local anaesthetics Flashcards

1
Q

how did they discover the first local anasthetic?

A

chewed cocaine and found it to have numbing sensation- applied it topically and had the same effect

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2
Q

what is the addictive functional groups in cocaine?

A

methyl ester

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3
Q

why does procaine have a short duration of action?

A

due to its ester group which is abled to be broken down into an alcohol and a carboxylic acid by esterase’s- less potent

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4
Q

how do local anasthetics work?

A

they work against sodium channels. they diffuse passively through a lipophilic membrane and find their target once through- has to be done this way as they are to big otherwise

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5
Q

do we really need the amine in local anasthetics?

A

yes- if IV- need to be able to be polar

no- if topical- but will not be as potent

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6
Q

what is the buchi model of anastetic binding

A

can only bind ortha or para NOT meta
- by doing this the substituent is able to donate el density through resonance- and making the bonding of the oxygen on the carbonyl more delta positive for stroonger binding.

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7
Q

what compound displays a 50 fold increase in binding over procaine?

A

Tetracaine

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8
Q

why does switching ester to amide increases stability?

A

as it is not efterified into an alcohol and carboxylic acid.- longer duration of action

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9
Q

what are the toxic s/e of lidocaine?

A

some CNS s/e

N-dealkylation after passing BBB

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