Local Anesthetics Worksheet Flashcards Preview

Fall'20 Pharmacology III > Local Anesthetics Worksheet > Flashcards

Flashcards in Local Anesthetics Worksheet Deck (129)
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1

LA consists of a ____ and a _____ portion.

Lipophillic
hydrophilic

2

the lipophilic and hydrophilic portions of a LA are separated by a connecting:

hydrocarbon chain

3

LA's are poorly soluble in

water

4

Because of the poor solubility in water, LA's are marketed as water soluble:

Hydrochloride salts

5

hydrochloride salt solutions are acidic or alkalodic? pH?

Acidic
pH 6

6

hydrochloride salt solutions contribute to the LA's what?

stability

7

what is it that contributes to the stability of LA's?

the hydrochloride salt solutions

8

substituting a butyl group for the amine group on the benzene ring of procaine results in:

tetracaine

9

Tetracaine is water or lipid soluble?

Lipid soluble

10

Compared to procaine, tetracaine is more

lipid soluble

11

How many times more potent is tetracaine than procaine?

10 times more potent

12

Which LA has a longer duration; procaine or tetracaine?

tetracaine

13

the longer duration of tetracaine corresponds to a ___ fold decrease rate of _______.

4-5
fold decreased rate of
metabolism

14

compared to the commercially available racemic mixtures of bupivacaine and mepivacaine, what appears to be less toxic?

the S Enantiomers of bupivacaine and mepivacaine

15

what LA is known for cardio toxicity?

bupivacaine

16

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

17

What 2 LAs are available for clinical use as racemic mixtures (50:50) of the enantiomers:

Mepivacaine and bupivacaine

18

Mepivacaine, bupivacaine, ropivacaine, and levobupivacaine are all:

chiral drugs that may have S or R configurations

19

Name 4 LA that are chiral drugs that may have S or R configurations:

Mepivacaine,
bupivacaine,
ropivacaine,
levobupivacaine

20

Halogenation of procaine to _______

Chloroprocaine

21

Halogentation of procaine to chloroprocaine results in a ____ fold increase of what?

3-4 fold incease
in hyrolysis rate of chloroprocaine

22

hydrolysis of chloroprocaine is done by:

plasma cholinesterase

23

Etidocaine resembles:

Lidocaine

24

Etidocaine resembles lidocaine but has a 50 fold increase in:

lipid solubility

25

Etidocaine resembles lidocaine but has a 2-3 fold

increase in the duration of action

26

What LA is 35 times more lipid soluble than mepivacaine?

bupivacaine

27

Bupivacaine has a potency and DOA _____ times that of mepivacaine.

3-4 times

28

These drugs have been incorporated into liposomes to prolong the DOA and decrease toxicity:

Lidocaine, tetracaine, and bupivacaine

29

Lidocaine, tetracaine, and bupivacaine have been incorporated into liposomes to do what two things?

Prolong DOA
Decrease toxicity

30

The FDA has approved this for local infiltration of anesthesia for hemorrhoidectomy and bunionectomy:

bupivacaine extended release liposome injection