Pharm: Exam 4- Local Anesthetics Flashcards
Which of the following local anesthetics is recognized as the standard to which all other local anesthetics are compared?
A. Cocaine
B. Procaine
C. Lidocaine
D. Bupivacaine
Correct Answer:
C. Lidocaine
Rationale:
Lidocaine, the first synthetic amide local anesthetic introduced in 1943, is considered the standard to which all other local anesthetics are compared due to its efficacy and safety profile.
Cocaine was the first local anesthetic used in which field of medicine?
A. Dentistry
B. Ophthalmology
C. Cardiology
D. Dermatology
Correct Answer:
B. Ophthalmology
Rationale:
According to the slide, cocaine, which is known for its cerebral stimulating qualities and ability to cause localized vasoconstriction, was first used as a local anesthetic in ophthalmology in 1884.
What was the first synthetic ester local anesthetic?
A. Benzocaine
B. Procaine
C. Tetracaine
D. Lidocaine
Correct Answer:
B. Procaine
Rationale:
Procaine, introduced in 1905, was the first synthetic ester local anesthetic developed as a less toxic alternative to cocaine.
Which class of antiarrhythmic drugs shares the mechanism of action with local anesthetics?
A. Class I - Sodium-channel blockers
B. Class II - Beta-blockers
C. Class III - Potassium-channel blockers
D. Class IV - Calcium-channel blockers
Correct Answer:
A. Class I - Sodium-channel blockers
Rationale:
Local anesthetics act as sodium-channel blockers, which is the mechanism of action for Class I antiarrhythmic drugs. They stabilize the cardiac cell membrane by inhibiting the influx of sodium ions during action potentials, which helps to treat dysrhythmias.
For a patient with obstructive sleep apnea (OSA), which medication is recommended to be given intraoperatively?
A. Acetaminophen
B. Ondansetron
C. Ofirmev
D. Lidocaine
Correct Answer:
C. Ofirmev
Rationale:
The chart indicates that for patients with OSA, Ofirmev (intravenous acetaminophen) at a dose of 1 gram is recommended intraoperatively. This is likely due to its analgesic properties and favorable safety profile, particularly for patients with OSA.
Which medication is administered preoperatively and continued postoperatively for pain management?
A. Gabapentin
B. Ketorolac
C. Magnesium
D. Celebrex or Advil
Correct Answer:
A. Gabapentin
Rationale:
Gabapentin is listed as being administered preoperatively at a dose of 300 mg PO and is also continued postoperatively at the same dosage of 300 mg taken three times a day (TID).
What is the maximum daily dose of ibuprofen & recommended dose intraoperatively?
A. 3200 mg/day
B. 300 - 750mg IV Q6
C. 2500 mg/day
D. 200- 800mg IV Q6
A & D
In the postoperative period, which form of magnesium is recommended if the patient was not receiving magnesium intraoperatively?
A. Magnesium sulfate
B. Super Mag
C. Magnesium aspartate
D. Magnesium oxide
E. Doesn’t matter
E. Doesn’t matter
Rationale:
Postoperatively, the chart indicates the use of either Super Mag 400 mg twice a day (BID), magnesium aspartate 615 mg three times a day (TID), or magnesium oxide 500 mg twice a day (BID), if the patient requires
Intra-op use 30-60mg/kg mag with MAX of 6g infused over 1 hour.
Which of the following plasma lidocaine concentrations is typically associated with therapeutic analgesic effects?
A. 0.5-1 mcg/ml
B. 1-5 mcg/ml
C. 5-10 mcg/ml
D. 10-15 mcg/ml
Correct Answer:
B. 1-5 mcg/ml
Rationale:
Therapeutic analgesia with lidocaine is achieved with plasma concentrations ranging from 1-5 mcg/ml. Concentrations below 1 mcg/ml may not provide adequate analgesia, and levels above 5 mcg/ml can start to produce side effects such as circum-oral numbness and tinnitus.
During the administration of lidocaine, what is the initial IV bolus dose recommended for an adult patient?
A. 0.5 mg/kg
B. 1 to 2 mg/kg
C. 2 to 4 mg/kg
D. Over 4 mg/kg
Correct Answer:
B. 1 to 2 mg/kg
Rationale:
For intravenous administration, lidocaine is typically started with an initial bolus of 1 to 2 mg/kg, administered over 2 to 4 minutes. This is to achieve a rapid therapeutic plasma concentration while minimizing the risk of adverse effects.
