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)