Flashcards in Local Anesthetics Worksheet Deck (129)
LA consists of a ____ and a _____ portion.
the lipophilic and hydrophilic portions of a LA are separated by a connecting:
LA's are poorly soluble in
Because of the poor solubility in water, LA's are marketed as water soluble:
hydrochloride salt solutions are acidic or alkalodic? pH?
hydrochloride salt solutions contribute to the LA's what?
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 is water or lipid soluble?
Compared to procaine, tetracaine is more
How many times more potent is tetracaine than procaine?
10 times more potent
Which LA has a longer duration; procaine or tetracaine?
the longer duration of tetracaine corresponds to a ___ fold decrease rate of _______.
fold decreased rate of
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?
the S enantiomers of Bupivacaine and mepivacaine produce less of this _____ _____ (two things) than the racemic mixtures or the R enantiomers of LA.
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:
Halogenation of procaine to _______
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:
Etidocaine resembles lidocaine but has a 50 fold increase in:
Etidocaine resembles lidocaine but has a 2-3 fold
increase in the duration of action
What LA is 35 times more lipid soluble than mepivacaine?
Bupivacaine has a potency and DOA _____ times that of mepivacaine.
These drugs have been incorporated into liposomes to prolong the DOA and decrease toxicity:
Lidocaine, tetracaine, and bupivacaine
Lidocaine, tetracaine, and bupivacaine have been incorporated into liposomes to do what two things?