Lidocaine
58 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to Lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which of the following is NOT typically associated with local anesthetic-induced CNS toxicity following inadvertent intravascular administration?

  • Hypertension and tachycardia (correct)
  • Circumoral and tongue numbness
  • Metallic taste
  • Tonic-clonic convulsions

A patient experiences neuropathic symptoms following a regional anesthetic. Which mechanism is most likely responsible?

  • Direct cardiac toxicity leading to reduced nerve perfusion
  • Pooling of the drug in the cauda equina (correct)
  • Systemic allergic reaction causing nerve inflammation
  • Excessive sodium channel blockade in peripheral nerves

How does cocaine uniquely affect the cardiovascular system compared to other local anesthetics?

  • It blocks norepinephrine uptake, causing vasoconstriction and increased blood pressure. (correct)
  • It directly blocks cardiac potassium channels, prolonging repolarization.
  • It directly stimulates cardiac sodium channels, increasing excitability.
  • It enhances vagal tone, leading to bradycardia.

A patient reports an allergic reaction after receiving a local anesthetic. Which type of local anesthetic is most likely responsible?

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

Which of the following local anesthetics is an ester?

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

Which strategy will most effectively reduce the onset time of a local anesthetic?

<p>Adding bicarbonate to increase the concentration of the nonionized form. (C)</p> Signup and view all the answers

A patient experiences local anesthetic systemic toxicity (LAST) after an accidental overdose. Which intervention is most appropriate?

<p>Administer Intralipid intravenously. (D)</p> Signup and view all the answers

Examine the following list of amide local anesthetics: lidocaine, bupivacaine, prilocaine, mepivacaine, ropivacaine, levobupivacaine, articaine and dibucaine. Which of the following values represents the number of 'i' characters within this entire list?

<p>30 (D)</p> Signup and view all the answers

Why does lidocaine without epinephrine have a higher pH (6.5) compared to lidocaine with epinephrine (4.5)?

<p>Epinephrine necessitates a lower pH to maintain its stability and prevent degradation. (C)</p> Signup and view all the answers

Why might a second injection of lidocaine be less effective if administered shortly after the first?

<p>The buffering capacity of the tissue fluids is reduced by the first injection. (D)</p> Signup and view all the answers

How does adding sodium bicarbonate to lidocaine with epinephrine enhance its anesthetic effect?

<p>By buffering the solution to a pH closer to physiological pH, reducing the need for tissue buffering. (C)</p> Signup and view all the answers

Why is the ratio of unionized to ionized lidocaine molecules critical for its anesthetic effect?

<p>Unionized molecules readily diffuse across lipid membranes to reach sodium channels. (C)</p> Signup and view all the answers

What is the primary reason for avoiding injections of local anesthetic into infected tissues?

<p>Infected sites often have an acidic pH due to lactic acid production, hindering effective anesthesia. (D)</p> Signup and view all the answers

Why might bubbling $CO_2$ gas into a vial of lidocaine sometimes reduce injection pain, despite the fact that acidic drugs are more painful when injected?

<p>The $CO_2$, when dissolved, forms carbonic acid, which may have a localized numbing effect. (B)</p> Signup and view all the answers

Considering the relationship between pH and drug effectiveness, what is the MOST likely reason lidocaine with epinephrine requires an adjustment with sodium bicarbonate?

<p>To optimize the proportion of the unionized form of lidocaine at the injection site. (D)</p> Signup and view all the answers

A vial of lidocaine has a ratio of 1:10,000 for unionized to ionized molecules at pH 4.5, but a ratio of 1:4 at pH 7.4. How does this pH-dependent ionization affect the drug's ability to provide effective anesthesia?

<p>A higher pH increases the proportion of unionized molecules, improving the drug's ability to cross lipid membranes and reach its target. (D)</p> Signup and view all the answers

Why are local anesthetics less effective in infected tissues?

<p>The acidic environment in infected tissues favors the ionized form of the anesthetic, reducing its ability to cross cell membranes. (D)</p> Signup and view all the answers

How does the co-administration of alpha-2 receptor agonists like clonidine or dexmedetomidine with local anesthetics prolong the duration of action?

<p>By blocking the release of Substance P, thus reducing sensory neuron firing. (D)</p> Signup and view all the answers

Why does the addition of sodium bicarbonate to a local anesthetic solution speed up the onset of action?

