**in progress** 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
* 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
- 0.2 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
0.25%
2.5 mg/mL
0.5%
5 mg/mL
1%
10 mg/mL
2%
20 mg/mL
2% lidocaine is the most common concentration used in the OR
4%
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?
Cocaine
Which anesthetic is great with surface anesthesia?
Lidocaine
Lidocaine nhalation does not alter airway resistance, but ______
vasodilation
What LA care not effective for topical anesthetic?
Procaine and Chloroprocaine
Rank topical anesthetic base on strength
Cocaine (4% to 10%) > Tetracaine (1% to 2%), Lidocaine (2% to 4%)
What is an LTA?
(lidocaine tracheal anesthesia)
(localized tracheal anesthesia)
(laryngeal tracheal anesthesia) Slide 23
Eutectic Mixture of LA (EMLA) contains what LA?
Dose:
Onset:
Lidocaine 2.5% and Prilocaine 2.5% = 5% LA
Dose: 1 to 2 gms/ 10 cm2 area
Onset: 45 mins
When do you have to wait two hours for EMLA?
2 hours
Skin grafting
EMLA 10 mins
Cautery of genital warts
Venipuncture, lumbar puncture
Arterial cannulation (Nitroglycerine)
Myringotomy
EMLA considerations
EMLA
Caution with methemoglobinemia
Not recommended for skin wounds
C/I with amide allergies
Other Topical Anesthesia Preparations besides EMLA
Other Preparations:
Amethocaine (EMLA-like)
Tetracaine 4% Gel
Lidocaine 7%
Tetracaine 7%
Local Infiltration
Local Infiltration
Local Infiltration
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?
Proximal 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
3 mins
15 mins
Peripheral Nerve Block Duration depends on _____ of local anesthetic.
dose
Continuous Infusion Blocks
- Improved pain control, less nausea, & greater satisfaction
- Additives are used
Examples of Peripheral Nerve Blocks
- Interscalene
- Axillary
- Femoral
- Sciatic
Sciatic Nerve Block…
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
IV D/C
For a segmental block in Neuraxial Anesthesia, what fibers will be affected first.
Myelinated Preganglionic B fibers (fastest) (SNS)
- This will affect BP (↓) an HR(↓)
Second fibers blocked?
What fibers will be blocked last.
Sequence of Blockade
- SNS
- Sensory
- Motor
Clinical Scenario: Neuraxial blockade
A.
B.
C.
D.
D. Leg Movement
How is a Spinal Anesthesia Block (SAB) produced?
Produced by direct injection of LA into subarachnoid
Spinal Anesthesia Block (SAB), what is used for confirmation?
CSF
What is the principal site of action for SAB?
Preganglionic fiber
What SAB, the _______ effect is on the same level of denervation.
sensory
_____ is 2 spinal segments cephalad of sensory
______ is 2 spinal segments below sensory
SNS
Motor
What dermatoses correspond with our cardiac accelerator?
T1 to T4
Clinical Scenario Slide: If the assessed sensory level after SAV is T6 ( Top of Xiphoid Process)….
Most common LA used in SAB
Most common: Tetracaine, Lidocaine, Bupivacaine, Ropivacaine, and Levobupivacaine
The dosage of SAB block is according to what three factors?
- 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
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 SAB, the _________ of LA is important in determining the spread of the drug.
specific gravity
Hyperbaric (LA sp. gr. > CSF) with _______ is additive
Hypobaric with ________ as additive
glucose
distilled water
Right-sided hip arthroplasty example
Hypobaric example
The most common LA used in Epidural Anesthesia
Lidocaine
What vasoconstrictors are available to use with LA?
Epinephrine
Phenylephrine