Lecture 19 4/4/24 Flashcards
Which steps of the nerve conduction pathway can be treated using local anesthetics?
-modulation
-transmission
-transduction
What are the characteristics of resting membrane potential?
-involves Na+/K+ pumps
-K+ moves into cells, Na+ moves out
-resting membrane potential stays around -60 to -70 mV
What are the characteristics of action potentials?
-start with a stimulation
-Na+ channels are activated
-influx of Na+ into cell
-membrane potential changes to positive
What is nociceptive wind up?
painful stimulation leads to more painful stimulation
What are the general characteristics of local anesthetics?
-Na+ channel blockers
-goal is to block sensory fibers
-composed of a lipophilic 6 carbon ring and a hydrophilic side chain linked by an intermediate hydrocarbon chain
How are esters metabolized?
hydrolyzed by cholinesterase enzymes in the plasma and liver
How are amides metabolized?
hepatic microsomal enzymes
What are the characteristics of amide metabolism?
-more complex and longer process compared to esters
-greater risk of toxicity
What is the regional perfusion technique?
increased pressure from a cuff/tourniquet leads to increased regional concentration of the local anesthetic
What are the characteristics of epidural catheters?
-provide regional anesthesia
-can be placed and left in for multiple days for continued access
What is a wound soaker catheter?
a catheter/drain that is incorporated into an incision for post-operative local anesthetic infusion
What is the pharmacology of local anesthetics?
-can exist in ionized or unionized forms
-unionized fraction is more lipid soluble and can cross nerve membrane
-weak bases; pKa of 8-9
-sufficient fraction of unionized form present at physiologic pH (7.4)
-ionized form more dominant in acidic environments (infection sites); cross into nerve cells more slowly
How does high lipophilicity impact how local anesthetics work?
-high potency
-longer onset of action
-longer duration of action
How does protein binding impact how local anesthetics work?
-correlates with slower elimination
-longer duration of action
What are the characteristics of lidocaine?
-amide LA
-one of the most frequently used
-quick onset and duration of action
-different concentrations and preparations available