<p>It shifts the equilibrium towards the non-ionized form, allowing better penetration across nerve membranes. (D)</p> Signup and view all the answers

What explains the phenomenon of tachyphylaxis observed with repeated injections of local anesthetics?

<p>Depletion of tissue buffering capacity, leading to reduced effectiveness of subsequent doses. (D)</p> Signup and view all the answers

Local anesthetics' mechanism of action depends on several factors. Which of the following is MOST influential?

<p>Potency correlates positively with the local anesthetics' lipid solubility. (D)</p> Signup and view all the answers

A patient with significant liver disease requires a local anesthetic. Which type of local anesthetic should be used cautiously and why?

<p>Amide-type anesthetics, because their metabolism in the liver is likely to be impaired, prolonging their half-life and increasing the risk of toxicity. (D)</p> Signup and view all the answers

Order the nerve fibers from MOST sensitive to LEAST sensitive to blockade by local anesthetics:

<p>Small myelinated &gt; Small unmyelinated &gt; Large myelinated (B)</p> Signup and view all the answers

A patient undergoing a dental procedure experiences an adverse reaction to a local anesthetic characterized by restlessness, tremors, and a metallic taste. What is the most likely cause?

<p>Excessive absorption of the local anesthetic leading to systemic toxicity. (C)</p> Signup and view all the answers

Which structural feature of local anesthetics is MOST closely associated with a longer duration of action?

<p>The presence of an amide linkage in the intermediate chain. (D)</p> Signup and view all the answers

Why is cocaine particularly useful for "ENT" procedures?

<p>Cocaine has excellent absorption from topical application and potent vasoconstrictor effects. (C)</p> Signup and view all the answers

A researcher is comparing two local anesthetics, one with high lipid solubility and one with low lipid solubility. Which of the following statements accurately describes the expected differences in their pharmacological effects?

<p>The anesthetic with higher lipid solubility is expected to have a faster onset of action. (D)</p> Signup and view all the answers

A patient receives an injection of a local anesthetic, and the nerve fibers located circumferentially within the nerve bundle are blocked first. What anatomical principle explains this?

<p>Local anesthetic diffuses inward from the injection site, reaching outer fibers first. (B)</p> Signup and view all the answers

What is the primary mechanism by which local anesthetics selectively block pain perception without significantly affecting other sensory modalities (e.g., touch, pressure) at lower concentrations?

<p>Preferentially blocking small, unmyelinated C fibers and small myelinated A-delta fibers involved in pain transmission. (C)</p> Signup and view all the answers

How does the state of the sodium channel (resting, open, or inactivated) influence the binding and effectiveness of local anesthetics?

<p>Local anesthetics have a higher affinity for sodium channels in the open and inactivated states, leading to a use-dependent block. (D)</p> Signup and view all the answers

Direct neurotoxicity can result from the local effects of anesthetics. What is the primary mechanism of this toxicity?

<p>Disruption of mitochondrial function and increased oxidative stress within neurons. (D)</p> Signup and view all the answers

What is the Bier Block technique?

<p>A method of regional anesthesia where a local anesthetic is injected into a vein. (A)</p> Signup and view all the answers

What is Intralipid?

<p>A fat emulsion used in parenteral nutrition (B)</p> Signup and view all the answers

Which one of the local anesthetics is considered cardiotoxic if it enters the peripheral circulation?

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

What is the approximate half-life ((t \frac{1}{2})) of lidocaine?

<p>10 minutes (B)</p> Signup and view all the answers

Why is epinephrine added to injectable lidocaine solutions?

<p>To cause vasoconstriction and slow drug removal (C)</p> Signup and view all the answers

What is the pH of a lidocaine injectable solution WITHOUT epinephrine?

<p>6.5 (C)</p> Signup and view all the answers

What is the significance of lidocaine's pKa of 7.86?

<p>It indicates that lidocaine is equally ionized and unionized at pH 7.86. (B)</p> Signup and view all the answers

Why might the pH of commercially prepared lidocaine solutions NOT be optimal for clinical efficacy?

<p>The pH is chosen to provide the greatest drug stability and shelf life. (A)</p> Signup and view all the answers

Why is the unionized form of lidocaine important for its mechanism of action?

