Local Anesthetics Flashcards
How does LA function?
Inhibits neural conduction by inhibiting Na ion influx
How does LA prevent Na ion influx?
LA diffuses across neural membrane into axoplasm
They enter the Na channels preventing them from assuming an active position
What are the three components of LA molecules ?
Lipophilic aromatic ring
Intermediate ester or amide chain
Terminal amine
What is the function of aromatic ring?
Improves lipid solubility
For local anaesthetics what is the benefit of greater lipid solubility ?
Enhances the potency of the LA since more can diffuse across the membrane
Why are inflamed tissues more difficult to anaesthetise ?
Inflamed tissues have an acidic environment favouring the water soluble configuration of LA over the lipid soluble
LA needs to be lipid soluble form to be able to cross nerve membrane
Which LA would be more effective in inflamed tissues?
Mepivicane since it has a pKa of 7.6
What is the pKa ?
pH at which 50% of molecule exists in water soluble state and 50% in lipid soluble state
The intermediate section of LA determines what?
Either amide or ester
Where the LA is metabolised
Where are esters metabolised?
Blood plasma esterases
Where are amides metabolised?
Liver
LA most commonly used are what group?
Amides
Esters only really in topicals
Why is bupivicaine so long acting ?
Greatest affinity of all LA to bind to alpha-1-acid glycoprotein making it more bioavailable
What is the risk of using bupivicaine?
Painful upon injection
Why is articaine more effective than lidocaine ?
- Produced at higher concentration
- Has thiopene ring making it greater lipid soluble