Local Anesthetics Flashcards
3 components of the LA molecule
lipophilic
intermediate
hydrophilic
aromatic portion of LA molecule
membrane penetration
lipophilic
ester/amide portion of LA molecule
metabolic pathway
alter tonicity
intermediate
amine portion of LA molecule
ionizable
determine charge
hydrophilic
2 types of LA
ester A
amide B
at normal body pH, LA are largely in the __ form
charged cationic
metabolic pathway of ester A
plasma
AND
liver
metabolic pathway of amide B
liver → CYP450
LA are classified as weak __
bases
uncharged LA are __ and cross membranes
lipophilic
injected LA are __ and block Na channels
hydrophilic
effect of infxn/inflammation on LA
infxn/inflammation → decreases pH → increased cationic/charged LA form → decreased membrane passage → decreased pain relief → increased dose required
t/f: buffered LA are more effective
T!
2 esters A
tetracaine
benzocaine
3 amides B
lidocaine
mepivacaine
bupivacaine
bc esters are metabolized by plasma and liver, they have __ duration than amides
and higher risk for __
shorter
allergic rxn
what 2 conditions increase t½ of amides 3x
liver dz
HF
3 factors that affect differential nerve block effectiveness
fiber size
firing rate of fibers
location of fibers
most important factor in effectiveness of differential nerve block
fiber size
which type of fiber is affected first in differential nerve block
small
2 smallest pain fibers
sensory pain
PG sympathetic
affected 1st in nerve block
what increases the effect of nerve bocks
neuron firing rate
what type of pain fiber has the fastest firing rate
active sensory pain fibers
what do you think when you see, dose dependent blockade
increased effectiveness of nerve block with faster firing rate of active sensory pain fibers
in terms of location, which type of pain fiber is affected first
periphery
2 types of pain transmission fibers
A delta
C
describe A delta fibers (2)
myelinated
big
describe C pain fibers (2)
unmyelinated
small
3 factors that decrease absorption of LA
oral
topical
intact skin