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)