Local anaesthesia Flashcards
What sensation are nociceptors involved in?
Pain
What does general anaesthesia cause?
Loss of conciousness
Whats does local anaesthesia cause?
Local reversible pain relief without loss of conciousness
How is an action potential produced?
- Neuronal resting membrane potential = negative
- Depolarisation = opening of voltage gated Na channels = positive membrane potential = action potential at threshold
- Na channels inactivate within a few ms = repolarisation
What is the cycle voltage gated Na channels go through?
Open
Closed
Inactive
What are the two anaesthetic pathways?
- Hydrophillic (use dependent = clinically most relevant)
- Hydrophobic (non use dependent)
In which form can molecules cross the phospholipid bilayer?
Uncharged
What % of the LA is found in the charged form in the body?
70-90%
Which % of the LA is found in the uncharged form in the body?
10-30%
Explain the hydrophilic pathway:
INSERT PIC
N.B. this pathway can only work when sodium channels are being used (increased pain = more Na channels = more LA can access and bind the LA binding site)Equilibrium between charged and uncharged form
Explain the hydrophobic pathway:
Insert pic
N.B. the LA stays in the uncharged form and moves through the membrane to the LA binding side and inhibits Na channel from inside membrane
What type of chemical are Local anaesthetics?
Weak bases
Which group in the local anaesthetic structure is lipophilic?
The aromatic group with various residues depending on anaesthetic
Which group in the local anaesthetic structure is hydrophilic when it accepts protons?
The amine group
Which group in the local anaesthetic structure is the intermediate chain?
Ester or amide
What breaks down the ester chains?
Broken down quickly by esterase’s in blood plasma