Local Anesthetics Worksheet Flashcards
LA consists of a ____ and a _____ portion.
Lipophillic
hydrophilic
the lipophilic and hydrophilic portions of a LA are separated by a connecting:
hydrocarbon chain
LA’s are poorly soluble in
water
Because of the poor solubility in water, LA’s are marketed as water soluble:
Hydrochloride salts
hydrochloride salt solutions are acidic or alkalodic? pH?
Acidic
pH 6
hydrochloride salt solutions contribute to the LA’s what?
stability
what is it that contributes to the stability of LA’s?
the hydrochloride salt solutions
substituting a butyl group for the amine group on the benzene ring of procaine results in:
tetracaine
Tetracaine is water or lipid soluble?
Lipid soluble
Compared to procaine, tetracaine is more
lipid soluble
How many times more potent is tetracaine than procaine?
10 times more potent
Which LA has a longer duration; procaine or tetracaine?
tetracaine
the longer duration of tetracaine corresponds to a ___ fold decrease rate of _______.
4-5
fold decreased rate of
metabolism
compared to the commercially available racemic mixtures of bupivacaine and mepivacaine, what appears to be less toxic?
the S Enantiomers of bupivacaine and mepivacaine
what LA is known for cardio toxicity?
bupivacaine
the S enantiomers of Bupivacaine and mepivacaine produce less of this _____ _____ (two things) than the racemic mixtures or the R enantiomers of LA.
Neurotoxicity
Cardiotoxicity
What 2 LAs are available for clinical use as racemic mixtures (50:50) of the enantiomers:
Mepivacaine and bupivacaine
Mepivacaine, bupivacaine, ropivacaine, and levobupivacaine are all:
chiral drugs that may have S or R configurations
Name 4 LA that are chiral drugs that may have S or R configurations:
Mepivacaine,
bupivacaine,
ropivacaine,
levobupivacaine
Halogenation of procaine to _______
Chloroprocaine
Halogentation of procaine to chloroprocaine results in a ____ fold increase of what?
3-4 fold incease
in hyrolysis rate of chloroprocaine
hydrolysis of chloroprocaine is done by:
plasma cholinesterase
Etidocaine resembles:
Lidocaine
Etidocaine resembles lidocaine but has a 50 fold increase in:
lipid solubility