PHAR232 - Local anaesthetics Flashcards
What is the goal of local anaesthetics ?
Prevent nociceptive signals
Completely relax the muscle
What are nomenclature structures derived from?
Cocaine
Mechanism of action of local anaesthetics
KNOW THIS PATHWAY AND YOUTUBE
Hydrophilic pathway - binding pocket most easily accessable when the channel is in use
Cannot go to inactive state until goes through active state
For the hydrophilic pathway, binding site is best accessed when the channel is _________. Therefore hydrophilic local anaesthetic drugs referred to as __________________.
In use
Use-dependent
If a drug binding via hydrophobic pathway use-dependent?
No
What is anaesthetic action dependent on?
Normal actiity of nerve
- Lipid solubility of drug
- pH of tissue
Mechanism of action
Are local anaesthetics weak or strong pKa bases?
weak
What is pKa?
50% molecule is ionised and 50% unionised
on a pH scale
If you have a pKa of 8 - 14, are you ionised or unionised?
un-ionised
If you have a pKa of 1 - 8, are you ionised or unionised?
ionised
Do ionised drugs cross a membrane?
No - they are repelled
Why are un-ionised drugs with a weaker pH base selected for anaesthetics and medications?
Un-ionised = weaker pH base
= easier to cross cell membrane
systemic considerations of action
Drug needs to be confined - common to add a vasoconstrictor e.g. adrenaline