A patient with a plasma lidocaine concentration of 7 mcg/ml is likely to experience which of the following symptoms?
A. Adequate analgesia without side effects
B. Circum-oral numbness and tinnitus
C. Seizures
D. Cardiovascular depression
B. Circum-oral numbness and tinnitus
Rationale:
A plasma lidocaine concentration of 5-10 mcg/ml can cause symptoms such as circum-oral numbness, tinnitus, muscle twitching, systemic hypotension, and myocardial depression. Seizures and cardiovascular depression are associated with higher plasma concentrations.
What is the maximum recommended duration for an infusion of lidocaine?
A. Up to 12 hours
B. Up to 24 hours
C. Up to 72 hours
D. There is no maximum as long as plasma levels are therapeutic
Correct Answer:
C. Up to 72 hours
Rationale:
According to the information provided, lidocaine infusion should be terminated between 12 to 72 hours based on clinical judgment and patient response. Prolonged infusion beyond 72 hours increases the risk of accumulation and adverse effects, especially in patients with existing
What structural feature determines whether a local anesthetic is classified as an ester or an amide?
A. The presence of a benzene ring
B. The bond between the lipophilic portion and the hydrocarbon chain
C. The bond between the hydrocarbon chain and the hydrophilic portion
D. The length of the hydrocarbon chain
E. The bond between the lipophilic portion and the hydrophilic portion
B. The bond between the lipophilic portion (aromatic part) and the hydrocarbon chain.
The hydrocarbon chain (intermediate chain) determines ester/amide
Local anesthetics are typically weak bases. How are they commonly administered in clinical settings to enhance their stability and solubility?
A. As freebase compounds
B. As neutral solutions
C. As hydrochloride (HCl) salts
D. As pure acid forms
Correct Answer:
C. As hydrochloride (HCl) salts
Rationale:
Local anesthetics, being weak bases, are usually formulated as hydrochloride (HCl) salts to enhance their stability and solubility when administered clinically.
What is the primary lipophilic component of a local anesthetic molecule?
A. Amino group
B. Intermediate chain
C. Aromatic part, typically a benzene ring
D. Hydrocarbon chain
C. Aromatic part, typically a benzene ring
Rationale:
The lipophilic portion of a local anesthetic molecule is the aromatic part, which is often a benzene ring. This structure facilitates the anesthetic’s ability to penetrate the lipid-rich cellular membranes.
Epinephrine is sometimes added to local anesthetic solutions. What is the purpose of this addition?
A. To decrease the pH of the solution
B. To increase the duration of action of the anesthetic
C. To provide anti-inflammatory effects
D. To act as an alternative pain reliever
Correct Answer:
B. To increase the duration of action of the anesthetic
Rationale:
Epinephrine is added to local anesthetic solutions to cause vasoconstriction at the site of administration. This reduces blood flow, which decreases the rate of absorption of the anesthetic into the bloodstream, prolonging its duration of action, and provides a more localized effect.
Which local anesthetic has the highest potency?
A. Procaine
B. Tetracaine
C. Lidocaine
D. Chloroprocaine
Correct Answer:
B. Tetracaine
Rationale:
The table lists tetracaine with a potency of 16, making it the highest compared to the other local anesthetics listed, such as procaine (1), chloroprocaine (4), and lidocaine (1).
What is the maximum single dose for infiltration anesthesia with bupivacaine?
A. 300 mg
B. 175 mg
C. 500 mg
D. 200 mg
Correct Answer:
B. 175 mg
Rationale:
The table specifies a maximum single dose of 175 mg for infiltration anesthesia with bupivacaine, indicating its safe upper limit for a single administration.
Which local anesthetic has the quickest onset of action?
A. Lidocaine
B. Chloroprocaine
C. Prilocaine
D. Bupivacaine
Correct Answer:
B. Chloroprocaine
Rationale:
Chloroprocaine is listed as having a rapid onset, which suggests it acts faster than the other local anesthetics presented in the table, including lidocaine (rapid), prilocaine (slow), and bupivacaine (slow).
which local anesthetic has the lowest protein binding percentage?
