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Abou Rabii
Qassim University – College of
Local Anesthetia Dentistry
3rd year - January 2010
Lecture Objective
Page 2
Local anaesthetics
Page 3
Cell Membrane Receptors
Page 4
Membrane potential and neurotransmission:
Page 5
Mechanism
Page 6
Mechanism
Page 7
Mechanism
Page 8
How Local Anesthetics Work
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LOCAL ANESTHETICS CALSIFICATION
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Differences of Esters and Amides
Two classes of local anesthetics are amino amides and amino esters.
Amides: Esters:
--Amide link b/t intermediate --Ester link b/t intermediate chain and chain
and aromatic ring aromatic ring
--Metabolized in liver and very --Metabolized in plasma
--Cause allergic reactions
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Pharmacokinetics
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Pharmacokinetics
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Vasoconstrictors
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Application of local anaesthesia
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Application of local anaesthesia
The local anesthetics used most frequently for infiltration anesthesia are
1- lidocaine
2- procaine
3- bupivacaine
Page 16
Application of local anaesthesia
4- Nerve block:
Injection of a solution of a local anesthetic into or about individual
peripheral nerves or nerve plexuses
Page 17
Factors Affect the Reaction of Local
Anesthetics
pH influence
Usually at range 7.6 – 8.9
Decrease in pH shifts equilibrium toward the ionized form, delaying the
onset action.
Lower pH, solution more acidic, gives slower onset of action
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Effect of inflammation on the
activity of local anaesthetics
Page 19
Factors affecting absorption of local
anaesthetics into the systemic circulation
Page 20
Factors Affect the Reaction of Local
Anesthetics (cont.)
Vasodilation
Vasoconstrictor is a substance used to keep the anesthetic solution in place
at a longer period and prolongs the action of the drug
vasoconstrictor delays the absorption which slows down the absorption into
the bloodstream
Lower vasodilator activity of a local anesthetic leads to a slower absorption
and longer duration of action
Vasoconstrictor used the naturally hormone called epinephrine (adrenaline).
Epinephrine decreases vasodilator.
Page 21
Undesired
systemic effects of
local anesthetics
Undesired systemic effects of local anesthetics
Page 23
Undesired systemic effects of local
anesthetics:
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Undesired effects of local anesthetics
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Undesired effects of local anesthetics
V- Cardiovascular system:
--- Decrease electrical excitability, conduction rate, and force of
contraction in the myocardium.
--- Cause arteriolar dilation.
--- Cocaine differs from the other local anesthetics: it blocks
norepinephrine reuptake, resulting in
vasoconstriction and hypertension, even cardiac arrhythmias.
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Local Anesthesia Allergic shock
Esters are highly allergenic, their use should be avoided and restricted to
special cases after allergy test.
There has never been a true, documented allergic reaction to an amine
anesthetic.
a patient may in fact be allergic only to the bisulfite preservative used to
stabilize the vasoconstrictor.
If the allergic reaction was not too serious, it may be worth trying again
with either mepivicaine or prilocaine without vasoconstrictor.
Anesthetic manufactures do not use preservatives in carpules that do not
also contain vasoconstrictor.
Page 27
Testing for anesthetic allergy using skin test
T.R.U.E. Test®
This is a patch test that applies 23 allergens to the skin contained in 12
polyester patches. One of the patches contains a mixture of several
anesthetics and is used to test for allergy to local anesthetics in general.
The mixture used includes two ester based anesthetics and one amine
based anesthetic. This mixture of anesthetics is called the "Caine Mix"
Page 28
Signs and symptoms of anesthetics allergic reaction
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Anaphylactic shock
Page 30
Management of anaphylactic shock : 1
Position the patient on his or her back with the feet elevated.
Maintain an airway
If the patient is not breathing on his own, use rescue breathing like you
learned in CPR class. Thanks for Dr. Yasser
Check the carotid artery for heartbeat and use chest compressions if
necessary.
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Management of anaphylactic shock : 2
The two drugs that you must have on hand to stabilize a patient in
anaphylactic shock are as follows:
– Epinephrine (adrenalin) 1:1000 subcutaneous injection. It opens the
bronchioles allowing free breathing, increases the blood pressure counteracting
shock and evens out and intensifies the heart beat. Its effects are drastic, but
short lived. The standard dose is 1 mg given in three doses five minutes
apart.
– Benedryl (diphenhydramine) 25-50 mgm injectable. This is an antihistamine
and can also be taken in pill form an hour before the procedure to help
prevent serious allergic reaction before it begins. Injectable diphenhydrimine
which can be administered either subcutaneously, or in the buccal fold if the
dentist is more comfortable with that route.
Page 32
Management of anaphylactic shock : 3
The following drugs are of little use to the dentist during the initial stages
of the emergency since they are generally used by EMS personnel
– Aminophylline This drug opens blocked breathing passages.
