Quiz 5 (Local Anesthetics) Flashcards
1st Local Anesthetic
1st Synthetic Local (Ester)
1st Amide Local
1st Local Anesthetic Cocaine 1884
1st Synthetic Local (Ester) Procaine 1905
1st Amide Local Lidocaine 1943
Chemical Structure of both amide and Ester
-Lipophilic and hydrophilic portion separated by hydrocarbon
-Lipophilic portion is the Benzene ring
Necessary for activity
Ester
-CO-
Amide
-NHC-
extracellular vs intracellular pH
Extra - 7.4
Intra - 7.0
Enantiomers
s
r
Left = sinister
Right = rectus
S enantiomers - What’s the benefit? 2 examples?
Found to be less neuro- and cardio-toxic
Ropivacaine and Levobupivacaine
MOA of local anesthetics (main site of action)
Inhibit Na+ ions passage through ion-selective Na+ channels:
- Slows rate of depolarization
- Threshold potential not reached
- No action potential propagated
L.A.’s Binds to receptors in ____________________ states
inactivated/activated
Nerves with more activity = ______ blockade
faster
look at slide 12
.
other sites of action for L.A.’s
-Voltage-dependent potassium ion channels
(Much lower affinity)
- Calcium ion currents (L-type)
- G protein-coupled receptors
Cm for motor about _____ sensory
twice
factors that increase and decrease Cm
Increases:
-Larger diameter
Decreases:
- Higher frequency
- Higher pH
Epidural vs Spinal Cm and dose
- Unchanged Cm
- Direct access to nerves = less amount
Nodes of Ranvier, Must block?
at least 2, preferably 3
order of blockade of fibers
B fibers C and A-delta fibers A-Gamma fibers A-Beta fibers A-Alpha fibers
which fibers travel faster?
Myelenated
ATP-TP-MVP acronym
- Autonomic
- Temperature
- Pain
- Touch
- Pressure
- Motor
- Vibration
- Proprioception
What form to cross lipid bylayer?
Un-ionized
Locals with pks nearest physiologic pH?
Faster onset
all are typically weak bases, which on is a weak acid and what pH?
Benzocaine
- pKa – 3.5
- Does not ionize based on pH
- Also does not block by same mechanism
- Mechanism is unknown