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
Role of pH in relation to local anaesthetics
Key side effects for consideration
KEY TOXICITY ISSUES - KNOW
Modes of delivery -
never inject into the nerve - will kill the nerve and leave them paralysed
Infiltration anaesthesia
Field block anaesthesia
Nerve block anaesthesia
Nerve plexus - sacral plexus
- DOnt nee to worry about pH or cellular membrane
What is another term for intravenous regional anaesthesia?
Bier’s block
IV regional anaesthesia
Traps blood at blessure, then releases the diaphram to enhance the area under anaesthia
What is the goal of IV regional anaesthesia?
Use vasculature to transport drug
youtube to reconsolidate
Window for use - generally 45 mins
SPINAL ANAESTHESIA
Lumbar puncture
KNOW WHY - STUDY THIS
Epidural anaesthesia
Epidural space injections