– Solu-cortef IV injection. This drug is a corticosteroid and reduces the
generalized allergic inflammatory reactions on a longer term basis. It will not
act rapidly enough to reverse anaphylaxis immediately, but is more of a long
term remedy.
– Wyamine injection. This drug is used to counteract hypotension (low blood
pressure and shock) on a prolonged basis.
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Choose the right Dose
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Preparations
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Minimum Toxic Dose
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Maximum Dose
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Page 38
Page 39
Dosage guidelines
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LA Management of
Special Ptient
Children
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What local anesthetic
All local anesthetics have a low margin of safety between the effective
dose and the toxic dose. The lethal dose for many local anesthetics is
only 3 times that of the effective dose.
Deaths following local anesthetic administration are almost always a
result of overdosage.
The maximum safe dose of lidocaine for a child is 4.5 mg/kg per dental
appointment.
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What local anesthetic
Page 44
What Technique
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Handicapped Patient
Several issues arise concerning the use of local anesthesia with this
population. One of these is lip biting
– Consideration should be given to choosing a short-acting local anesthetic to
reduce the possibilityof post-operative trauma from lip biting.
– Another choice would be to avoid mandibular blocks and utilize infiltration,
periodontal ligament
A second issue with local anesthesia is the inability to determine from a
non-communicative patient when an acceptable level of anesthesia has
been obtained.
– When in doubt second injections and alternative routes (e.g., buccal, mylohyoid,
intraligamentary)
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Handicapped Patient
Page 47
Patients receiving anticoagulation or suffering from
bleeding disorders
oral procedures must be done at the beginning of the day because this
allows more time to deal with immediate re-bleeding problems.
Also the procedures must be performed early in the week, allowing
delayed re-bleeding episodes, usually occurring after 24-48 h, to be dealt
with during the working weekdays.
Local anesthetic containing a vasoconstrictor should be administered by
infiltration or by intraligamentary injection wherever practical.
Regional nerve blocks should be avoided when possible.
Local vasoconstriction may be encouraged by infiltrating a small amount
of local anesthetic containing adrenaline (epinephrine) close to the site of
surgery.
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Pregnant woman
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Pregnant woman
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For Information :
Pregnancy drug Clases
Medications are grouped into 1 of 5 categories based on the potential for
producing birth defects. The categories are A, B, C, D and X. Generally
speaking, drugs that fall into either class A or B are considered safe and
are routinely used. There may be exceptions.
Category A: Controlled studies in pregnant women fail to demonstrate a
risk to the fetus in the first trimester with no evidence of risk in later
trimesters. The possibility of harm appears remote.
Category B: Presumed safety based on animal studies, with no
controlled studies in pregnant women, or animal studies have shown an
adverse effect that was not confirmed in controlled studies in women in
the first trimester and there is no evidence of a risk in later trimesters.
Category C: Studies in women and animals are not available or
studies in animals have revealed adverse effects on the fetus and there
are no controlled studies in women. Drugs should be given only if the
potential benefits justify the potential risk to the fetus.
Category D: There is positive evidence of human fetal risk (unsafe),
however in some cases such as a life-threatening illness the potential risk
may be justified if there are no other alternatives.
Category X: Highly unsafe: risk of use outweighs any potential benefit.
Drugs in this category are contraindicated in women who are or may
become pregnant.
Page 51
GERIATRIC PATIENT
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LIVER DISORDERS
Potential complications:
1. Impaired drug detoxication e.g. sedative, analgesics, general
anesthesia.
2. Bleeding disorders ( decrease clotting factors, excess fibrinolysis,
impaired vitamin K absorption).
3. Transmission of viral hepatitis.
Management
Avoid LA metabolized in liver: Amides (Lidocaine, Mepicaine), esters
should be used
Page 53
Drug-Drug Interaction
Page 54
References
Calatayud Jesús and González Ángel. History of the Development and Evolution of
Local Anesthesia Since the Coca Leaf. © 2003 American Society of Anesthesiologists
Volume 98(6) June 2003 pp 1503-1508.
Peter C. Meltzer, Shanghao Liu, Heather S. Blanchette, Paul Blundell, Bertha K.
Madras. Design and Synthesis of an Irreversible Dopamine-Sparing Cocaine
Antagonist. @ Bioorganic & Medicinal Chemistry Volume 10, Issue 11 , November
2002, Pages 3583-3591
Shigeki Isomura, Timothy Z. Hoffman, Peter Wirsching, and Kim D. Janda. Synthesis,
Properties, and Reactivity of Cocaine Benzoylthio Ester Possessing the Cocaine
Absolute Configuration. J. AM. CHEM. SOC. 2002, Issue 124, p.3661-3668
Mazoit, Jean-Xavier; Dalens, Bernard J. Pharmacokinetics of local anesthetics in
infants and children. Clinical Pharmacokinetics (2004), 43(1), 17-32.
Page 55
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