Lecture 27: Local Anesthetics and Euthanasia Flashcards
Local anesthetics are either __ or __
Esters or amides
Which have shorter duration of action: esters or amides
Esters
Which have increased systemic toxicity: esters or amides
Esters
Esters and amides are typically administered as ___to increase stability and solubility
Salts
Local anesthetics are weak ___with pKa’s ___
Bases, 7.5-9
At physiological pH local anesthetics are predominately ionized or non-ionized?
Ionized
Where is the binding site for local anesthetics
Inner membrane
Local anesthetics need to be ___to cross the cell membrane
Non-ionized
Once inside the cell, local anesthetics become ___
Ionized
The ionized form of local anesthetics binds to ___channels
Na+
What is the hydrophobic pathway
Neutral local anesthetics through the membrane
If you have an abscess where do you want to apply local anesthetic and why
0.5-1 inches away from abscess because abscesses are acidic so it will become ionized and not penetrate abscesses and therefore animal will feel everything
What is the mechanism of action for local anesthetics
Blocks Na+ channels and inhibits neuronal firing
Local anesthetic have high affinity for what Na+ channels and low affinity for what Na+ channels
High affinity: activated/ open and inactivated channels
Low affinity: resting/ closed channels
Local anesthetic blocks are ore effective in ___firing axons than ___axons
Rapidly firing, resting axons
Extent of a local anesthetic block is ___ and ___ dependent
Voltage (potential) and time (firing)
Local anesthetics increase the threshold for excitation due to ___
Decreasing Na+ influx
Local anesthetic slows impulse conduction as more ___are blocked
Channels
Complete block from local anesthetic results from progressive ___
Decrease in the rate of action potential firing
Duration of action for local anesthetics is dependent on ___
Time at site of action
T or F: local anesthetics rapidly diffuse away from site of application
True
What affects systemic absoprtion
- Dosage
- Site of injection (vascular vs fat)
- Drug tissue binding
- Chemical properties of drugs
- Local blood flow
- Vasoconstricting agents- epinephrine
How does epinephrine affect systemic absoprtion
- Decreases diffusion of drug
- Prolongs duration of action
- Decreases systemic absoprtion
- Decreases systemic toxicity
Vasoconstricts
Why would you need to space out blebs of local anesthetic when performing a line block with epinephrine in a cow
Because epinephrine will vasoconstrict and you can get tissue necrosis
How are amides metabolized
Liver by CYP450s
Toxicity from amides is more likely in what patients
Patients with hepatic disease of reduced hepatic blood flow
How are esters metabolized
Butyrylcholinesterases in the plasma
How are esters and amides eliminated
Renal