Local Anesthetics Flashcards
1
Q
General MOA of local anesthetics
A
inhibit voltage gated Na channels (VGSD) ion flux – bocks conduction of AP in nociceptive nerve fibers achieving rapid analgesia w/o sedation
2
Q
VGSC structure
A
pore-forming alpha subunit, 4 beta subunits Depolarization: alpha residues shift to open Repolarize: alpha residues go back Inactive:
3
Q
Nociceptive fiber quality
A
less myelination, more sensitive to sodium channel inhibition (relative selectivity)
- LA’s are NOT totally selective for nociceptive fibers.
4
Q
TRPV1 receptor
A
selectively expressed in nociceptive fibers; when administer capsaicin (TRPV1 ligand) with LA, selectively blocks pain receptors.
5
Q
Benzocaine
A
Ester
6
Q
Procaine
A
Ester
7
Q
Tetracaine
A
Ester
8
Q
Lidocaine
A
Amide
1-3 hours
9
Q
Bupivacaine
A
Amide
DOA - 2-5 hours
10
Q
Mepivacaine
A
Amide
DOA - 1.5-3 hours
11
Q
Prilocaine
A
Amide
12
Q
Ropivacaine
A
Amide
13
Q
Dibucaine
A
Amide
14
Q
Esters
A
- Structure related to cocaine
- Short half life (
15
Q
Amides
A
- Longer lasting effect
- Metabolized by Cyp 450
