Lecture 5.5 - LA Drugs Flashcards
all Local anesthetics (LA) end in _____;
amides have ___ i(s) in their name. esters have ___ i(s)
-“Caine”;
2 ie (lidocaine, mepivacaine, bupivacaine);
1 (ie benzocaine, cocaine, procaine, tetracaine)
amides vs ester LA: lower PKA? faster onset? fast hydrolysis by esterases? long half life due to CYP hydrolysis?
amide;
amide;
esters;
amide
esters are metabolized into ____ which has a risk of what?
para-aminobenzoic acid (PABA), allergy risk
articaine is a _____. it has a thiophene ring that _____ lipophilicity; it also has a ester so it is hydrolyzed ____ = ____ toxicity problems
amide;
increases;
v quickly, lower
LA effects:
____ is associated with painful transient neurologic symptoms;
bupivacaine (long half life) is especially associated with ____ toxicity
chloroprocaine is used via ____ for cesarean section
lidocaine (short duration);
cardio;
epidural
LA effects:
____ has very high lipophilicity and is only used topically, although rarely.
cocaine is used when ____ is needed
benzocaine;
vasoconstriction (also if u tryna get high)
LA CNS effect:
initially, NaV channels on ____ neurons are inhibited, inducing ____. ____ Can be used to treat this. LAs also cause reversible local ____ Damage
GABAergic;
seizures/CNS excitation;
benzos;
nerve
LA effects:
which occur first, CNS probs or Cardiac probs?
whats the exception to this
CNS;
bupivicaine
Cardiac effects:
can occur with accidental ____ injection. is there an excitatory or inhibitory effect on the heart?
what channel is bound?
veinous;
inhibitory (ie depressed rate/force of contraction);
NaV5
if cardiac arrest occurs, _____ resuscitation can be attempted. the goal of this is to….
lipid;
remove lipophillic drug from inside the cell
slower rate of injection ____ the risk of toxicity
reduces
lidocaine and mepivacaine are typically used for _____;
_____ is used for epidurals
nerve block;
bupivicaine
