Questions and CORRECT Answers
Ester nomenclature - CORRECT ANSWER - Drugs with one "i"
Amide nomenclature - CORRECT ANSWER - Drugs with two "i"s
Naturally occurring Local? - CORRECT ANSWER - Cocaine
Most widely used Local? - CORRECT ANSWER - Lidocaine
Reversal for Locals? - CORRECT ANSWER - Oraverse
3 Sections of a Local Anesthetic Molecule? - CORRECT ANSWER - 1. Benzene Ring
(Lipophilic-Lipid Soluble)
2. Ester (O) or Amide (N) Linkage
3. Quartenery Amine (Hydrophilic-Water Soluble)
Ester metabolism - CORRECT ANSWER - metabolized by cholinesterase, which are
found in plasma. this metabolism is rapid which makes esters short acting.
Longest acting ester - CORRECT ANSWER - tetracaine
Amide metabolism - CORRECT ANSWER - metabolized by liver enzymes= longer acting
Explain allergies to Local Anesthetics - CORRECT ANSWER - 1. Most commonly found
with esters (bc people are exposed to the lipophilic portion PABA daily via cosmetics).
2. When allergic to an ester you're allergic to all esters but not to amides
, 3. When allergic to an amide youre ONLY allergic to that amide
MOA of Locals - CORRECT ANSWER - blocking Na channels in nerves
Ionized portion of Locals - CORRECT ANSWER - Water soluble, can't penetrate nerve
but able to block Na channel once inside the axoplasm.
Non-ionized portion of locals - CORRECT ANSWER - lipid soluble, penetrate nerve
Exception to typical MOA of Locals? - CORRECT ANSWER - Benzocaine, is water
soluble but can penetrate and block nerve.
Target site of drugs is on what side of the membrane? - CORRECT ANSWER -
cytoplasmic
What makes the Local diffuse in? makes it stop? - CORRECT ANSWER - Concentration
gradient (greater outside the nerve than inside)
Absorption
Locals are _____ drugs? - CORRECT ANSWER - basic
pKa effects what parameter of Locals? how? - CORRECT ANSWER - Onset, lower pKa
(closer to 7.4=more non ionized) the faster the onset
Fastest Local Anesthetic? Why is this drug special? - CORRECT ANSWER -
Choloropropaine
Exception to pKa rule of Locals.