Local Anesthetics Flashcards
What local anesthetic class is responsible for more allergic reactions?
Esters (due to PABA metabolite)
What is LAST?
Local Anesthetic Systemic Toxicity
What causes LAST syndrome?
Excess plasma concentration of LA from:
- Accidental IV injection
- Systemic absorption from tissue redistribution and clearance metabolism.
What factors affect the magnitude of systemic absorption of local anesthetic?
- Dose
- Vascularity of site
- Concurrent Epi use
- Properties of the drug itself
Would local anesthetic administered via the trachea have a higher or lower chance of systemic absorption than local anesthetic delivered brachially?
Trachea has higher chance of systemic absorption.
What serum electrolyte condition will exacerbate local anesthetic toxicity?
Why?
Hyperkalemia (lowers seizure threshold)
What s/s would be seen with a plasma lidocaine concentration of 1-5 mcg/ml?
Analgesia
What s/s would be seen with a plasma lidocaine concentration of 5-10 mcg/ml?
- Mouth numbness
- Tinnitus
- Muscle twitching
- ↓BP
- Myocardial depression
What s/s would be seen with a plasma lidocaine concentration of 10-15 mcg/ml?
- Seizures
- Unconsciousness
What s/s would be seen with a plasma lidocaine concentration of 15-25 mcg/ml?
- Apnea
- Coma
What s/s would be seen with a plasma lidocaine concentration of >25 mcg/ml?
Cardiovascular Depression
How does lidocaine affect EKGs?
How does it do this?
- Prolongation of PR interval and QRS widening.
- Blockade of Na⁺ channels
Which three drugs are most responsible for cardiac adverse effects when reaching toxic levels systemically?
Bupivacaine > Ropivacaine > Lidocaine
How does Lipid Emulsion rescue work?
Lipids encapsulate the local anesthetic and transport it away from cardiac and CNS tissue.
Also provides fat for myocardial metabolism.
What is the bolus dose of Lipid Emulsion?
1.5 mL/kg of 20% lipid emulsion
What is the infusion dose of lipid emulsion?
How long should it be given?
0.25 mL/kg/minute for at least 10 minutes
What is the max dose for lipid emulsion that should be given?
8 mL/kg
What preservative commonly used for amide local anesthetics canbe responsible for allergies?
Methylparaben
Why does pregnancy predispose one to cardiovascular toxicity from LA’s?
Pregnancy = ↓ plasma cholinesterases
Which two factors predispose our OB population to local anesthetic toxicity?
- ↓ plasma esterases
- ↓ plasma proteins
Should a local anesthetic toxicity patient be hyperventilated or hypoventilated?
Why?
Hyperventilation = ↓ CO₂ = ↓ acidosis
If cardiac arrest occurs with LAST syndrome, how should our epinephrine dosing change?
Small doses (10mcg - 100mcg boluses) are preferred with LAST ACLS.
How much vasopressin should be given if a patient is suffering from hypotension from LAST syndrome?
Trick question. Vasopression should not be given with LAST syndrome.
56kg so 1.5mLs x 56kg = 84mLs
20% infusion = 200mgs / 1mL
84mLs x 200mgs = 16,800mgs administered
What is Cocaine’s MOA?
Blocks presynaptic re-uptake of NE and Dopamine → Increases postsynaptic levels and ↑SNS.
What drug is best for treating cocaine toxicity?
Nitroprusside
If Drug V (weak base) has a pKa of 9.1, will the drug be more ionized or nonionized at physiological pH?
pKa - pH
9.1 - 7.4 = +1.7
Drug V will be more ionized at physiological pH.
Weak Bases, pKa before pH
Weak Acids, pKa afterpH
If the pKa of LA (a weak base) is at 4.5, will the drug be more ionized or nonionized at physiological pH?
pKa - pH
4.5 - 7.4 = -2.9
LA will be more non-ionized at physiological pH.
Weak Bases, pKa before pH
Weak Acids, pKa afterpH
LA1’s pKa is 9.2, and LA2’s pKa is 7.5. Which of the following are correct when placed in physiological pH? Select 2 answers.
A. LA2 has more non-ionized components
B. LA1 has more ionized components
C. LA2 has more ionized components
D. LA1 has more non-ionized components
B and C
LA1
9.2 - 7.4 = +1.8 (ionized)
LA2
7.5 - 7.4 = +0.1 (ionized)
Weak Bases, pKa before pH
Weak Acids, pKa afterpH
What is epinephrine 1:200,000 mean?
Convert that to mcg/mL.
1:200,000 means 1 gram of epinephrine is dissolved in 200,000 mL of solvent.
- 1g/200,000 mL
- 1000mg/200,000 mL
- 1 mg/200 mL
- 1000 mcg/200 mL
- 10 mcg/2 mL
- 5 mcg/mL
Compute 1:500,000 to mcg/mL
2 mcg/mL
- 1 g/500,000 mL
- 1000 mg/500,000 mL
- 1 mg /500 mL
- 1000 mcg/500 mL
- 10 mcg/5 mL
- 2 mcg/mL
Shortcut: 1,000,000 divided by the solvent number. 1 million/500,000 = 2 mcg/mL
Compute 1:500,000 Epi to mcg/mL
1,000,000/ 500,000=2
2 mcg/mL
Compute 1:10,000 Epi to mcg/mL
1,000,000/ 10,000 = 100
100 mcg/mL
Compute 1:1000 Epi to mcg/mL
1,000,000/ 1000 = 1000
1000 mcg/mL
0.25% equates to how many mg per mL ?
2.5 mg/mL
0.5% equates to how many milligrams per milliliter?
5 mg/mL
1% equates to how many milligrams per mL ?
10 mg/mL
2% equates to how many milligrams per mL ?
20 mg/mL
2% lidocaine is the most common concentration used in the OR
4% equates to how many milligrams per mL ?
40 mg/mL
112.5 mg of Bupivacaine with Epi and 250 mg of Lidocaine with Epi were given during surgery.
What are the percentages of each LA based on the recommended max single dose in mg?
Max single dose of Bupivacaine with Epi: 225 mg
112.5/225 = 50%
Max single dose of Lidocaine with Epi: 500 mg
250/500 = 50%
When the peripheral nerve block is wearing off, what comes back first? Proximal or Distal?
Proximal comes back first & then distal.
Peripheral Nerve Block onset of action is dependent on the local anesthetic’s _________.
pK
The duration of a peripheral nerve block depends on the _____ of the local anesthetic.
dose
What is the sequence of blockades for a segmental block in Neuraxial Anesthesia?
- SNS (Myelinated preganglionic B fibers)
- Sensory (Myelinated A, B fibers, unmyelinated C fibers)
- Motor (Myelinated A-δ and unmyelinated C fibers)
For SAB, the _______ effect is 2 spinal segments cephalad of the sensory block.
For SAB, the _______ effect is 2 spinal segments below the sensory block.
SNS
Motor
What can be added to LA so that its specific gravity can increase?
What can be added to LA so that its specific gravity can decrease?
Glucose added → hyperbaric solution.
Distilled water added → hypobaric solution
Regarding weak bases, the pKa is ________ pH.
before
ex. pKa 9, pH 7 → 9 - 7 = +2
Regarding weak acids, the pKa is ________ pH.
after
ex. pKa 9, pH 7 → 7 - 9 = -2
Nicely negative numbers are _________.
non-ionized