A. Procaine
B. Tetracaine
C. Mepivacaine
D. Ropivacaine
Correct Answer:
A. Procaine
Rationale:
Procaine has the lowest protein binding at 6%, which can affect its duration of action and toxicity profile, as local anesthetics with lower protein binding typically have a shorter duration and a higher free fraction in the plasma
Local anesthetics have different durations of action after infiltration. Which anesthetic would you choose for a procedure requiring a long duration of anesthesia?
A. Procaine
B. Lidocaine
C. Bupivacaine
D. Prilocaine
Correct Answer:
C. Bupivacaine
Rationale:
Bupivacaine is listed with a duration of action after infiltration of 240-480 minutes, making it suitable for longer procedures. In comparison, procaine (45-60 min), lidocaine (60-120 min), and prilocaine (60-120 min) have shorter durations of action.
Which local anesthetic is known for its high lipid solubility and is, therefore, very potent?
A. Procaine
B. Lidocaine
C. Tetracaine
D. Ropivacaine
Correct Answer:
C. Tetracaine
Rationale:
The table lists tetracaine as having a potency of 16, which is the highest among the presented anesthetics, suggesting high lipid solubility and consequent high potenc
Which of the following local anesthetics has both high lipid solubility and high protein binding, contributing to a long duration of action and a slower onset?
A. Mepivacaine
B. Bupivacaine
C. Procaine
D. Prilocaine
Correct Answer:
B. Bupivacaine
Rationale:
Bupivacaine is known for its high lipid solubility 28 and high protein binding (greater than 95%), which contributes to its longer duration of action and potential for a slower onset when compared to drugs with lower protein binding. The highest lipid solubility is Tetracaine at 80 and the lowest is Prilocaine at 0.9
What can prolong the duration of action of local anesthetics?
A. Combining with antihistamines
B. Addition of dexamethasone
C. Decreasing the lipid solubility
D. Administering the drug in an acidic pH
Correct Answer:
B. Addition of dexamethasone
Rationale:
Adding dexamethasone or epinephrine to local anesthetics can prolong their duration of action. Epinephrine induces vasoconstriction, slowing absorption into the bloodstream and prolonging the local effect. Dexamethasone has been shown to extend the duration of action when used as an adjunct.
Why is it essential to memorize the “maximum single dose for infiltration” for local anesthetics?
A. To avoid systemic toxicity
B. To ensure rapid onset of action
C. To prevent allergic reactions
D. To prolong the duration of anesthesia
Correct Answer:
A. To avoid systemic toxicity
Rationale:
Knowing the maximum single dose for infiltration of local anesthetics is critical to prevent systemic toxicity. Exceeding these limits can result in toxic plasma concentrations, leading to adverse effects ranging from mild systemic symptoms to severe complications like seizures or cardiovascular depression.
What is the advantage of using a liposome delivery system for local anesthetics?
A. Increases the potency of the local anesthetic
B. Provides a timed release for prolonged duration of action
C. Completely eliminates the toxicity of the local anesthetic
D. Allows for immediate onset of action
Correct Answer:
B. Provides a timed release for prolonged duration of action
Rationale:
Liposome delivery systems can encapsulate a higher amount of local anesthetic and provide a consistent release of the drug in the tissues, thereby prolonging the duration of action and potentially decreasing toxicity.
How do local anesthetics prevent the propagation of action potentials?
A. By binding to voltage-gated potassium channels
B. By increasing the permeability of the cell membrane to sodium ions
C. By binding to voltage-gated sodium channels and inhibiting sodium passage
D. By activating the H gate from the outside of the cell membrane
Correct Answer:
C. By binding to voltage-gated sodium channels and inhibiting sodium passage
Rationale:
Local anesthetics bind to the intracellular portion of voltage-gated sodium channels, inhibiting sodium ion passage through nerve membranes and thus preventing the nerve from reaching the threshold potential necessary for action potential propagation.
Which factor can increase the sensitivity of nerve endings to local anesthetics?
A. Alkaline tissue pH
B. Infrequent nerve stimulation
C. Large diameter of nerve fibers
D. Repetitively stimulated nerves
Correct Answer:
D. Repetitively stimulated nerves
Rationale:
Repetitive stimulation of nerves increases their sensitivity to local anesthetics, meaning less drug is needed to achieve the desired anesthetic effect.
