly added to local anesthetics?

To decrease systemic absorption

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

Procaine

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

True

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

False

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

False

Adding vasoconstrictors to local anesthetics decreases the density of blockade.

False

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

True

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