Local anesthetics Flashcards
What is the mechanism of action of local anesthetics?
Blocks voltage-gated Na channels in neuronal cell membrane; slows rate of depolarization (threshold potential not reached; action potential not propagated)
True/False: in general, smaller diameter fibers and those with less myelination are blocked first.
True
What is the exception to the order of nerve blockade with local anesthetics?
Brachial plexus block. Motor fibers are blocked first
What is the order of nerve blockade when using local anesthetics?
1) B fibers (preganglionic sympathetic)
2) A-delta and C fibers (pain)
3) A-gamma (proprioception)
4) A-beta (touch, pressure)
5) A-alpha (motor)
True/False: all local anesthetics are weak acids.
False. All are weak bases; pK ~7.7-9
How does pK affect local anesthetics?
Lower pK (closer to tissue pH) –> faster onset
How does protein binding affect local anesthetics?
Higher protein binding –> longer duration of action
How does lipid solubility affect local anesthetics?
Higher lipid solubility –> higher potency
What are some commonly used amides?
Lidocaine, bupivacaine (Marcaine), mepivacaine (Carbocaine), ropivacaine, prilocaine (with lidocaine in EMLA cream)
True/False: all local anesthetics can be given IV or used for intravenous regional anesthesia (IVRA).
False. Lidocaine is the only LA that can be given IV or used for IVRA
What are the pharmacodynamics of lidocaine?
Fast onset, short duration of action (1-2 hours when used in loco-regional techniques
What are the effects of lidocaine when used systemically (IV)?
Anti-arrhythmic; decreases MAC (MAC-sparing); analgesic; free radical scavenger; improves GI motility
What are the pharmacodynamics and adverse effects of bupivacaine?
Intermediate onset; duration of 3-8 hours; has the highest CV toxicity
What are the pharmacodynamics and uses of mepivacaine?
Fast onset; duration of 1.5-3 hours; used for intra-articular nerve block (common in large animal)
What are the pharmacodynamics and adverse effects of ropivacaine?
Intermediate onset; duration of 3-8 hours; less cardiotoxic than bupivacaine