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? (4)
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 medications prolongs the duration of local anesthetics?(5)
- 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