In an acidotic patient, what effect does the condition have on the action of local anesthetics?
A. Enhances the action of local anesthetics
B. Converts more local anesthetic to its ionized form, reducing effectiveness
C. Increases the lipid solubility of local anesthetics
D. Does not affect the action of local anesthetics
Correct Answer:
B. Converts more local anesthetic to its ionized form, reducing effectiveness
Rationale:
If a patient is acidotic, the acidic environment will convert more of the local anesthetic to its ionized form, which is less lipid-soluble and less able to penetrate nerve cell membranes to exert its effect.
Which fibers are most rapidly affected by local anesthetics?
A. Unmyelinated C fibers
B. Myelinated B fibers
C. Myelinated A-delta fibers
D. Preganglionic B fibers
Correct Answer:
D. Preganglionic B fibers
Rationale:
Preganglionic B fibers are the fastest blocked by local anesthetics, affecting the sympathetic nervous system responses such as blood pressure and heart rate.
What is the Minimum Effective Concentration (MEC) for local anesthetics analogous to in volatile anesthetics?
A. The minimum inhibitory concentration (MIC)
B. The maximum allowable concentration (MAC)
C. The median effective concentration (EC50)
D. The blood concentration for induction (BCI)
Correct Answer:
B. The minimum aleveolar concentration (MAC)
Rationale:
MEC or Cm for local anesthetics is similar to MAC for volatile anesthetics. It represents the concentration needed to achieve a clinical effect without causing systemic toxicity
What effect does a local anesthetic’s pKa value have on its onset of action?
A. pKa has no influence on the onset of action.
B. A higher pKa significantly speeds up the onset of action.
C. A pKa value closer to physiologic pH correlates with a slower onset of action.
D. A pKa value closer to physiologic pH is associated with the most rapid onset of action.
Correct Answer:
D. A pKa value closer to physiologic pH is associated with the most rapid onset of action.
Rationale:
Local anesthetics with pKa values close to the physiological pH will have a greater proportion of the drug in the non-ionized form at physiological pH, which more readily penetrates nerve membranes, leading to a more rapid onset of action.
What is the consequence of lidocaine’s intrinsic vasodilator activity?
A. Decreased systemic absorption
B. Increased potency and shorter duration of action (DOA)
C. Decreased potency and longer duration of action
D. Greater systemic absorption
Correct Answer:
D. Greater systemic absorption
Rationale:
Intrinsic vasodilator activity of local anesthetics like lidocaine increases local blood flow, which can lead to greater systemic absorption of the drug. With a decrease in potency and shorter duration of action.
During pregnancy, why might local anesthetic dosing need to be adjusted?
A. Pregnancy decreases the sensitivity to local anesthetics.
B. Pregnancy does not affect the pharmacodynamics of local anesthetics.
C. Increased sensitivity in pregnancy may require higher doses.
D. Pregnancy is associated with increased sensitivity, requiring careful dosing.
Correct Answer:
D. Pregnancy is associated with increased sensitivity, requiring careful dosing.
Rationale:
Pregnant patients often exhibit increased sensitivity to local anesthetics, potentially due to physiological changes that affect the drug’s pharmacokinetics and pharmacodynamics, necessitating careful dosing to avoid toxicity.
How does the site of injection influence the duration of action of local anesthetics?
A. More vascular sites result in a shorter duration of action due to rapid absorption.
B. Less vascular sites lead to a prolonged duration of action due to slower absorption.
C. The site of injection has no impact on the duration of action.
D. A and B are correct.
Correct Answer:
D. A and B are correct.
Rationale:
The site of injection significantly impacts the duration of action for local anesthetics. More vascular sites will have shorter durations due to faster systemic absorption, whereas less vascular sites like subcutaneous tissue will have a longer duration of action.
Which site of injection is associated with the highest blood concentration of local anesthetics?
A. Subcutaneous
B. Intravenous
C. Caudal
D. Sciatic
Correct Answer:
B. Intravenous
Rationale:
According to the hierarchy presented, intravenous injections result in the highest blood concentrations of local anesthetics, due to direct entry into the vascular system.
For procedures like circumcisions and hernia repairs in children, which regional anesthesia technique is commonly used?
