L10: Local Anesthetics (Garcia) Flashcards
chars. of amides
- stable in solution
- enzymatic degradation in the liver
- no p-Aminobenzoic acid metabolite
chars. of esters
- unstable in solution
- metabolized in plasma (cholinesterase enzymes)
- p-Aminobenzoic acid metabolite (allergic rxns)
amide drugs (DNK)
lidocaine bupivacaine mepivacaine ropivacaine EMLA
ester drugs (DNK)
cocaine
benzocaine
procaine
tetracaine
chars. of lidocaine
- must have high plasma conc. before causes toxicity
- short half-life; metabolized quickly
bupivacaine chars.
- very lipid soluble; will get highest plasma conc. quickest (easier to get toxicity)
- can cause CNS, CV side effects if given IV
which safer: bupivacaine or ropivacaine
ropivacaine (lidocaine safer than ropivacaine)
only local anesthetic absorbable into cornified skin
EMLA
-expensive
factors that affect onset***
lipophilicity
pKa
conc.
dose and volume
proximity to nerve (closer –> faster onset)
type of nerve (thinner, myelinated nerves easier to block)
how does pKa affect onset?***
(pH at which drug will be 50/50 ionized and non-ionized form)
-must be non-ionized to go through membrane, so in an acidic env. of infection/inflamm., even more in ionized form and will have harder time getting into membrane
factors that affect duration***
vascular effect: closer to vascular bed will have faster effect
tissue blood flow
vasoconstrictor (will caused prolonged duration)
dose
affinity to Na receptor
MOA of local anesthetic***
- Na channel blocker
- acts on neuron axon
- affects depolarization
- decreases n. conduction
- affects both sensory and motor neurons
- may cause vasodilation
factors affecting action
pH/pKa (lower the pH, less the drug works) proximity dose volume spread (related to volume)
CS of neurologic toxicity from local anesthetics
tremor
nervousness
seizures
CC/CNS ratio (higher better; want drugs that have high conc. in serum for CV collapse compared to CNS effect; don’t want cardiotoxic effects to occur until much higher concs.)
CS of CV toxicity from L.A.
bradycardia
sinus arrest
fibrillation
bupivacaine