LOCAL ANAESTHETIC AGENT

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COMERCIALLY
PREPARED LOCAL
ANESTHESIA CONSISTS
OF:

Local anesthetic agent

(xylocaine, lignocaine 2%)
Vasoconstrictor (adrenaline
1: 80,000)
Reducing agent (sodium
metabisulphite)
Preservative
(methylparaben,capryl 2
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 REDUCING AGENT

• Vasoconstrictors are unstable in solution and may

oxidize especially on prolong exposure to sunlight
this results in turning of the solution brown and
this discoloration is an indication that such a
solution must be discarded.
• To overcome this problem a small quantity of
sodium metabisulphite is added - competes for the
available oxygen.
• SHELF LIFE INCREASES
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 PRESERVATIVE

• Modern local anesthetic solution are very

stable and often have a shelf of two years or
more. Their sterility is maintained by the
inclusion of small amount of a preservative
such as capryl hydrocuprienotoxin.
• Some preservative such as methylparaben have
been shown to allergic reaction in sensitized
subjects.
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 FUNGICIDE

• In the past some solutions tended to become

cloudy due to the proliferation of minute fungi.

• In several modern solutions a small quantity of

thymol is added to serve as fungicide and
prevent this occurrence.

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 VEHICLE

• The anesthetic agent and the additives referred

to above are dissolved in distilled water &
sodium chloride.
• This isotonic solution minimizes discomfort
during injection.

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. The chemical characteristics are so
balanced that they have both lipophilic
and hydrophilic properties.

If hydrophilic group predominates, the

ability to diffuse into lipid rich nerves is
diminished. If the molecule is too
lipophilic it is of little clinical value as
an injectable anesthetic, since it is
insoluble in water and unable to diffuse
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 LOCAL ANESTHETIC AGENT

The local anesthetics used in dentistry are

divided into two groups:

ESTER GROUP
AMIDE GROUP

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 CLASSIFICATION OF LOCAL
ANESTHETICS
ESTERS
Esters of benzoic acid Esters of Para-
Butacaine amino benzoic acid
Cocaine Chloroprocai
Benzocaine n

Hexylcaine Procaine

Piperocaine Propoxycain
e
Tetracaine
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 AMIDES
Articaine
Bupivacaine
Dibucaine ABCDE LMPR
Etidocaine
Lidocaine
Mepivacaine
Prilocaine
Ropivacaine
QUINOLINE

Centbucridine
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PHARMACOKINETICS OF LOCAL
ANESTHETICS
UPTAKE:
When injected into soft tissue most local
anesthetics produce dilation of vascular bed.
Cocaine is the only local anesthetic that
produces vasoconstriction, initially it
produces vasodilation which is followed by
prolonged vasoconstriction.
Vasodilation is due to increase in the rate of
absorption of the local anesthetic into the
blood, thus decreasing the duration of pain 13
ORAL ROUTE:

Except cocaine, local anesthetics are poorly

absorbed from GIT
Most local anesthetics undergo hepatic first-
pass effect following oral administration.

72% of dose is biotransformed into inactive

metabolites

TOCAINIDE HYDROCHLORIDE an
analogue of lidocaine is effective orally 14
TOPICAL ROUTE:

Local anesthetics are absorbed at different rates

after application to mucous membranes, in the
tracheal mucosa uptake is as rapid as with
intravenous administration.

In pharyngeal mucosa uptake is slow

In bladder mucosa uptake is even slower

Eutectic mixture of local anesthesia (EMLA)

has been developed to provide surface
anesthesia for intact skin.
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INJECTION:
The rate of uptake of local
anesthetics after injection is
related to both the vascularity of
the injection site and the
vasoactivity of the drug.
IV administration of local
anesthetics provide the most rapid
elevation of blood levels and is
used for primary treatment of
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 DISTRIB
UTION
Once absorbed in the blood stream
local anesthetics are distributed through
out the body to all tissues.
Highly perfused organs such as brain,
head, liver, kidney, lungs have higher
blood levels of anesthetic than do less
higher perfused organs.

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 The blood level is influenced by the
following factors:
Rate of absorption into the blood stream.
Rate of distribution of the agent from the
vascular compartment to the tissues.
Elimination of drug through metabolic
and/or excretory pathways.
All local anesthetic agents readily cross the
blood-brain barrier, they also readily cross 18
 METABOLISM
(BIOTRANSFORMATION)
ESTER LOCAL ANESTHETICS:
• Ester local anesthetics are hydrolyzed in the
plasma by the enzyme
pseudocholinesterase.
• Chloroprocaine the most rapidly
hydrolyzed, is the least toxic. Tertracaine
hydrolyzed 16 times more slowly than
Chloroprocaine ,hence it has the greatest
potential toxicity.
• Procaine undergo hydrolysis to PABA and 19
 AMIDE LOCAL ANESTHETICS
The metabolism of amide local anesthetics is
more complicated then esters. The primary site
of biotransformation of amide drugs is liver.
Entire metabolic process occurs in the liver for
lidocaine, articaine, etidocaine, and bupivacaine.
Prilocaine undergoes more rapid
biotransformation then the other amides.
Monoethylglycinexylidide and glycinexylidide

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 EXCREATION
1. Kidneys are the primary excretory organs
for both the local anesthetic and its
metabolites
2. A percentage of given dose of local
anesthetic drug is excreted unchanged in the
urine.
3. Esters appear in only very small
concentration as the parent compound in
urine.
4. 10% of cocaine dose is found in the urine
unchanged. 21
MRD

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 VASOCONSTRICTORS
• Constrict vessels and decrease blood flow
to the site of injection.
• Absorption of LA into bloodstream is
slowed, producing lower levels in the
blood.
• Lower blood levels lead to decreased risk
of overdose (toxic) reaction.
• Higher LA concentration remains around
the nerve increasing the LA's duration of
action. 23
• Minimize bleeding at the site of administration.
• Naturally Occurring Vasoconstrictors:
- Epinephrine
- Norepinephrine
• Vasoconstrictors should be included unless
contraindicated.
• Mode of Action –
1. Attach to and directly stimulate adrenergic
receptors .
2. Act indirectly by provoking the release of
endogenous catecholamine from intraneuronal
storage sites.
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 VASOCONSTRICTORS
CATECHOLAMINES NONCATECHOLAMINES
• epinephrine • Amphetamine
• nor epinephrine • Methamphetamine
 levonordefrin • Ephedrine
• Isoproterenol • Methoxamine
• Dopamine • Phenylephrine

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• Concentrations of Vasoconstrictor in Local
Anesthetics - 1:50,000 ,1:100,000, 1:200,000 -
0.020mg/ml ,0.010mg/ml, 0.005 mg/ml

• Calculation 1:50,000= 1gram/50,000ml=

1000mg/50,000ml= 1mg/50ml= 0.02mg/ml
• Levonordefrin - One fifth as active as
epinephrine
• Vasoconstrictors - Unstable in Solution Sodium
metabisulfite added Known allergen
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• Max dose of vasoconstrictors
- Healthy patient approximately 0.2mg
- Patient with significant cardiovascular history:
0.04mg
• Max Dose for Vasoconstrictors (CV patient) 1
carpule = 1.8cc 1:100,000=.01mg/cc
0.01 X 1.8cc= 0.018mg 0.04/0.018=2.22 carpules
• In a healthy adult patient 0.2/0.018=11.1 carpules

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