PAIN OSCE Flashcards
MOA of local anesthetics
Blocks Na+ channels
* bind receptors in phospholipid membrane
* Stops transmission of action potential
There are at least 9 Na+ channel binding sites
* heterogeneous structure
How are LA classified
Classified by their ability to react w/specific receptor sites in Na+ channel
* 4 sites w/in sodium channel
- w/in Na+ channel (tertiary amine local anesthetics)
- outer surface of Na+ channel (tetrodotoxin, saxitoxin)
3-4. Activation or inactivation gates (Scorpion venom)
Characterize Sodium Channels in Neurons
Na+ migrates inward bc:
1. concentration (Greater outside)
2. electrostatic gradient positive ion attracted by neg. intracellular potential)
Resting nerve membrane=impermeable to Na+
* prevents massive influx
Na+ travels external to internal=Depolarizing event
What is highly conc around nodes of ranvier?
Na+ Channels
Where does LA act?
Nodal areas (Nodes of Ranvier)
* blocks depolarization
Can you block one node of ranvier w/local anesthetic to implement action
No, must block multiple nodes of ranvier
LA must bathe 8-10 mm of neuron to block
Characterize the resting state of neurons
Slightly permeable to Na+
Freely Permeable to K+ & Cl-
What stimuli excite pain receptors? How sensitive are receptors to these stimuli?
Mechanical, Thermal, Chemical
Does local anesthetic block more than pain
Does not block proprioception
* Pressure, vibration, temperature
What is important regarding local anesthetic application
volume
concentration
pH
what can remove LA at the site of LA administration
Most is lost at the perineurium
* absorbed by Nutrient blood vessels & lymphatics
* greatest barrier to diffusion
What form of LA penetrates the lipid bilayer of the nerve axon membrane?
Base form
Drugs w/what pka have a slower onset
High pka=slower onset
pka 7.5-9.0
What is the pH of LA w/o vasoconstrictors
pH 5.5-7
Characterize LA pH w/vasoconstrictors
LA w/vasoconstrictor are acidified to retard oxidation & prolong shelf life
Sodium Bisulfite
* antioxidant
* increase shelf lie
2% Lidocaine HCL
* pH: 6.8
* acidified to pH 4.2 w/sodium bisulfite
* at pH 4.2 it will take longer for anesthetic to function at full effect
What are the properties of LA
Reversibly block nerve conduction
* Must be lipophilic & hydrophilic for effective parenteral injection
Drugs that are not hydrophilic=Topical Drugs
LA w/o hydrophilic component is used for what?
Topical
Benzocaine gel
What influences drug removal & how do we modulate it?
Factors that remove:
* Increased protein binding
* Vascularity of injection site
* presence or absence of vasoactive substance
What is the max dose of each type of LA
What is the typical amount of episodes in a cartridge of LA
18 micrograms=.018 mg
What is the typical amount of LA in a cartridge (1%)
18 mg
What is the significance of epi in LA
20 ug of epi: Doubles pre-op plasma conc.
200 ug of epi surpases
* heavy exercise
* surgery
* pheochromocytoma
Increases cardiac work
* MI & arrhythmias are more likely to occur
do LA have significant systemic effects?
Aside from their influence on cardiovascular & CNS fxn
* LA exert few systemic effects
What determines LA toxic Potential
The uptake of LA into systemic circulation & removal by redistribution, metabolism & excretion
Drug w/potent vasodilating properties may enhance their own uptake=esters
What occurs to LA when entering the circulation
Proteins made in liver (Albumin)
* if liver is not working properly, less will be bound to plasma proteins
entering circulation, LA is partially (5-95%) bound to plasma proteins
* a1-acidglycoprotein
* albumin
* RBCs
how does pregnancy impact LA
–
Lidocaine across the BBB contributes to what?
CNS Depression
Tonic-Clonic convulsions
Septocaine
4 %
* aka articaine
* shortest duration
lidocaine
2%
* aka xylocaine
* safest in children