Professional Documents
Culture Documents
local anesthetics
Why are local anesthetics
different??
Local anesthetic, when used for
the management of pain, differs
from other drugs used in
dentistry in one important regard
i.e. almost all other drugs reach
blood stream & exert their effect,
while the action of local
anesthetics ceases when these
enter the blood stream.
Uptake of local
anesthetic..
When injected into soft tissue, L.A.
exerts action on blood vessels of the
area.
esters amides
with different types of
metabolism..
esters
Hydrolyzed in plasma by enzyme
pseudocholinesterase.
Rate of hydrolysis is different for
different compounds.
e.g. chlorprocaine is most rapidly
hydrolysed while tetracaine is
hydrolysed 16 times slowly.
PABA is the metabolic product causing
most of the allergic reactions.
Approx. 1 in 2800 people have atypical
form of pseudocholinesterase
Inability to hydrolysed LA & other
chemically related drugs.
atypical form of pseudocholinesterase
is hereditary trait so family history is
important.
amides
Biotransformation
products
Significant in cases of renal &
cardiac failure.
e.g. orthotoluidine, a metabolite of
prilocaine , may cause clinically
significant methemoglobinemia.
Also, metabolites of lidocaine i.e.
monoethylglycinexylidide &glycine
xylidide may produce sedation.
excretion
Kidneys are primary excretory
organs.
A small dose may appear
unchanged in urine.
Esters are usually present as
metabolites while amides as parent
compounds.
Patients with severe renal impairment
pose a potential of toxicity
Action of L.A.
Systemic local
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
Factors Affect the Reaction of Local
Anesthetics (cont.)
Vasodilation
greater vasodilator activity = increased blood flow through
the region=rapid removal of anesthetic molecule from the
injection site.
thus decreased anesthetic potency & decreased duration
• Though having strong addicting CNS action but it was widely Used,
neverthless for 30 yr.
procaine because of
rapid
hydrolysis.
METABOLISM-
hydrolysed in the both hydrolysed in the
presence
plasma & the liver of plasma choline
estrases
Lidocaine
• In 1940, the first modern local
anesthetic agent came in use that is
lidocaine , trade name Xylocaine®
• It developed as a derivative of
xylidine
• dental surgeries
• Belongs to the amide class, cause
little allergenic reaction; it’s
hypoallergenic
• Sets on quickly and produces a
desired anesthesia effect for several
hours
• It’s accepted broadly as the local
anesthetic in United States today
• POTENCY-2( compared with procaine)
• TOXICITY-2( Compared with procaine)
• METABOLISM-In liver by microsomal
fixed
function oxidases , to mono ethyl
glycerine
& xylidine.
EXCREATION- Via kidneys
SYSTEMIC EFFECTS
• NERVOUS SYSTEM-
Lidocaine, in toxic doses,first produces stimulation
then depression of the CNS.
Lidocaineadminister I.V is capable of producing a
degree of analgesia & even general anesthesia.
RESPIRATORY SYSTEM-
small doses of lidocaine have a mild bronchodilating
effect
respiratory arrest is the most common cause of death
related to over dose of local anesthetics.
CARDIOVASCULAR SYSTEM-
Effect of lidocaine on the cvs varies in acc with dose
- the drug, indoses of 50 to 100mg (1.5mg /kg) is givaen I.V during
general anesthesia & surgery to correct ventricular arrhythmias.
In general moderately large doses produces a
-decrease in the electrical excitability force of ofthe myocardium
-decrease in the force of contraction( negative inotropic effect)
-decrease in the rate of electrical impulse conduction( negative
chronotropic effect)
Although these effects make lidocaine one of the most popular anti
arrhythmic agent.
Three special drugs used in dental
• Bupivicaine (Marcaine®anesthesia
--Produce very long acting anesthetic effect to delay the post operative pain
from the surgery for as long as possible
--0.5% solution with vasoconstrictor
--toxicity slowed because the pKa is very basic
--Onset time is longer than other drugs b/c most of the radicals (about 80%) bind
to sodium channel proteins effectively
--less than four times that of lidocaine.
• Prilocaine (Citanest®)
--Identical pKa and same conc. with lidocaine
--Almost same duration as lidocaine
--Less toxic in higher doses than lidocaine b/c small vasodilatory activity
• Articaine (Septocaine®)
--newest local anesthetic drug approved by FDA in 2000
--Same pKa and toxicity as lidocaine, but its half life is less than about ¼ of
lidocaine
--Used with vasoconstrictor.