<p>The unionized form can cross cell membranes to reach intracellular sodium channels. (D)</p> Signup and view all the answers

What is the MOST likely reason that adjusting commercial lidocaine to a higher pH with sodium bicarbonate might enhance its anesthetic effect?

<p>It decreases the proportion of the charged form, facilitating diffusion across nerve membranes. (B)</p> Signup and view all the answers

A researcher aims to enhance the efficacy of lidocaine by modifying its formulation. Which approach would MOST directly improve lidocaine's ability to permeate nerve cell membranes, thereby accelerating its onset of action?

<p>Buffering the solution to a pH slightly above lidocaine's pKa. (A)</p> Signup and view all the answers

Why does lidocaine need to be in an uncharged form to cross neuronal membranes?

<p>Uncharged molecules readily dissolve in lipids, facilitating membrane passage. (C)</p> Signup and view all the answers

What distinguishes amide local anesthetics from ester local anesthetics in terms of metabolism?

<p>Amides are metabolized by amidases in the liver, while esters are metabolized by esterases found in most tissues. (C)</p> Signup and view all the answers

Which of the following best describes the direct mechanism of action of lidocaine on neurons?

<p>Blocking of voltage-gated sodium channels, preventing sodium influx. (A)</p> Signup and view all the answers

Why are systemic effects such as seizures or cardiac arrest a major concern with local anesthetics like lidocaine?

<p>Inadvertent intravascular injection can lead to high systemic concentrations. (C)</p> Signup and view all the answers

What is the function of the 'caine' stem, common to many local anesthetics?

<p>It is a historical reference indicating the drug's anesthetic properties. (C)</p> Signup and view all the answers

How does the intrinsic equilibrium between charged and uncharged forms of lidocaine influence its mechanism of action?

<p>The uncharged form crosses cell membranes, while the charged form binds to the sodium channel. (C)</p> Signup and view all the answers

Why does neurotoxicity primarily occur with spinal and epidural applications of local anesthetics?

<p>These applications place the local anesthetic in direct contact with neuronal elements. (A)</p> Signup and view all the answers

An investigational local anesthetic, “Faslocaine,” has been developed with structural modifications that render it permanently charged, regardless of tissue pH. While in vitro studies show it has potent sodium channel blocking activity, in vivo tests reveal minimal analgesic effect. What explains this discrepancy?

<p>The charged nature prevents Faslocaine from crossing lipid membranes to reach intracellular sodium channels. (A)</p> Signup and view all the answers

Based on the studies reviewed, what is a consistent finding regarding the use of sodium bicarbonate-adjusted lidocaine?

<p>Faster onset of action compared to non-adjusted lidocaine. (C)</p> Signup and view all the answers

Why might the pH of saline, when injected subcutaneously, cause more pain than lidocaine at a similar pH?

<p>Lidocaine possesses anesthetic properties that reduce pain perception, regardless of pH. (A)</p> Signup and view all the answers

In the context of local anesthetics, what does a pH further away from the pKa of the drug potentially indicate?

<p>Improved drug penetration and faster onset of action. (A)</p> Signup and view all the answers

How does the addition of epinephrine to lidocaine affect the duration of the anesthetic effect?

<p>Epinephrine prolongs the duration by causing vasoconstriction and reducing drug absorption. (D)</p> Signup and view all the answers

A study in rats adjusted lidocaine's pH from 6.58 to 7.99 with sodium bicarbonate, which decreased the degree and duration of the block. How might this outcome differ in humans, and what factors could account for the variation?

<p>Humans might show a different response due to variations in physiology, nerve structure, and tissue composition. (D)</p> Signup and view all the answers

Which of the following BEST explains why adjusting the pH of lidocaine with epinephrine might lead to improved surgical anesthesia?

<p>The adjustment optimizes the ratio of ionized to unionized drug, improving nerve penetration. (D)</p> Signup and view all the answers

Why do studies on pH-adjusted lidocaine sometimes yield conflicting results regarding the onset and duration of action?

<p>Variations in study design, injection technique, and patient populations influence outcomes. (D)</p> Signup and view all the answers

Based on the conflicting findings regarding pH adjusted lidocaine, devising a study to definitively assess the effects of pH-adjusted lidocaine compared to non-adjusted lidocaine would require careful consideration of several factors. Which of the following considerations would be MOST critical to ensure the validity and generalizability of the study's findings?

