Lecture 17 (Exam 4 Local Anesthetics Part II) Flashcards
What is the average pKa of local anesthetics?
8
What is the function of the Alkalinization of LA Solutions?
What are the benefits of alkalinization?
Alkalinization increases the percentage of lipid-soluble or non-ionized forms.
Benefits:
* Faster onset of action
* ↑ Onset Peripheral and epidural blocks by 3 to 5 mins.
* Enhances the depth
* Increase the spread (i.e., epidural)
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 adjuvant medication prolongs the duration of local anesthetics?
- Dexmedetomidine
- Magnesium
- Clonidine
- Ketamine
- Dexamethasone
What will be the results of combining LA Chloroprocaine & Bupivacaine?
- Produce a rapid onset
- Tachyphylaxis (bupivacaine)
What is added to 30 mL of LA to alkalinize the drug?
1 mL of 8.4% Sodium Bicarbonate
This will increase the non-ionized form of LA.
Make sure the mixture does not contain any precipitate.
The toxic effects of combining LA are _______
Additive. (1+1 =2)
Compare the onset of action between chloroprocaine and bupivacaine.
Chloroprocaine: Rapid
Bupivacaine: Slow
What vasoconstrictors are available to use with LA?
Epinephrine
Phenylephrine
Why is it important to use vasoconstrictors with LA?
The duration of action of a LA is proportional to the time the drug is in contact with nerve fibers. For this reason, epinephrine may be added to LA solutions to produce vasoconstriction, which limits systemic absorption and maintains the drug concentration in the vicinity of the nerve fibers to be anesthetized.
What are the results of using vasoconstrictors with LA?
- Produce vasoconstriction
- Increased neuronal uptake of LA
- α-adrenergic effects may have some degree of analgesia
- No effect on the onset rate of LA
- Enhanced cardiac irritability with inhaled anesthetics
- Systemic absorption → HTN (tachycardia)
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
How much epinephrine or phenylephrine is given with bupivacaine or lidocaine for a subarachnoid block (SAB)?
- 0.2 mg Epi
- 2 mg Phenylephrine
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
This is the epinephrine that we find in our crash carts.
0.25% concentration is how many mg/mL
2.5 mg/mL
0.5% concentration is how many mg/mL
5 mg/mL
1% concentration is how many mg/mL?
10 mg/mL
2% concentration is how many mg/mL?
20 mg/mL
2% lidocaine is the most common concentration used in the OR
4% concentration is how many mg/mL?
40 mg/mL
Your surgeon injected 20 mLs of Bupivacaine 0.25% with 1:200,000 of Epi.
What are the total mgs for Bupivacaine and the total mcgs for Epinephrine?
Bupivacaine:
0.25% = 2.5 mgs/mL
2.5 mgs x 20 mLs = 50 mgs total
Epinephrine:
1:200,000 = 5 mcg/mL
5 mcg x 20 mLs = 100 mcg total
Lidocaine Recommended Max Single Dose:
Lidocaine Recommended Max Single Dose with/Epi
Lidocaine Recommended Max Single Dose for Spinal
300 mg
500 mg w/ Epi
100 mg
Mepivacaine Recommended Max Single Dose
Mepivacaine Recommended Max Single Dose with/Epi
Mepivacaine Recommended Max Single Dose for Spinal
400 mg
500 mg w/ Epi
100 mg
Prilocaine Recommended Max Single Dose
600 mg
Bupivacaine Recommended Max Single Dose
Bupivacaine Recommended Max Single Dose with/Epi
Bupivacaine Recommended Max Single Dose for Spinal
175 mg
225 mg w/ Epi
20 mg
Clinical Scenario Question
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%
Where are topical anesthetics applicable?
Applicable on the mucous membranes of the nose, mouth, tracheobronchial tree, esophagus, or GU tract.
Which anesthetic has localized vasoconstriction that will decrease blood loss and improve surgical visualization?
Cocaine (4-10%)
Which anesthetic is great with surface anesthesia?
Lidocaine (2-4%)
Lidocaine inhalation does not alter airway resistance, but ______
vasodilation
What LA care not effective for topical anesthetic?
Procaine and Chloroprocaine
These drugs do not penetrate mucous membranes as effectively as cocaine or lidocaine.
What is an LTA?
- Lidocaine tracheal anesthesia
- Localized tracheal anesthesia
Eutectic Mixture of LA (EMLA) contains what LA?
Dose:
Onset:
Lidocaine 2.5% + Prilocaine 2.5% = 5% LA
Dose: 1 to 2 gms/ 10 cm2 area
Onset: 45 mins
EMLA has to be applied for ______ hours before skin graft.
2 hours
EMLA can be applied for 10 minutes before any of these procedures:
Cautery of genital warts
Venipuncture, lumbar puncture
Arterial cannulation (Nitroglycerine)
Myringotomy
EMLA considerations
- Caution with methemoglobinemia
- Not recommended for skin wounds
- contraindicated with amide allergies
Other Topical Anesthesia Preparations besides EMLA
- Amethocaine (EMLA-like)
- Tetracaine 4% Gel
- Lidocaine 7%
- Tetracaine 7%
What is considered local infiltration with LA?
