Local Anesthetics II (Exam IV) 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.
- Faster onset of action
- Speeds onset of peripheral and epidural blocks by 3 to 5 mins.
- Enhances the depth
- Increase the spread (i.e., epidural)
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
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 prolong the duration of local anesthetics?
- Dexmedetomidine
- Magnesium
- Clonidine
- Ketamine
- Dexamethasone
Adjuvant mixed with LAs:
Dexmedetomidine IV?
Increased duration of:
-Both motor and sensory blocks
-First analgesic request after spinal anestheisa.
Adjuvant mixed with LAs:
Magnisum IV?
Increased duration with SAB with or without opioids.
Adjuvant mixed with LAs:
Clonidine & ketamine?
Pediatric regional anesthesia has a prolonged duration.
Adjuvant mixed with LAs:
Dexamethasone?
Increased duration either IV or mixed with LA.
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
- chloroprocaine & bupivacaine combo.
This will increase the non-ionized form of LA.
Make sure the mixture does not contain any precipitate.
Combining local anesthetics and getting toxic effects is a synergistic process. T/F ?
False. Additive. (1+1 =2)
Compare the onset of action between chloroprocaine and bupivacaine.
Chloroprocaine: Rapid
Bupivacaine: Slow
Both medications have the same potency of 4!
What vasoconstrictors can be utilized with local anesthetics?
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