<p>The specific surgical site where the anesthetic is administered. (B)</p> Signup and view all the answers

Flashcards

Nociception

Awareness of pain.

Sodium Channels

Local anesthetics work by blocking these channels in axons.

Cocaine

The first local anesthetic introduced in 1884.

Aromatic Ring

A key chemical structure present in all local anesthetics.

Signup and view all the flashcards

Ester Linkage

Type of linkage associated with shorter duration of action.

Signup and view all the flashcards

Charged Cationic Form

Most local anesthetics exist primarily as this at physiological pH.

Signup and view all the flashcards

Reduced Effectiveness

Impact of low pH on the efficacy of local anesthetics.

Signup and view all the flashcards

Vasoconstrictors

They reduce blood flow and prolong the action of local anesthetics.

Signup and view all the flashcards

Liver

The location where amides are primarily biotransformed.

Signup and view all the flashcards

Potassium

This contributes to the recovery phase of the action potential.

Signup and view all the flashcards

Lipid Solubility

This increases the potency of local anesthetics.

Signup and view all the flashcards

Small Fibers

Fibers that are preferentially blocked by local anesthetics.

Signup and view all the flashcards

More Marked Blockade

Effect of high firing rates on drug blockade.

Signup and view all the flashcards

Sodium Bicarbonate

Adding this speeds up onset of action.

Signup and view all the flashcards

Tachyphylaxis

Repeated injections can induce this phenomenon.

Signup and view all the flashcards

Local Anesthetic CNS Toxicity

Toxicity resulting from local anesthetics, potentially causing circumoral numbness, metallic taste, twitching, convulsions, and CNS depression.

Signup and view all the flashcards

Local Anesthetic Neurotoxicity

Nerve damage due to concentrated drug pooling in the cauda equina, leading to neuropathic symptoms.

Signup and view all the flashcards

Cardiovascular Effects of Local Anesthetics

Excess local anesthetics blocking cardiac sodium channels, which depresses pacemaker activity and conduction. Cocaine is an exception because it blocks NE uptake, which increases blood pressure.

Signup and view all the flashcards

Allergic Reactions to Local Anesthetics

Ester-type local anesthetics are metabolized to PABA derivatives which can cause allergic reactions. Amides rarely cause reactions.

Signup and view all the flashcards

Amide Local Anesthetics

Local anesthetics that include lidocaine, bupivacaine, prilocaine, mepivacaine, ropivacaine, levobupivacaine, articaine and dibucaine

Signup and view all the flashcards

Ester Local Anesthetics

Local anesthetics including chloroprocaine, cocaine, procaine, tetracaine, and benzocaine

Signup and view all the flashcards

Intralipid

Intravenous lipid emulsion used to treat local anesthetic overdose.

Signup and view all the flashcards

Bicarbonate with Local Anesthetics

Adding bicarbonate increases the nonionized form of the local anesthetic and speeds up onset.

Signup and view all the flashcards

Lidocaine's Optimal pH for Stability

The pH at which lidocaine is most stable for a longer shelf life.

Signup and view all the flashcards

Lidocaine's Optimal pH for Function

The pH at which lidocaine works best once injected into human tissue.

Signup and view all the flashcards

Epinephrine's Role with Lidocaine

Epinephrine causes vasoconstriction, prolonging the anesthetic effect by keeping it at the injection site longer.

Signup and view all the flashcards

Purpose of Adding Sodium Bicarbonate

Adding sodium bicarbonate increases the pH closer to the physiological pH, improving effectiveness and reducing injection pain.

Signup and view all the flashcards

Drug Form for Membrane Penetration

Only unionized (lipid-soluble) drugs can effectively cross cell membranes to reach sodium channels.

Signup and view all the flashcards

pH of Infected Tissue

Infected sites have a low (acidic) pH due to lactic acid production by bacteria, reducing anesthetic effectiveness.

Signup and view all the flashcards

Pain and Drug pH

Acidic drugs cause more pain upon injection compared to neutral drugs (pH 7.4).