A. Brachial plexus block
B. Caudal block
C. Sciatic nerve block
D. Tracheal instillation
B. Caudal block
Rank the following regional anesthesia techniques in order of increasing systemic absorption of local anesthetics:
A. Caudal
B. Intravenous
C. Subcutaneous
D. Epidural
Correct Answer Order:
1.Subcutaneous (Lowest systemic absorption)
2. Epidural
3. Caudal
4.Intravenous (Highest systemic absorption)
How does lipid solubility affect the potency of local anesthetics?
A. Greater lipid solubility decreases the potency of the anesthetic.
B. Lipid solubility has no impact on the potency of the anesthetic.
C. Lesser lipid solubility leads to increased potency of the anesthetic.
D. Increased lipid solubility is directly related to greater potency of the anesthetic.
Correct Answer:
D. Increased lipid solubility is directly related to greater potency of the anesthetic.
Rationale:
The potency of local anesthetics is directly related to their lipid solubility, as this property enables the drug to penetrate the lipid-rich neuronal membranes more effectively.
Which of the following factors can influence the rate of clearance for local anesthetics?
A. Patient age and body temperature
B. Cardiac output and protein binding
C. Dosage and duration of action
D. Site of injection and rate of tissue distribution
Correct Answer:
B. Cardiac output and protein binding
Rationale:
The rate at which a local anesthetic is cleared from the body depends on the cardiac output and the extent to which the drug binds to proteins. An increased cardiac output leads to increased metabolism of the drug, and the percentage bound is inversely related to the percentage available in plasma.
Which class of local anesthetics is most rapidly metabolized, and why?
A. Amides, because they are less protein-bound and more available in plasma.
B. Esters, because they undergo rapid hydrolysis by cholinesterase enzymes in the plasma.
C. Amides, because they have the highest lipid solubility and protein binding.
D. Esters, because they are metabolized in the liver by CYP450 enzymes.
Correct Answer:
B. Esters, because they undergo rapid hydrolysis by cholinesterase enzymes in the plasma.
Rationale:
Esters are generally metabolized more rapidly than amides because they are hydrolyzed by cholinesterase enzymes present in plasma, which occurs faster than the metabolism of amides by liver enzymes.
Why are amides less likely to cause allergic reactions compared to esters?
A. Amides are not metabolized into para-aminobenzoic acid (PABA), a known allergen.
B. Amides have higher protein binding, which reduces the immune response.
C. Amides are more rapidly cleared from the body, reducing the chance of an allergic reaction.
D. Amides have lower lipid solubility, which makes them less allergenic.
Correct Answer:
A. Amides are not metabolized into para-aminobenzoic acid (PABA), a known allergen.
Rationale:
Esters can be metabolized into PABA, which is associated with allergic reactions. Amides, on the other hand, do not have this metabolic pathway and thus are less likely to cause allergic reactions.
In the elderly, the dose of local anesthetics is often reduced. What is the primary reason for this adjustment?
A. Increased body fat percentage in the elderly leading to higher drug storage.
B. Decreased rate of clearance due to reduced cardiac output and protein plasma levels.
C. Higher baseline cardiac output in the elderly leading to rapid drug clearance.
D. Enhanced sensitivity of the elderly to the pharmacologic effects of local anesthetics.
Correct Answer:
B. Decreased rate of clearance due to reduced cardiac output and protein plasma levels.
Rationale:
As individuals age, they typically experience a decrease in cardiac output and a reduction in protein plasma levels, which can lead to a slower rate of clearance for local anesthetics, necessitating a lower dose to avoid toxicity.
Which local anesthetic has a protein binding percentage of 55% and a single dose for infiltration of 600mg depending on what ?
Options:
A. Lidocaine
B. Prilocaine
C. Bupivacaine
D. Ropivacaine
Correct Answer:
B. Prilocaine
Rationale:
According to the slide, Prilocaine, classified under amides, has a protein binding of 55% and a maximum single dose for infiltration of 400 mg on chart but slide 32 says 600mg so who fucking knows.
What is the maximum single dose for infiltration and protein binding percentage of Lidocaine?
Options:
A. 300 mg, 70%
B. 175 mg, >97%
C. 500 mg, 6%
D. 400 mg, 55%
Correct Answer:
A. 300 mg, 70%
Rationale:
Lidocaine, which is an amide local anesthetic, has a maximum single dose for infiltration of 300 mg and a protein binding percentage of 70%.