--Enters blood barrier smoothly
--The drug is widely used in most nations today
Conclusion
COMPLICATIONS OF LA.
• Syncope (fainting)
• Muscle trismus
• Pain or hyperalgesia an infections.
• Edema
• Infections
• Broken needles
• Prolonged anaesthesia
• Hematoma
• Sloughing of tissues
• Facial nerve paralysis
• Soft tissue injury
Broken needles
Hematoma
Soft tissue injury
Effects of over dosage of local
anesthesia
On CNS
On CVS
•Anxiety, restlessness
•Cardiac muscle
•Sighing respiration, beats
tremors less effectively
1. Concentration
2. Dose
3. Route of ad.
4. Rate of injection
5. Vascularity of the injection site
6. Presence of vacsoconstrictors.
Causes of Overdose
2. Biotransformation & elimination.
3. Excessive total dose.
4. Rapid absorption into the
circulation.
5. Intravascular injection.
Classification of
Orofacialanesthetic
techniques:
I. LOCAL INFILTRATION
II. FIELD BLOCK
III. NERVE BLOCK
I. LOCAL INFILTRATION
• Technique that anesthetizes the terminal nerve
endings of the dental plexus.
•
SYRINGE and NEEDLE
• t
Needle assembling
Techniques of
Maxillary Regional
I. Local Infiltration
• a. Supraperiosteal Injection
• b. Periodontal Ligament Injection
• c. Intraseptal Injection
• d. Intrapulpal Injection
• e. Local Palatal infiltration
•
Technique:
• Insert the needle at the injection site to a depth of
no more than to a depth of no more than a few
millimeters and aspirate. Then inject one third to
one half (0.6-1.2cc) of a cartridge of anesthetic
solution slowly, over the course of thirty seconds.
Supraperiosteal (Local)
Infiltration
Periodontal Ligament
(Intraligamentary
- useful adjunct to the nerve block.
Technique:
• Insert the needle (bevel facing the root), to the
depth of the gingival sulcus
• Advance the needle until resistance is met. A small
amount of anesthetic (0.2cc) is then administered
slowly over the course of twenty to thirty seconds.
It is normal to experience resistance to the flow of
anesthetic.
Periodontal Ligament
(Intraligamentary Injection)
Intrapulpal
Injection
- involves anesthesia of the nerve within the
pulp canal of the individual tooth to be treated.
- may be used once the pulp chamber is open.
Technique:
• Advance the needle into the pulp canal and
deposit another 0.2cc of local anesthetic solution.
• It may be necessary to bend the needle in order
to gain access to the chamber.
Local Palatal Infiltration
Technique:
• While maintaining pressure behind the
injection site, deposit anesthetic solution as
the soft tissue is penetrated. Advance the
needle until bone is contacted
Local Palatal Infiltration
Techniques of Anesthesia for Treatment of
Upper Quadrant for Multiple Teeth
PSAN Block
• Also known as the tuberosity block or the
zygomatic block,
Technique:
• Insert the needle at the injection site at a 45 degree
angle directed superiorly, medially, and posteriorly
(one continuous movement).
Technique-:
• With a cotton swab, hold pressure over the incisive
papilla.
• Insert the needle just lateral to the papilla with the
bevel against the tissue.
• Advance the needle slowly toward the incisive
foramen while depositing small volumes of
anesthetic and maintaining pressure on the papilla.
Nasopalatine Nerve Block
Techniques of
Mandibular
• I. Local Infiltration
• a. Supraperiosteal Injection
• b. Periodontal Ligament Injection
• c. Intraseptal Injection
• d. Intrapulpal Injection
• are executed in the same manner as described above for maxillary
anesthesia.
• II. Nerve block
• a. Inferior Alveolar Nerve Block
• b. Buccal Nerve Block
• c. Gow-Gates Technique
• d. Vazirani-Akinosi
Closed Mouth Mandibular Block
• e. Mental Nerve Block
• f. Incisive Nerve Block
Techniques of Anesthesia for
Treatment of Lower Quadrant for
Multiple Teeth
Inferior Alveolar Nerve
Block
Most commonly employed technique