Anesthetics - Local Flashcards
amide local anasthetics
lidocaine, prilocaine, bupivacaine
ester local anesthetics
procaine, tetracaine
MOA of local anesthetics
voltage-gate sodium channel block; drug has preference for activated & inactivated states so frequency of nerve depol is important in allowing binding
describe the differential blockade
small myelinated & non-myelinated fibers are most sensitive (B & C fibers) while large myelinated fibers are least sensitive (A)
describe the chemistry of the local anesthetics
Majority are weak bases with Pka ~ 8 (therefore at extraneural pH of 9, 10:1 of base will be non-ionized & at intraneural pH of 7, 10:1 will be ionized)
describe the anatomical distribution of local anesthetics
Anesthetic runs proximal to distal & recovery runs proximal to distal
describe systemic toxicity of local anesthetics
tinnitus, metallic taste, oral numbness, seizures
which drugs can cause methemoglobinemia
prilocaine > benzocaine
how do you treat methemoglobinemia
∙ IV methylene blue as antidote
∙ or ascorbic acid
which is more potent and more cardiotoxic
bupivacaine
which are SA
procaine (slow onest & short duration)
which are intermediate acting
lidocaine, prilocaine (rapid onset)
which are LA
bupivacaine, tetracaine (slow onset)
describe metabolism & elimination of amides
hepatic metabolized & renal elimination – metabolism affected by CV status, liver dz, toxemia of pregnancy, cimetidine, volatile anesthetics, b-blockers
reversal agent for vasoconstrictor
phentolamine (non selective alpha antagonist)
describe metabolism & elimination of esters
non-specific esterase enzymes & renal elimination – metabolism affected by liver dz, pregnancy, chemo & atypical enzyme activity
what causes the differences in onset & duration
Differences in onset & duration from lipid solubility, dissociation constant, chemical linkage & protein binding
topical use only
benzocaine
what is the purpose of giving with vasoconstrictor
remove concentration gradient and prevent systematization
use for mucosal membranes
benzocaine
DDIs for vasoconstrictors
possible with BB, TCAs, halothane, HTN, heart block, cerebral vascular insufficiency
which is useful for post op analgesia
bupivacaine
AE of benzocaine
methemoglobinemia
describe baricity
Baricity = density compared to CSF. Drug distribution depends of baricity and patient orientation. ↑solution temperature = ↑spread (due to ↓viscosity).