Which local anesthetic undergoes metabolism by microsomal enzymes in the liver at the most rapid rate?
Options:
A. Lidocaine
B. Bupivacaine
C. Prilocaine
D. Ropivacaine
Correct Answer:
C. Prilocaine
Rationale:
The slide indicates that among the listed amides, Prilocaine is metabolized at the most rapid rate by liver microsomal enzymes.
Which type of local anesthetic is primarily metabolized by cholinesterase enzyme in plasma rather than in the liver?
Options:
A. Amides
B. Esters
C. Both A and B
D. Neither A nor B
Correct Answer:
B. Esters
Rationale:
Esters are primarily metabolized by hydrolysis through cholinesterase enzymes in the plasma, as mentioned in the slide. An exception is cocaine, which is metabolized in the liver.
What percentage of cocaine is excreted unchanged in the urine?
Options:
A. Less than 5%
B. Approximately 10-12%
C. Over 95%
D. None of the above, cocaine is fully metabolized
Correct Answer:
B. Approximately 10-12%
Rationale:
Unlike most local anesthetics that are metabolized before renal excretion, cocaine has a unique characteristic where 10-12% can be excreted unchanged in the urine.
Which 2 of the following local anesthetics has an intermediate rate of metabolism by liver enzymes?
Options:
A. Etidocaine
B. Ropivacaine
C. Lidocaine
D. Mepivacaine
Correct Answer:
C. Lidocaine D. Mepivacaine
Rationale:
Lidocaine has an intermediate rate of metabolism when processed by liver microsomal enzymes, alongside Mepivacaine.
The majority of local anesthetics have a low percentage of unchanged drug excreted in the urine. What is the primary reason for this characteristic?
Options:
A. High rate of protein binding
B. High rate of metabolism by liver enzymes
C. Poor water solubility of the drugs
D. Active transport mechanisms in the renal tubules
Correct Answer:
C. Poor water solubility of the drugs
Rationale:
Local anesthetics are typically weak bases with poor water solubility, which means that a relatively small amount of the unchanged drug can be excreted through the kidneys. As the slides indicate, less than 5% of the unchanged drug is usually found in the urine, primarily due to their poor solubility in water. This means that most of the drug is metabolized before it is excreted.
Lower levels of plasma cholinesterases during pregnancy can influence the metabolism of which type of local anesthetics?
A. Amides
B. Esters
C. Both amides and esters
D. Neither amides nor esters
Answer: B. Esters
Rationale: Esters are rapidly hydrolyzed by plasma cholinesterases, and lower levels of these enzymes during pregnancy would affect the metabolism of ester local anesthetics.
Why might amides be more concerning for fetal exposure during pregnancy compared to esters?
A. They have a lower rate of placental transfer.
B. They are rapidly metabolized by the fetus.
C. They have higher protein binding, potentially leading to greater fetal accumulation.
D. They are less potent than esters.
Answer: C. They have higher protein binding, potentially leading to greater fetal accumulation.
Rationale: Higher protein binding in the fetus can result in more of the drug being retained, and the significant transplacental transfer of amides compounds this effect.
What is the phenomenon of ‘ion trapping’ in the context of fetal acidosis and local anesthetics?
A. Nonionized local anesthetics are unable to cross the placental barrier.
B. Ionized local anesthetics can more easily cross back into the maternal circulation.
C. Fetal acidosis can lead to nonionized local anesthetics becoming ionized within the fetus, leading to accumulation.
D. Local anesthetics do not become ionized in the fetus regardless of pH levels.
Answer: C. Fetal acidosis can lead to nonionized local anesthetics becoming ionized within the fetus, leading to accumulation.
Rationale: Nonionized forms of local anesthetics cross the placental barrier but may become ionized in the acidic environment of the fetal bloodstream, leading to accumulation since the ionized form cannot easily cross back into the maternal circulation.
Which intervention can be used to manage increased local anesthetic concentrations in the fetus due to acidosis?
A. Administering bicarbonate to the mother
B. Increasing fetal plasma cholinesterase levels
C. Decreasing the maternal dose of local anesthetics
D. Administering calcium gluconate to the mother
Answer: A. Administering bicarbonate to the mother
Rationale: Administering bicarbonate to the mother can help correct fetal acidosis, potentially reducing the ion trapping of local anesthetics in the fetus.
