wk1- intro to LA Flashcards
uses for LA
- diagnostic
- therapeutic
- surgery
modes of delivery of LA
- topical
- infiltrative
- ring block
- peripheral nerve block
- EMLA
- iontophoresis
define LA and how do they work
reversible loss of sensation in an area of the body
they block sodium ion channels so sodium cannot flow into neurons
this inhibits the transmission of APs along individual neurons
anatomy of LA
aromatic ring- confers lipid solubility
intermediate linkage- permits classification and mode of metabolism (amide or ester)
terminal amine- charged or uncharged to make it water or lipid soluble
types of LA
amide
ester
ester
metabolism, toxicity, allergy, stability, onset of action, pKa
M: rapid by protein cholinesterase
T: less likely
A: more likely
S: photo/temp labile
O: slower
pKa: higher (8.5-8.9)
amide
metabolism, toxcity, allergy, stability, onset, pKa
M: slower, by the liver
T: more likely
A: less likely
S: very stable
O: moderate to fast
Pka: Close to 7.4
types of esters
cocaine
chloroprocaine
tetracaine
types of amides
bupivacaine
lidocaine
ropivacaine
LA and physiochemical properties
LA- weak base that needs to be unionised to reach site of action inside the neuron
then dissociation causes it to become in ionised form that binds to sodium ion channel once inside neuron
unpronated LA molecules can what
pass through cell membranes because theyre lipophilic
what is a proton
H plus
if pH decreases (more acidic)
more protons
if pH increses (more alkaline)
less protons
define pKA
pH where drug is 50% ionised and unionised