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local analgescs, refer to the image in the docs to
see what the different…
local analgescs
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electrical excitability
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inactivated
inactivated vs deactivated
- Inactivation: ion flow blocked by gating mechanism (not the closing of the channel but the closing of the BOTTOM part of the channel)
- Deactivation: ion flow blocked by the CLOSING IN THE CENTRE of the channel
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classification of LA
ester type
(3 or fewer SYLLABUS)
Ester LAs are hydrolysed to
p-aminobenzoic acid (PABA) derivatives,
which cause allergic reactions in a small
percentage of the population
cocaine
Cocaine blocks NA reuptake, increased NA causes vasoconstriction and hypertension
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amide type
(>3 SYLLABUS)
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prilocaine (EXCEPTION)
O-toluidine (metabolite of prilocaine) causes methaemoglobin → a dysfunctional haemoglobin that cannot carry oxygen
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toxicity
large doses
method to mitigate: combine LA with epinephrine → cause vasodilation → LA takes longer to be distributed from the site of action
specific drugs
- Bupivacaine is more cardiotoxic than most other LAs
- Cocaine blocks NA reuptake, increased NA causes vasoconstriction and hypertension
- O-toluidine (metabolite of prilocaine) causes methaemoglobin → a dysfunctional haemoglobin that cannot carry oxygen
- Ester LAs are hydrolysed to p-aminobenzoic acid (PABA) derivatives, which cause allergic reactions in a small percentage of the population
ways to mitigate
- Ester LAs: good for people with liver disease since its metabolised by blood esterases
- Amides: good for people with PABA allergies since they will not be converted into PABA
Mechanism of action
refer to the explanation blanks part --> remember that LAs exist as bases before they are able to protonate
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