Which of the following statements about the pharmacokinetics of Lidocaine is correct?
A. Lidocaine is primarily metabolized in the kidneys, with the main metabolite being Xylidide.
B. Hepatic disease has no significant impact on the metabolism and elimination of Lidocaine.
C. Lidocaine’s maximum recommended infiltration dose is 300 mg when used without epinephrine and 500 mg when combined with epinephrine.
D. Lidocaine does not have anti-dysrhythmic properties and is used exclusively for local anesthesia
Answer and Rationale:
C. Lidocaine’s maximum recommended infiltration dose is 300 mg when used without epinephrine and 500 mg when combined with epinephrine.
Rationale: The correct answer is C. The slide indicates that Lidocaine undergoes oxidative dealkylation in the liver, not the kidneys, making A incorrect. Hepatic disease does indeed affect the metabolism and elimination of Lidocaine, which rules out B. D is incorrect as the slide specifies that Lidocaine has anti-dysrhythmic properties. Therefore, the correct statement is C, as it accurately reflects the information given on the maximum doses of Lidocaine with and without epinephrine.
A 70 kg patient is being treated for methemoglobinemia after receiving Prilocaine. What is the maximum recommended dose of Methylene Blue for this patient?
A. 60 mg IV over 5 minutes
B. 140 mg IV over 5 minutes
C. 560 mg IV over 5 minutes
D. None of the above
Answer and Rationale:
B. 140 mg IV over 5 minutes
Rationale: Methemoglobinemia can occur when Prilocaine is metabolized to its metabolite, orthotoluidine, which then converts hemoglobin to methemoglobin, reducing the oxygen-carrying capacity of the blood and leading to symptoms like cyanosis. The treatment for methemoglobinemia is Methylene Blue, administered at 1-2 mg/kg IV. Given the patient’s weight of 70 kg, and not exceeding the total dose limit of 7 to 8 mg/kg as stated on the slide, the maximum recommended dose would be 70 kg x 2 mg/kg = 140 mg given over 5 minutes, which corresponds to answer B. A is underdosed
Which of the following is a characteristic that differentiates Mepivacaine from Lidocaine?
A. Shorter duration of action
B. Greater Vasodilatory activity
C. Prolonged elimination in fetus and newborn
D. Metabolized by N-dealkylation
Answer and Rationale:
C. Prolonged elimination in fetus and newborn.
Rationale: Mepivacaine is similar to Lidocaine in many respects; however, it lacks vasodilatory activity, which confers a longer duration of action. Another distinguishing factor is that Mepivacaine has prolonged elimination in the fetus and newborn, and hence, it is not typically used for obstetrical anesthesia (OB). This characteristic is highlighted in the slide as a key difference, making option C the correct answer. Options A and B are incorrect as they describe properties that are not associated with Mepivacaine when compared to Lidocaine. Option D is incorrect as the slide does not discuss the metabolism of Mepivacaine via N-dealkylation; this is mentioned in relation to Bupivacaine.
Which local anesthetic has a maximum single infiltration dose of 300mg when used plain and 500mg when combined with epinephrine?
A. Mepivacaine
B. Bupivacaine
C. Lidocaine
D. Ropivacaine
Answer: C. Lidocaine
Rationale: Lidocaine’s maximum recommended doses are 300mg for plain and 500mg when combined with epinephrine, to slow absorption and prolong the effect.
Which local anesthetic, when metabolized, can lead to methemoglobinemia if the dose exceeds 600mg?
A. Tetracaine
B. Lidocaine
C. Prilocaine
D. Bupivacaine
Answer: C. Prilocaine
Rationale: Prilocaine’s metabolite orthotoluidine can convert hemoglobin to methemoglobin, leading to methemoglobinemia at high doses.
Which statement accurately reflects the transplacental transfer characteristics of local anesthetics?
A. Esters and amides both have significant transplacental transfer.
B. Amides, not esters, have significant transplacental transfer
C. Esters have a higher transplacental transfer than amides.
D. Protein binding has no impact on the transplacental transfer of local anesthetics.
Answer: B. Amides, not esters, have significant transplacental transfer
Rationale: Esters are rapidly hydrolyzed by plasma cholinesterases, reducing their transplacental transfer compared to amides. Protein binding also affects the rate and degree of diffusion across the placental barrier.