Extravascular placement of LA (subcutaneous injection)
What LAs are used on inguinal operative sites?
- Lidocaine 1% or 2%
- Ropivacaine 0.25%
- Bupivacaine 0.25%
How can you double the duration of LA for local infiltration?
Epinephrine 1:200,000
What are the contraindications of using epinephrine on LA for local infiltrations?
- Not intracutaneously or into tissues at end arteries
- Fingers, toes, ears, nose, penis
Can cause necrosis.
How is Peripheral Nerve Block achieved?
MOA?
Achieved by LA injection into tissues surrounding individual peripheral nerves or nerve plexuses.
MOA: diffusion from outer mantle to central core of nerve along a concentration gradient.
* Smallest sensory and ANS fibers first, then larger motor and proprioceptive axons.*
Signs and Sx of Peripheral Nerve Block?
The proximal area (site of LA administration) is affected first and then distal.
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 _________.
Lidocaine OOA:
Bupivacaine OOA:
LA pK
Lidocaine OOA: 3 mins
Bupivacaine OOA: 15 mins
Peripheral Nerve Block Duration depends on _____ of local anesthetic.
dose
Continuous Infusion Blocks benefits.
- Improved pain control
- Less nausea
- Greater satisfaction
- Additives are used with continuous infusion blocks (ie: Ketolorac, Ketamine, Decadron)
What is a Region Bier Block?
Bier Block IV injection of LA into an extremity isolated from the rest of the systemic circulation with a tourniquet.
Sensation and muscle tone dependent on tourniquet
What LA is commonly used in Bier Block?
Lidocaine
Bier Block Steps
- IV start
- Exsanguination
- Double cuff
- LA injection
- Surgeon will perform procedure
- IV D/C
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)
Clinical Scenario: Neuraxial blockade is the last reference with which assessment parameters
A. NIBP
B. Heart Rate
C. Cold Alcohol Pad
D. Leg Movement
D. Leg Movement
How is a Spinal Anesthesia Block (SAB) produced?
Produced by direct injection of LA into subarachnoid
What is used for confirmation of a Spinal Anesthesia Block (SAB)?
CSF
What is the principal site of action for SAB?
Preganglionic fiber
For SAB, the _______ effect is on the same level of denervation.
sensory
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
If the sensory block is at T5, where is the SNS block?
T3
This SNS block will trigger an asystole event.
What dermatoses correspond with our cardiac accelerator?
T1 to T4
Clinical Scenario Slide:
If the assessed sensory level after SAB is T6 ( Top of Xiphoid Process), what are the blocked SNS and motor levels?
SNS Block: T4
Motor Block: T8
Most common LA used in SAB
Most common: Tetracaine, Lidocaine, Bupivacaine, Ropivacaine, and Levobupivacaine
What factors affect SAB dosage?
- Height of patient (volume of subarachnoid space)
- Segmental level of anesthesia desired
- Duration of anesthesia desired
For SAB, _____ is more important than _______ of drug (%) or the volume (mLs) of the solution injection.
Dose; Concentration
SAB Dose:
5 ft = _____mL of 0.75% Bupivacaine
+ ______ mL for every inch above…. 2 cc total ( 1½ hours to 2 hours)
1 mL
0.1 mL
For someone who is 5’5”, you will give 1.5 mL of bupivacaine for a SAB.
For SAB, the _________ of LA is important in determining the spread of the drug.
specific gravity
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
Which side will you want to position a right-hip arthroplasty patient on if they receive a hyperbaric LA solution?
Right side lying, the hyperbaric solution will “sink.”
Which side will you want to position a right-hip arthroplasty patient on if they receive a hypobaric LA solution?
Left side lying, the hypobaric solution will “float”.
The most common LA used in Epidural Anesthesia.
Lidocaine
Good diffusion through tissue and safer
What is the onset of epidural anesthesia?
Onset: 15 to 30 minutes
Epi 1:200,000 with ___________ offers no advantage in an epidural block.
bupivacaine
Can epidural anesthesia cross the placental barrier with OB and C-section patients?
Yes
What is the difference between SAB and epidural blocks?
No differential zone of SNS, sensory, and motor blockade.
What is considered an acceptable additive to both epidural and SAB to produce a synergistic effect?
Opioids
What is Tumescent?
Subcutaneous infiltration of large volume (5L or more)
What makes up the tumescent solution?
- Diluted Lidocaine (0.05% to 0.1%)
- Epinephrine 1:100,000
What causes the tumescent effect?
The taunt stretching of overlying blanched skin d/t large volume → Tumescent Effect
Fat can be aspirated without blood loss and provide prolonged post-op analgesia.
Where is tumescent usually administered?
- Thigh
- Abdomen
- Hips
- Buttocks
When is the plasma peak for tumescent?
12 to 14 hours s/p injection.
Regional Anesthesia Lidocaine with Epi Dose.
7 mg/kg
Highly diluted Lidocaine with Epi Tumescent dose (mg/kg).
35 to 55 mg/kg
What is the theory with the Tissue Buffering System?
1 gram of SQ can absorb up to 1 mg of Lidocaine