Week 6 Review of Local Anesthetics Flashcards
T/F: Local anesthetics can produce a reversible conduction blockade of impulses along the central and peripheral nerve pathways.
True
When and what was the 1st local anesthetic?
- Cocaine
- 1884
When and what was the 1st synthetic local ester?
- Procaine
- 1905
When and what was the 1st local amide?
-lidocaince
1943
What separates the lipophilic and hydrophilic portion of the chemical structure?
-hydrocarbon
which makes it a amide or ester
What part of the chemical structure makes the drug lipophilic active?
-Benzene Ring
What is the chemical chain for a ester?
-CO
What is the chemical chain for a amide?
-NHC
T/F: The quaternary amine is hydrophilic.
TRUE
What is the pH extracellular (usually)?
7.4
What is the pH intracellular (usually)?
7.0
What type of enantiomers does racemic use?
-s enantiomers and r enantiomers
T/F: A pure isomers uses both enantiomers s and r.
FALSE
What two drugs are pure isomers and what enantiomer do they use?
- Ropivacaine
- Levobupivacaine
- Enantiomers s
What is the benefit of a S enantiomer?
- Less nuero toxic
- Less cardio toxic
What is the mechanism of action for a local anesthetic?
-INHIBITS Na IONS PASSAGE THROUGH ION-SELECTIVE Na CHANNELS
- Slows rate of depolarization
- Threshold potential not reached
- No action potential propogated
What does a local anesthetic NOT alter?
- Resting membrane potential
- Threshold potential
What does the alpha Na+ channel subunit do?
Allows ion conduction and binds local
T/F: Local anesthetic bind to receptors in inactivated or open states.
True
What occurs if local is not permeable to the Na+?
The threshold and action potential cannot be obtained.
Is local anesthetic a strong or weak bond?
Weak
The local anesthetic binds both to the internal and external Na+ channel: which is the to be more important?
Internal channel
How does frequency dependent blockade work for local anesthetics?
- Access only obtained when receptor is in activated open state
- Nerves with more activity means faster blockade
- More frequent firing means more opportunity for access
What is minimum concentration?
minimum concentration to produce conduction blockade
What factors influence minimum concentration?
INCREASES
-Nerve diameter
DECREASES
- Higher frequency
- Higher pH
About how much more blockade is required for a motor blockade then a sensory blockade?
2 times as much
How many nodes of Ranvier must a local anesthetic block to obtain local anesthetic?
2 to 3