Signup and view all the flashcards

CO2 gas

CO2 bubbling may be used to adjust pH, but this contrasts other methods using bases to achieve similar physiological effects, use extreme caution.

Signup and view all the flashcards

Cocaine & Local Anesthetics

Local anesthetics are derived from this, although it's an ester.

Signup and view all the flashcards

Lidocaine Mechanism

Block voltage-gated sodium channels in neurons.

Signup and view all the flashcards

Primary Use of Lidocaine

Local area anesthesia.

Signup and view all the flashcards

Lidocaine Site of Action

The sodium channel on neurons.

Signup and view all the flashcards

Lidocaine Binding Form

Charged (water-soluble) form binds to the sodium channel.

Signup and view all the flashcards

Lidocaine ADRs

May cause sedation, seizures, cardiac death due to injection into the vascular system.

Signup and view all the flashcards

Lidocaine Neurotoxicity

Neurotoxicity, mostly from spinal/epidural application.

Signup and view all the flashcards

Lidocaine Half-Life (t ½)

The half-life (t ½) of lidocaine is approximately 10 minutes, while other amide local anesthetics range from 5 to 28 minutes.

Signup and view all the flashcards

Epinephrine with Lidocaine

Epinephrine is added to injectable lidocaine to cause vasoconstriction, slowing the drug's removal from the injection site, prolonging its effects.

Signup and view all the flashcards

pH of Lidocaine Solution

The pH of injectable lidocaine solution is approximately 6.5.

Signup and view all the flashcards

pH of Lidocaine + Epinephrine

The pH of injectable lidocaine solution with added epinephrine is approximately 4.5.

Signup and view all the flashcards

Lidocaine pKa

The pKa of lidocaine is 7.86. At this pH, lidocaine exists in 50% ionized (water-soluble) and 50% unionized (lipid-soluble) forms.

Signup and view all the flashcards

Lidocaine Stability vs. Efficacy

Pharmaceutical companies prepare lidocaine solutions at a pH that maximizes the drug's stability and shelf life, which may not be the optimal pH for clinical efficacy.

Signup and view all the flashcards

Drug Form and Onset of Action

The fastest onset of action occurs when a drug is predominantly in its lipid-soluble, unionized form, allowing it to cross cell membranes and block sodium channels on axons.

Signup and view all the flashcards

Acidity and Injection Pain

Acidic injectable drugs tend to cause more pain upon injection compared to neutral or alkaline drugs.

Signup and view all the flashcards

Bicarbonate with Lidocaine

Adding sodium bicarbonate to lidocaine increases the pH, making it less painful to inject.

Signup and view all the flashcards

pH Adjusted Lidocaine Benefits

Adjusting lidocaine with sodium bicarbonate leads to better surgical anesthesia and complete nerve block.

Signup and view all the flashcards

Onset of Action: Buffered Lidocaine

Buffered lidocaine has a faster onset of action compared to unbuffered lidocaine.

Signup and view all the flashcards

Lidocaine pH and Penetration

Raising the pH of lidocaine may decrease pain because it makes the drug penetrate nerve membranes better.

Signup and view all the flashcards

Saline pH and Pain Perception

Saline's pH is 6.5 and patients do not report pain. The anesthetic provides pain relief regardless of pH.

Signup and view all the flashcards

Epinephrine and Vasoconstriction

Epinephrine causes vasoconstriction, keeping the drug at the injection site longer.

Signup and view all the flashcards

Lidocaine with Epi: pH effects

Adjusting the pH of lidocaine with epinephrine hastens onset without affecting degree or duration of block.

Signup and view all the flashcards

Reduced Injection Pain

Adjusting lidocaine closer to a neutral pH reduces pain upon injection.

Signup and view all the flashcards

Study Notes

  • Intralipid is an intravenous lipid emulsion for overdose
  • See “Lipid Resuscitation” on the top of pg 494 in Katzung
  • Adding bicarbonate to a local anesthetic is a strategy sometimes used in clinical practice, which raises the effective concentration of the nonionized (lipid soluble) form and thus shortens the onset time of a regional block
  • Lidocaine crosses lipid membranes to find the sodium receptor

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Quiz Team

More Like This

Lidocaine Drug Card Flashcards
10 questions
Lidocaine: Uses and Contraindications
8 questions
Use Quizgecko on...
Browser
Browser