Local Anesthetics Flashcards
How many types of Local Anesthetics are there?
A) Esters
B) Amides
C) Both Esters and Amides
D) Neither
C) Esters and Amides
What is the primary mechanism of action (MOA) for local anesthetics?
A) Inhibition of K+ channels
B) Binding to GPCR receptors
C) Blocking voltage-gated Na+ channels
D) Activating Ca2+ channels
C) Blocking voltage-gated Na+ channels during the activated and/or inactivated state.
Blocks/inhibits Na+ current to ↓excitability of neuronal, cardiac, or CNS tissue.
Local anesthetics can also bind to which of the following channels or receptors besides Na+ channels?
A) K+ and Ca2+ channels, and GPCR receptors
B) Only Ca2+ channels
C) Only K+ channels
D) Only GPCR receptors
A) K+ and Ca2+ channels, and GPCR receptors
Blocks/inhibits Na+ current to ↓excitability of neuronal, cardiac, or CNS tissue.
What is the goal for the Minimum Effective Concentration (MEC) of a local anesthetic?
A) To block 1-2 nodes of Ranvier
B) To block 3-4 nodes of Ranvier
C) To block 2-3 nodes of Ranvier
D) To block 4-5 nodes of Ranvier
C) To block 2-3 nodes of Ranvier
Why are local anesthetics often mixed with epinephrine?
A) To increase their pH
B) To enhance their lipid solubility
C) To reduce their intrinsic vasodilatory effects
D) To decrease their potency
C) To reduce their intrinsic vasodilatory effects
What is the effect of having a local anesthetic with a pKa that is closest to the physiologic pH?
A) Slower onset of action
B) Faster onset of action
C) Increased ionization of the drug
D) Decreased lipid solubility
B) Faster onset of action
LA are Weak bases with pKa above physiologic pH
What is the primary determinant of the potency of a local anesthetic?
A) Its pKa
B) Its pH
C) Its lipid solubility
D) Its rate of metabolism
C) Its lipid solubility
How does acidosis affect the efficacy of local anesthetics?
A) It decreases the ionized fraction of the drug, increasing efficacy
B) It increases the ionized fraction of the drug, decreasing efficacy
C) It has no effect on the drug’s efficacy
D) It improves lipid solubility, enhancing efficacy
B) It increases the ionized fraction of the drug, decreasing efficacy
Local anesthetics are classified as weak bases. How does this influence their behavior in physiological conditions?
A) They remain mostly ionized in alkaline conditions
B) They are less effective in acidic conditions
C) They are more potent in acidic environments
D) They are rapidly metabolized in alkaline conditions
Answer: B) They are less effective in acidic conditions
How are ester-type local anesthetics metabolized and eliminated from the body?
A) Metabolized by hepatic enzymes and excreted in feces
B) Reduced by plasma cholinesterases and excreted in urine
C) Metabolized in the liver and excreted in bile
D) Broken down in the kidneys and excreted in urine
B) Reduced by plasma cholinesterases and excreted in urine
Which type of local anesthetic is primarily eliminated by hepatic metabolism?
A) Esters
B) Amides
C) Both Esters and Amides
D) Neither
B) Amides
Which type of local anesthetic is primarily metabolized by microsomal enzymes in the liver?
A) Esters
B) Amides
C) Both Amides and Esters
D) Neither
B) Amides
Which ester-type local anesthetic is metabolized in the liver instead of by plasma cholinesterase?
A) Procaine
B) Tetracaine
C) Cocaine
D) Chloroprocaine
C) Cocaine
Which factors most significantly influence the rate of clearance of local anesthetics?
A) Dose of medication and frequency of administration
B) Rate of tissue distribution, cardiac output, and protein binding
C) Route of administration and duration of action
D) pH of the local environment and rate of metabolism
B) Rate of tissue distribution, cardiac output, and protein binding
Which type of local anesthetic undergoes hydrolysis primarily by plasma cholinesterase?
A) Amides
B) Esters
C) Both Amides and Esters
D) Neither
B) Esters
Which amide local anesthetic is metabolized the most rapidly?
A) Bupivacaine
B) Mepivacaine
C) Prilocaine
D) Lidocaine
C) Prilocaine
Prilocaine (most rapid) > lidocaine and mepivacaine (intermediate) > etidocaine, bupivacaine and ropivacaine (slowest).
Amides are slower than esters overall.
Which part of the sodium channel do local anesthetics bind to?
A) L-gate
B) N-gate
C) H-gate (α subunit)
D) M-gate
C) H-gate (α subunit)
How do local anesthetics affect the sodium channel’s function?
A) They increase the rate of sodium channel activation
B) They block sodium ion channels to inhibit neuronal depolarization
C) They enhance the inactivation of sodium channels
D) They facilitate rapid repolarization of the channel
B) They block sodium ion channels to inhibit neuronal depolarization
What is the primary effect of local anesthetics binding to the H-gate of the sodium channel?
A) Enhancement of depolarization
B) Prevention of repolarization
C) Prevention of depolarization during inactivated and activated states
D) Facilitation of sodium ion influx
Answer: C) Prevention of depolarization during inactivated and activated states