Intro to Regional Anesthesia - PM Flashcards
Local Anesthetics are?
Drugs that reversibly bind to voltage-gated sodium channels (NAv)
NAv channels have what three functional states?
resting (closed), open, inactive
Symptoms of toxicity can occur from any route of administration, but what is the most prominent method?
Inadvertent intravascular injection
What is the antidote for local anesthetics?
Time, there is no reversal agent
What are the two intermediate carbon groups?
Esters and amides
What is responsible for the classification of Local Anesthetic?
the intermediate linkage
What are the 5 Esters?
Procaine, Chloroprocain, Tetracaine, Cocaine, Benzocaine
What are the Amides?
Lidocaine, Mepivacaine, Prilocaine, Bupivacaine, Ropivacaine, Articaine. (They all have two i’s)
Lipophilic
means fat loving. Wants to bind to lipids.
Hydrophobic
means fear of water.
In general, duration of action is mostly correlated with?
Protein binding, so the more protein bound a LA is, the longer the duration of action.
In general, what correlates most with potency?
Lipid solubility. A LA’s high lipid solubility equals a high level of potency.
pKa
expresses relationship between uncharged (non-ionized & lipid soluble) and charged (ionized & water soluble) drug concentrations. The drug specific pKa is the pH at which the concentrations are 50/50.
LA’s typically have what kind of base?
Weak (pka’s higher than 7.45) (Lower than 7.35 would be a strong base)
What does adding a vasoconstrictor do to a LA?
hint - 5 things
- Limits spread of agent
- longer duration of effect
- Reduces systemic absorption
- Hemostasis for improved visulization
- Possibility of using a smaller dose of LA overall
What are potential negative effects of using a vasoconstrictor and a LA together?
Tissue ischemia leading to necrosis in end organ
Use of Epi with an LA is contraindicated in/on?
nose, fingers, toes, or penis, and should be avoided in avulsed flaps and areas with tenuous blood supply.
What is the reversal of epi if injected into contraindicated tissue?
phentolamine (1.5-5mg)
LA prepackaged with epi are usually indicated with what?
Red top and red lettering on label
What does buffering an unionized drug with Sodium Bicarb do?
Speeds its penetration to the nerve tissue
What are the LA’s that possess mild vasoconstrictive properties?
Ropivacaine and Lidocaine
Most LA’s produce 1._____ that results in increased 2. _____ which can lead to an increase in LA 3.______ . This in turn shortens the duration of 4._____ and increased the probability of 5. ____ effects.
- relaxation of vascular smooth muscles
- vasodilation and increased blood flow
- absorption
- action
- toxic
Cocaine (in a clinical setting) is only administered in what way?
topically
What tissue receives the greatest amount of LA from distribution?
muscle tissue (acts as a depot due to greater tissue mass)