Miscellaneous of Local Anesthetics Flashcards
What is the effect of sodium bicarbonate on a local anesthetic?
Speeds onset of action, especially commercially prepared epinephrine containing
What is the result of alkalinazation of local anesthetics?
Increases the % of unionized (free base) drug to cross the nerve membrane= speeds onset of action
What is the clinical use of alkalinization of LA?
Used clinically with epidural blocks or to reduce pain of subQ infiltration
What are locals ineffective in?
Acidotic infected tissue
1 mL of 8.4% sodium bicarbonate = _____ local anesthetic (except bupivacaine)
10 mL
What is the pH of commerically prepared LA usually between?
3.9-6.5
What is the relationship of dexmedetomidine and local anesthetics?
Dexmedetomidine has been used in local anesthetic admixtures and a central effect is proposed for prolongation of the local anesthetic effect
What is the relationship of intrathecal magnesium and local anesthetics?
has shown initial promising results (duration of spinal anesthesia was increased)
What does the addition of clonidine and ketamine to regional anesthesia have on pediatric patients?
- prolongs the actions of the local anesthetic
- Good pharmacokinetic and pharmacodynamic profiles of efficacy and safety
What is the relationship of epinephrine and local anesthetics?
Epinephrine (1:200,000 or 5 ug/ml) may be added to local anesthetic solutions to produce vasoconstriction
What is the goal of epinephrine use with LA?
vasoconstriction (goal: prolong duration, not onset as with alkalization)
What is the effect of epinephrine use with LA?
Limits systemic absorption and maintains the drug concentration in the vicinity of the nerve fibers to be anesthetized
What effect does epinephrine to a lidocaine or mepivacaine solution have?
prolongs the duration of conduction blockade and decreases systemic absorption of local anesthetics by 20-30% (less so with bupivacaine)
May be some analgesic effect with __________ properties of epinephrine
alpha-2
What is the principle side effects of local anesthetics?
effects are allergic reactions and systemic toxicity due to excessive plasma and tissue concentrations of local anesthetics
What is the systemic toxicity of LA?
in association with regional anesthesia is estimated to result in seizures in 1 to 4 per 1,000 patient exposures to local anesthetics
What is the most common LA associated with systemic toxicity?
Bupivacaine
What is the allergic reactions associated with LA?
rare, accounting for less than 1% of all adverse reactions to local anesthetics
Which LA are more likely to cause allergic reactions with LA?
Esters that produce metabolites related to PABA are more likely than amide local anesthetics to evoke an allergic reaction
What is a theory of the cause of allergic reactions of LA?
- may be due to methylparaben or similar substances used in preservatives in commercial preparations of ester and amide local anesthetics
- Preservatives are structurally similar to PABA
Cross sensitivity between local anesthetics reflects the common ___________
metabolite PABA
What is true about a patient with a known allergy to an ester LA?
can receive an amide local anesthetic without an increased risk of an allergic reaction
What is true about a patient with a known allergy to an amide LA?
An ester local anesthetic can be administered to a patient with a known allergy to an amide local anesthetic
What is true about LA solutions?
should be preservative free
What is the characteristic developments of Local Anesthetic Systemic Toxicity (LAST)?
Excess plasma concentration
- Inadvertent vascular injection
- Large amount absorbed into circulation from large volume blocks
- Continuous infusion or accumulation of metabolites
What is the magnitude of LAST depends on?
on dose administered, vascularity of injection site, presence of vasoconstrictor, & physiochemical properties of LA drug
How soon can LAST occur?
LAST can present more than 15 minutes after injection; monitoring should continue for at least 30 minutes after injection
What is the biggest culprit of Local Anesthetic Systemic Toxicity (LAST)?
Bupivacaine
What is the impact of neuraxial adjuncts/ opioids have?
way to prolong blocks and analgesia to use less LA
What is involved in systemic toxicity?
the CNS and cardiovascular system
What is the first CNS symptoms?
The CNS inhibitory neurons block first (voltage-gated Na+, K+, Ca++)
What occurs after CNS inhibitory neurons block from LAST?
Seizure (excitatory unchecked initially)
What is the CNS toxicity from LAST?
(from low plasma concentration to increased) : numbness of tongue & circumoral tissues, restlessness, vertigo, tinnitus, difficulty focusing, slurred speech
What occurs as a result of CNS toxicity with LAST?
Skeletal muscle twitching signals imminent tonic-clonic seizures
Review LAST progression effects.
Slide 79
______ can increase LA toxicity
Hyperkalemia
________ can lower seizure threshold
Increase PaCO2
_________ can lower seizure threshold of lidocaine
Increase in serotonin
What is a component of the cardiac symptoms of LAST?
requires greater plasma concentrations than needed for CNS symptoms
What are the inital cardiac symptoms of LAST?
- Increase heart rate
- increase blood pressure (Co-occuring with CNS sign)
What are other associated cardiac effects of LAST?
- dysrhythmias
- heart block
- hypotension, bradydysrhythmia
- reduced cardiac contractility
- asystole
What is true about higher doses of LA and LAST?
- At higher doses, LA also blocks cardiac Na+ channels
- Blocked Ca++ and K+ channels along with inhibition of cAMP production
LAST: ________ more sensitive and blocked first
CNS
What cardiac effects of Lidocaine and LAST?
prolongation of P-R interval and QRS complex
What are the characteristics of bupivacine that make it cardiotoxic?
Protein sites quickly saturated with IV injection leaving significant free form unbound (more cardiotoxic than lidocaine)
What are cardiac toxic side effects of bupivacaine?
Precipitous hypotension, cardiac dysrhythmias and AV block (PVC, QRS widening, VT).
Cardiac Toxicity of bupivacaine is plasma concentration: ________
8-10 mcg/ml
What can help to decreased the cardiac toxicity of bupivacaine?
Threshold for toxicity decreased with beta blockers and Ca++ channel blockers as well as epinephrine and phenylephrine
What are the characteristics of Levobupivacaine and ropivacaine?
prepared with less cardiac toxic S-isomer
What is the mnemonic for greatest systemic absorption to least?
BICEPS B-blood/tracheal I-intercostal C-caudal and para cervical E-epidurals P-perivascular brachial plexus S-sciatic/spinal S-subcutaneous
LAST Prevention: What should be used to avoid this side effect?
Use lowest effective dose of LA (volume & concentration)
LAST prevention: What is n injection technique to decrease the likelihood of occurring?
administer 3-5 ml aliquots pausing 15-30 minutes between each injection
LAST prevention: What needs to be done before each injection?
Aspirate the needle or catheter before each injection
LAST prevention: what needs to be done in potentially toxic doses of LA?
Use an intravascular marker
What is the result of epinephrine being injected into the intravascular space?
Adults: epinephrine 10-15 mcg will produce a 10-beat increase in HR or 15mmHg or greater increase in SBP
What is key to stopping LAST?
Early recognition is key/Stop LA administration
What are some theraputic interventions for LAST?
- Prompt airway support (oxygenate/ventilate)
- Circulatory support
- Treat seizures
What medications can be used for circulatory support with LAST?
epinephrine & amiodarone (avoid vasopressin, Ca++ channel blockers and beta blockers)
What medications can be used for seizure support with LAST?
with BZD (midazolam or diazepam – raise seizure threshold) or propofol (if tolerated); paralyze & intubate if refractory seizures