Local Anesthesia Flashcards
3 parts of local anesthesia
aromatic group
intermediate linkage
amine group
aromatic group
lipophilic properties
intermediate linkage
spacial separation between lipophilic and hydrophilic ends
connects them with ester or amide
amine group
affects pKa and speed of onset
difference between amide and ester
amide - union of carboxylic acid and amine (peptide bond is amide)
ester -union of carboxylic acid and alcohol
except for procaine, all injectable dental locals are (amines or esters)
amines
topicals are mostly (amines or esters)
esters
the amine portion is the ____
base
what is special about free bases?
the amine portion is a free base
only free bases can cross the cell membranes, so onset of action is faster for lower pKa’s (stronger acids) because they give up their protons more easily and become uncharged “free bases”
onset is faster for ____
low pKa’s (strong acids)
acidic environments like inflamed tissue…
have slow onset, since the base remains protonated in the low pH environment (impedes local anesthesia development)
locals stabilize ________
membranes
decrease rate of depolarization and repolarization
locals prevent _____
rapid sodium influx
needed to make an AP
why are the pharmacokinetics of locals unique?
they become ineffective when absorbed into the system / blood stream
local anesthetics wear off when…
redistributed throughout the body to all tissues (when the numbness goes away)