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local anesthesia chapter 3
pharm...
42
Dentistry
Undergraduate 3
08/27/2014

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Term
what does local anesthesia do>
Definition
blocks pain by blocking sodium channels
Term
what are the factors that can affect Local anesthesia?
Definition

potency

 

time of onset

 

duration of LA  agent

Term
what are ideal properties of L.A.
Definition

potent

reversible

abscence  of local reactions

abscence of systemic reactions

rapid onset

satisfactory duration

adequate tissue penetration

low cost

stability in solution (long shelf life)

ease of metabolism and excretion

Term
this form of anesthetic is known for high chance for allergic reactions.  they are non injectible but they are topical.
Definition
esters
Term
where are esters metabolized?
Definition

 in blood plasma 

 

(remember bloody ester lol)

Term
where are amides metabolized
Definition
amides metabolized in liver
Term
amides may be contraindicated in what cases
Definition

alcohol abuse

 

liver issues (hep C)

 

the reason is that the liver may be compromised and may not be able to metabolize

Term
what are the components of molecular structure.
Definition

lipophilic aromatic ring(improves lipid solubility and penetration of L.A.

 

intermediate hydrocarbon (may be ester or amide)

 

hydrophilic terminal amine (on / off switch allowing L.A. to exist as lipid soluble or water soluble assisting with blocking conduction.

Term
what are the routes of delivery for L.A.
Definition

topical (high risk of toxicity)

 

injectible (less toxic)

Term
why are topicals a higher concentration that injectible
Definition

they help diffuse across membranes

 

but they have high risk for toxicity

Term
what does the intermediate hydrocarbon do?
Definition

determines course of biotransformation

plasma or liver enzymes.

 

for ester or amide

Term
what bonds are involved in hydrophilic terminal amine
Definition

tertiary-3 bonds lipid soluble

 

quarternary-4 bonds positively charged water soluble

Term
pro of injectible
Definition
works well because placement is near nerve
Term
ph of local always starts out more )acidic or basic)before injection.
Definition
ph of local always starts out more acidic
Term
adding vasoconstrictors is good because?
Definition
limits toxicity and lowers ph (makes it more acidic) and acts as a preservative.
Term
what must solution do to become more basic? why do this?
Definition

solution must conver to tertiary lipid soluble base structure.

 

it needs to be more basic to penetrate the nerve.

 

some attach to recepters and some end up free bases.

Term
what is pka
Definition
free base or dissociated ions
Term
the higher the pka the (slower or faster?) it is to work.
Definition
high pka indicates long uptake and longer time to work.
Term
lidocaine has a pka of 7.7 and it is 29 % base will this have a slow or fast onset?
Definition
onset will be faster for lidocaine.
Term
does marcaine have slow or fast onset>?
Definition
marcaine has the slowest onset and lasts the longest.
Term
what can happen in area of infection and injection site?
Definition

-tissue is more acidic

-slows release of free base

-stays quarternary (water soluble)

-difficult site for LA

-edema

Term
what determines the onset of action?
Definition

PKA determines the onset of action.

 

low pka is short onset

high pka is longer drawn out onset

Term
what bundles receive la last?
Definition
core bundles (center of nerve)
Term
what bundles receice LA first?
Definition
mantle bundles
Term
induction time
Definition
time interval between initial deposition of anesthetic solution and complete conduction blockade.
Term
what is important to do when re-injecting?
Definition
re-inject before mantle fibers recover.
Term
tachyphylaxis
Definition
increased tolerance to drug administration repeatedly
Term
absorption of LA depends on
Definition

dose

 

route

 

vascularity

 

presence or abscence of vasoconstrictors

Term
explain distribution of LA in body
Definition

-in blood supply to systemic

 

-goes to vital organs

 

-crosses blood-brain barrier

 

-if alot ends up in tissues, toxicity can occur

Term
half life for drugs
Definition
time it takes to eliminate half of the drug
Term
half life for lidocaine is?
Definition
90 min half life for lidocaine
Term
bupivicaine/marcaine has half life of??
Definition
3.5 hours LASTS long!!!!!!
Term
in esters what is the major cause of allergic reactions?
Definition
PABA (paraaminobenzoic acid)
Term
dental topicals commonly used?
Definition

benzocaine

 

tetracaine

 

procaine (used by medical professionals also known as novacaine which is no longer used due to high chance for allergy)

Term
examples of amides
Definition

lidocaine/xylocaine

 

mepivicaine/carbocaine

 

bupivicaine/marcaine

Term
what LA is partially biotransformed in liver and partially metabolized in lungs?
Definition
Prilocaine is biotransformed in liver and lungs
Term
what % of septicaine/articaine is biotransformed in liver.
Definition
5-10% of articaine is biotransformed in liver
Term
what is the major organ that excretes LA
Definition
kidneys excrete LA
Term
what are some effects of CNS from local anesthesia?
Definition

crosses blood brain barrier

 

muscle twitching, tremors

 

high blood levels, depressed, unconscious, convulsions, hypotension.

 

respiratory arrest

Term
the affects local has on CVS and CNS depend apon?
Definition

 amount of vasodilation

 

concentration of drug

 

route

 

rate of injection

 

vascularity of area of injection

Term
CVS problems with Local
Definition

increase in bp and respiration

 

moderate overdose can cause depression, mi, circulatory distress.

Term
if symptoms arise within 5 minutes of injection is it more or less severe?
Definition
more severe the faster the symptoms appear for CVS
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