Local Anesthetics - Kruse Flashcards
Function of local anesthetics
Bind and block VGSC’s w/in nerves, blocking action potential potentiation
2 classes of local anesthetics (w/ members)
Amides - Lidocaine, Mepivacaine, Bupivacaine, Ropivacaine, Articaine
Esters - Benzocaine, Cocaine, Procaine, Tetracaine
How to remember which ones are amides (vs. esters)?
Amides = have 2 "i"s in the name Esters = have 1 "i" in the name
Duration of action of amides vs. esters
Esters - more prone to hydrolysis = shorter duration of action
What may be indicated to be used with the shorter duration drugs (esters)?
Vasoconstrictors (epinephrine) - to reduce systemic absorption and destruction (alpha-1 agonist)
How is cocaine unique?
Intrinsic sympathomimetic vasoconstrictive properties (only ester that does NOT need epinephrine)
Metabolism of esters vs. amides
Esters - PLASMA butyrylcholinesterase
Amides - LIVER P450 enzymes
Potential contraindication to using amides
Hepatic disease - can accumulate amide drug metabolites and cause toxicity
Potency of local anesthetics
More lipophilic = more potent = longer duration of action
Which are the more lipophilic ones?
So?
Tetracaine, Bupivacaine, Ropivacaine
More potent and longer duration of action
Which nerve fibers are blocked more often by local anesthetics?
Smaller, more myelinated fibers
Motor before sensory (motor = more peripheral)
Proximal sensory before distal sensory (extremities)
Rank nerve fibers in order from MOST to LEAST affected by local anesthetics (6 total)
- B - small, myelinated
- C - small, unmyelinated
- A-delta
- A-gamma
- A-beta
- A-alpha
3 major routes of administration
- Topical
- Injections
- IV regional
Infiltration anesthesia
Injection directly into vicinity of peripheral nerve endings
Block anesthesia
Examples?
Injection directly into major nerve trunk (anesthetize region distal to site of injection)
Femoral nerve (distal to knee surgery), brachial plexus (UE or shoulder surgery)
Spinal anesthesia
Injection into CSF in lumbar space (anesthetize portion of body below the level)
Epidural anesthesia
Injection or continuous infusion into epidural space (all regions of spinal cord)
IV regional anesthesia
Short procedures (
While epinephrine (alpha-1 agonists) may be used as a vasoconstrictor along w/ a local anesthetic to prolong the life of the drug, where should the epinephrine NOT be placed?
Where should it be placed WITH CAUTION?
Tissues supplied by end arteries (fingers, toes, ears, nose, penis)
Vasoconstriction could cause GANGRENE
Muscle tissues (Beta-2 agonist in muscle vasculature could cause vasodilation and systemic toxicity)
Which local anesthetic does NOT need epinephrine?
Cocaine - potent vasoconstrictor (sympathomimetic)
2 types of undesired effects from local anesthetic toxicity
- Systemic (CV or CNS depression)
2. Direct neurotoxicity (when given near major nerve trunks or spinal cord)
A patient needs a large amount of a local anesthetic. What is indicated for protective measures?
A parenteral benzodiazepine (Diazepam or Midazolam) - to provide prophylaxis against CNS toxicity by raising seizure threshold
Why might you need a benzo along with a local anesthetic?
Systemic anesthetic –> depression of cortical inhibitory pathways –> unopposed activity of excitatory pathways (seizure)
Side effects of local anesthetics on CV system
Decreased heart conduction –> hypotension
Cocaine –> hypertension, arrhythmias, ischemia (via vasoconstriction)
In addition to being an anesthetic, Lidocaine can be used as a _____
Anti-arrhythmic (slow down heart, let it re-set)
If a patient is allergic to an ester type, what should you do?
Try an amide type (most likely allergic to other ester types)
Benzocaine
Topical ONLY + anesthetic lubricant for tubes
Bupivacaine
Long duration –> prolonged anesthesia
SENSORY over MOTOR
Cocaine
Inhibition of catecholamine reuptake –> euphoria
Topical in upper respiratory tract
Dibucaine
SKIN TOPICAL ONLY
Lidocaine
Alternative if allergic to ester type
Faster, intenser, longer-lasting, more extensive than Procaine
Anti-arrhythmic
Procaine
Lower potency, slower onset, shorter duration
INFILTRATION ANESTHESIA ONLY
Metabolite (PABA) inhibits sulfonamide antibiotics