Summary of local anesthesia

FUNCTION:
The loss of sensation in a circumscribed area of the body caused by depression of excitation in
nerve endings or inhibition of the conduction process in peripheral nerves without inducing
loss of consciousness.

Properties of a local anaesthetic:

1. It should not be irritating to the tissue to which it is applied.
2. It should not cause any permanent alteration of nerve structure.
3. Its systemic toxicity should be low.
4. It must be effective regardless of whether it is injected into the tissue or is applied
locally to mucous membranes.
5. The time of onset of anaesthesia should be as short as possible.
6. The duration of action must be long enough to permit completion of the procedure yet
not so long as to require an extended recovery.
7. It should have potency sufficient to give complete anaesthesia without the use of
harmful concentrated solutions.
8. It should be relatively free from producing allergic reactions.
9. It should be stable in solution and should readily undergo biotransformation in the body.
10. It should be sterile or capable of being sterilized by heat without deterioration.

Commercially prepared LA consists of:

 Local anaesthetic agent

 Vasoconstrictor
o Constrict vessels and decrease blood flow to the site of injection
o Absorption of LA into bloodstream is slowed, producing lower levels in the
blood.
o Lower blood levels lead to decreased risk of overdose (toxic) reaction.
o Higher LA concentrations remain around the nerve increasing the LA’s duration
of action.
o Minimise bleeding at the site of admin.
o Naturally occurring Vasoconstrictors: Epinephrine; Norepinephrine
o Vasoconstrictors should be included unless contraindicated.
o Mode of action: attach to and directly stimulate adrenergic receptors. Act
indirectly by provoking the release of endogenous catecholamine from
intraneuronal storage sites.
o *Concentrations of VC in LA: 1gram:50000ml (0.020mg/ml); 1:100000
(0.010mg/ml); 1:200000 (0.005mg/ml)
o Max dose of vasoconstrictors:
 Healthy patient approx. 0.2mg
 Cardio history:0.04mg
 Max dose for VC (cardiovascular patient): 1 carpule = 1.8cc; 1:100 000
= 0.01mg/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
  Reducing agent
o Vasoconstrictor are unstable in solution and may oxidise especially on prolong
exposure to sunlight. Solution will turn brown and this must be discarded.
Hence, reducing agent such as a small quantity of sodium metabisulphite is
added- competes for the available O2. To increase shelf life.

 Preservative
o Capryl hydrocuprienotoxin are added to maintain the sterility
o Methylparaben has been shown to cause allergic reaction in some sensitized
subjects

 Fungicide
o Thymol

 Vehicle
o The anaesthetic agent and the additives referred to above are dissolved in
distilled water & sodium chloride. This isotonic solution minimises discomfort
during injections
The chemical characteristics have both lipophilic and hydrophilic properties.
LOCAL ANESTHETICS used in dentistry divided into 2 groups:
 Ester group (intermediate chain: ester linkage)
 Amide group (intermediate chain: amide linkage)

 Lidocaine is the most commonly chosen anaesthetic today.

 The most popular contains epinephrine 1:100,000 and provides good anaesthesia for
healthy patients.
 Lidocaine with epinephrine 1:50,000 is used for haemostasis, but because of the
rebound effect noted earlier, it should be used sparingly.
 3% Mepivacaine without a vasoconstrictor is used as anaesthetic for patients who
cannot take a vasoconstrictor or for short procedures. It is appropriate for use in
Pedodontics and for use on geriatric patients.
 2% Mepivacaine with vasoconstrictor provides pulpal anaesthesia that is similar to
lidocaine with epinephrine, but haemostasis is not as intense.
 The action of prilocaine plain varies with the area injected (longer with a nerve block),
but usually provides anaesthesia similar to lidocaine and mepivacaine with
vasoconstrictor.
 Prilocaine with vasoconstrictor gives good anaesthetic effect and uses a 1:200,000
concentration of epinephrine.
 Bupivacaine is used when pulpal anaesthesia is desired for longer appointments and
when postoperative pain is anticipated.
 Some practitioners may prescribe nonsteroidal anti-inflammatory agents prior to the
appointment, use an intermediate duration anaesthetic for the procedure, and even will
inject bupivacaine just prior to the patient's dismissal, and direct the patient to take
oral analgesics for a certain number of days following the procedure.
 Bupivacaine is not recommended for children or handicapped patients because of the
increased risk of postoperative injury (chewing on a numb lip).
 Articaine is a newer anaesthetic typically given in a 4% solution with 1:100,000
epinephrine. It is widely used in Europe and has recently gained popularity in the U.S.
Articaine reportedly is more potent than Lidocaine and, therefore, requires less to
achieve a similar state of anesthesia. Practitioners reported rarely missing an Inferior
Alveolar nerve block with Articaine. However, concern has arisen about its potential
for tissue necrosis and persistent nerve parasthesia. An update regarding the latest on
Articaine will be discussed at the end of this course.