Lecture2 Flashcards
What are the three primary effects of Localized anesthetics?
Decreases rate of depolarization
Depolarization is not sufficient enough to reach threshold
Impulse is not propagated, never reaching CNS
What ratio of positive charge to neutral charge do we want in LAs?
75:25
What is the normal pH of tissues? and what direction does it go with inflammation?
7.4 and it decreases (acidic)
What does sodium metabisulfite do to the LA’s and why is it added?
It acidifies to prevent oxidation of the vasoconstrictor
What is the mode of action of LAs?
Decrease the permeability of sodium ions and conduction blockade.
What tissue has the highest perfusion rate and potential of toxicity?
Skeletal muscles (largest mass in the body)
Can LA cross BBB or the placental barrier?
Yes both
The longer it takes to hydrolyze esters, the higher or lower the toxicity?
higher toxicity
Where are amides metabolized? and which one is partially in the lungs?
In the liver, prilocaine
What is the metabolic byproduct of prilocaine?
O-toluidine leading to methemoglobinemia
Amide and ester half lives?
Amides: 90-160 minutes
Esters: .1-.7 hrs
*Increased half life is increased toxicity
Amino esters are metabolized by what?
Plasma pseudocholinesterases
*Benzocaine (topical anesthetic), cocaine (both vasoconstrict and dilate, procaine (used for vastdilation)
What are the amino amides?
articaine, bupivicaine, lidocaine, mepivocaine, prilocaine
Why are LA vasoconstrictors?
decreased perfusion (localized response), lower plasma levels, more LA into the nerve, less bleeding at site
what are the three catecholamines that are vasoconstrictors and what do they bind to?
Epinephrine, norepinephrine, and levonodefrin.
They activate alpha receptors