Local + Nitrous SG Flashcards
three parts of local anesthesia
- aromatic group
- intermediate linkage
- amine group
aromatic group
confers lipophilic properties
intermediate linkage
supplies spacial separation between lipophilic and hydrophilic ends and connects them with either an ester or amide linkage
amide group
secondary or tertiary
affects pka, lipid vs water solubility, and influences speed of onset
ester
union of a carboxylic acid and alcohol
amide
union of a carboxylic acid and an amine (peptide bone is an amide)
except for ______, the injectable dental locals are ______
procaine
amides
the topicals are mostly _______ (esters or amides)
esters
list the amides
lidocaine (xylocaine)
mepivicaine (carbocaine)
articaine (septocaine)
buprivacaine (marcaine)
etidocaine (duranest)
prilocaine (citanest)
list the esters of benzoic acid
butacaine
cocaine
benzocaine
hexlycaine
piperocaine
tetracaine (pontocaine)
list the esters of para aminobenzoic acid
chloroprocaine
procaine (novocaine)
proxycaine
what is the only injectable ester?
procaine (novocaine)
another name for lidocaine
xylocaine
another name for mepivicaine
carbocaine
another name for articaine
septocaine
another name for buprivacaine
marcaine
another name for etidocaine
duranest
another name for prilocaine
citanest
another name for tetracaine
pontocaine
another name for procaine
novocaine
the amine portion is a _____ (acid / base)
base
only _____ can cross cell membranes, so onset of action is faster for ____ (low / high) pKa because they give up their protons more easily and become uncharged “free bases”
free bases
low
pKa
how strongly the organic portion of the local anesthetic molecule holds onto its proton
drugs with a high pKa are _____(weak / strong) acids.
weaker acids (stronger. bases)
Do weak acids hold on to their protons tightly? what does this mean for onset?
weak acids / strong bases hold their proton more tightly, remaining positively charged, and cross cell membranes poorly
thus they have a slower onset
drugs with low pKa are _______ (weak / strong) acids
strong acids (weak bases)
do strong acids hold on to their protons tightly? what does this mean for onset?
strong acids / weak bases shed their proton more easily, become non-ionized free bases and cross membranes more easily
acidic environments like inflamed tissue have ____ (slow / fast) onset
slow onset
since the base remains protonated in the low pH environment
locals ______ membranes and prevent ________
stabilize
rapid sodium influx
why are the pharmacokinetics of locals unique?
they become ineffective when absorbed by the system
what happens when locals are redistributed?
effects wear off
metabolic half life is not related to ______ but is related to _____
duration of anesthesia
toxicity
half life
the rate at which a local anesthetic drug is removed from the blood
does half life impact toxicity?
yes
can local anesthetic agents cross the BBB?
yes
can local anesthetics cross the placenta?
yes (and get into breast milk)
why does metabolism affect overall toxicity?
because it is the balance between rates of absorption at the injection site and the removal from the blood that determines the levels in the tissues
duration of action is related to ______ of the local
protein bonding
is duration of action related to metabolic transformation?
no
all locals are (vasodilators / vasoconstrictors)
vasodilators
which local is a vasoconstrictor?
cocaine
Why are vasoconstrictors added to most LAs?
because LAs are vasodilators, blood washes them away. need something to balance this so they stay in desired area longer
with vasodilation, there is (2 things)
- an increased rate of absorption
- decreased duration and level of pain control
an increase in the anesthetic in the blood will lead to _______
overdose
vasoconstrictors are needed for _________
slow redistribution
why use vasoconstrictors?
because local anesthetics possess vasodilation properties
what are vasoconstrictors?
drugs that constrict blood vessels and there by control tissue perfusion
which vasoconstrictor is used most often?
epinephrine
epinephrine effects
alpha
beta 1
beta 2
small amounts of urine are excreted in ______
urine unchanged
soft tissue anesthesia
always develops before pulpal
5 hours
pulpal anesthesia
relatively short window
60 minutes
does nerve block or infiltraiton last longer?
nerve block
primary metbaolism of esters
plasma hydrolysis by the enzyme pseudocholinesterase
cocaine is metabolized primarily in
liver
amides are metabolized in
liver
the status of liver function is a factor in
toxiity
relative contraindications in terms of metabolism of amides
- liver failure
- heart failure resulting in lower liver perfusion
articaine (septocaine) is metbaolized primarily by
plasma carboxyesterase
accumulation of biotransformation product _______ in the blood can produce _____
orthotoluidine
methemoglobin
what two LAs produce methemoglobin?
prilocaine
articaine
methemoglobin is produce in hemoglobin in which the iron ion has been oxidized to the _____ instead of ____ state
ferric (fe+3)
ferrous (fe+2)
if a significant percent of the total hemoglobin is affected, it can result in _____
poor oxygen delivery to tissues
methemoglobin can be reversed rapidly with ____-
IV methylene blue
why is pulse oximetry unreliable with methemoglobin?
methemoglobin has absorption frequency that draws the pulse oximeter to 85%
excretion of local anesthetics
kidney for local anesthetic agents and metabolites
when do local anesthetics lose their effect?
when absorbed into the blood stream
the rate at which a local is removed from the plasma is expressed as its…
metbaolic half life
duration of local anesthetics from shortest to longest
carboxaine
xylocaine
septocaine
marcaine
which anesthetic is not recommended in pedo or in cognitively impaired adults?
marcaine
max dose for lidocaine with epinephrine
4.4
max dose for mepivicaine
4.4
max dose for bupivicaine
1.3
max dose for septocaine
7
epinephrine’s effects on the myocardium
- increased cardiac output
- increased stroke volume
- increased oxygen consumption
- decrease overally efficiency of the myocardium
when does LA become toxic?
when the tissue levels int he CNS or heart become too high
maximum recommended doses of drugs should be calculated by…
body weight (and not exceded)